Section Reviews; Anti-infectives: Section Review Anti-infectives: HIV protease inhibitors in early development
- 1 August 1996
- journal article
- Published by Taylor & Francis in Expert Opinion on Investigational Drugs
- Vol. 5 (8) , 977-983
- https://doi.org/10.1517/13543784.5.8.977
Abstract
Over the last ten years, two important intervention points in the life cycle of the human immunodeficiency virus (HIV) which involve two viral-specific enzymes, HIV reverse transcriptase (RT) and HIV protease, have been the target of intense research efforts to identify useful therapeutic agents. Several nucleoside analogues which are RT inhibitors have been approved for use in humans. Several nonnucleoside RT inhibitors are now under development. Within the last twelve months, three different HIV protease inhibitors - saqui-navir, ritonavir and indinavir - have been approved for marketing, thus validating the concept of HIV protease as an important therapeutic target. In this review, several new HIV protease inhibitors that are in early clinical development will be discussed. These compounds are VX-478, AG-1343 (nelfinavir mesylate), palinavir, KNI-272, DMP-450, U-103017 and CGP 61755.Keywords
This publication has 20 references indexed in Scilit:
- Results on New AIDS Drugs Bring Cautious OptimismScience, 1996
- In vitro antiviral activity of 141W94 (VX-478) in combination with other antiretroviral agentsAntiviral Research, 1996
- HIV protease inhibitors head to marketNature Biotechnology, 1995
- Crystal structure of HIV-1 protease in complex with VX-478, a potent and orally bioavailable inhibitor of the enzymeJournal of the American Chemical Society, 1995
- Rapid turnover of plasma virions and CD4 lymphocytes in HIV-1 infectionNature, 1995
- Viral dynamics in human immunodeficiency virus type 1 infectionNature, 1995
- Risking Everything? Risk Behavior, Behavior Change, and AIDSScience, 1994
- Protein binding of human immunodeficiency virus protease inhibitor KNI-272 and alteration of its in vitro antiretroviral activity in the presence of high concentrations of proteinsAntimicrobial Agents and Chemotherapy, 1994
- In vitro anti-human immunodeficiency virus (HIV) activities of transition state mimetic HIV protease inhibitors containing allophenylnorstatineAntimicrobial Agents and Chemotherapy, 1993
- Kynostatin (KNI-227 and -272, highly potent anti-HIV agents: conformationally constrained tripeptide inhibitors of HIV protease containing allophenylnorstatine.CHEMICAL & PHARMACEUTICAL BULLETIN, 1992