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Completed

NCT Number: NCT03078556

Bioequivalence Study of Fixed Dose Versus Single Entities of Dolutegravir and Lamivudine

This study aims to compare the bioequivalence of two experimental fixed dose combination (FDC) tablets versus single entity products of dolutegravir (DTG) and lamivudine (3TC) in healthy adult subjects. The study will be carried out in two parts. Part 1 of the study will be open label, up to 3 periods design with a wash out period of at least 7 days between treatment periods. Subjects will be randomized to receive either single entities or formulation 1 FDC of DTG and 3TC in a crossover manner in first 2 periods. The first 16 subjects who complete the first two treatment periods and consent to continue will receive a single dose of FDC formulation 1 tablet administered with a high fat meal for a third treatment period. In Part 2 of the study, subjects will be randomized to receive either single entities or formulation 2 FDC of DTG and 3TC in a crossover manner in first 2 periods. Similarly the first 16 subjects will then receive FDC formulation 2 tablets with high fat meal in treatment period 3. Subjects will have a follow-up visit within 7-14 days after the last dose of study drug. Approximately 76 healthy subjects will be included in Part 1 of the study and if Part 2 of the study is conducted, another 76 healthy subjects will be included. The total duration will be approximately 11 weeks.

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Key information

Conditions

Infection, Human Immunodeficiency Virus Acquired Immunodeficiency Syndrome Blood-Borne Infections Communicable Diseases Genital Diseases HIV Infections Immune System Diseases Immunologic Deficiency Syndromes Infections Lentivirus Infections RNA Virus Infections Retroviridae Infections Sexually Transmitted Diseases Sexually Transmitted Diseases, Viral Slow Virus Diseases Urogenital Diseases Virus Diseases

Age range

18 year–55 year

Sex eligibility

All sexes

Study type

Interventional

Phase

Phase 1

Primary location

GSK Investigational Site

Overland Park, Kansas, 66211, United States

Who can participate

Healthy volunteers accepted: Yes

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

Inclusion criteria

  • Between 18 and 55 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, laboratory tests and cardiac evaluation (history, electrocardiogram [ECG]).
  • A subject with a clinical abnormality or laboratory parameter(s) which is/are not specifically listed in the inclusion or exclusion criteria, outside the reference range for the population being studied may be included only if the investigator, in consultation with the Medical Monitor if required, agree and document that the finding is unlikely to introduce additional risk factors and will not interfere with the study procedures.
  • Subject must be able to swallow 2 tablets at the same time (Reference tablets only).
  • Body weight >=50 kilogram (kg) for men and >=45 kg for women and body mass index (BMI) within the range 18.5-31.0 kg per meter square (kg/m^2).
  • Male or Female. Female subject: is eligible to participate if she is not pregnant (as confirmed by a negative serum or urine human chorionic gonadotrophin [hCG] test), not lactating, and at least one of the following conditions applies: 1. non-reproductive potential defined as: pre-menopausal females with one of the following: documented tubal ligation; documented hysteroscopic tubal occlusion procedure with follow-up confirmation of bilateral tubal occlusion; hysterectomy; documented bilateral Oophorectomy. Postmenopausal defined as 12 months of spontaneous amenorrhea; in questionable cases a blood sample with simultaneous follicle stimulating hormone (FSH) and estradiol levels consistent with menopause. Females on hormone replacement therapy (HRT) and whose menopausal status is in doubt will be required to use one of the highly effective contraception methods if they wish to continue their HRT during the study. Otherwise, they must discontinue HRT to allow confirmation of post-menopausal status prior to study enrolment. 2. Reproductive potential and agrees to follow one of the options listed in the Modified List of Highly Effective Methods for Avoiding Pregnancy in Females of Reproductive Potential (FRP) from 30 days prior to the first dose of study medication and until at least five terminal half-lives OR until any continuing pharmacologic effect has ended, whichever is longer after the last dose of study medication and completion of the follow-up visit.
  • Capable of giving signed informed consent which includes compliance with the requirements and restrictions.

Exclusion criteria

  • Alanine aminotransferase (ALT) and bilirubin >1.5x upper limit of normal (ULN) (isolated bilirubin >1.5xULN is acceptable if bilirubin is fractionated and direct bilirubin <35 percentage).
  • Current or chronic history of liver disease, or known hepatic or biliary abnormalities (with the exception of Gilbert's syndrome or asymptomatic gallstones).
  • QT interval corrected for heart rate according to Fridericia's formula (QTcF) > 450 milliseconds (msec).
  • Unable to refrain from the use of prescription or non-prescription drugs, including vitamins, herbal and dietary supplements (including St John's Wort) within 7 days (or 14 days if the drug is a potential enzyme inducer) or 5 half-lives (whichever is longer) prior to the first dose of study medication, unless in the opinion of the Investigator and ViiV Medical Monitor the medication will not interfere with the study procedures or compromise subject safety.
  • History of regular alcohol consumption within 6 months of the study defined as: An average weekly intake of >14 drinks for males or >7 drinks for females. One drink is equivalent to 12 gram (g) of alcohol: 12 ounces [360 milliliter (mL)] of beer, 5 ounces (150 mL) of wine or 1.5 ounces (45 mL) of 80 proof distilled spirits.
  • Urinary cotinine levels indicative of smoking or history or regular use of tobacco- or nicotine-containing products within 1 month prior to screening.
  • History of sensitivity to any of the study medications, or components thereof or a history of drug or other allergy that, in the opinion of the investigator or Medical Monitor, contraindicates their participation.
  • Creatinine clearance (CrCL) <90 mL/minute.
  • A positive hepatitis B surface antigen (HBsAg) or a positive hepatitis B core antibody with a negative hepatitis B surface antibody, positive hepatitis C antibody test result at screening or within 3 months prior to first dose of study treatment.
  • A positive pre-study drug/alcohol screen.
  • A positive test for HIV antibody.
  • Where participation in the study would result in donation of blood or blood product in excess of 500 mL within 56 days.
  • The subject has participated in a clinical trial and has received an investigational product within the following time period prior to the first dosing day in the current study: 30 days, 5 half-lives or twice the duration of the biological effect of the investigational product (whichever is longer).
  • Exposure to more than four new chemical entities within 12 months prior to the first dosing day.

Treatment and study plan

Dolutegravir

Drug

Single dose of DTG 50 mg tablet along with 3TC (EPIVIR) tablet will be given to randomized subjects in parts 1 and 2 with 240 mL of room temperature water. DTG will be a white, film coated, round tablet engraved with SV 572 on one side and 50 on the other side.

Lamivudine

Drug

Single dose 3TC (commercial name: EPIVIR) 300 mg tablet along with DTG tablet will be given to randomized subjects in parts 1 and 2 with 240 mL of room temperature water.<br>3TC will be gray, diamond shaped tablet, engraved "GX EJ7" on one side and plain on the other side.

Dolutegravir + Lamivudine FDC Formulation 1

Drug

Single dose of DTG 50 mg combined with 3TC 300 mg in a FDC formulation 1 tablet will be administered to randomized subjects in treatment periods 1 and 2 (under fasted state) of Part 1 and the first 16 subjects in treatment period 3 (under fed) of Part 1 with 240 mL of room temperature water. &lt;br&gt;FDC formulation 1 tablets will be oval, biconvex, white, film coated tablet engraved 'SV H7I' on one face.

Dolutegravir + Lamivudine FDC Formulation 2

Drug

Single dose of DTG 50 mg combined with 3TC 300 mg in a FDC formulation 2 tablet will be administered to randomized subjects in treatment periods 1 and 2 (under fasted state) and the first 16 subjects in treatment period 3 (under fed) of Part 2 with 240 mL of room temperature water. &lt;br&gt;FDC formulation 2 tablets will be oval, biconvex, white, film coated tablet engraved 'SV 13N' on one face.

Primary outcomes

  1. Area Under the Concentration-time Curve From Time 0 Extrapolated to Infinity [AUC (0-Inf)] of Plasma DTG and 3TC in the Fasted State: Part 1

    Time frame: Pre-dose and 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 3.5, 4, 5, 6, 8, 12, 16, 24, 48 and 72 hours post-dose

    Blood samples were collected at indicated time points to study the pharmacokinetic (PK) profile of DTG and 3TC when administered as FDC tablet compared to co-administration of separate tablet formulations of DTG and 3TC in fasted state. The 4-hour post-dose sample was drawn prior to the participant's first post-dose meal. At each time point, 2 mL of blood was collected. PK parameters of monolayer FDC tablet formulation of DTG and 3TC was evaluated under fasted condition in Periods 1 and 2 of Part 1.

  2. AUC (0-Inf) of Plasma DTG and 3TC in the Fasted State: Part 2

    Time frame: Pre-dose and 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 3.5, 4, 5, 6, 8, 12, 16, 24, 48 and 72 hours post-dose

    Blood samples were collected at given time points to study the PK profile of DTG and 3TC when administered as FDC tablet compared to co-administration of separate tablet formulations of DTG and 3TC in fasted state. The 4-hour post-dose sample was drawn prior to the participant's first post-dose meal. At each time point, 2 mL of blood was collected. PK parameters of bilayer FDC tablet formulation of DTG and 3TC was evaluated under fasted conditions in Periods 1 and 2 of Part 2.

  3. Area Under the Concentration-time Curve From Time 0 to the Last Quantifiable Time Point (AUC[0-t]) of Plasma DTG and 3TC in the Fasted State: Part 1

    Time frame: Pre-dose and 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 3.5, 4, 5, 6, 8, 12, 16, 24, 48 and 72 hours post-dose

    Blood samples were collected at indicated time points to study the PK profile of DTG and 3TC when administered as FDC tablet compared to co-administration of separate tablet formulations of DTG and 3TC in fasted state. The 4-hour post-dose sample was drawn prior to the participant's first post-dose meal. At each time point, 2 mL of blood was collected. PK parameters of monolayer FDC tablet formulation of DTG and 3TC was evaluated under fasted condition in Periods 1 and 2 of Part 1.

  4. AUC(0-t) of Plasma DTG and 3TC in the Fasted State: Part 2

    Time frame: Pre-dose and 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 3.5, 4, 5, 6, 8, 12, 16, 24, 48 and 72 hours post-dose

    Blood samples were collected at indicated time points to study the PK profile of DTG and 3TC when administered as FDC tablet compared to co-administration of separate tablet formulations of DTG and 3TC in fasted state. The 4-hour post-dose sample was drawn prior to the participant's first post-dose meal. At each time point, 2 mL of blood was collected. PK parameters of bilayer FDC tablet formulation of DTG and 3TC was evaluated under fasted condition in Periods 1 and 2 of Part 2.

  5. Maximum Observed Concentration (Cmax) of Plasma DTG and 3TC in the Fasted State: Part 1

    Time frame: Pre-dose and 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 3.5, 4, 5, 6, 8, 12, 16, 24, 48 and 72 hours post-dose

    Blood samples were collected at indicated time points to study the PK profile of DTG and 3TC when administered as FDC tablet compared to co-administration of separate tablet formulations of DTG and 3TC in fasted state. The 4-hour post-dose sample was drawn prior to the participant's first post-dose meal. At each time point, 2 mL of blood was collected. PK parameters of monolayer FDC tablet formulation of DTG and 3TC was evaluated under fasted condition in Periods 1 and 2 of Part 1.

  6. Cmax of Plasma DTG and 3TC in the Fasted State: Part 2

    Time frame: Pre-dose and 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 3.5, 4, 5, 6, 8, 12, 16, 24, 48 and 72 hours post-dose

    Blood samples were collected at indicated time points to study the PK profile of DTG and 3TC when administered as FDC tablet compared to co-administration of separate tablet formulations of DTG and 3TC in fasted state. The 4-hour post-dose sample was drawn prior to the participant's first post-dose meal. At each time point, 2 mL of blood was collected. PK parameters of bilayer FDC tablet formulation of DTG and 3TC was evaluated under fasted condition in Periods 1 and 2 of Part 2.

Secondary outcomes

  1. Absorption Lag Time (Tlag) of DTG and 3TC in Fasted State: Part 1

    Time frame: Pre-dose and 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 3.5, 4, 5, 6, 8, 12, 16, 24, 48 and 72 hours post-dose

    Blood samples were collected at indicated time points to study the PK profile of DTG and 3TC when administered as FDC tablet compared to co-administration of separate tablet formulations of DTG and 3TC in fasted state. The 4-hour post-dose sample was drawn prior to the participant's first post-dose meal. At each time point, 2 mL of blood was collected. PK parameters of monolayer FDC tablet formulation of DTG and 3TC was evaluated under fasted condition in Periods 1 and 2 of Part 1.

  2. Tlag of DTG and 3TC in Fasted State: Part 2

    Time frame: Pre-dose and 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 3.5, 4, 5, 6, 8, 12, 16, 24, 48 and 72 hours post-dose

    Blood samples were collected at indicated time points to study the PK profile of DTG and 3TC when administered as FDC tablet compared to co-administration of separate tablet formulations of DTG and 3TC in fasted state. The 4-hour post-dose sample was drawn prior to the participant's first post-dose meal. At each time point, 2 mL of blood was collected. PK parameters of bilayer FDC tablet formulation of DTG and 3TC was evaluated under fasted condition in Periods 1 and 2 of Part 2.

  3. Time to Reach Maximum Plasma Concentration (Tmax) of DTG and 3TC in the Fasted State: Part 1

    Time frame: Pre-dose and 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 3.5, 4, 5, 6, 8, 12, 16, 24, 48 and 72 hours post-dose

    Blood samples were collected at indicated time points to study the PK profile of DTG and 3TC when administered as FDC tablet compared to co-administration of separate tablet formulations of DTG and 3TC in fasted state. The 4-hour post-dose sample was drawn prior to the participant's first post-dose meal. At each time point, 2 mL of blood was collected. PK parameters of monolayer FDC tablet formulation of DTG and 3TC was evaluated under fasted condition in Periods 1 and 2 of Part 1.

  4. Tmax of DTG and 3TC in the Fasted State: Part 2

    Time frame: Pre-dose and 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 3.5, 4, 5, 6, 8, 12, 16, 24, 48 and 72 hours post-dose

    Blood samples were collected at indicated time points to study the PK profile of DTG and 3TC when administered as FDC tablet compared to co-administration of separate tablet formulations of DTG and 3TC in fasted state. The 4-hour post-dose sample was drawn prior to the participant's first post-dose meal. At each time point, 2 mL of blood was collected. PK parameters of bilayer FDC tablet formulation of DTG and 3TC was evaluated under fasted condition in Periods 1 and 2 of Part 2

  5. Time of the Last Quantifiable Concentration (Tlast) of DTG and 3TC in the Fasted State: Part 1

    Time frame: Pre-dose and 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 3.5, 4, 5, 6, 8, 12, 16, 24, 48 and 72 hours post-dose

    Blood samples were collected at indicated time points to study the PK profile of DTG and 3TC when administered as FDC tablet compared to co-administration of separate tablet formulations of DTG and 3TC in fasted state. The 4-hour post-dose sample was drawn prior to the participant's first post-dose meal. At each time point, 2 mL of blood was collected. PK parameters of monolayer FDC tablet formulation of DTG and 3TC was evaluated under fasted condition in Periods 1 and 2 of Part 1.

  6. Tlast of DTG and 3TC in the Fasted State: Part 2

    Time frame: Pre-dose and 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 3.5, 4, 5, 6, 8, 12, 16, 24, 48 and 72 hours post-dose

    Blood samples were collected at indicated time points to study the PK profile of DTG and 3TC when administered as FDC tablet compared to co-administration of separate tablet formulations of DTG and 3TC in fasted state. The 4-hour post-dose sample was drawn prior to the participant's first post-dose meal. At each time point, 2 mL of blood was collected. PK parameters of bilayer FDC tablet formulation of DTG and 3TC was evaluated under fasted condition in Periods 1 and 2 of Part 2

  7. Time to Reach Half the Maximum Plasma Concentration (t1/2) of DTG and 3TC in the Fasted State: Part 1

    Time frame: Pre-dose and 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 3.5, 4, 5, 6, 8, 12, 16, 24, 48 and 72 hours post-dose

    Blood samples were collected at indicated time points to study the PK profile of DTG and 3TC when administered as FDC tablet compared to co-administration of separate tablet formulations of DTG and 3TC in fasted state. The 4-hour post-dose sample was drawn prior to the participant's first post-dose meal. At each time point, 2 mL of blood was collected. PK parameters of monolayer FDC tablet formulation of DTG and 3TC was evaluated under fasted condition in Periods 1 and 2 of Part 1.

  8. t1/2 of DTG and 3TC in the Fasted State: Part 2

    Time frame: Pre-dose and 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 3.5, 4, 5, 6, 8, 12, 16, 24, 48 and 72 hours post-dose

    Blood samples were collected at indicated time points to study the PK profile of DTG and 3TC when administered as FDC tablet compared to co-administration of separate tablet formulations of DTG and 3TC in fasted state. The 4-hour post-dose sample was drawn prior to the participant's first post-dose meal. At each time point, 2 mL of blood was collected. PK parameters of bilayer FDC tablet formulation of DTG and 3TC was evaluated under fasted condition in Periods 1 and 2 of Part 2

  9. Apparent Elimination Rate Constant (Lambda z) of DTG and 3TC in the Fasted State: Part 1

    Time frame: Pre-dose and 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 3.5, 4, 5, 6, 8, 12, 16, 24, 48 and 72 hours post-dose

    Blood samples were collected at indicated time points to study the PK profile of DTG and 3TC when administered as FDC tablet compared to co-administration of separate tablet formulations of DTG and 3TC in fasted state. The 4-hour post-dose sample was drawn prior to the participant's first post-dose meal. At each time point, 2 mL of blood was collected. PK parameters of monolayer FDC tablet formulation of DTG and 3TC was evaluated under fasted condition in Periods 1 and 2 of Part 1.

  10. Lambda z of DTG and 3TC in in the Fasted State: Part 2

    Time frame: Pre-dose and 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 3.5, 4, 5, 6, 8, 12, 16, 24, 48 and 72 hours post-dose

    Blood samples were collected at indicated time points to study the PK profile of DTG and 3TC when administered as FDC tablet compared to co-administration of separate tablet formulations of DTG and 3TC in fasted state. The 4-hour post-dose sample was drawn prior to the participant's first post-dose meal. At each time point, 2 mL of blood was collected. PK parameters of bilayer FDC tablet formulation of DTG and 3TC was evaluated under fasted condition in Periods 1 and 2 of Part 2.

  11. Percentage of Extrapolated AUC (0 to Inf) of DTG and 3TC in the Fasted State: Part 1

    Time frame: Pre-dose and 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 3.5, 4, 5, 6, 8, 12, 16, 24, 48 and 72 hours post-dose

    Blood samples were collected at indicated time points to study the PK profile of DTG and 3TC when administered as FDC tablet compared to co-administration of separate tablet formulations of DTG and 3TC in fasted state. The 4-hour post-dose sample was drawn prior to the participant's first post-dose meal. At each time point, 2 mL of blood was collected. PK parameters of monolayer FDC tablet formulation of DTG and 3TC was evaluated under fasted condition in Periods 1 and 2 of Part 1.

  12. Percentage of Extrapolated AUC(0 to Inf) of DTG and 3TC in the Fasted State: Part 2

    Time frame: Pre-dose and 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 3.5, 4, 5, 6, 8, 12, 16, 24, 48 and 72 hours post-dose

    Blood samples were collected at indicated time points to study the PK profile of DTG and 3TC when administered as FDC tablet compared to co-administration of separate tablet formulations of DTG and 3TC in fasted state. The 4-hour post-dose sample was drawn prior to the participant's first post-dose meal. At each time point, 2 mL of blood was collected. PK parameters of bilayer FDC tablet formulation of DTG and 3TC was evaluated under fasted condition in Periods 1 and 2 of Part 2.

  13. AUC of 0 to 24 Hours (AUC[0-24]) of DTG and 3TC in the Fasted State: Part 1

    Time frame: Pre-dose and 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 3.5, 4, 5, 6, 8, 12, 16, 24, 48 and 72 hours post-dose

    Blood samples were collected at indicated time points to study the PK profile of DTG and 3TC when administered as FDC tablet compared to co-administration of separate tablet formulations of DTG and 3TC in fasted state. The 4-hour post-dose sample was drawn prior to the participant's first post-dose meal. At each time point, 2 mL of blood was collected. PK parameters of monolayer FDC tablet formulation of DTG and 3TC was evaluated under fasted condition in Periods 1 and 2 of Part 1.

  14. AUC(0-24) of DTG and 3TC in the Fasted State: Part 2

    Time frame: Pre-dose and 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 3.5, 4, 5, 6, 8, 12, 16, 24, 48 and 72 hours post-dose

    Blood samples were collected at indicated time points to study the PK profile of DTG and 3TC when administered as FDC tablet compared to co-administration of separate tablet formulations of DTG and 3TC in fasted state. The 4-hour post-dose sample was drawn prior to the participant's first post-dose meal. At each time point, 2 mL of blood was collected. PK parameters of bilayer FDC tablet formulation of DTG and 3TC was evaluated under fasted condition in Periods 1 and 2 of Part 2.

  15. Apparent Oral Clearance (CL/F) of DTG and 3TC in the Fasted State: Part 1

    Time frame: Pre-dose and 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 3.5, 4, 5, 6, 8, 12, 16, 24, 48 and 72 hours post-dose

    Blood samples were collected at indicated time points to study the PK profile of DTG and 3TC when administered as FDC tablet compared to co-administration of separate tablet formulations of DTG and 3TC in fasted state. The 4-hour post-dose sample was drawn prior to the participant's first post-dose meal. At each time point, 2 mL of blood was collected. PK parameters of monolayer FDC tablet formulation of DTG and 3TC was evaluated under fasted condition in Periods 1 and 2 of Part 1.

  16. CL/F of DTG and 3TC in the Fasted State: Part 2

    Time frame: Pre-dose and 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 3.5, 4, 5, 6, 8, 12, 16, 24, 48 and 72 hours post-dose

    Blood samples were collected at indicated time points to study the PK profile of DTG and 3TC when administered as FDC tablet compared to co-administration of separate tablet formulations of DTG and 3TC in fasted state. The 4-hour post-dose sample was drawn prior to the participant's first post-dose meal. At each time point, 2 mL of blood was collected. PK parameters of bilayer FDC tablet formulation of DTG and 3TC was evaluated under fasted condition in Periods 1 and 2 of Part 2.

  17. Apparent Oral Volume of Distribution (Vz/F) of DTG and 3TC in the Fasted State: Part 1

    Time frame: Pre-dose and 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 3.5, 4, 5, 6, 8, 12, 16, 24, 48 and 72 hours post-dose

    Blood samples were collected at indicated time points to study the PK profile of DTG and 3TC when administered as FDC tablet compared to co-administration of separate tablet formulations of DTG and 3TC in fasted state. The 4-hour post-dose sample was drawn prior to the participant's first post-dose meal. At each time point, 2 mL of blood was collected. PK parameters of monolayer FDC tablet formulation of DTG and 3TC was evaluated under fasted condition in Periods 1 and 2 of Part 1.

  18. Vz/F of DTG and 3TC in the Fasted State: Part 2

    Time frame: Pre-dose and 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 3.5, 4, 5, 6, 8, 12, 16, 24, 48 and 72 hours post-dose

    Blood samples were collected at indicated time points to study the PK profile of DTG and 3TC when administered as FDC tablet compared to co-administration of separate tablet formulations of DTG and 3TC in fasted state. The 4-hour post-dose sample was drawn prior to the participant's first post-dose meal. At each time point, 2 mL of blood was collected. PK parameters of bilayer FDC tablet formulation of DTG and 3TC was evaluated under fasted condition in Periods 1 and 2 of Part 2.

  19. Concentration at 24 Hours Post-dose (C24) of DTG and 3TC in the Fasted State: Part 1

    Time frame: Pre-dose and 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 3.5, 4, 5, 6, 8, 12, 16, 24, 48 and 72 hours post-dose

    Blood samples were collected at indicated time points to study the PK profile of DTG and 3TC when administered as FDC tablet compared to co-administration of separate tablet formulations of DTG and 3TC in fasted state. The 4-hour post-dose sample was drawn prior to the participant's first post-dose meal. At each time point, 2 mL of blood was collected. PK parameters of monolayer FDC tablet formulation of DTG and 3TC was evaluated under fasted condition in Periods 1 and 2 of Part 1.

  20. C24 of DTG and 3TC in the Fasted State: Part 2

    Time frame: Pre-dose and 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 3.5, 4, 5, 6, 8, 12, 16, 24, 48 and 72 hours post-dose

    Blood samples were collected at indicated time points to study the PK profile of DTG and 3TC when administered as FDC tablet compared to co-administration of separate tablet formulations of DTG and 3TC in fasted state. The 4-hour post-dose sample was drawn prior to the participant's first post-dose meal. At each time point, 2 mL of blood was collected. PK parameters of bilayer FDC tablet formulation of DTG and 3TC was evaluated under fasted condition in Periods 1 and 2 of Part 2.

  21. Last Quantifiable Concentration (Clast) of DTG and 3TC in the Fasted State: Part 1

    Time frame: Pre-dose and 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 3.5, 4, 5, 6, 8, 12, 16, 24, 48 and 72 hours post-dose

    Blood samples were collected at indicated time points to study the PK profile of DTG and 3TC when administered as FDC tablet compared to co-administration of separate tablet formulations of DTG and 3TC in fasted state. The 4-hour post-dose sample was drawn prior to the participant's first post-dose meal. At each time point, 2 mL of blood was collected. PK parameters of monolayer FDC tablet formulation of DTG and 3TC was evaluated under fasted condition in Periods 1 and 2 of Part 1.

  22. Clast of DTG and 3TC in the Fasted State: Part 2

    Time frame: Pre-dose and 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 3.5, 4, 5, 6, 8, 12, 16, 24, 48 and 72 hours post-dose

    Blood samples were collected at indicated time points to study the PK profile of DTG and 3TC when administered as FDC tablet compared to co-administration of separate tablet formulations of DTG and 3TC in fasted state. The 4-hour post-dose sample was drawn prior to the participant's first post-dose meal. At each time point, 2 mL of blood was collected. PK parameters of bilayer FDC tablet formulation of DTG and 3TC was evaluated under fasted condition in Periods 1 and 2 of Part 2.

  23. AUC (0-Inf) of Plasma DTG and 3TC in the Fed State: Part 1

    Time frame: Pre-dose and 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 3.5, 4, 5, 6, 8, 12, 16, 24, 48 and 72 hours post-dose

    Blood samples for PK analysis of DTG and 3TC were collected at given time points to study the PK profile of DTG and 3TC FDC tablet(s). The 4-hour post-dose sample was drawn prior to the participant's first post-dose meal. At each time point, 2 mL of blood was collected. The effect of food on DTG and 3TC monolayer FDC tablet formulations was assessed in Period 3 of Part 1.

  24. AUC (0-Inf) of Plasma DTG and 3TC in the Fed State: Part 2

    Time frame: Pre-dose and 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 3.5, 4, 5, 6, 8, 12, 16, 24, 48 and 72 hours post-dose

    Blood samples for PK analysis of DTG and 3TC were collected at given time points to study the PK profile of DTG and 3TC FDC tablet(s). The 4-hour post-dose sample was drawn prior to the participant's first post-dose meal. At each time point, 2 mL of blood was collected. The effect of food on DTG and 3TC bilayer FDC tablet formulations was assessed in Period 3 of Part 2.

  25. AUC (0-t) of Plasma DTG and 3TC in the Fed State: Part 1

    Time frame: Pre-dose and 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 3.5, 4, 5, 6, 8, 12, 16, 24, 48 and 72 hours post-dose

    Blood samples for PK analysis of DTG and 3TC were collected at given time points to study the PK profile of DTG and 3TC FDC tablet(s). The 4-hour post-dose sample was drawn prior to the participant's first post-dose meal. At each time point, 2 mL of blood was collected. The effect of food on DTG and 3TC monolayer FDC tablet formulations was assessed in Period 3 of Part 1.

  26. AUC (0-t) of Plasma DTG and 3TC in the Fed State: Part 2

    Time frame: Pre-dose and 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 3.5, 4, 5, 6, 8, 12, 16, 24, 48 and 72 hours post-dose

    Blood samples for PK analysis of DTG and 3TC were collected at given time points to study the PK profile of DTG and 3TC FDC tablet(s). The 4-hour post-dose sample was drawn prior to the participant's first post-dose meal. At each time point, 2 mL of blood was collected. The effect of food on DTG and 3TC bilayer FDC tablet formulations was assessed in Period 3 of Part 2.

  27. Cmax of Plasma DTG and 3TC in the Fed State: Part 1

    Time frame: Pre-dose and 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 3.5, 4, 5, 6, 8, 12, 16, 24, 48 and 72 hours post-dose

    Blood samples for PK analysis of DTG and 3TC were collected at given time points to study the PK profile of DTG and 3TC FDC tablet(s). The 4-hour post-dose sample was drawn prior to the participant's first post-dose meal. At each time point, 2 mL of blood was collected. The effect of food on DTG and 3TC monolayer FDC tablet formulations was assessed in Period 3 of Part 1.

  28. Cmax of Plasma DTG and 3TC in the Fed State: Part 2

    Time frame: Pre-dose and 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 3.5, 4, 5, 6, 8, 12, 16, 24, 48 and 72 hours post-dose

    Blood samples for PK analysis of DTG and 3TC were collected at given time points to study the PK profile of DTG and 3TC FDC tablet(s). The 4-hour post-dose sample was drawn prior to the participant's first post-dose meal. At each time point, 2 mL of blood was collected. The effect of food on DTG and 3TC bilayer FDC tablet formulations was assessed in Period 3 of Part 2.

  29. Tlag of DTG and 3TC in Fed State: Part 1

    Time frame: Pre-dose and 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 3.5, 4, 5, 6, 8, 12, 16, 24, 48 and 72 hours post-dose

    Blood samples for PK analysis of DTG and 3TC were collected at given time points to study the PK profile of DTG and 3TC FDC tablet(s). The 4-hour post-dose sample was drawn prior to the participant's first post-dose meal. At each time point, 2 mL of blood was collected. The effect of food on DTG and 3TC monolayer FDC tablet formulations was assessed in Period 3 of Part 1.

  30. Tlag of DTG and 3TC in Fed State: Part 2

    Time frame: Pre-dose and 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 3.5, 4, 5, 6, 8, 12, 16, 24, 48 and 72 hours post-dose

    Blood samples for PK analysis of DTG and 3TC were collected at given time points to study the PK profile of DTG and 3TC FDC tablet(s). The 4-hour post-dose sample was drawn prior to the participant's first post-dose meal. At each time point, 2 mL of blood was collected. The effect of food on DTG and 3TC bilayer FDC tablet formulations was assessed in Period 3 of Part 2.

  31. Tmax of DTG and 3TC in the Fed State: Part 1

    Time frame: Pre-dose and 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 3.5, 4, 5, 6, 8, 12, 16, 24, 48 and 72 hours post-dose

    Blood samples for PK analysis of DTG and 3TC were collected at given time points to study the PK profile of DTG and 3TC FDC tablet(s). The 4-hour post-dose sample was drawn prior to the participant's first post-dose meal. At each time point, 2 mL of blood was collected. The effect of food on DTG and 3TC monolayer FDC tablet formulations was assessed in Period 3 of Part 1.

  32. Tmax of DTG and 3TC in the Fed State: Part 2

    Time frame: Pre-dose and 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 3.5, 4, 5, 6, 8, 12, 16, 24, 48 and 72 hours post-dose

    Blood samples for PK analysis of DTG and 3TC were collected at given time points to study the PK profile of DTG and 3TC FDC tablet(s). The 4-hour post-dose sample was drawn prior to the participant's first post-dose meal. At each time point, 2 mL of blood was collected. The effect of food on DTG and 3TC bilayer FDC tablet formulations was assessed in Period 3 of Part 2.

  33. T1/2 of DTG and 3TC in the Fed State: Part 1

    Time frame: Pre-dose and 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 3.5, 4, 5, 6, 8, 12, 16, 24, 48 and 72 hours post-dose

    Blood samples for PK analysis of DTG and 3TC were collected at given time points to study the PK profile of DTG and 3TC FDC tablet(s). The 4-hour post-dose sample was drawn prior to the participant's first post-dose meal. At each time point, 2 mL of blood. The effect of food on DTG and 3TC monolayer FDC tablet formulations was assessed in Period 3 of Part 1.

  34. T1/2 of DTG and 3TC in the Fed State: Part 2

    Time frame: Pre-dose and 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 3.5, 4, 5, 6, 8, 12, 16, 24, 48 and 72 hours post-dose

    Blood samples for PK analysis of DTG and 3TC were collected at given time points to study the PK profile of DTG and 3TC FDC tablet(s). The 4-hour post-dose sample was drawn prior to the participant's first post-dose meal. At each time point, 2 mL of blood was collected. The effect of food on DTG and 3TC bilayer FDC tablet formulations was assessed in Period 3 of Part 2.

  35. Lambda z of DTG and 3TC in in the Fed State: Part 1

    Time frame: Pre-dose and 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 3.5, 4, 5, 6, 8, 12, 16, 24, 48 and 72 hours post-dose

    Blood samples for PK analysis of DTG and 3TC were collected at given time points to study the PK profile of DTG and 3TC FDC tablet(s). The 4-hour post-dose sample was drawn prior to the participant's first post-dose meal. At each time point, 2 mL of blood was collected. The effect of food on DTG and 3TC monolayer FDC tablet formulations was assessed in Period 3 of Part 1.

  36. Lambda z of DTG and 3TC in in the Fed State: Part 2

    Time frame: Pre-dose and 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 3.5, 4, 5, 6, 8, 12, 16, 24, 48 and 72 hours post-dose

    Blood samples for PK analysis of DTG and 3TC were collected at given time points to study the PK profile of DTG and 3TC FDC tablet(s). The 4-hour post-dose sample was drawn prior to the participant's first post-dose meal. At each time point, 2 mL of blood was collected. The effect of food on DTG and 3TC bilayer FDC tablet formulations was assessed in Period 3 of Part 2.

  37. Clast of DTG and 3TC in in the Fed State: Part 1

    Time frame: Pre-dose and 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 3.5, 4, 5, 6, 8, 12, 16, 24, 48 and 72 hours post-dose

    Blood samples for PK analysis of DTG and 3TC were collected at given time points to study the PK profile of DTG and 3TC FDC tablet(s). The 4-hour post-dose sample was drawn prior to the participant's first post-dose meal. At each time point, 2 mL of blood was collected. The effect of food on DTG and 3TC monolayer FDC tablet formulations was assessed in Period 3 of Part 1.

  38. Clast of DTG and 3TC in in the Fed State: Part 2

    Time frame: Pre-dose and 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 3.5, 4, 5, 6, 8, 12, 16, 24, 48 and 72 hours post-dose

    Blood samples for PK analysis of DTG and 3TC were collected at given time points to study the PK profile of DTG and 3TC FDC tablet(s). The 4-hour post-dose sample was drawn prior to the participant's first post-dose meal. At each time point, 2 mL of blood was collected. The effect of food on DTG and 3TC bilayer FDC tablet formulations was assessed in Period 3 of Part 2.

  39. Percentage of Extrapolated AUC (0-inf) in the Fed State: Part 1

    Time frame: Pre-dose and 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 3.5, 4, 5, 6, 8, 12, 16, 24, 48 and 72 hours post-dose

    Blood samples for PK analysis of DTG and 3TC were collected at given time points to study the PK profile of DTG and 3TC FDC tablet(s). The 4-hour post-dose sample was drawn prior to the participant's first post-dose meal. At each time point, 2 mL of blood was collected. The effect of food on DTG and 3TC monolayer FDC tablet formulations was assessed in Period 3 of Part 1.

  40. Percentage of Extrapolated AUC (0-inf) in the Fed State: Part 2

    Time frame: Pre-dose and 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 3.5, 4, 5, 6, 8, 12, 16, 24, 48 and 72 hours post-dose

    Blood samples for PK analysis of DTG and 3TC were collected at given time points to study the PK profile of DTG and 3TC FDC tablet(s). The 4-hour post-dose sample was drawn prior to the participant's first post-dose meal. At each time point, 2 mL of blood was collected. The effect of food on DTG and 3TC bilayer FDC tablet formulations was assessed in Period 3 of Part 2.

  41. AUC(0-24) of DTG and 3TC in the Fed State: Part 1

    Time frame: Pre-dose and 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 3.5, 4, 5, 6, 8, 12, 16, 24, 48 and 72 hours post-dose

    Blood samples for PK analysis of DTG and 3TC were collected at given time points to study the PK profile of DTG and 3TC FDC tablet(s). The 4-hour post-dose sample was drawn prior to the participant's first post-dose meal. At each time point, 2 mL of blood was collected. The effect of food on DTG and 3TC monolayer FDC tablet formulations was assessed in Period 3 of Part 1.

  42. AUC(0-24) of DTG and 3TC in the Fed State: Part 2

    Time frame: Pre-dose and 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 3.5, 4, 5, 6, 8, 12, 16, 24, 48 and 72 hours post-dose

    Blood samples for PK analysis of DTG and 3TC were collected at given time points to study the PK profile of DTG and 3TC FDC tablet(s). The 4-hour post-dose sample was drawn prior to the participant's first post-dose meal. At each time point, 2 mL of blood was collected. The effect of food on DTG and 3TC bilayer FDC tablet formulations was assessed in Period 3 of Part 2.

  43. CL/F of DTG and 3TC in the Fed State: Part 1

    Time frame: Pre-dose and 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 3.5, 4, 5, 6, 8, 12, 16, 24, 48 and 72 hours post-dose

    Blood samples for PK analysis of DTG and 3TC were collected at given time points to study the PK profile of DTG and 3TC FDC tablet(s). The 4-hour post-dose sample was drawn prior to the participant's first post-dose meal. At each time point, 2 mL of blood was collected. The effect of food on DTG and 3TC monolayer FDC tablet formulations was assessed in Period 3 of Part 1.

  44. CL/F of DTG and 3TC in the Fed State: Part 2

    Time frame: Pre-dose and 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 3.5, 4, 5, 6, 8, 12, 16, 24, 48 and 72 hours post-dose

    Blood samples for PK analysis of DTG and 3TC were collected at given time points to study the PK profile of DTG and 3TC FDC tablet(s). The 4-hour post-dose sample was drawn prior to the participant's first post-dose meal. At each time point, 2 mL of blood was collected. The effect of food on DTG and 3TC bilayer FDC tablet formulations was assessed in Period 3 of Part 2.

  45. Tlast of DTG and 3TC in the Fed State: Part 1

    Time frame: Pre-dose and 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 3.5, 4, 5, 6, 8, 12, 16, 24, 48 and 72 hours post-dose

    Blood samples for PK analysis of DTG and 3TC were collected at given time points to study the PK profile of DTG and 3TC FDC tablet(s). The 4-hour post-dose sample was drawn prior to the participant's first post-dose meal. At each time point, 2 mL of blood was collected. The effect of food on DTG and 3TC monolayer FDC tablet formulations was assessed in Period 3 of Part 1.

  46. Tlast of DTG and 3TC in the Fed State: Part 2

    Time frame: Pre-dose and 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 3.5, 4, 5, 6, 8, 12, 16, 24, 48 and 72 hours post-dose

    Blood samples for PK analysis of DTG and 3TC were collected at given time points to study the PK profile of DTG and 3TC FDC tablet(s). The 4-hour post-dose sample was drawn prior to the participant's first post-dose meal. At each time point, 2 mL of blood was collected. The effect of food on DTG and 3TC bilayer FDC tablet formulations was assessed in Period 3 of Part 2.

  47. Vz/F of DTG and 3TC in the Fed State: Part 1

    Time frame: Pre-dose and 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 3.5, 4, 5, 6, 8, 12, 16, 24, 48 and 72 hours post-dose

    Blood samples for PK analysis of DTG and 3TC were collected at given time points to study the PK profile of DTG and 3TC FDC tablet(s). The 4-hour post-dose sample was drawn prior to the participant's first post-dose meal. At each time point, 2 mL of blood was collected. The effect of food on DTG and 3TC monolayer FDC tablet formulations was assessed in Period 3 of Part 1.

  48. Vz/F of DTG and 3TC in the Fed State: Part 2

    Time frame: Pre-dose and 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 3.5, 4, 5, 6, 8, 12, 16, 24, 48 and 72 hours post-dose

    Blood samples for PK analysis of DTG and 3TC were collected at given time points to study the PK profile of DTG and 3TC FDC tablet(s). The 4-hour post-dose sample was drawn prior to the participant's first post-dose meal. At each time point, 2 mL of blood was collected. The effect of food on DTG and 3TC bilayer FDC tablet formulations was assessed in Period 3 of Part 2.

  49. C24 of DTG and 3TC in the Fed State: Part 1

    Time frame: Pre-dose and 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 3.5, 4, 5, 6, 8, 12, 16, 24, 48 and 72 hours post-dose

    Blood samples for PK analysis of DTG and 3TC were collected at given time points to study the PK profile of DTG and 3TC FDC tablet(s). The 4-hour post-dose sample was drawn prior to the participant's first post-dose meal. At each time point, 2 mL of blood was collected. The effect of food on DTG and 3TC monolayer FDC tablet formulations was assessed in Period 3 of Part 1.

  50. C24 of DTG and 3TC in the Fed State: Part 2

    Time frame: Pre-dose and 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 3.5, 4, 5, 6, 8, 12, 16, 24, 48 and 72 hours post-dose

    Blood samples for PK analysis of DTG and 3TC were collected at given time points to study the PK profile of DTG and 3TC FDC tablet(s). The 4-hour post-dose sample was drawn prior to the participant's first post-dose meal. At each time point, 2 mL of blood was collected. The effect of food on DTG and 3TC bilayer FDC tablet formulations was assessed in Period 3 of Part 2.

  51. Change From Baseline in Systolic Blood Pressure (SBP) and Diastolic Blood Pressure (DBP): Part 1 and 2

    Time frame: Up to Day 31 in Part 1 and Part 2

    SBP and DBP were measured in the supine or semi-supine position after 5 minutes rest. The Baseline value was considered to be the participant's last available assessment prior to time of the first dose. Change from Baseline was defined as post dose visit value minus Baseline value. Data for SBP and DBP for Part 1 and 2 is presented.

  52. Change From Baseline in Heart Rate (HR): Part 1 and 2

    Time frame: Up to Day 31 in Part 1 and Part 2

    HR was measured in the supine or semi-supine position after 5 minutes rest. The Baseline value was considered to be the participant's last available assessment prior to time of the first dose. Change from Baseline was defined as post dose visit value minus Baseline value. Data for HR for Part 1 and 2 is presented.

  53. Number of Participants With Adverse Events (AEs) and Serious Adverse Events (SAEs): Part 1 and 2

    Time frame: Up to Week 11

    An AE is any untoward medical occurrence in a clinical investigation participant, temporally associated with the use of a medicinal product, whether or not considered related to the medicinal product. Any untoward event resulting in death, life threatening, requires hospitalization or prolongation of existing hospitalization, results in disability/incapacity, congenital anomaly/birth defect, any other situation according to medical or scientific judgment or all events of possible drug-induced liver injury with hyperbilirubinaemia were categorized as SAE. Participants having any AE or SAE are presented.

Sponsors and collaborators

Lead sponsor

ViiV Healthcare

Industry

Collaborators

  • GlaxoSmithKline

Registry information

Official study title

An Open-label, Randomized, Single Dose, Crossover, Pivotal Bioequivalence Study of Fixed-dose Combination Tablets of Dolutegravir and Lamivudine Versus Dolutegravir and Lamivudine Single Entities and Food Effect Assessment in Healthy Volunteers

Important dates

Study start
2017
Primary completion
2017
Study completion
2017
First posted
Mar 13, 2017
Registry last updated
Feb 21, 2019

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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