A Phase 1, Single Dose, Crossover, Relative Bioavailability Study of a Dolutegravir Dispersible Tablet as Compared to a Dolutegravir Pediatric Granule Formulation and Effect of Different Types of Water on the Dispersible Tablet in Healthy Volunteers(200401)

NCT02185300 Phase 1 COMPLETED

Dolutegravir (DTG) is an HIV-1 integrase inhibitor approved in the United States, Canada, Australia and EU. A dispersible tablet has been developed for pediatric use as an alternative to the granule formulation, already in development, and the approved film-coated tablet. This is a single-center, randomized, open-label, 5-way crossover study in healthy adult subjects. The study will evaluate the relative bioavailability of five dosing regimens: 20 mg DTG pediatric granules (Treatment A) and of DTG 20 mg dispersible tablets (DTG 20 mg DT) after dispersed in: low mineral content(LMC) water (Treatment B); dispersed in CONTREX™ mineral water (Treatment C); dispersed in low mineral content water and consumed after standing for 30 minutes (Treatment D) and dispersed in CONTREX mineral water and consumed after standing for 30 minutes (Treatment E). Safety evaluations and serial PK samples will be collected during each treatment period. A follow-up visit will occur 7-14 days after the last dose of study drug. CONTREX is a trademark of Nestlé Waters Corporation.

Details

Lead sponsor	ViiV Healthcare
Phase	Phase 1
Status	COMPLETED
Enrolment	15
Start date	2014-07
Completion	2014-09

Conditions

• Infection, Human Immunodeficiency Virus

Interventions

• Dolutegravir Pediatric Granules
• Dolutegravir Dispersible Tablet

Primary outcomes

• Composite of pharmacokinetic (PK) parameters following single dose administration of DTG 20 mg DT dispersed in LMC water — Day 1 (pre-dose, 0.25, 0.5, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 8, 12 hours post dose), Day 2 (24 hours) and Day 3 (48 hours)
  PK parameters include area under the concentration-time curve from time zero extrapolated to infinite time (AUC \[0-infinity\]) Maximum observed concentration (Cmax) and apparent oral clearance (CL/F)
• Composite of PK parameters following single dose administration of DTG 20 mg DT dispersed in CONTREX mineral water — Day 1 (pre-dose, 0.25, 0.5, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 8, 12 hours post dose), Day 2 (24 hours) and Day 3 (48 hours)
  PK parameters include AUC (0-infinity), Cmax and CL/F
• Composite of PK parameters following single dose administration of DTG 20 mg DT dispersed in LMC water with 30-minute holding — Day 1 (pre-dose, 0.25, 0.5, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 8, 12 hours post dose), Day 2 (24 hours) and Day 3 (48 hours)
  PK parameters include AUC (0-infinity), Cmax and CL/F

Countries

United States