This is a phase 1, open label study in healthy participants to assess the pharmacokinetics of cabotegravir and rilpivirine in plasma following the administration of a single 600 milligram (mg) and a 900 mg intramuscular (IM) injection respectively, to separate vastus lateralis muscles on each leg. Cabotegravir is an integrase inhibitor being developed in combination with rilpivirine, a non-nucleoside reverse transcriptase inhibitor, for the treatment of human immunodeficiency virus (HIV). The objective is to evaluate pharmacokinetics, tolerability, and safety of cabotegravir long acting plus rilpivirine long acting administered concomitantly as two separate IM injections in the vastus lateralis muscle of adult healthy participants. The screening phase will be of 30 days, oral lead-in (OLI) phase of 28 days, there will be washout period of 10-14 days, followed by an injection phase and follow-up period will be up to 52-weeks. Approximately 15 adult healthy participants will be enrolled.
Study Type
INTERVENTIONAL
Allocation
NA
Purpose
TREATMENT
Masking
NONE
Enrollment
15
Cabotegravir tablets will be white to almost white oval shaped film coated tablets with a unit dose of 30 mg and will be administered orally.
Rilpivirine tablets will be off-white, round, biconvex film coated tablets with a unit dose of 25 mg and will be administered orally.
Cabotegravir long-acting will be a sterile white to slightly pink suspension containing 200 mg per mL of GSK1265744 as free acid for administration by intramuscular injection.
Rilpivirine long-acting will be a sterile white suspension containing 300 mg per mL of rilpivirine as the free base for administration by intramuscular injection.
GSK Investigational Site
Glendale, California, United States
Maximum Observed Concentration (Cmax) of Cabotegravir (CAB) Following Single IM Injection
Blood samples were collected at indicated time points for pharmacokinetic (PK) analysis of CAB.
Time frame: Day 1 (pre-dose, 1 hour, 2 hours) and one post-dose sample on day 2, day 4, day 5, day 8, day 10, day 15, day 17, day 22, day 28, week 8, week 12, week 24, week 36 and week 52
Cmax of Rilpivirine (RPV) Following Single IM Injection
Blood samples were collected at indicated time points for PK analysis of RPV.
Time frame: Day 1 (pre-dose, 1 hour, 2 hours) and one post-dose sample on day 2, day 4, day 5, day 8, day 10, day 15, day 17, day 22, day 28, week 8, week 12, week 24, week 36 and week 52
Time of Cmax (Tmax) of CAB Following Single IM Injection
Blood samples were collected at indicated time points for PK analysis of CAB.
Time frame: Day 1 (pre-dose, 1 hour, 2 hours) and one post-dose sample on day 2, day 4, day 5, day 8, day 10, day 15, day 17, day 22, day 28, week 8, week 12, week 24, week 36 and week 52
Tmax of RPV Following Single IM Injection
Blood samples were collected at indicated time points for PK analysis of RPV.
Time frame: Day 1 (pre-dose, 1 hour, 2 hours) and one post-dose sample on day 2, day 4, day 5, day 8, day 10, day 15, day 17, day 22, day 28, week 8, week 12, week 24, week 36 and week 52
Area Under the Plasma Concentration-time Curve (AUC) From Time Zero to Time (AUC[0-t]) of CAB Following Single IM Injection
Blood samples were collected at indicated time points for PK analysis of CAB.
Time frame: Day 1 (pre-dose, 1 hour, 2 hours) and one post-dose sample on day 2, day 4, day 5, day 8, day 10, day 15, day 17, day 22, day 28, week 8, week 12, week 24, week 36 and week 52
AUC(0-t) of RPV Following Single IM Injection
Blood samples were collected at indicated time points for PK analysis of RPV.
Time frame: Day 1 (pre-dose, 1 hour, 2 hours) and one post-dose sample on day 2, day 4, day 5, day 8, day 10, day 15, day 17, day 22, day 28, week 8, week 12, week 24, week 36 and week 52
AUC From Time Zero Extrapolated to Infinity (AUC[0-infinity]) of CAB Following Single IM Injection
Blood samples were collected at indicated time points for PK analysis of CAB.
Time frame: Day 1 (pre-dose, 1 hour, 2 hours) and one post-dose sample on day 2, day 4, day 5, day 8, day 10, day 15, day 17, day 22, day 28, week 8, week 12, week 24, week 36 and week 52
AUC(0-infinity) of RPV Following Single IM Injection
Blood samples were collected at indicated time points for PK analysis of RPV.
Time frame: Day 1 (pre-dose, 1 hour, 2 hours) and one post-dose sample on day 2, day 4, day 5, day 8, day 10, day 15, day 17, day 22, day 28, week 8, week 12, week 24, week 36 and week 52
Apparent Terminal Phase Half-life (t1/2) of CAB Following Single IM Injection
Blood samples were collected at indicated time points for PK analysis of CAB.
Time frame: Day 1 (pre-dose, 1 hour, 2 hours) and one post-dose sample on day 2, day 4, day 5, day 8, day 10, day 15, day 17, day 22, day 28, week 8, week 12, week 24, week 36 and week 52
t1/2 of RPV Following Single IM Injection
Blood samples were collected at indicated time points for PK analysis of RPV.
Time frame: Day 1 (pre-dose, 1 hour, 2 hours) and one post-dose sample on day 2, day 4, day 5, day 8, day 10, day 15, day 17, day 22, day 28, week 8, week 12, week 24, week 36 and week 52
Geometric Mean of Absorption Rate Constant (KALA) of CAB Following Single IM Injection
Blood samples were collected at indicated time points for PK analysis of CAB.
Time frame: Day 1 (pre-dose, 1 hour, 2 hours) and one post-dose sample on day 2, day 4, day 5, day 8, day 10, day 15, day 17, day 22, day 28, week 8, week 12, week 24, week 36 and week 52
Geometric Mean of Absorption Rate Constant (KALA) of RPV Following Single IM Injection
Blood samples were collected at indicated time points for PK analysis of RPV.
Time frame: Day 1 (pre-dose, 1 hour, 2 hours) and one post-dose sample on day 2, day 4, day 5, day 8, day 10, day 15, day 17, day 22, day 28, week 8, week 12, week 24, week 36 and week 52
Number of Participants With Liver Related Adverse Events (AEs)
An AE is any untoward medical occurrence in a clinical study participant, temporally associated with the use of a study intervention, whether or not considered related to the study intervention.
Time frame: Up to 56 weeks
Number of Participants With Liver Related Abnormalities
Blood samples were collected to assess abnormalities related to liver.
Time frame: Up to 56 weeks
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