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

NCT06033547 | Completed Phase 1 DMC FDA Drug

• 1 other identifier: 219406
• Study Type: interventional
• Target: 56
• Locations: 1 country
• Sites: 1

Brief Summary

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.

Conditions

HIV Infections

Keywords

Cabotegravir; Pharmacokinetics

Outcome Measures

Primary Outcomes (28)

• Maximum observed plasma concentration (Cmax) of cabotegravir

  Up to Week 52

• Time of maximum observed plasma concentration (tmax) of cabotegravir

  Up to Week 52

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

  Up to Week 4

• Plasma Concentration of cabotegravir at Week 4

  Week 4

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

  Up to Week 52

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

  Up to Week 52

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

  Up to Week 52

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

  Up to Week 52

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

  Up to Week 52

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

  Up to Week 52

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

  Up to Week 52

• Absolute values of haematology parameters: Reticulocytes (Percentage of reticulocytes)

  Up to Week 52

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

  Up to Week 52

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

  Up to Week 52

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

  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.

  Up to Week 52

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

  Up to Week 52

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

  Up to Week 52

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

  Baseline (Day 1) and up to Week 52

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

  Baseline (Day 1) and up to Week 52

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

  Baseline (Day 1) and up to Week 52

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

  Baseline (Day 1) and up to Week 52

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

  Baseline (Day 1) and up to Week 52

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

  Baseline (Day 1) and up to Week 52

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

  Baseline (Day 1) and up to Week 52

• 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)

  Baseline (Day 1) and up to Week 52

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

  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

  Baseline (Day 1) and up to Week 52

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

  Baseline (Day 1) and up to Week 52

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

  Baseline (Day 1) and up to Week 52

Secondary Outcomes (9)

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

  Up to Week 52

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

  Up to Week 52

• Plasma Concentration of cabotegravir at Week 8,12 and 24

  Week 8, 12 and 24

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

  Up to Week 52

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

  Up to Week 52

Study Arms (2)

Part A: Participants receiving Cabotegravir Formulation F

EXPERIMENTAL

Drug: Cabotegravir Formulation F

Part B: Participants receiving Cabotegravir Formulation G

EXPERIMENTAL

Drug: Cabotegravir Formulation G

Interventions

Cabotegravir Formulation F DRUG

Cabotegravir Formulation F will be administered

Part A: Participants receiving Cabotegravir Formulation F

Cabotegravir Formulation G DRUG

Cabotegravir Formulation G will be administered

Part B: Participants receiving Cabotegravir Formulation G

Eligibility Criteria

• Age: 18 Years - 55 Years
• Sex: all
• Healthy Volunteers: Yes
• Age Groups: Adult (18-64)

You may qualify if:

• 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

You may not qualify if:

• 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.
• 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).

Sponsors & Collaborators

• ViiV Healthcare: lead

Study Sites (1)

GSK Investigational Site

Austin, Texas, 78744, United States

Location

MeSH Terms

Conditions

HIV Infections

Condition Hierarchy (Ancestors)

Blood-Borne Infections; Communicable Diseases; Infections; Sexually Transmitted Diseases, Viral; Sexually Transmitted Diseases; Lentivirus Infections; Retroviridae Infections; RNA Virus Infections; Virus Diseases; Genital Diseases; Urogenital Diseases; Immunologic Deficiency Syndromes; Immune System Diseases

Study Design

• Study Type: interventional
• Phase: phase 1
• Allocation: NON RANDOMIZED
• Masking: NONE
• Purpose: TREATMENT
• Intervention Model: SEQUENTIAL
• Sponsor Type: INDUSTRY
• Responsible Party: SPONSOR
• Expanded Access: Yes

Study Record Dates

• First Submitted: August 31, 2023
• First Posted: September 13, 2023
• Study Start: September 12, 2023
• Primary Completion: July 25, 2025
• Study Completion: July 25, 2025
• Last Updated: February 6, 2026

Record last verified: 2026-02

Data Sharing

• IPD Sharing: Will share
• Shared Documents: STUDY PROTOCOL, SAP, ICF, CSR
• Time Frame: Anonymized IPD will be made available within 6 months of publication of primary, key secondary and safety results for studies in product with approved indication(s) or terminated asset(s) across all indications.
• Access Criteria: Anonymized IPD is shared with researchers whose proposals are approved by an Independent Review Panel and after a Data Sharing Agreement is in place. Access is provided for an initial period of 12 months but an extension may be granted, when justified, for up to 6 months.

Locations

US (1)