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The role of dolutegravir in the management of HIV infections

Authors Miller M, Liedtke MD, Lockhart SM, Rathbun RC

Received 14 November 2014

Accepted for publication 5 January 2015

Published 19 February 2015 Volume 2015:8 Pages 19—29


Checked for plagiarism Yes

Review by Single-blind

Peer reviewer comments 4

Editor who approved publication: Professor Suresh Antony

Misty M Miller,1 Michelle D Liedtke,1 Staci M Lockhart,2 R Chris Rathbun1

1Department of Pharmacy: Clinical and Administrative Sciences, University of Oklahoma College of Pharmacy, Oklahoma City, OK, USA; 2AbbVie Inc., Oklahoma City, OK, USA

Abstract: Dolutegravir is the most recent integrase strand transfer inhibitor approved for HIV-1 infection in both treatment-naïve and experienced patients. As a tricyclic carbamoyl pyridone analog, dolutegravir is rapidly absorbed and distributes through the cerebrospinal fluid. It is hepatically metabolized by uridine diphosphate glucuronosyl transferase 1A1; no inhibition or induction of cytochrome P450 enzymes is noted. As a substrate of CYP 3A4, dolutegravir is affected by rifampin, efavirenz, tipranavir/ritonavir, fosamprenavir/ritonavir, and dose increase is required. Dolutegravir inhibits the organic cation transporter 2, resulting in decreased creatinine clearance with no apparent decrease in renal function. Other adverse effects are minimal but include diarrhea, headache, and nausea. Clinical trials in treatment-naïve and experienced patients are ongoing and will be presented in this text.

Keywords: antiretroviral, integrase inhibitor, Tivicay®, treatment-naïve studies, treatment-experienced studies

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