A promising protease inhibitor
Indication
HIV/AIDS
Development status
Phase I
Patents
U.S. granted and World pending
Partner
Merck & Co., Inc.
HIV/AIDS - Protease Inhibitor Program
Scientific references
Articles
- Dandache, S. et al. In vitro antiviral activity and cross-resistance profile of PL-100, a novel protease inhibitor of human immunodeficiency virus type 1. Antimicrob Agents Chemother. 2007 Nov;51(11):4036-43. Epub 2007 Jul 16.
- Stranix, B., et al. Lysine sulfonamides as Novel HIV-Protease Inhibitors: Nε-disubstituted ureas. Bioorganic and Medicinal Chemistry Letters 2004, Vol. 14, pp 3971 - 3974.
- Stranix, B., et al. Lysine sulfonamides as Novel HIV-Protease Inhibitors: Optimization of the Nε-Acyl-Phenyl Spacer. Bioorganic and Medicinal Chemistry Letters 2003, Vol. 13, pp 4289 - 4292.
Presentations
- Wu, J.J. et al. PL-100, a Next Generation Protease Inhibitor against Drug-Resistant HIV: In Vitro and In Vivo Metabolism. 46th Interscience Conference on Antimicrobial Agents and Chemotherapy (ICAAC) held in San Francisco, September 2006.
- Dandache, S. et al. PL-100, a Novel Protease Inhibitor with a High Genetic Barrier. XVI International AIDS Conference, Toronto, Canada, August 2006.
- Wu, J.J. et al. The HIV-1 Protease Inhibitor PL-100 Has a High Genetic Barrier and Selects a Novel Patterns of Mutations. XV International HIV Drug Resistance Workshop: Basic Principles and Clinical Implications, Sitges, Spain, June 2006
- Wu, J. et al. PPL-100 and its derivatives, a novel class of potent human immunodeficiency virus type 1 protease inhibitors: resistance and pharmacokinetics. XIV International HIV Drug Resistance Workshop, Quebec City, Canada, June 2005.
- Wu, J. et al. Pharmacological and cross-resistance profiling of PL-100 and its pro-drug, PPL-100. 6th International Workshop on Clinical Pharmacology of HIV Therapy, Quebec City, Canada, April 2005.
- Sévigny, G, et al. Cross-resistance profile of the novel lysine-containing HIV-1 protease inhibitor PL-100. XIII International HIV Drug Resistance Workshop, Canary Islands, Spain, June 2004.
- Sévigny, G, et al. Improving the resistance profile of HIV-1 protease inhibitors. Protease Targets and Drug Discovery Symposium, Philadelphia, PA, U.S.A., December 2003.
- Stranix, B., et al. Synthesis and SAR studies of novel HIV protease inhibitors, containing a lysine backbone. 39th International Union of Pure and Applied Chemistry Congress and 86th Conference of the Canadian Society For Chemistry, Ottawa, Canada, August 2003.
- Sévigny, G. et al. Antiviral activity of P-1946, a novel anti-HIV protease inhibitor. XII International HIV Drug Resistance Workshop, Los Cabos, Mexico, June 2003.