HIV maturation inhibitor formulations

Abstract

Co-formulations of HIV maturation inhibitor compound with one or two other HIV compounds, and methods of treatment, are set forth.

Description

field of invention [0001] The present invention relates to formulations for anti-HIV containing two and three drug combinations of antiretroviral compounds. In particular, the invention relates to combinations of HIV maturation inhibitor compounds and one or two other antiretroviral compounds, including dolutegravir and atazanavir. The invention also relates to methods of administering these formulations to a patient in need of treatment. Background of the invention [0002] HIV-1 (Human Immunodeficiency Virus-1) infection remains a major medical problem, with tens of millions still infected worldwide at the end of 2013. The number of cases of HIV and AIDS (Acquired Immunodeficiency Syndrome) is increasing rapidly. In 2005, approximately 5 million new infections were reported and 3.1 million deaths from AIDS. Currently available drugs for the treatment of HIV include nucleoside reverse transcriptase (RT) inhibitors or approved single-pill combinations: zidovudine (or AZT ...

AI Technical Summary

Problems solved by technology

However, despite these impressive results, 30% to 50% of patients may ultimately fail combination drug therapy

Insufficient drug potency, noncompliance, limited tissue penetration, and drug-specific limitations in certain cell types (eg, most nucleoside analogs cannot be phosphorylated in resting cells) may lead to incomplete suppression of susceptible viruses

Furthermore, the high replication rate and rapid turnover of HIV-1 and the frequent incorporation of mutations lead to the emergence of drug-resistant variants and treatment failure when suboptimal drug concentrations are present