Abacavir/Lamivudine Fixed-Dose Combination Tablet for the Treatment of HIV-1 Infection

Abstract

The fixed-dose combination tablet of the two nucleotide reverse transcriptase inhibitors abacavir (ABC) and lamivudine (3TC) was licensed in 2004. It is dosed once daily with no food restrictions and licensed for the treatment of HIV infection in treatment-naive individuals in combination with another class of antiretroviral. Its virological efficacy has been demonstrated in clinical studies with up to 96-week follow-up in combination with non-nucleoside reverse transcriptase inhibitors and protease inhibitors. Less lipodystrophy is seen with abacavir than stavudine or zidovudine. Resistance mutations selected by ABC/3TC leave options for future treatment. Abacavir hypersensitivity reaction occurs in 5% of those receiving ABC and genetic susceptibility testing is undergoing trial. ABC/3TC is a largely well-tolerated nucleoside reverse transcriptase inhibitor backbone with proven efficacy.

Design, Synthesis and Biological Evaluation of a Series of Thioamides as Non-Nucleoside Reverse Transcriptase Inhibitors

“…(1), is one of the many potent NNRT inhibitors developed through systematic structure modifications of the PETT series [11]. Although modern AIDS therapy uses a combination of drugs to suppress the appearance of drug-resistant virus strains [14][15][16], evolution of enzyme resistant strains still poses major problem in the management of AIDS. One of the many single mutations is K103N, a lysine to asparagine at amino acid 103 in viral reverse transcriptase enzyme, negates the activity of all currently approved non-nucleoside reverse transcriptase inhibitors [17].…”