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Bioequivalence of a Dolutegravir, Abacavir, and Lamivudine Fixed-Dose Combination Tablet and the Effect of Food

Weller, Stephen MS*; Chen, Shuguang PhD*; Borland, Julie BS*; Savina, Paul MS*; Wynne, Brian MD; Piscitelli, Stephen C. PharmD*

JAIDS Journal of Acquired Immune Deficiency Syndromes: August 1st, 2014 - Volume 66 - Issue 4 - p 393–398
doi: 10.1097/QAI.0000000000000193
Clinical Science

Background: The integrase inhibitor dolutegravir and nucleoside analogues abacavir and lamivudine are once-daily treatment options for HIV. This study (NCT01622790) evaluated, first, the bioequivalence (BE) of a fixed-dose combination (FDC) tablet containing dolutegravir 50 mg, abacavir 600 mg, and lamivudine 300 mg (dolutegravir/abacavir/lamivudine FDC) vs coadministered dolutegravir 50 mg and abacavir/lamivudine combination tablets (Epzicom) and, second, the effect of food on the dolutegravir/abacavir/lamivudine FDC tablet.

Methods: Study part A (66 healthy subjects) was a single-dose, open-label, randomized, 2-period crossover study to evaluate the BE of the dolutegravir/abacavir/lamivudine FDC tablet and dolutegravir + abacavir/lamivudine tablets in the fasted state. In study part B, 12 subjects from part A received the dolutegravir/abacavir/lamivudine FDC tablet with a high-fat meal. BE and food effect were assessed by analysis of variance to determine the ratio of geometric least squares means and associated 90% confidence intervals for key pharmacokinetic parameters for each of dolutegravir, abacavir, and lamivudine.

Results: Sixty-two subjects completed part A. The dolutegravir/abacavir/lamivudine tablet was bioequivalent to the dolutegravir + abacavir/lamivudine tablets; 90% confidence intervals for the geometric least squares mean ratios fell within the 0.8–1.25 BE criteria. The effect of food on the dolutegravir/abacavir/lamivudine FDC tablet was similar to previous food effects observed with the separate formulations. The safety profile was comparable between treatments, with no observed serious or grade 3/4 adverse events.

Conclusions: The BE of the dolutegravir/abacavir/lamivudine FDC tablet was demonstrated; it may be administered without regard to meals.

*GlaxoSmithKline, Research Triangle Park, NC; and

GlaxoSmithKline, Collegeville, PA.

Correspondence to: Stephen C. Piscitelli, PharmD, GlaxoSmithKline, Infectious Diseases, 5 Moore Drive, Research Triangle Park, NC 27709 (e-mail:

Supported by ViiV Healthcare. All authors are employees of GlaxoSmithKline.

The authors have no conflicts of interest to disclose.

Presented at 53rd Interscience Conference on Antimicrobial Agents and Chemotherapy, September 10–13, 2013, Denver, CO.

Received December 20, 2013

Accepted March 26, 2014

© 2014 by Lippincott Williams & Wilkins