부산대학교 도서관

Dolutegravir is the most recent integrase strand transfer inhibitor approved for HIV-1 infection in both treatment-naive 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-naive and experienced patients are ongoing and will be presented in this text. Keywords: antiretroviral, integrase inhibitor, Tivicay®, treatment-naive studies, treatment-experienced studies
Introduction to treatment developments in HIV Treatment developments in HIV infection have been largely dominated by the integrase inhibitors (INSTIs) in recent years with the approval of elvitegravir (EVG) coformulated [...]