NCT01467531

A Phase 1, Open-Label, Crossover Study to Evaluate the Pharmacokinetics and Safety of GSK1265744 and Rilpivirine and Dolutegravir and Rilpivirine in Healthy Adult Subjects

Completed Phase 1 Last updated 11 October 2012

What this trial tests

Phase 1 trial testing Dolutegravir in Infections, Human Immunodeficiency Virus and Hepatitis in 28 participants. Completed in 1 February 2012.

Timeline

1 November 2011

Primary endpoint
1 February 2012

1 February 2012

Quick facts

Lead sponsor	ViiV Healthcare
Phase	Phase 1
Status	Completed
Study type	INTERVENTIONAL
Allocation	non randomized
Design	single group
Masking	none
Enrollment	28
Start date	1 November 2011
Primary completion	1 February 2012
Estimated completion	1 February 2012
Sites	1 location across United States

Drugs / interventions tested

• Dolutegravir (DOLUTEGRAVIR) — full drug profile →
• Rlipivirine — full drug profile →
• GSK1265744 — full drug profile →

Conditions studied

• Infections, Human Immunodeficiency Virus and Hepatitis — all drugs for Infections, Human Immunodeficiency Virus and Hepatitis →

Sponsor

ViiV Healthcare — full company profile →

Who can join

Adults 18 to 55, any sex, with Infections, Human Immunodeficiency Virus and Hepatitis. Healthy volunteers can join.

What's being measured

Primary outcomes are the specific endpoints the trial is designed to prove or disprove.

• Composite of Pharmacokinetic Parameters following Dolutegravir administration with and without rilpivirine
  Time frame: Cohort 1: Period 1 and 3 on Day 5: pre-dose, 1, 2, 3, 4, 8, 12 and 24 hours post dose.
  Area under the concentration-time curve from time zero (pre-dose) to last time of quantifiable concentration within a subject across all treatments (AUC(0-tau)), Maximum observed concentration (Cmax), Time of occurrence of Cmax (tmax), Pre-dose (trough) concentration at the end of the dosing interval (Ctau)
• Composite of Pharmacokinetic Parameters following GSK1265744 administration with and without rilpivirine
  Time frame: Cohort 2: Period 2 and 3, Day 12: pre-dose, 1, 2, 3, 4, 5, 6, 9, 12, 16, and 24hrs post dose.
  steady state, AUC(0-t), Cmax, tmax, and Ctau
• Composite of Pharmacokinetic Parameters following rilpivirine administration with and without Dolutegravir
  Time frame: Cohort 1: Period 2, Day 11: pre-dose, 1, 2, 3, 4, 5, 6, 9, 12, 16, and 24hrs post dose. Period 3: Day 5 pre-dose 1, 2, 3, 4, 5, 6, 9, 12, 16, and 24hrs post dose
  steady state, AUC(0-tau), Cmax, tmax, and Ctau
• Composite of Pharmacokinetic Parameters following rilpivirine administration with and without GSK1265744
  Time frame: Cohort 2: Periods 1 and 3: Day 12: pre-dose, 1, 2, 3, 4, 8, 12 and 24hrs post dose
  AUC(0-tau), Cmax, tmax, and Ctau

Sponsor's own description

This will be a single-center, two-cohort, three-period study in healthy adult subjects. Approximately 16 healthy subjects will be enrolled in Cohort 1 to provide data from 14 evaluable subjects. Approximately 12 healthy subjects will be enrolled in Cohort 2 to provide data from 10 evaluable subjects. Subjects will have a screening visit within 30 days prior to the first dose of study drug, three treatment periods, and a follow-up visit 7-14 days after the last dose of study drug. There will be a washout period between Period 1 and Period 2 but no washout between Period 2 and Period 3. Day 1 of Period 3 will start the day after the last day in Period 2. The study will be conducted on an out-patient basis except for days where serial pharmacokinetic sampling and safety assessments are scheduled.

Publications & conference data

3 peer-reviewed publications reference this trial (live from Europe PMC):

1. Lack of pharmacokinetic interaction between rilpivirine and integrase inhibitors dolutegravir and GSK1265744.
   Ford SL, Gould E, Chen S, Margolis D, et al · · 2013 · cited 66× · PMID 23979733 · DOI 10.1128/aac.01235-13
2. Long-Acting Cabotegravir for HIV/AIDS Prophylaxis.
   Engelman KD, Engelman AN. · · 2021 · cited 19× · PMID 34029457 · DOI 10.1021/acs.biochem.1c00157
3. Recent Advances in Nanoparticle-Based Antiretroviral Drug Delivery Systems for HIV Treatment and Prevention: A Comprehensive Review.
   Das G, Shin HS, Patra JK. · · 2025 · PMID 41287764 · DOI 10.2147/ijn.s540578