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Updated: May 2, 2026

Rapid Screening of HIV Reverse Transcriptase and Integrase Inhibitors
Published on: April 9, 2014
Drug safety profile of integrase strand transfer inhibitors
Maria del Mar Gutierrez1, Maria Gracia Mateo, Francesc Vidal
1Universitat Autònoma de Barcelona, Hospital de la Santa Creu i Sant Pau, Infectious Diseases Unit , Av. Sant Antoni Ma Claret, 167, 08025 Barcelona , Spain +34935565624 ; +34935565938 ; pdomingo@santpau.cat.
Introduction:
HIV-1 integrase strand transfer inhibitors (INSTIs) are a novel class of antiretroviral drugs with a good safety profile. Several INSTIs have been developed clinically.
Areas Covered:
The purpose of this review is to examine the safety data of the three FDA-approved INSTIs: Raltegravir (RAL), Elvitegravir (EVG) and Dolutegravir (DTG). The most relevant papers related to the safety profile of integrase inhibitors were selected and summarized.
Expert Opinion:
INSTIs have demonstrated a favorable safety profile in Phase II and III trials. The most common clinical adverse events reported were diarrhea, nausea and headache. DTG and cobicistat, a component of Stribild(™), increase serum creatinine and decrease estimated creatinine clearance due to inhibition of active tubular secretion of creatinine without affecting renal glomerular function. INSTIs intrinsic potency, together with an outstanding safety profile, preludes an important role for these drugs to build up highly active antiretroviral treatment (HAART) in the near future.
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