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OpenTrials
Completed

NCT Number: NCT06033547

A Study to Investigate the Pharmacokinetics, Safety, and Tolerability of Two Different Formulations of Long-acting Cabotegravir in Healthy Adult Participants

The primary purpose of the study is to investigate the safety, tolerability, and pharmacokinetic (PK) profiles of two different cabotegravir formulations in healthy adult participants. The study will initially start with the assessment of Cabotegravir Formulation F. Once the clinical batch of Cabotegravir Formulation G is available, this formulation will be assessed.

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Key information

Who can participate

Healthy volunteers accepted: Yes

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

Inclusion criteria

  • Participants who are overtly healthy as determined by medical evaluation including medical history, physical examination, laboratory tests, and cardiac monitoring
  • Body weight =>40 kilogram (kg) and body mass index (BMI) within the range =>18 to =<32 kilogram per meter square (kg/m^2)
  • Participants who are negative on a single test for Severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2)(approved molecular polymerase chain reaction [PCR] laboratory or point of care test) performed on the day of admission. A negative result is required prior to the administration of study intervention on Day 1.
  • Contraceptive use by men and women should be consistent with local regulations regarding the methods of contraception for those participating in clinical studies
  • Participants assigned female at birth are eligible to participate if they are not pregnant or breastfeeding, and at least one of the following conditions applies:
  • Is not a woman of childbearing potential (WOCBP) OR
  • Is a WOCBP and using a contraceptive method that is highly effective, with a failure rate of <1% from the time of screening and inclusive of the entire time while on the study.
  • A WOCBP must have a negative highly sensitive pregnancy test (urine or serum as required by local regulations) within the 30 days before the first dose of study intervention.
  • Capable of giving written informed consent

Exclusion criteria

  • Current presence or history of cardiovascular, respiratory, hepatic, renal, gastrointestinal, endocrine, haematological, or neurological disorders.
  • Current or chronic history of liver disease or known hepatic or biliary abnormalities.
  • History of ongoing or clinically relevant seizure disorder within the previous 2 years, including participants who have required treatment for seizures within this time period.
  • Participants who in the investigator's judgment, poses a significant suicidality risk. Participant's history of suicidal behavior and/or suicidal ideation should be considered when evaluating for suicide risk.
  • Positive SARS-CoV-2 polymerase chain reaction test, having signs and symptoms which in the opinion of the investigator are suggestive of COVID-19 (i.e., fever, cough etc) within 14 days of inpatient admission, or having contact with known COVID-19 positive person/s in the 14 days prior to inpatient admission.
  • Human immunodeficiency virus (HIV-1 or HIV-2) infection as indicated by positive antibody/antigen test.
  • History of or on-going high-risk behaviors that, in the opinion of the investigator, may put the participant at increased risk for HIV infection including, but not limited to, participants in HIV discordant relationships, or men who report current or prior unprotected anal sex with other men and those reporting prior or current injecting drug use.
  • Presence of hepatitis B surface antigen (HBsAg), or positive hepatitis C antibody test result at screening or within 3 months prior to first dose of study treatment.
  • Abnormal blood pressure.
  • Evidence of previous myocardial infarction.
  • Any conduction abnormality (including but not specific to left or right complete bundle branch block, atrioventricular [AV] block [2nd degree or higher], Wolff- Parkinson-White [WPW] syndrome).
  • Any significant arrhythmia which, in the opinion of the investigator or the medical monitor, will interfere with the safety for the individual participant.
  • One or more exclusionary values for a screening Electrocardiogram (ECG).
  • Alanine transaminase (ALT) >1.5x upper limit of normal (ULN).
  • Bilirubin >1.5xULN (isolated bilirubin >1.5xULN is acceptable if bilirubin is fractionated and direct bilirubin <35 percent [%]).
  • Estimated Glomerular Filtration Rate (eGFR) <60 milliliter per minute (mL/min) using the Chronic Kidney Disease - Improved Prediction Equations (CKD-EPI) Creatinine Equation (2021).
  • Haemoglobin <12.5 gram per deciliter (g/dL) for men and <11 g/dL for women.
  • Positive pre-study drug/alcohol screen.
  • Regular use of tobacco- or nicotine-containing products within 3 months prior to screening; or urinary cotinine levels indicative of smoking or history or regular use of tobacco- or nicotine-containing products (e.g., nicotine patches or vaporizing devices).
  • Regular alcohol consumption within 6 months prior to the study defined as an average weekly intake of >14 units for males or >7 units for females.
  • Regular use of known drugs of abuse.
  • Concurrent participation in another clinical trial (except imaging trials); or has participated in a clinical trial and received an investigational product within the following time period prior to the first dosing day in this study: 30 days, 5 half-lives or twice the duration of the biological effect of the investigational product (whichever is longer).
  • Participation in the study would result in loss of blood or blood products in excess of 500 mL within 56 days.
  • Exposure to more than four (4) new chemical entities within 12 months prior to the first dosing day.
  • History of sensitivity to any of the study interventions (or components thereof), a history of drug allergy or other allergy that, in the opinion of the investigator or medical monitor, contraindicates their participation
  • Current or anticipated need for chronic anti-coagulation therapy (with the exception of low-dose aspirin =< 325 mg/day)
  • Hereditary coagulation and platelet disorders (e.g., haemophilia or Von Willebrand disease [VWD]).
  • Participant has a tattoo overlying the location of injection or an underlying skin disease or condition (e.g., infection, inflammation, dermatitis, eczema, drug rash, drug allergy, psoriasis, food allergy, urticaria) that, in the opinion of the investigator, may interfere with interpretation of injection site reactions or administration of study intervention.
  • Any other clinical condition, behaviour or prior therapy that, in the opinion of the investigator, would make the participant unsuitable for the study; unable to comply with dosing requirements; or unable to comply with study visits.

Treatment and study plan

Cabotegravir Formulation F

Drug

Cabotegravir Formulation F will be administered

Cabotegravir Formulation G

Drug

Cabotegravir Formulation G will be administered

Primary outcomes

  1. Maximum observed plasma concentration (Cmax) of cabotegravir

    Time frame: Up to Week 52

  2. Time of maximum observed plasma concentration (tmax) of cabotegravir

    Time frame: Up to Week 52

  3. Area under the concentration - time curve from time zero to 4 weeks following the injection (AUC[0-4]) of cabotegravir

    Time frame: Up to Week 4

  4. Plasma Concentration of cabotegravir at Week 4

    Time frame: Week 4

  5. Number of participants with adverse events (AEs) based on severity

    Time frame: Up to Week 52

  6. Absolute value of haematology parameter: Platelet count (cells per microliter)

    Time frame: Up to Week 52

  7. Absolute value of haematology parameter: Red Blood Cell Count (RBC) (million cells per microliter)

    Time frame: Up to Week 52

  8. Absolute values of haematology parameters: haemoglobin (Hgb) (grams per decilitre)

    Time frame: Up to Week 52

  9. Absolute values of haematology parameters: haematocrit (Proportion of red blood cells in blood)

    Time frame: Up to Week 52

  10. Absolute value of haematology parameter: Mean Corpuscle Volume (MCV) (Femtoliters)

    Time frame: Up to Week 52

  11. Absolute value of haematology parameter: Mean Corpuscle haemoglobin (MCH) (Picograms)

    Time frame: Up to Week 52

  12. Absolute values of haematology parameters: Reticulocytes (Percentage of reticulocytes)

    Time frame: Up to Week 52

  13. Absolute values of haematology parameters: Neutrophils, Lymphocytes, Monocytes, Eosinophils, Basophils (giga cells per litre)

    Time frame: Up to Week 52

  14. Absolute values of Clinical Chemistry parameters: Glucose (fasting), Blood Urea Nitrogen (BUN), Creatinine, Sodium, Potassium, Calcium, Direct Bilirubin and Total Bilirubin (milligrams per decilitre)

    Time frame: Up to Week 52

  15. Absolute values of Clinical Chemistry parameters: AST/SGOT, ALT/ SGPT, ALP and CPK (International Units per litre)

    Time frame: Up to Week 52

    Clinical chemistry parameters such as Aspartate Aminotransferase (AST) / Serum Glutamic-Oxaloacetic Transaminase (SGOT), Alanine Aminotransferase (ALT)/ Serum Glutamic-Pyruvic Transaminase and (SGPT), Alkaline phosphatase (ALP) and Creatinine Phosphokinase (CPK) will be analysed.

  16. Absolute values of Clinical chemistry parameters: Total Protein (Grams per deciliter)

    Time frame: Up to Week 52

  17. Absolute values of Clinical chemistry parameters: Estimated Glomerular Filtration Rate (eGFR2) (millilitres per minute)

    Time frame: Up to Week 52

  18. Change from Baseline in haematology parameter: Platelet count (cells per microliter)

    Time frame: Baseline (Day 1) and up to Week 52

  19. Change from Baseline in haematology parameter: Red Blood Cell Count (RBC) (million cells per microliter)

    Time frame: Baseline (Day 1) and up to Week 52

  20. Change from baseline in haematology parameters: haematocrit (Proportion of red blood cells in blood)

    Time frame: Baseline (Day 1) and up to Week 52

  21. Change from baseline in haematology parameter: Mean Corpuscle Volume (MCV) (Femtoliters)

    Time frame: Baseline (Day 1) and up to Week 52

  22. Change from baseline in haematology parameter: Mean Corpuscle haemoglobin (MCH) (Picograms)

    Time frame: Baseline (Day 1) and up to Week 52

  23. Change from baseline in haematology parameters: Reticulocytes (Percentage of reticulocytes)

    Time frame: Baseline (Day 1) and up to Week 52

  24. Change from baseline in haematology parameters: Differential count of Neutrophils, Lymphocytes, Monocytes, Eosinophils, Basophils (giga cells per litre)

    Time frame: Baseline (Day 1) and up to Week 52

  25. Change from baseline in Clinical Chemistry parameters: Glucose (fasting), Blood Urea Nitrogen (BUN), Creatinine, Sodium, Potassium, Calcium, Direct Bilirubin and Total Bilirubin (milligrams per decilitre)

    Time frame: Baseline (Day 1) and up to Week 52

  26. Change from baseline in Clinical Chemistry parameters: AST/SGOT, ALT/ SGPT, ALP and CPK (International Units per litre)

    Time frame: Baseline (Day 1) and up to Week 52

    Clinical chemistry parameters such as Aspartate Aminotransferase (AST) / Serum Glutamic-Oxaloacetic Transaminase (SGOT), Alanine Aminotransferase (ALT)/ Serum Glutamic-Pyruvic Transaminase and (SGPT), Alkaline phosphatase (ALP) and Creatinine Phosphokinase (CPK) will be analysed

  27. Change from baseline in Clinical chemistry parameters: Total Protein (Grams per deciliter)

    Time frame: Baseline (Day 1) and up to Week 52

  28. Change from baseline in Clinical chemistry parameters: Estimated Glomerular Filtration Rate (eGFR) (millilitres per minute)

    Time frame: Baseline (Day 1) and up to Week 52

Secondary outcomes

  1. Area under the concentration - time curve from time zero to infinity (AUC[0-inf]) of cabotegravir

    Time frame: Up to Week 52

  2. Area under the concentration - time curve from time zero to time of last quantifiable concentration [AUC(0-last)] of cabotegravir

    Time frame: Up to Week 52

  3. Plasma Concentration of cabotegravir at Week 8,12 and 24

    Time frame: Week 8, 12 and 24

  4. Apparent terminal phase half-life (t1/2) of cabotegravir

    Time frame: Up to Week 52

  5. Apparent long-acting absorption rate constant (KA-LA) of cabotegravir

    Time frame: Up to Week 52

  6. Dose proportionality of cabotegravir based on AUC(0-inf), AUC(0-last), Cmax, and plasma concentration (Unit of measure: Slope of log dose)

    Time frame: Up to Week 52

  7. Number of participants with maximum post-baseline QTc values compared to baseline by category (to <=450 milliseconds (msec) or no change, to >450 msec to <=480 msec, to >480 msec to <=500 msec, and to >500 msec)

    Time frame: Up to Week 52

  8. Number of participants with maximum post-baseline increase in QTc values compared to baseline based on category (increase <=30 msec, increase of 31-60 msec, and increase of >60 msec)

    Time frame: Up to Week 52

  9. Number of participants with worst case post-baseline values relative to potential clinical importance criteria compared to baseline for diastolic blood pressure (DBP), systolic blood pressure (SBP) and pulse rate

    Time frame: Up to Week 52

    Number of participants with worst case post-baseline values relative to potential clinical importance criteria compared to baseline will be categorized into change to low, change to within range or no change, and change to high

Sponsors and collaborators

Lead sponsor

ViiV Healthcare

Industry

Registry information

Official study title

A Phase I, Open-label, Single Dose Escalation Study to Evaluate the Pharmacokinetics, Safety and Tolerability of Two Different Formulations of Long-acting Cabotegravir Administered to Healthy Adult Participants

Important dates

Study start
2023
Primary completion
2025
Study completion
2025
First posted
Sep 13, 2023
Registry last updated
Feb 6, 2026

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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