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
- 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), San Francisco, USA, September 27-30, 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 13-17, 2006
- Dandache, S. et al. PL-100, a Novel Protease Inhibitor with a High Genetic Barrier. XVI International AIDS Conference, Toronto, Canada, August 13-18, 2006.
- Stranix, B., et al. Lysine sulfonamides as novel HIV-protease inhibitors: Ne-acyl aromatic amino acids. Bioorganic & Medicinal Chemistry Letters, volume 16, issue 13, 2006: 3459-3462.
- Wu, J.J., et al. Preclinical and clinical evaluation of PPL-100, a next generation HIV protease inhibitor. HIV DART 2006, Cancun, Mexico, December 10-14, 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 7-11, 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 28-30, 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 8-12, 2004.
- Stranix, B., et al. Lysine sulfonamides as Novel HIV-Protease Inhibitors: Nε-disubstituted ureas. Bioorganic and Medicinal Chemistry Letters, 14, 2004: 3971 - 3974.
- Sévigny, G, et al. Improving the resistance profile of HIV-1 protease inhibitors. Protease Targets and Drug Discovery Symposium, Philadelphia, USA., December 2003.
- Stranix, B., et al. Lysine sulfonamides as Novel HIV-Protease Inhibitors: Optimization of the Nε-Acyl-Phenyl Spacer. Bioorganic and Medicinal Chemistry Letters, 13, 2003: 4289 - 4292.
- 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. Activity of a novel anti-HIV protease inhibitor against viral strains resistant to commercially-available drugs. 2nd IAS Conference on HIV pathogenesis and treatment, July 13-16, 2003, Paris, France.
