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OpenTrials
Completed

NCT Number: NCT04053023

Linerixibat and Obeticholic Acid Drug Interaction Study in Healthy Subjects

In participants with inadequate response/intolerance to ursodeoxycholic acid (UDCA) taking obeticholic acid (OCA) who experience pruritus (due to primary biliary cholangitis [PBC], OCA, or both) the addition of linerixibat to OCA therapy may be considered following marketing approval. It is therefore important to characterize any potential effect of linerixibat on the pharmacokinetics of OCA in humans at clinically relevant dosages. Accordingly, a drug-drug interaction (DDI) study with linerixibat (potential perpetrator) and OCA (potential victim) will be conducted to inform both future clinical trials with linerixibat and the potential concomitant administration of these drugs in a clinical setting. This is a single-center, one part (with optional second part) open-label, single sequence crossover, drug interaction study to investigate the effect of linerixibat on plasma concentrations of OCA and OCA conjugates in healthy participants. Approximately 19 participants will be enrolled in part A and further 19 participants in part B (if performed) in the study and will have a phone call follow-up till 7-14 days post-last linerixibat dose.

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Key information

Conditions

Cholestasis Bile Duct Diseases Biliary Tract Diseases Cholestasis, Intrahepatic Digestive System Diseases Fibrosis Liver Cirrhosis Liver Cirrhosis, Biliary Liver Diseases Pathologic Processes Pathological Conditions, Signs and Symptoms

Age range

18 year–80 year

Sex eligibility

All sexes

Study type

Interventional

Phase

Phase 1

Primary location

GSK Investigational Site

Cambridge, CB2 0GG, United Kingdom

Who can participate

Healthy volunteers accepted: Yes

Only the study team can determine whether someone qualifies for participation.

Inclusion criteria

  • Between 18 and 80 years of age inclusive, at the time of signing the informed consent.
  • Healthy, as determined by the investigator or medically qualified designee, based on a medical evaluation including medical history, physical examination, vital signs, laboratory tests, and ECG. A participant with a clinical abnormality or laboratory parameter (i.e., outside the reference range for the population being studied), which is not specifically listed in the eligibility criteria, may be included only if the investigator agrees in consultation with the GlaxoSmithKline (GSK) medical monitor and documents in the source documentation that the finding is unlikely to introduce additional risk factors and will not interfere with the study procedures or outcomes.
  • Body weight > 50 kilogram (kg) and body mass index (BMI) within the range 18.5 to 32 kg per square meter (inclusive).
  • Capable of giving signed informed consent which includes compliance with the requirements and restrictions listed in the informed consent form (ICF) and protocol.
  • Male and female- A female participant is eligible to participate if she is not pregnant not breastfeeding, and at least one of the following conditions applies; not a woman of childbearing potential (WOCBP) or a WOCBP who agrees to follow contraceptive guidance during the treatment period and until at least 4 weeks after the last dose of study treatment. The investigator is responsible for review of medical history, menstrual history, and recent sexual activity to decrease the risk for inclusion of a woman with an early undetected pregnancy.

Exclusion criteria

  • Any active dermatologic disorder leading to or with the potential to cause pruritus or a recent history of unexplained clinically significant itching locally or generally within the prior 3 months
  • Current or chronic history of liver disease, or known hepatic or biliary abnormalities (with the exception of Gilbert's syndrome or asymptomatic gallstones) and/or confirmed hepatocellular carcinoma or biliary cancer
  • Participants with a history of cholecystectomy
  • Current symptomatic cholelithiasis or inflammatory gall bladder disease
  • Significant history of or current cardiovascular, respiratory, hepatic, renal, gastrointestinal, endocrine, hematological, or neurological disorders capable of significantly altering the absorption, metabolism, or elimination of drugs; constituting a risk when taking the study intervention; or interfering with the interpretation of data
  • Any clinically relevant abnormality identified at the screening medical assessment (physical examination/medical history) clinical laboratory tests, or 12-lead ECG
  • Current episode, recent history (within 1 month of screening visit), or chronic history of clinically significant diarrhea
  • Lymphoma, leukaemia, or any malignancy within the past 5 years except for basal cell or squamous epithelial carcinomas of the skin that have been resected with no evidence of metastatic disease for 3 years
  • Any current medical condition (e.g. psychiatric disorder, senility, dementia, or other condition), clinical or laboratory abnormality, or examination finding that the investigator considers would put the participant at unacceptable risk, which may affect study compliance or prevent understanding of the aims or investigational procedures or possible consequences of the study
  • Regular use of known drugs of abuse or history of drug abuse or dependence within 6 months of the study
  • Regular alcohol consumption within 6 months prior to the study defined as an average weekly intake of >14 units for females and >21 units for males. One unit is equivalent to 8 gram of alcohol: a glass (approximately [~] 240 milliliter [mL]) of beer, 1 small glass (~100 mL) of wine or 1 (~25 mL) measure of spirits
  • History of or regular use of tobacco- or nicotine-containing products (confirmed by smokerlyzer test) in the 3 months prior to screening.
  • Administration of any IBAT inhibitor (including linerixibat) or OCA in the 3 months prior to screening
  • Past or intended use of over-the-counter or prescription medication (including vitamins and dietary or herbal supplements) within 7 days (or 14 days if the drug is a potential enzyme inhibitor) or 5 half-lives (whichever is longer) prior to the first dose of study medication, unless approved by the investigator in conjunction with GSK medical monitor.
  • Current enrollment in a clinical trial, recent participation in a clinical trial and has received an investigational product within 30 days (or 5 half-lives of previous trial intervention, whichever is longer) before the first dose in the current study
  • Exposure to more than 4 new chemical entities within 12 months before the first dose in the current study.
  • Screening ALT or AST >1.5 times the upper limit of normal (ULN)
  • Bilirubin >1.5 times ULN (isolated bilirubin >1.5 times ULN is acceptable if bilirubin is fractionated and direct bilirubin <35%)
  • Presence of Hepatitis B surface antigen (HBsAg) at screening or positive Hepatitis C antibody test result at screening or within 3 months of the screening visit
  • Positive serum pregnancy test at screening or positive urine pregnancy test at admission in WOCBP only
  • Positive human immunodeficiency virus (HIV) antibody test
  • QTc >450 millisecond (msec) on ECG performed at screening.
  • Positive pre-study drug/alcohol screen or positive drug/alcohol screen at any time during the study.
  • Female participants unable or unwilling to comply with specific contraception restrictions.
  • Where participation in the study would result in donation of blood or blood products in excess of 500 mL within a 56-day period.
  • Unwillingness or inability to follow the procedures outlined in the protocol for the expected duration of study participation.
  • Sensitivity to any of the study interventions, or components thereof, or drug or other allergy that, in the opinion of the investigator or medical monitor, contraindicates participation in the study.

Treatment and study plan

GSK2330672 (linerixibat)

Drug

GSK2330672 is available as a tablet with unit dose strength of 45 mg.

Obeticholic acid

Drug

Obeticholic acid is available as a tablet with a unit dose strength of 10 mg (or 5 mg dependent on evaluation of Part A).

Primary outcomes

  1. Part A- Area Under the Concentration-time Curve From Time 0 to Time of the Last Quantifiable Concentration (AUC[0-t]) for Total-OCA at Steady State: OCA Arm

    Time frame: Day 17: Pre-dose; Day 18: Pre-dose, 0.25, 0.50, 0.75, 1, 1.5, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 14 and 24 hours (Day 19) post-dose

    Blood samples were collected at indicated time points for pharmacokinetic analysis of total-OCA. Pharmacokinetic parameters were calculated using standard non-compartmental analysis. Pharmacokinetic (PK) Parameters Population consisted of all participants for whom pharmacokinetic parameters were derivable.

  2. Part A- AUC(0-t) for Total-OCA at Steady State: OCA + Linerixibat Arm

    Time frame: Days 35 and 36: Pre-dose; Day 37: Pre-dose, 0.25, 0.50, 0.75, 1, 1.5, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 14 and 24 hours (Day 38) post-dose

    Blood samples were collected at indicated time points for pharmacokinetic analysis of total-OCA. Pharmacokinetic parameters were calculated using standard non-compartmental analysis.

  3. Part A- Area Under the Concentration-time Curve From Time 0 to 24 Hour (AUC[0-24]) for Total-OCA at Steady State: OCA Arm

    Time frame: Day 17: Pre-dose; Day 18: Pre-dose, 0.25, 0.50, 0.75, 1, 1.5, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 14 and 24 hours (Day 19) post-dose

    Blood samples were collected at indicated time points for pharmacokinetic analysis of total-OCA. Pharmacokinetic parameters were calculated using standard non-compartmental analysis.

  4. Part A- AUC(0-24) for Total-OCA at Steady State: OCA + Linerixibat Arm

    Time frame: Days 35 and 36: Pre-dose; Day 37: Pre-dose, 0.25, 0.50, 0.75, 1, 1.5, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 14 and 24 hours (Day 38) post-dose

    Blood samples were collected at indicated time points for pharmacokinetic analysis of total-OCA. Pharmacokinetic parameters were calculated using standard non-compartmental analysis.

  5. Part A- Maximum Observed Concentration (Cmax) for Total-OCA at Steady State: OCA Arm

    Time frame: Day 17: Pre-dose; Day 18: Pre-dose, 0.25, 0.50, 0.75, 1, 1.5, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 14 and 24 hours (Day 19) post-dose

    Blood samples were collected at indicated time points for pharmacokinetic analysis of total-OCA. Pharmacokinetic parameters were calculated using standard non-compartmental analysis.

  6. Part A- Cmax for Total-OCA at Steady State: OCA + Linerixibat Arm

    Time frame: Days 35 and 36: Pre-dose; Day 37: Pre-dose, 0.25, 0.50, 0.75, 1, 1.5, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 14 and 24 hours (Day 38) post-dose

    Blood samples were collected at indicated time points for pharmacokinetic analysis of total-OCA. Pharmacokinetic parameters were calculated using standard non-compartmental analysis.

  7. Part A- Average Trough Concentration (Ctrough) for Total-OCA at Steady State: OCA Arm

    Time frame: Day 17: Pre-dose; Day 18: Pre-dose, 0.25, 0.50, 0.75, 1, 1.5, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 14 and 24 hours (Day 19) post-dose

    Blood samples were collected at indicated time points for pharmacokinetic analysis of total-OCA. Pharmacokinetic parameters were calculated using standard non-compartmental analysis. Average of Ctrough measurement from study Days 17, 18 and 19 has been presented.

  8. Part A- Average Ctrough for Total-OCA at Steady State: OCA + Linerixibat Arm

    Time frame: Days 35 and 36: Pre-dose; Day 37: Pre-dose, 0.25, 0.50, 0.75, 1, 1.5, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 14 and 24 hours (Day 38) post-dose

    Blood samples were collected at indicated time points for pharmacokinetic analysis of total-OCA. Pharmacokinetic parameters were calculated using standard non-compartmental analysis. Average of Ctrough measurement from study Days 35, 36, 37 and 38 has been presented.

  9. Part B- AUC(0-t) for Total-OCA at Steady State: OCA Arm

    Time frame: Day 17: Pre-dose; Day 18: Pre-dose, 0.25, 0.50, 0.75, 1, 1.5, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 14 and 24 hours (Day 19) post-dose

    Blood samples were planned to be collected at indicated time points for pharmacokinetic analysis of total-OCA.

  10. Part B- AUC(0-t) for Total-OCA at Steady State: OCA + Linerixibat Arm

    Time frame: Days 35 and 36: Pre-dose; Day 37: Pre-dose, 0.25, 0.50, 0.75, 1, 1.5, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 14 and 24 hours (Day 38) post-dose

    Blood samples were planned to be collected at indicated time points for pharmacokinetic analysis of total-OCA.

  11. Part B- AUC(0-24) for Total-OCA at Steady State: OCA Arm

    Time frame: Day 17: Pre-dose; Day 18: Pre-dose, 0.25, 0.50, 0.75, 1, 1.5, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 14 and 24 hours (Day 19) post-dose

    Blood samples were planned to be collected at indicated time points for pharmacokinetic analysis of total-OCA.

  12. Part B- AUC(0-24) for Total-OCA at Steady State: OCA + Linerixibat Arm

    Time frame: Days 35 and 36: Pre-dose; Day 37: Pre-dose, 0.25, 0.50, 0.75, 1, 1.5, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 14 and 24 hours (Day 38) post-dose

    Blood samples were planned to be collected at indicated time points for pharmacokinetic analysis of total-OCA.

  13. Part B- Cmax for Total-OCA at Steady State: OCA Arm

    Time frame: Day 17: Pre-dose; Day 18: Pre-dose, 0.25, 0.50, 0.75, 1, 1.5, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 14 and 24 hours (Day 19) post-dose

    Blood samples were planned to be collected at indicated time points for pharmacokinetic analysis of total-OCA.

  14. Part B- Cmax for Total-OCA at Steady State: OCA + Linerixibat Arm

    Time frame: Days 35 and 36: Pre-dose; Day 37: Pre-dose, 0.25, 0.50, 0.75, 1, 1.5, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 14 and 24 hours (Day 38) post-dose

    Blood samples were planned to be collected at indicated time points for pharmacokinetic analysis of total-OCA.

  15. Part B- Ctrough for Total-OCA at Steady State: OCA Arm

    Time frame: Day 17: Pre-dose; Day 18: Pre-dose, 0.25, 0.50, 0.75, 1, 1.5, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 14 and 24 hours (Day 19) post-dose

    Blood samples were planned to be collected at indicated time points for pharmacokinetic analysis of total-OCA.

  16. Part B- Ctrough for Total-OCA at Steady State: OCA + Linerixibat Arm

    Time frame: Days 35 and 36: Pre-dose; Day 37: Pre-dose, 0.25, 0.50, 0.75, 1, 1.5, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 14 and 24 hours (Day 38) post-dose

    Blood samples were planned to be collected at indicated time points for pharmacokinetic analysis of total-OCA.

Secondary outcomes

  1. Part A- Time to Reach Maximum Observed Plasma Concentration (Tmax) for Total-OCA: OCA Arm

    Time frame: Day 17: Pre-dose; Day 18: Pre-dose, 0.25, 0.50, 0.75, 1, 1.5, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 14 and 24 hours (Day 19) post-dose

    Blood samples were collected at indicated time points for pharmacokinetic analysis of total-OCA. Pharmacokinetic parameters were calculated using standard non-compartmental analysis.

  2. Part A- Tmax for Total-OCA: OCA + Linerixibat Arm

    Time frame: Days 35 and 36: Pre-dose; Day 37: Pre-dose, 0.25, 0.50, 0.75, 1, 1.5, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 14 and 24 hours (Day 38) post-dose

    Blood samples were collected at indicated time points for pharmacokinetic analysis of total-OCA. Pharmacokinetic parameters were calculated using standard non-compartmental analysis.

  3. Part A- Assessment of Steady State Using Ctrough of Total-OCA: OCA Arm

    Time frame: Day 17: Pre-dose; Day 18: Pre-dose, 0.25, 0.50, 0.75, 1, 1.5, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 14 hours and 24 hours (Day 19) post-dose

    Blood samples were collected at indicated time points for pharmacokinetic analysis of total-OCA. Pharmacokinetic parameters were calculated using standard non-compartmental analysis.

  4. Part A- Assessment of Steady State Using Ctrough of Total-OCA: OCA + Linerixibat Arm

    Time frame: Days 35 and 36: Pre-dose; Day 37: Pre-dose, 0.25, 0.50, 0.75, 1, 1.5, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 14 hours and 24 hours (Day 38) post-dose

    Blood samples were collected at indicated time points for pharmacokinetic analysis of total-OCA. Pharmacokinetic parameters were calculated using standard non-compartmental analysis.

  5. Part A- AUC(0-t) for OCA: OCA Arm

    Time frame: Day 17: Pre-dose; Day 18: Pre-dose, 0.25, 0.50, 0.75, 1, 1.5, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 14 and 24 hours (Day 19) post-dose

    Blood samples were collected at indicated time points for pharmacokinetic analysis of OCA. Pharmacokinetic parameters were calculated using standard non-compartmental analysis.

  6. Part A- AUC(0-t) for OCA: OCA + Linerixibat Arm

    Time frame: Days 35 and 36: Pre-dose; Day 37: Pre-dose, 0.25, 0.50, 0.75, 1, 1.5, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 14 and 24 hours (Day 38) post-dose

    Blood samples were collected at indicated time points for pharmacokinetic analysis of OCA. Pharmacokinetic parameters were calculated using standard non-compartmental analysis.

  7. Part A- AUC(0-24) for OCA: OCA Arm

    Time frame: Day 17: Pre-dose; Day 18: Pre-dose, 0.25, 0.50, 0.75, 1, 1.5, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 14 and 24 hours (Day 19) post-dose

    Blood samples were collected at indicated time points for pharmacokinetic analysis of OCA. Pharmacokinetic parameters were calculated using standard non-compartmental analysis.

  8. Part A- AUC(0-24) for OCA: OCA + Linerixibat Arm

    Time frame: Days 35 and 36: Pre-dose; Day 37: Pre-dose, 0.25, 0.50, 0.75, 1, 1.5, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 14 and 24 hours (Day 38) post-dose

    Blood samples were collected at indicated time points for pharmacokinetic analysis of OCA. Pharmacokinetic parameters were calculated using standard non-compartmental analysis.

  9. Part A- Cmax for OCA: OCA Arm

    Time frame: Day 17: Pre-dose; Day 18: Pre-dose, 0.25, 0.50, 0.75, 1, 1.5, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 14 and 24 hours (Day 19) post-dose

    Blood samples were collected at indicated time points for pharmacokinetic analysis of OCA. Pharmacokinetic parameters were calculated using standard non-compartmental analysis.

  10. Part A- Cmax for OCA: OCA + Linerixibat Arm

    Time frame: Days 35 and 36: Pre-dose; Day 37: Pre-dose, 0.25, 0.50, 0.75, 1, 1.5, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 14 and 24 hours (Day 38) post-dose

    Blood samples were collected at indicated time points for pharmacokinetic analysis of OCA. Pharmacokinetic parameters were calculated using standard non-compartmental analysis.

  11. Part A- Average Ctrough for OCA: OCA Arm

    Time frame: Day 17: Pre-dose; Day 18: Pre-dose, 0.25, 0.50, 0.75, 1, 1.5, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 14 and 24 hours (Day 19) post-dose

    Blood samples were collected at indicated time points for pharmacokinetic analysis of OCA. Pharmacokinetic parameters were calculated using standard non-compartmental analysis. Average of Ctrough measurement from study Days 17, 18 and 19 has been presented.

  12. Part A- Average Ctrough for OCA: OCA + Linerixibat Arm

    Time frame: Days 35 and 36: Pre-dose; Day 37: Pre-dose, 0.25, 0.50, 0.75, 1, 1.5, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 14 and 24 hours (Day 38) post-dose

    Blood samples were collected at indicated time points for pharmacokinetic analysis of OCA. Pharmacokinetic parameters were calculated using standard non-compartmental analysis. Average of Ctrough measurement from study Days 35, 36, 37 and 38 has been presented.

  13. Part A- Tmax for OCA: OCA Arm

    Time frame: Day 17: Pre-dose; Day 18: Pre-dose, 0.25, 0.50, 0.75, 1, 1.5, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 14 and 24 hours (Day 19) post-dose

    Blood samples were collected at indicated time points for pharmacokinetic analysis of OCA. Pharmacokinetic parameters were calculated using standard non-compartmental analysis.

  14. Part A- Tmax for OCA: OCA + Linerixibat Arm

    Time frame: Days 35 and 36: Pre-dose; Day 37: Pre-dose, 0.25, 0.50, 0.75, 1, 1.5, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 14 and 24 hours (Day 38) post-dose

    Blood samples were collected at indicated time points for pharmacokinetic analysis of OCA. Pharmacokinetic parameters were calculated using standard non-compartmental analysis.

  15. Part A- AUC(0-t) for Tauro-OCA: OCA Arm

    Time frame: Day 17: Pre-dose; Day 18: Pre-dose, 0.25, 0.50, 0.75, 1, 1.5, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 14 and 24 hours (Day 19) post-dose

    Blood samples were collected at indicated time points for pharmacokinetic analysis of tauro-OCA. Pharmacokinetic parameters were calculated using standard non-compartmental analysis.

  16. Part A- AUC(0-t) for Tauro-OCA: OCA + Linerixibat Arm

    Time frame: Days 35 and 36: Pre-dose; Day 37: Pre-dose, 0.25, 0.50, 0.75, 1, 1.5, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 14 and 24 hours (Day 38) post-dose

    Blood samples were collected at indicated time points for pharmacokinetic analysis of tauro-OCA. Pharmacokinetic parameters were calculated using standard non-compartmental analysis.

  17. Part A- AUC(0-24) for Tauro-OCA: OCA Arm

    Time frame: Day 17: Pre-dose; Day 18: Pre-dose, 0.25, 0.50, 0.75, 1, 1.5, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 14 and 24 hours (Day 19) post-dose

    Blood samples were collected at indicated time points for pharmacokinetic analysis of tauro-OCA. Pharmacokinetic parameters were calculated using standard non-compartmental analysis.

  18. Part A- AUC(0-24) for Tauro-OCA: OCA + Linerixibat Arm

    Time frame: Days 35 and 36: Pre-dose; Day 37: Pre-dose, 0.25, 0.50, 0.75, 1, 1.5, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 14 and 24 hours (Day 38) post-dose

    Blood samples were collected at indicated time points for pharmacokinetic analysis of tauro-OCA. Pharmacokinetic parameters were calculated using standard non-compartmental analysis.

  19. Part A- Cmax for Tauro-OCA: OCA Arm

    Time frame: Day 17: Pre-dose; Day 18: Pre-dose, 0.25, 0.50, 0.75, 1, 1.5, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 14 and 24 hours (Day 19) post-dose

    Blood samples were collected at indicated time points for pharmacokinetic analysis of tauro-OCA. Pharmacokinetic parameters were calculated using standard non-compartmental analysis.

  20. Part A- Cmax for Tauro-OCA: OCA + Linerixibat Arm

    Time frame: Days 35 and 36: Pre-dose; Day 37: Pre-dose, 0.25, 0.50, 0.75, 1, 1.5, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 14 and 24 hours (Day 38) post-dose

    Blood samples were collected at indicated time points for pharmacokinetic analysis of tauro-OCA. Pharmacokinetic parameters were calculated using standard non-compartmental analysis.

  21. Part A- Average Ctrough for Tauro-OCA: OCA Arm

    Time frame: Day 17: Pre-dose; Day 18: Pre-dose, 0.25, 0.50, 0.75, 1, 1.5, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 14 and 24 hours (Day 19) post-dose

    Blood samples were collected at indicated time points for pharmacokinetic analysis of tauro-OCA. Pharmacokinetic parameters were calculated using standard non-compartmental analysis. Average of Ctrough measurement from study Days 17, 18 and 19 has been presented.

  22. Part A- Average Ctrough for Tauro-OCA: OCA + Linerixibat Arm

    Time frame: Days 35 and 36: Pre-dose; Day 37: Pre-dose, 0.25, 0.50, 0.75, 1, 1.5, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 14 and 24 hours (Day 38) post-dose

    Blood samples were collected at indicated time points for pharmacokinetic analysis of tauro-OCA. Pharmacokinetic parameters were calculated using standard non-compartmental analysis. Average of Ctrough measurement from study Days 35, 36, 37 and 38 has been presented.

  23. Part A- Tmax for Tauro-OCA: OCA Arm

    Time frame: Day 17: Pre-dose; Day 18: Pre-dose, 0.25, 0.50, 0.75, 1, 1.5, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 14 and 24 hours (Day 19) post-dose

    Blood samples were collected at indicated time points for pharmacokinetic analysis of tauro-OCA. Pharmacokinetic parameters were calculated using standard non-compartmental analysis.

  24. Part A- Tmax for Tauro-OCA: OCA + Linerixibat Arm

    Time frame: Days 35 and 36: Pre-dose; Day 37: Pre-dose, 0.25, 0.50, 0.75, 1, 1.5, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 14 and 24 hours (Day 38) post-dose

    Blood samples were collected at indicated time points for pharmacokinetic analysis of tauro-OCA. Pharmacokinetic parameters were calculated using standard non-compartmental analysis.

  25. Part A- AUC(0-t) for Glyco-OCA: OCA Arm

    Time frame: Day 17: Pre-dose; Day 18: Pre-dose, 0.25, 0.50, 0.75, 1, 1.5, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 14 and 24 hours (Day 19) post-dose

    Blood samples were collected at indicated time points for pharmacokinetic analysis of glyco-OCA. Pharmacokinetic parameters were calculated using standard non-compartmental analysis.

  26. Part A- AUC(0-t) for Glyco-OCA: OCA + Linerixibat Arm

    Time frame: Days 35 and 36: Pre-dose; Day 37: Pre-dose, 0.25, 0.50, 0.75, 1, 1.5, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 14 and 24 hours (Day 38) post-dose

    Blood samples were collected at indicated time points for pharmacokinetic analysis of glyco-OCA. Pharmacokinetic parameters were calculated using standard non-compartmental analysis.

  27. Part A- AUC(0-24) for Glyco-OCA: OCA Arm

    Time frame: Day 17: Pre-dose; Day 18: Pre-dose, 0.25, 0.50, 0.75, 1, 1.5, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 14 and 24 hours (Day 19) post-dose

    Blood samples were collected at indicated time points for pharmacokinetic analysis of glyco-OCA. Pharmacokinetic parameters were calculated using standard non-compartmental analysis.

  28. Part A- AUC(0-24) for Glyco-OCA: OCA + Linerixibat Arm

    Time frame: Days 35 and 36: Pre-dose; Day 37: Pre-dose, 0.25, 0.50, 0.75, 1, 1.5, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 14 and 24 hours (Day 38) post-dose

    Blood samples were collected at indicated time points for pharmacokinetic analysis of glyco-OCA. Pharmacokinetic parameters were calculated using standard non-compartmental analysis.

  29. Part A- Cmax for Glyco-OCA: OCA Arm

    Time frame: Day 17: Pre-dose; Day 18: Pre-dose, 0.25, 0.50, 0.75, 1, 1.5, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 14 and 24 hours (Day 19) post-dose

    Blood samples were collected at indicated time points for pharmacokinetic analysis of glyco-OCA. Pharmacokinetic parameters were calculated using standard non-compartmental analysis.

  30. Part A- Cmax for Glyco-OCA: OCA + Linerixibat Arm

    Time frame: Days 35 and 36: Pre-dose; Day 37: Pre-dose, 0.25, 0.50, 0.75, 1, 1.5, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 14 and 24 hours (Day 38) post-dose

    Blood samples were collected at indicated time points for pharmacokinetic analysis of glyco-OCA. Pharmacokinetic parameters were calculated using standard non-compartmental analysis.

  31. Part A- Average Ctrough for Glyco-OCA: OCA Arm

    Time frame: Day 17: Pre-dose; Day 18: Pre-dose, 0.25, 0.50, 0.75, 1, 1.5, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 14 and 24 hours (Day 19) post-dose

    Blood samples were collected at indicated time points for pharmacokinetic analysis of glyco-OCA. Pharmacokinetic parameters were calculated using standard non-compartmental analysis. Average of Ctrough measurement from study Days 17, 18 and 19 has been presented.

  32. Part A- Average Ctrough for Glyco-OCA: OCA + Linerixibat Arm

    Time frame: Days 35 and 36: Pre-dose; Day 37: Pre-dose, 0.25, 0.50, 0.75, 1, 1.5, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 14 and 24 hours (Day 38) post-dose

    Blood samples were collected at indicated time points for pharmacokinetic analysis of glyco-OCA. Pharmacokinetic parameters were calculated using standard non-compartmental analysis. Average of Ctrough measurement from study Days 35, 36, 37 and 38 has been presented.

  33. Part A- Tmax for Glyco-OCA: OCA Arm

    Time frame: Day 17: Pre-dose; Day 18: Pre-dose, 0.25, 0.50, 0.75, 1, 1.5, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 14 and 24 hours (Day 19) post-dose

    Blood samples were collected at indicated time points for pharmacokinetic analysis of glyco-OCA. Pharmacokinetic parameters were calculated using standard non-compartmental analysis.

  34. Part A- Tmax for Glyco-OCA: OCA + Linerixibat Arm

    Time frame: Days 35 and 36: Pre-dose; Day 37: Pre-dose, 0.25, 0.50, 0.75, 1, 1.5, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 14 and 24 hours (Day 38) post-dose

    Blood samples were collected at indicated time points for pharmacokinetic analysis of glyco-OCA. Pharmacokinetic parameters were calculated using standard non-compartmental analysis.

  35. Part B- Tmax for Total-OCA: OCA Arm

    Time frame: Day 17: Pre-dose; Day 18: Pre-dose, 0.25, 0.50, 0.75, 1, 1.5, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 14 and 24 hours (Day 19) post-dose

    Blood samples were planned to be collected at indicated time points for pharmacokinetic analysis of total-OCA.

  36. Part B- Tmax for Total-OCA: OCA + Linerixibat Arm

    Time frame: Days 35 and 36: Pre-dose; Day 37: Pre-dose, 0.25, 0.50, 0.75, 1, 1.5, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 14 and 24 hours (Day 38) post-dose

    Blood samples were planned to be collected at indicated time points for pharmacokinetic analysis of total-OCA.

  37. Part B- AUC(0-t) for OCA: OCA Arm

    Time frame: Day 17: Pre-dose; Day 18: Pre-dose, 0.25, 0.50, 0.75, 1, 1.5, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 14 and 24 hours (Day 19) post-dose

    Blood samples were planned to be collected at indicated time points for pharmacokinetic analysis of OCA.

  38. Part B- AUC(0-t) for OCA: OCA + Linerixibat Arm

    Time frame: Days 35 and 36: Pre-dose; Day 37: Pre-dose, 0.25, 0.50, 0.75, 1, 1.5, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 14 and 24 hours (Day 38) post-dose

    Blood samples were planned to be collected at indicated time points for pharmacokinetic analysis of OCA.

  39. Part B- AUC(0-24) for OCA: OCA Arm

    Time frame: Day 17: Pre-dose; Day 18: Pre-dose, 0.25, 0.50, 0.75, 1, 1.5, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 14 and 24 hours (Day 19) post-dose

    Blood samples were planned to be collected at indicated time points for pharmacokinetic analysis of OCA.

  40. Part B- AUC(0-24) for OCA: OCA + Linerixibat Arm

    Time frame: Days 35 and 36: Pre-dose; Day 37: Pre-dose, 0.25, 0.50, 0.75, 1, 1.5, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 14 and 24 hours (Day 38) post-dose

    Blood samples were planned to be collected at indicated time points for pharmacokinetic analysis of OCA.

  41. Part B- Cmax for OCA: OCA Arm

    Time frame: Day 17: Pre-dose; Day 18: Pre-dose, 0.25, 0.50, 0.75, 1, 1.5, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 14 and 24 hours (Day 19) post-dose

    Blood samples were planned to be collected at indicated time points for pharmacokinetic analysis of OCA.

  42. Part B- Cmax for OCA: OCA + Linerixibat Arm

    Time frame: Days 35 and 36: Pre-dose; Day 37: Pre-dose, 0.25, 0.50, 0.75, 1, 1.5, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 14 and 24 hours (Day 38) post-dose

    Blood samples were planned to be collected at indicated time points for pharmacokinetic analysis of OCA.

  43. Part B- Ctrough for OCA: OCA Arm

    Time frame: Day 17: Pre-dose; Day 18: Pre-dose, 0.25, 0.50, 0.75, 1, 1.5, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 14 and 24 hours (Day 19) post-dose

    Blood samples were planned to be collected at indicated time points for pharmacokinetic analysis of OCA.

  44. Part B- Ctrough for OCA: OCA + Linerixibat Arm

    Time frame: Days 35 and 36: Pre-dose; Day 37: Pre-dose, 0.25, 0.50, 0.75, 1, 1.5, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 14 and 24 hours (Day 38) post-dose

    Blood samples were planned to be collected at indicated time points for pharmacokinetic analysis of OCA.

  45. Part B- Tmax for OCA: OCA Arm

    Time frame: Day 17: Pre-dose; Day 18: Pre-dose, 0.25, 0.50, 0.75, 1, 1.5, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 14 and 24 hours (Day 19) post-dose

    Blood samples were planned to be collected at indicated time points for pharmacokinetic analysis of OCA.

  46. Part B- Tmax for OCA: OCA + Linerixibat Arm

    Time frame: Days 35 and 36: Pre-dose; Day 37: Pre-dose, 0.25, 0.50, 0.75, 1, 1.5, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 14 and 24 hours (Day 38) post-dose

    Blood samples were planned to be collected at indicated time points for pharmacokinetic analysis of OCA.

  47. Part B- AUC(0-t) for Tauro-OCA: OCA Arm

    Time frame: Day 17: Pre-dose; Day 18: Pre-dose, 0.25, 0.50, 0.75, 1, 1.5, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 14 and 24 hours (Day 19) post-dose

    Blood samples were planned to be collected at indicated time points for pharmacokinetic analysis of tauro-OCA.

  48. Part B- AUC(0-t) for Tauro-OCA: OCA + Linerixibat Arm

    Time frame: Days 35 and 36: Pre-dose; Day 37: Pre-dose, 0.25, 0.50, 0.75, 1, 1.5, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 14 and 24 hours (Day 38) post-dose

    Blood samples were planned to be collected at indicated time points for pharmacokinetic analysis of tauro-OCA.

  49. Part B- AUC(0-24) for Tauro-OCA: OCA Arm

    Time frame: Day 17: Pre-dose; Day 18: Pre-dose, 0.25, 0.50, 0.75, 1, 1.5, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 14 and 24 hours (Day 19) post-dose

    Blood samples were planned to be collected at indicated time points for pharmacokinetic analysis of tauro-OCA.

  50. Part B- AUC(0-24) for Tauro-OCA: OCA + Linerixibat Arm

    Time frame: Days 35 and 36: Pre-dose; Day 37: Pre-dose, 0.25, 0.50, 0.75, 1, 1.5, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 14 and 24 hours (Day 38) post-dose

    Blood samples were planned to be collected at indicated time points for pharmacokinetic analysis of tauro-OCA.

  51. Part B- Cmax for Tauro-OCA: OCA Arm

    Time frame: Day 17: Pre-dose; Day 18: Pre-dose, 0.25, 0.50, 0.75, 1, 1.5, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 14 and 24 hours (Day 19) post-dose

    Blood samples were planned to be collected at indicated time points for pharmacokinetic analysis of tauro-OCA.

  52. Part B- Cmax for Tauro-OCA: OCA + Linerixibat Arm

    Time frame: Days 35 and 36: Pre-dose; Day 37: Pre-dose, 0.25, 0.50, 0.75, 1, 1.5, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 14 and 24 hours (Day 38) post-dose

    Blood samples were planned to be collected at indicated time points for pharmacokinetic analysis of tauro-OCA.

  53. Part B- Ctrough for Tauro-OCA: OCA Arm

    Time frame: Day 17: Pre-dose; Day 18: Pre-dose, 0.25, 0.50, 0.75, 1, 1.5, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 14 and 24 hours (Day 19) post-dose

    Blood samples were planned to be collected at indicated time points for pharmacokinetic analysis of tauro-OCA.

  54. Part B- Ctrough for Tauro-OCA: OCA + Linerixibat Arm

    Time frame: Days 35 and 36: Pre-dose; Day 37: Pre-dose, 0.25, 0.50, 0.75, 1, 1.5, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 14 and 24 hours (Day 38) post-dose

    Blood samples were planned to be collected at indicated time points for pharmacokinetic analysis of tauro-OCA.

  55. Part B- Tmax for Tauro-OCA: OCA Arm

    Time frame: Day 17: Pre-dose; Day 18: Pre-dose, 0.25, 0.50, 0.75, 1, 1.5, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 14 and 24 hours (Day 19) post-dose

    Blood samples were planned to be collected at indicated time points for pharmacokinetic analysis of tauro-OCA.

  56. Part B- Tmax for Tauro-OCA: OCA + Linerixibat Arm

    Time frame: Days 35 and 36: Pre-dose; Day 37: Pre-dose, 0.25, 0.50, 0.75, 1, 1.5, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 14 and 24 hours (Day 38) post-dose

    Blood samples were planned to be collected at indicated time points for pharmacokinetic analysis of tauro-OCA.

  57. Part B- AUC(0-t) for Glyco-OCA: OCA Arm

    Time frame: Day 17: Pre-dose; Day 18: Pre-dose, 0.25, 0.50, 0.75, 1, 1.5, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 14 and 24 hours (Day 19) post-dose

    Blood samples were planned to be collected at indicated time points for pharmacokinetic analysis of glyco-OCA.

  58. Part B- AUC(0-t) for Glyco-OCA: OCA + Linerixibat Arm

    Time frame: Days 35 and 36: Pre-dose; Day 37: Pre-dose, 0.25, 0.50, 0.75, 1, 1.5, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 14 and 24 hours (Day 38) post-dose

    Blood samples were planned to be collected at indicated time points for pharmacokinetic analysis of glyco-OCA.

  59. Part B- AUC(0-24) for Glyco-OCA: OCA Arm

    Time frame: Day 17: Pre-dose; Day 18: Pre-dose, 0.25, 0.50, 0.75, 1, 1.5, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 14 and 24 hours (Day 19) post-dose

    Blood samples were planned to be collected at indicated time points for pharmacokinetic analysis of glyco-OCA.

  60. Part B- AUC(0-24) for Glyco-OCA: OCA + Linerixibat Arm

    Time frame: Days 35 and 36: Pre-dose; Day 37: Pre-dose, 0.25, 0.50, 0.75, 1, 1.5, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 14 and 24 hours (Day 38) post-dose

    Blood samples were planned to be collected at indicated time points for pharmacokinetic analysis of glyco-OCA.

  61. Part B- Cmax for Glyco-OCA: OCA Arm

    Time frame: Day 17: Pre-dose; Day 18: Pre-dose, 0.25, 0.50, 0.75, 1, 1.5, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 14 and 24 hours (Day 19) post-dose

    Blood samples were planned to be collected at indicated time points for pharmacokinetic analysis of glyco-OCA.

  62. Part B- Cmax for Glyco-OCA: OCA + Linerixibat Arm

    Time frame: Days 35 and 36: Pre-dose; Day 37: Pre-dose, 0.25, 0.50, 0.75, 1, 1.5, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 14 and 24 hours (Day 38) post-dose

    Blood samples were planned to be collected at indicated time points for pharmacokinetic analysis of glyco-OCA.

  63. Part B- Ctrough for Glyco-OCA: OCA Arm

    Time frame: Day 17: Pre-dose; Day 18: Pre-dose, 0.25, 0.50, 0.75, 1, 1.5, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 14 and 24 hours (Day 19) post-dose

    Blood samples were planned to be collected at indicated time points for pharmacokinetic analysis of glyco-OCA.

  64. Part B- Ctrough for Glyco-OCA: OCA + Linerixibat Arm

    Time frame: Days 35 and 36: Pre-dose; Day 37: Pre-dose, 0.25, 0.50, 0.75, 1, 1.5, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 14 and 24 hours (Day 38) post-dose

    Blood samples were planned to be collected at indicated time points for pharmacokinetic analysis of glyco-OCA.

  65. Part B- Tmax for Glyco-OCA: OCA Arm

    Time frame: Day 17: Pre-dose; Day 18: Pre-dose, 0.25, 0.50, 0.75, 1, 1.5, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 14 and 24 hours (Day 19) post-dose

    Blood samples were planned to be collected at indicated time points for pharmacokinetic analysis of glyco-OCA.

  66. Part B- Tmax for Glyco-OCA: OCA + Linerixibat Arm

    Time frame: Days 35 and 36: Pre-dose; Day 37: Pre-dose, 0.25, 0.50, 0.75, 1, 1.5, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 14 and 24 hours (Day 38) post-dose

    Blood samples were planned to be collected at indicated time points for pharmacokinetic analysis of glyco-OCA.

  67. Part A- Number of Participants With Any Adverse Events (AEs) and Serious Adverse Events (SAEs)

    Time frame: Up to Day 52

    An AE is any untoward medical occurrence in a clinical study participant, temporally associated with the use of a study treatment, whether or not considered related to the study treatment. An SAE is defined as any untoward medical occurrence that, at any dose; results in death, is life-threatening, requires inpatient hospitalization or prolongation of existing hospitalization, results in persistent disability/incapacity, is a congenital anomaly/birth defect or any other situation according to medical or scientific judgement. All Participants Population consisted of all participants who took at least 1 dose of study intervention.

  68. Part B- Number of Participants With Any AEs and SAEs

    Time frame: Up to Day 52

    An AE is any untoward medical occurrence in a clinical study participant, temporally associated with the use of a study treatment, whether or not considered related to the study treatment. An SAE is defined as any untoward medical occurrence that, at any dose; results in death, is life-threatening, requires inpatient hospitalization or prolongation of existing hospitalization, results in persistent disability/incapacity, is a congenital anomaly/birth defect or any other situation according to medical or scientific judgement.

  69. Part A- Change From Baseline in PR Interval, QRS Duration, QT Interval, QT Interval Corrected Using Bazzet's Formula (QTcB), Corrected QT Interval Using Fredericia's Formula (QTcF): OCA Arm

    Time frame: Baseline (Day -1), and at Day 17

    Twelve lead electrocardiograms (ECGs) were obtained to measure PR interval, QRS duration, QT interval, QTcB and QTcF. Twelve-lead ECGs were performed with the participant in a supine position after a rest of at least 5 minutes. Baseline was considered as Day -1. Change from Baseline was calculated by subtracting the Baseline value from the post-dose visit value.

  70. Part A- Change From Baseline in PR Interval, QRS Duration, QT Interval, QTcB, QTcF: OCA + Linerixibat Arm

    Time frame: Baseline (Day -1), and at Day 38

    Twelve lead ECGs were obtained to measure PR interval, QRS duration, QT interval, QTcB and QTcF. Twelve-lead ECGs were performed with the participant in a supine position after a rest of at least 5 minutes. Baseline was considered as Day -1. Change from Baseline was calculated by subtracting the Baseline value from the post-dose visit value.

  71. Part B- Change From Baseline in PR Interval, QRS Duration, QT Interval, QTcB, QTcF

    Time frame: Baseline (Day -1), and up to Day 38

    Twelve lead ECGs were planned to be measured PR interval, QRS duration, QT interval, QTcB and QTcF. Twelve-lead ECGs were planned to be performed with the participant in a supine position after a rest of at least 5 minutes.

  72. Part A- Change From Baseline in Systolic Blood Pressure (SBP) and Diastolic Blood Pressure (DBP): OCA Arm

    Time frame: Baseline (Day -1), Days 1 and 17

    SBP and DBP were measured in a supine position after 5 minutes of rest for the participants in a quiet setting without distractions. Baseline was considered as Day -1. Change from Baseline was calculated by subtracting the Baseline value from the post-dose visit value.

  73. Part A- Change From Baseline in SBP and DBP: OCA + Linerixibat Arm

    Time frame: Baseline (Day -1) and at Day 38

    SBP and DBP were measured in a supine position after 5 minutes of rest for the participants in a quiet setting without distractions. Baseline was considered as Day -1. Change from Baseline was calculated by subtracting the Baseline value from the post-dose visit value.

  74. Part A- Change From Baseline in Pulse Rate: OCA Arm

    Time frame: Baseline (Day -1), Days 1 and 17

    Pulse rate was measured in a supine position after 5 minutes of rest for the participants in a quiet setting without distractions. Baseline was considered as Day -1. Change from Baseline was calculated by subtracting the Baseline value from the post-dose visit value.

  75. Part A- Change From Baseline in Pulse Rate: OCA + Linerixibat Arm

    Time frame: Baseline (Day -1) and at Day 38

    Pulse rate was measured in a supine position after 5 minutes of rest for the participants in a quiet setting without distractions. Baseline was considered as Day -1. Change from Baseline was calculated by subtracting the Baseline value from the post-dose visit value.

  76. Part A- Change From Baseline in Respiratory Rate: OCA Arm

    Time frame: Baseline (Day -1), Days 1 and 17

    Respiratory rate was measured in supine position after 5 minutes of rest for the participants in a quiet setting without distractions. Baseline was considered as Day -1. Change from Baseline was calculated by subtracting the Baseline value from the post-dose visit value.

  77. Part A- Change From Baseline in Respiratory Rate: OCA + Linerixibat Arm

    Time frame: Baseline (Day -1) and at Day 38

    Respiratory rate was measured in supine position after 5 minutes of rest for the participants in a quiet setting without distractions. Baseline was considered as Day -1. Change from Baseline was calculated by subtracting the Baseline value from the post-dose visit value.

  78. Part A- Change From Baseline in Body Temperature: OCA Arm

    Time frame: Baseline (Day -1), Days 1 and 17

    Body temperature was measured in supine position after 5 minutes of rest for the participants in a quiet setting without distractions. Baseline was considered as Day -1. Change from Baseline was calculated by subtracting the Baseline value from the post-dose visit value.

  79. Part A- Change From Baseline in Body Temperature: OCA + Linerixibat Arm

    Time frame: Baseline (Day -1) and at Day 38

    Body temperature was measured in supine position after 5 minutes of rest for the participants in a quiet setting without distractions. Baseline was considered as Day -1. Change from Baseline was calculated by subtracting the Baseline value from the post-dose visit value.

  80. Part B- Change From Baseline in SBP and DBP

    Time frame: Baseline (Day -1), and up to Day 38

    SBP and DBP were planned to be measured in a supine position after 5 minutes of rest for the participants in a quiet setting without distractions.

  81. Part B- Change From Baseline in Pulse Rate

    Time frame: Baseline (Day -1), and up to Day 38

    Pulse rate was planned to be measured in a supine position after 5 minutes of rest for the participants in a quiet setting without distractions.

  82. Part B- Change From Baseline in Respiratory Rate

    Time frame: Baseline (Day -1), and up to Day 38

    Respiratory rate was planned to be measured in a supine position after 5 minutes of rest for the participants in a quiet setting without distractions.

  83. Part B- Change From Baseline in Body Temperature

    Time frame: Baseline (Day -1), and up to Day 38

    Body temperature was planned to be measured in a supine position after 5 minutes of rest for the participants in a quiet setting without distractions.

  84. Part A- Change From Baseline in Hematology Parameters: Basophils, Eosinophils, Lymphocytes, Monocytes, Neutrophils, Platelet Count, Leukocytes: OCA Arm

    Time frame: Baseline (Day -1) and at Day 17

    Blood samples were collected to analyze the hematology parameters: basophils, eosinophils, lymphocytes, monocytes, neutrophils, platelet count and leukocytes. Baseline was considered as Day -1. Change from Baseline was calculated by subtracting the Baseline value from the post-dose visit value.

  85. Part A- Change From Baseline in Hematology Parameters: Basophils, Eosinophils, Lymphocytes, Monocytes, Neutrophils, Platelet Count, Leukocytes: OCA + Linerixibat Arm

    Time frame: Baseline (Day -1) and at Day 38

    Blood samples were collected to analyze the hematology parameters: basophils, eosinophils, lymphocytes, monocytes, neutrophils, platelet count and leukocytes. Baseline was considered as Day -1. Change from Baseline was calculated by subtracting the Baseline value from the post-dose visit value.

  86. Part A- Change From Baseline in Hematology Parameter: Hemoglobin: OCA Arm

    Time frame: Baseline (Day -1) and at Day 17

    Blood samples were collected to analyze the hematology parameter: hemoglobin. Baseline was considered as Day -1. Change from Baseline was calculated by subtracting the Baseline value from the post-dose visit value.

  87. Part A- Change From Baseline in Hematology Parameter: Hemoglobin: OCA + Linerixibat Arm

    Time frame: Baseline (Day -1) and at Day 38

    Blood samples were collected to analyze the hematology parameter: hemoglobin. Baseline was considered as Day -1. Change from Baseline was calculated by subtracting the Baseline value from the post-dose visit value.

  88. Part A- Change From Baseline in Hematology Parameter: Hematocrit: OCA Arm

    Time frame: Baseline (Day -1) and at Day 17

    Blood samples were collected to analyze the hematology parameter: hematocrit. Baseline was considered as Day -1. Change from Baseline was calculated by subtracting the Baseline value from the post-dose visit value.

  89. Part A- Change From Baseline in Hematology Parameter: Hematocrit: OCA + Linerixibat Arm

    Time frame: Baseline (Day -1) and at Day 38

    Blood samples were collected to analyze the hematology parameter: hematocrit. Baseline was considered as Day -1. Change from Baseline was calculated by subtracting the Baseline value from the post-dose visit value.

  90. Part A- Change From Baseline in Hematology Parameter: Erythrocytes Mean Corpuscular Hemoglobin: OCA Arm

    Time frame: Baseline (Day -1) and at Day 17

    Blood samples were collected to analyze the hematology parameter: erythrocytes mean corpuscular hemoglobin. Baseline was considered as Day -1. Change from Baseline was calculated by subtracting the Baseline value from the post-dose visit value.

  91. Part A- Change From Baseline in Hematology Parameter: Erythrocytes Mean Corpuscular Hemoglobin: OCA + Linerixibat Arm

    Time frame: Baseline (Day -1) and at Day 38

    Blood samples were collected to analyze the hematology parameter: erythrocytes mean corpuscular hemoglobin. Baseline was considered as Day -1. Change from Baseline was calculated by subtracting the Baseline value from the post-dose visit value.

  92. Part A- Change From Baseline in Hematology Parameter: Erythrocytes Mean Corpuscular Volume: OCA Arm

    Time frame: Baseline (Day -1) and at Day 17

    Blood samples were collected to analyze the hematology parameter: erythrocytes mean corpuscular volume. Baseline was considered as Day -1. Change from Baseline was calculated by subtracting the Baseline value from the post-dose visit value.

  93. Part A- Change From Baseline in Hematology Parameter: Erythrocytes Mean Corpuscular Volume: OCA + Linerixibat Arm

    Time frame: Baseline (Day -1) and at Day 38

    Blood samples were collected to analyze the hematology parameter: erythrocytes mean corpuscular volume. Baseline was considered as Day -1. Change from Baseline was calculated by subtracting the Baseline value from the post-dose visit value.

  94. Part A- Change From Baseline in Hematology Parameters: Erythrocytes, Reticulocytes: OCA Arm

    Time frame: Baseline (Day -1) and at Day 17

    Blood samples were collected to analyze the hematology parameters: erythrocytes and reticulocytes. Baseline was considered as Day -1. Change from Baseline was calculated by subtracting the Baseline value from the post-dose visit value.

  95. Part A- Change From Baseline in Hematology Parameters: Erythrocytes, Reticulocytes: OCA + Linerixibat Arm

    Time frame: Baseline (Day -1) and at Day 38

    Blood samples were collected to analyze the hematology parameters: erythrocytes and reticulocytes. Baseline was considered as Day -1. Change from Baseline was calculated by subtracting the Baseline value from the post-dose visit value.

  96. Part B- Change From Baseline in Hematology Parameters: Basophils, Eosinophils, Lymphocytes, Monocytes, Neutrophils, Platelet Count, Leukocytes

    Time frame: Baseline (Day -1), and up to Day 38

    Blood samples were planned to be collected to analyze the hematology parameters: basophils, eosinophils, lymphocytes, monocytes, neutrophils, platelet count and leukocytes.

  97. Part B- Change From Baseline in Hematology Parameter: Hemoglobin

    Time frame: Baseline (Day -1), and up to Day 38

    Blood samples were planned to be collected to analyze the hematology parameter: hemoglobin.

  98. Part B- Change From Baseline in Hematology Parameter: Hematocrit

    Time frame: Baseline (Day -1), and up to Day 38

    Blood samples were planned to be collected to analyze the hematology parameter: hematocrit.

  99. Part B- Change From Baseline in Hematology Parameter: Erythrocytes Mean Corpuscular Hemoglobin

    Time frame: Baseline (Day -1), and up to Day 38

    Blood samples were planned to be collected to analyze the hematology parameter: erythrocytes mean corpuscular hemoglobin.

  100. Part B- Change From Baseline in Hematology Parameter: Erythrocytes Mean Corpuscular Volume

    Time frame: Baseline (Day -1), and up to Day 38

    Blood samples were planned to be collected to analyze the hematology parameter: erythrocytes mean corpuscular volume.

  101. Part B- Change From Baseline in Hematology Parameters: Erythrocytes, Reticulocytes

    Time frame: Baseline (Day -1), and up to Day 38

    Blood samples were planned to be collected to analyze the hematology parameters: erythrocytes and reticulocytes.

  102. Part A- Change From Baseline in Chemistry Parameters: Glucose, Calcium, Potassium, Sodium, Urea: OCA Arm

    Time frame: Baseline (Day -1) and at Day 17

    Blood samples were collected to analyze the chemistry parameters: glucose, calcium, potassium, sodium and urea. Baseline was considered as Day -1. Change from Baseline was calculated by subtracting the Baseline value from the post-dose visit value.

  103. Part A- Change From Baseline in Chemistry Parameters: Glucose, Calcium, Potassium, Sodium, Urea: OCA + Linerixibat Arm

    Time frame: Baseline (Day -1) and at Day 38

    Blood samples were collected to analyze the chemistry parameters: glucose, calcium, potassium, sodium and urea. Baseline was considered as Day -1. Change from Baseline was calculated by subtracting the Baseline value from the post-dose visit value.

  104. Part A- Change From Baseline in Chemistry Parameters: Bilirubin, Creatinine, Direct Bilirubin: OCA Arm

    Time frame: Baseline (Day -1) and at Day 17

    Blood samples were collected to analyze the chemistry parameters: bilirubin, creatinine and direct bilirubin. Baseline was considered as Day -1. Change from Baseline was calculated by subtracting the Baseline value from the post-dose visit value.

  105. Part A- Change From Baseline in Chemistry Parameters: Bilirubin, Creatinine, Direct Bilirubin: OCA + Linerixibat Arm

    Time frame: Baseline (Day -1) and at Day 38

    Blood samples were collected to analyze the chemistry parameters: bilirubin, creatinine and direct bilirubin. Baseline was considered as Day -1. Change from Baseline was calculated by subtracting the Baseline value from the post-dose visit value.

  106. Part A- Change From Baseline in Chemistry Parameters: Alanine Aminotransferase (ALT), Alkaline Phosphatase (ALP), Aspartate Aminotransferase (AST): OCA Arm

    Time frame: Baseline (Day -1) and at Day 17

    Blood samples were collected to analyze the chemistry parameters: ALT, ALP and AST. Baseline was considered as Day -1. Change from Baseline was calculated by subtracting the Baseline value from the post-dose visit value.

  107. Part A- Change From Baseline in Chemistry Parameters: ALT, ALP, AST: OCA + Linerixibat Arm

    Time frame: Baseline (Day -1) and at Day 38

    Blood samples were collected to analyze the chemistry parameters: ALT, ALP and AST. Baseline was considered as Day -1. Change from Baseline was calculated by subtracting the Baseline value from the post-dose visit value.

  108. Part A- Change From Baseline in Chemistry Parameter: Protein: OCA Arm

    Time frame: Baseline (Day -1) and at Day 17

    Blood samples were collected to analyze the chemistry parameter: protein. Baseline was considered as Day -1. Change from Baseline was calculated by subtracting the Baseline value from the post-dose visit value.

  109. Part A- Change From Baseline in Chemistry Parameter: Protein: OCA + Linerixibat Arm

    Time frame: Baseline (Day -1) and at Day 38

    Blood samples were collected to analyze the chemistry parameter: protein. Baseline was considered as Day -1. Change from Baseline was calculated by subtracting the Baseline value from the post-dose visit value.

  110. Part B- Change From Baseline in Chemistry Parameters: Glucose, Calcium, Potassium, Sodium, Urea

    Time frame: Baseline (Day -1), and up to Day 38

    Blood samples were planned to be collected to analyze the chemistry parameters: glucose, calcium, potassium, sodium and urea.

  111. Part B- Change From Baseline in Chemistry Parameters: Bilirubin, Creatinine, Direct Bilirubin

    Time frame: Baseline (Day -1), and up to Day 38

    Blood samples were planned to be collected to analyze the chemistry parameters: bilirubin, creatinine and direct bilirubin.

  112. Part B- Change From Baseline in Chemistry Parameters: ALT, ALP, AST

    Time frame: Baseline (Day -1), and up to Day 38

    Blood samples were planned to be collected to analyze the chemistry parameters: ALT, ALP and AST.

  113. Part B- Change From Baseline in Chemistry Parameter: Protein

    Time frame: Baseline (Day -1), and up to Day 38

    Blood samples were planned to be collected to analyze the chemistry parameter: protein.

  114. Part A- Number of Participants With Worst Case Urinalysis Results Post-Baseline Relative to Baseline: OCA Arm

    Time frame: Baseline (Day -1) and at Day 17

    Urine samples were collected from participants for urinalysis for measuring potential of hydrogen (pH) and glucose, protein, blood, ketones, bilirubin, urobilinogen, nitrite, leukocytes levels by dipstick. Abnormal urinalysis was sent for microscopic examination for cellular casts, erythrocytes, granular casts, hyaline casts, and leukocytes and were counted as cells per high-power field (cells/HPF). Baseline was considered as Day -1. Number of participants with worst case urinalysis result by microscopic examination have been presented.

  115. Part A- Number of Participants With Worst Case Urinalysis Results Post-Baseline Relative to Baseline: OCA + Linerixibat Arm

    Time frame: Baseline (Day -1) and at Day 38

    Urine samples were collected from participants for urinalysis for measuring pH and glucose, protein, blood, ketones, bilirubin, urobilinogen, nitrite, leukocytes levels by dipstick. Abnormal urinalysis was sent for microscopic examination for cellular casts, erythrocytes, granular casts, hyaline casts, and leukocytes and were counted as cells/HPF. Baseline was considered as Day -1. Number of participants with worst case urinalysis result by microscopic examination have been presented.

  116. Part B- Number of Participants With Worst Case Urinalysis Results Post-Baseline Relative to Baseline

    Time frame: Baseline (Day -1), and up to Day 38

    Urine samples were planned to be collected from participants for urinalysis for measuring pH and glucose, protein, blood, ketones, bilirubin, urobilinogen, nitrite, leukocytes levels by dipstick. Abnormal urinalysis was planned to be sent for microscopic examination for cellular casts, erythrocytes, granular casts, hyaline casts, and leukocytes.

  117. Part A- AUC(0-t) for Linerixibat: OCA + Linerixibat Arm

    Time frame: Days 20 and 33: Pre-dose, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11 and 12 hours post-dose

    Blood samples were collected at indicated time points for pharmacokinetic analysis of linerixibat. Pharmacokinetic parameters were analyzed using standard non-compartmental methods.

  118. Part A- Area Under the Concentration-time Curve From Time Zero to 12 Hours (AUC[0-12]) for Linerixibat: OCA + Linerixibat Arm

    Time frame: Days 20 and 33: Pre-dose, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11 and 12 hours post-dose

    Blood samples were collected at indicated time points for pharmacokinetic analysis of linerixibat. Pharmacokinetic parameters were analyzed using standard non-compartmental methods.

  119. Part A- Cmax for Linerixibat: OCA + Linerixibat Arm

    Time frame: Days 20 and 33: Pre-dose, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11 and 12 hours post-dose

    Blood samples were collected at indicated time points for pharmacokinetic analysis of linerixibat. Pharmacokinetic parameters were analyzed using standard non-compartmental methods.

  120. Part A- Tmax for Linerixibat: OCA + Linerixibat Arm

    Time frame: Days 20 and 33: Pre-dose, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11 and 12 hours post-dose

    Blood samples were collected at indicated time points for pharmacokinetic analysis of linerixibat. Pharmacokinetic parameters were analyzed using standard non-compartmental methods.

  121. Part B- AUC(0-t) for Linerixibat: OCA + Linerixibat Arm

    Time frame: Days 20 and 33: Pre-dose, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11 and 12 hours post-dose

    Blood samples were planned to be collected at indicated time points for pharmacokinetic analysis of linerixibat.

  122. Part B- AUC(0-12) for Linerixibat: OCA + Linerixibat Arm

    Time frame: Days 20 and 33: Pre-dose, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11 and 12 hours post-dose

    Blood samples were planned to be collected at indicated time points for pharmacokinetic analysis of linerixibat.

  123. Part B- Cmax for Linerixibat: OCA + Linerixibat Arm

    Time frame: Days 20 and 33: Pre-dose, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11 and 12 hours post-dose

    Blood samples were planned to be collected at indicated time points for pharmacokinetic analysis of linerixibat.

  124. Part B- Tmax for Linerixibat: OCA + Linerixibat Arm

    Time frame: Days 20 and 33: Pre-dose, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11 and 12 hours post-dose

    Blood samples were planned to be collected at indicated time points for pharmacokinetic analysis of linerixibat.

Sponsors and collaborators

Lead sponsor

GlaxoSmithKline

Industry

Registry information

Official study title

An Open-label, Single Sequence Crossover, Drug Interaction Study to Investigate the Effect of Linerixibat (GSK2330672) on Plasma Concentrations of Obeticholic Acid and Conjugates in Healthy Participants

Important dates

Study start
2019
Primary completion
2019
Study completion
2019
First posted
Aug 12, 2019
Registry last updated
Jul 24, 2020

OpenTrials presents study information sourced from ClinicalTrials.gov. The official registry record should be consulted for the latest information.

View the official ClinicalTrials.gov record (opens in a new tab)

This listing is for discovery and informational purposes only. It is not medical advice, does not guarantee that a study is recruiting, and does not determine eligibility. Contact the study team and a qualified healthcare professional when considering participation.

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