Phase 1
N=138
Study to Evaluate Pharmacokinetic (PK), Safety and Tolerability of Cabotegravir (CAB) 400 Milligrams Per Milliliter (mg/mL) Formulation in Healthy Adult Participants
HIV Infections
Bottom Line
View on ClinicalTrials.gov: NCT04484337 ↗Enrolled (actual)
138
Serious AEs
2.2%
Results posted
May 2026
Primary outcome: Primary: Part 1 Injection 1: Time of Maximum Observed Plasma Concentration (Tmax) for CAB 400 mg/ml Formulation for Cohorts 1,2,3,4, 4b & 4h — 197.731; 150.215; 122.009; 145.648 Hour (h)
Study Design & Population
- Study type
- Interventional
- Phase
- Phase 1
- Interventions
- Cabotegravir sodium (Oral Lead In) (Drug); Cabotegravir 400 mg/mL (Drug); Cabotegravir 200 mg/mL (Drug); Topical Non-steroidal anti-inflammatory drug (NSAID) (Drug); Topical steroid (Drug); Topical NSAID placebo (Drug); Recombinant human hyaluronidase PH20 (rHuPH20) (Drug); Topical steroid placebo (Drug)
- Age
- Adult · 18+ yrs
- Sex
- All
- Sponsor
- ViiV Healthcare
- Primary completion
- May 2023
Outcome Measures
| Outcome | Result | p-value |
|---|---|---|
| PRIMARY Part 1 Injection 1: Time of Maximum Observed Plasma Concentration (Tmax) for CAB 400 mg/ml Formulation for Cohorts 1,2,3,4, 4b & 4h |
197.731; 150.215; 122.009; 145.648; 206.228; 137.853 | — |
| PRIMARY Part 1 Injection 2: Tmax for CAB 400 mg/ml Formulation for Cohorts 1,2,3,4 & 4b |
135.231; 111.656; 108.305; 147.029; 144.092; 155.350 | — |
| PRIMARY Part 2 Injection 1: Tmax for CAB 400 mg/ml Formulation for Cohort 5 |
163.093 | — |
| PRIMARY Part 2 Injection 2: Tmax for CAB 400 mg/ml Formulation for Cohort 5 |
— | — |
| PRIMARY Part 1 Injection 2: Apparent Terminal Phase Half-life (T1/2) for CAB 400 mg/ml Formulation for Cohorts 1,2,3,4 & 4b |
451.4; 333.8; 375.1; 628.8; 2886; 645.0 | — |
| PRIMARY Part 2 Injection 2: T1/2 for CAB 400 mg/ml Formulation for Cohort 5 |
— | — |
| PRIMARY Part 1 Injection 2: Terminal Absorption Elimination Rate Constant (KALA) for CAB 400 mg/ml Formulation for Cohorts 1,2,3,4 & 4b |
0.001535; 0.002076; 0.001847; 0.001101; 0.001376; 0.001074 | — |
| PRIMARY Part 2 Injection 2: KALA for CAB 400 mg/ml Formulation for Cohort 5 |
— | — |
| PRIMARY Part 1 Injection 1: Plasma Trough Concentrations (Ctau) of CAB 400 mg/ml Formulation for Cohorts 1,2,3,4, 4b & 4h |
2.528; 1.907; 1.490; 1.295; 1.220; 0.8572 | — |
| PRIMARY Part 1 Injection 2: Ctau of CAB 400 mg/ml Formulation for Cohorts 1,2,3,4, 4b |
2.853; 1.333; 1.542; 1.290; 1.590; 1.646 | — |
| PRIMARY Part 2 Injection 1: Ctau of CAB 400 mg/ml Formulation for Cohort 5 |
0.3787; 1.843; 0.3024 | — |
| PRIMARY Part 1 Injection 1: Area Under the Concentration Time Curve From Time Zero to Last Quantifiable Time Point (AUC(0-t)) of CAB 400 mg/ml Formulation for Cohorts 1, 2, 3, 4, 4b and 4h |
2734; 2640; 2261; 1510; 1142; 945.2 | — |
| PRIMARY Part 1 Injection 2: AUC(0-t) of CAB 400 mg/ml Formulation for Cohorts 1, 2, 3, 4 and 4b |
4731; 2050; 3170; 2417; 2409; 2649 | — |
| PRIMARY Part 1 Injection 1: Maximum Observed Plasma Concentration (Cmax) of CAB 400 mg/ml Formulation for Cohorts 1, 2, 3, 4, 4b and 4h |
6.507; 6.760; 6.743; 3.873; 2.750; 2.495 | — |
| PRIMARY Part 1 Injection 2: Cmax of CAB 400 mg/ml Formulation for Cohorts 1, 2, 3, 4, 4b |
7.095; 3.538; 5.873; 3.074; 3.718; 3.312 | — |
| SECONDARY Part 1 and Part 2: Number of Participants With Adverse Events (AEs) in Injection Phase and Follow up Phase |
17; 9; 11; 18; 12; 12 | — |
| SECONDARY Part 1 and Part 2: Number of Participants With Liver Biochemistry Abnormalities in Injection Phase and Follow up Phase |
0; 1; 0; 0; 0; 0 | — |
| SECONDARY Cmax for CAB Following Oral 30 mg Administration |
3.728; 3.921; 5.007; 4.526; 4.090; 3.573 | — |
| SECONDARY Tmax for CAB Following Oral 30 mg Administration |
1.9; 2.031; 1.000; 1.957; 1.000; 1.692 | — |
| SECONDARY AUC(0-t) for CAB Following Oral 30 mg Administration |
50.725; 60.91; 69.29; 70.31; 60.62; 56.03 | — |
| SECONDARY Concentration at 24 Hours (C24) for CAB Following Oral 30 mg Administration |
1.5450422; 1.971; 2.125; 2.229; 1.760; 1.748 | — |
| SECONDARY Ctau for CAB Following Oral 30 mg Administration |
5.0488137; 3.629; 3.074; 2.230; 5.456; 3.576 | — |
| SECONDARY Cmax of CAB 200 for Cohort 4h |
2.507 | — |
| SECONDARY Tmax of CAB 200 for Cohort 4h |
175.064 | — |
| SECONDARY AUC(0-t) of CAB 200 for Cohort 4h |
3087 | — |
| SECONDARY Ctau of CAB 200 for Cohort 4h and in ATLAS/FLAIR Study |
1.008; 0.9216 | — |
| SECONDARY T1/2 of CAB 200 & CAB 400 for Cohort 4h |
1233; 210.8 | — |
| SECONDARY KALA of CAB 200 & CAB 400 for Cohort 4h |
0.0005615; 0.003288 | — |
Summary
This is an active control, randomized study to investigate the safety, tolerability and PK of repeat dose administration of long-acting CAB 400 mg/mL formulation intramuscular (IM) (gluteus medius and vastus lateralis) and subcutaneous (SC) (abdominal) injections in healthy adult participants.
Eligibility Criteria
Inclusion Criteria
- Participant must be 18 to 50 years of age inclusive, at the time of signing the informed consent.
- Participants who are overtly healthy as determined by medical evaluation.
- A participant with a clinical abnormality or laboratory parameters which is/are not specifically listed in the inclusion or exclusion criteria, outside the reference range for the population being studied may be included if the investigator determines and documents that the finding is unlikely to introduce additional risk factors and will not interfere with the study procedures.
- Participants who are negative on two consecutive tests for Severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2), performed at Screening and within 5 days of admission to the Phase I unit, using an approved molecular test (Polymerase chain reaction [PCR]).
- Body weight more than or equal to (>=)40 kilogram (kg) and body mass index (BMI) within the range 18 to 32 kilogram per square meter (kg/m^2).
- Male participants are eligible to participate if they agree to use contraceptive methods and refrain from donating sperm.
- A female participant is eligible to participate if she is 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 less than ( )1.5 times 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 450 milliseconds (msec).
- A known hypersensitivity to hyaluronidases (Cohort 4h only).
- The participant has an underlying skin disease or disorder (infection, inflammation, dermatitis, eczema, drug rash, drug allergy, psoriasis, food allergy, urticaria) that would interfere with assessment of injection sites.
- Current or anticipated need for chronic anti-coagulation with the exception of the use of low dose acetylsalicylic acid (less than or equal to [ 100 beats per minute (bpm), for females 100 bpm.
- PR Interval: For males and females 220 msec.
- QRS duration: For males and females 120 msec.
- QT duration corrected for heart rate by Fridericia's formula (QTcF) interval: For males and females >450 msec.
- 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).
- Sinus Pauses >3 seconds.
- Any significant arrhythmia which, in the opinion of the Investigator or GlaxoSmithKline (GSK)/ViiV Medical monitor, will interfere with the safety for the individual participant.
- Non-sustained or sustained ventricular tachycardia (>=3 consecutive ventricular ectopic beats).
- Positive HIV antibody/antigen test. Participants will be advised regarding safer sex. In the event a participant acquires HIV during the course of the study they will be required to withdraw from the study and will be referred urgently to an HIV treatment center for further management.
- Regular use of known drugs of abuse.
- Regular use of tobacco- or nicotine-containing products within 3 months prior to screening.
- History of sensitivity to any of the study medications, or components thereof or a history of drug or other allergy.
- Participants with a history of intolerance to or with contraindications to the use of topical non-steroidal anti-inflammatory drugs (NSAIDs) or topical steroids will be excluded from participation in Cohort 4b.
- 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.
- Urinary cotinine levels indicative of smoking or history or regular use of tobacco- or nicotine-containing products (e.g. nicotine patches or vaporizing devices) within 6 months prior to screening.
- The participant has a tattoo or other derma
Data sourced from ClinicalTrials.gov (NCT04484337). Outcome figures and adverse-event rates are extracted automatically from the registry's posted results and are provided for clinician reference, not as a substitute for the primary publication.