BMS-232632 (Novartis/Bristol-Myers Squibb). 2001

G Witherell
Questcor Pharmaceuticals Inc, Hayward, CA 94545, USA. gwitherell@questcor.com

BMS-232632, an azapeptide HIV protease inhibitor, is in development by Bristol-Myers Squibb (BMS), under license from Novartis, as a potential treatment for HIV/AIDS [248556]. Early preclinical work was carried out by Novartis [248556]. BMS-232632 was developed as part of a series of compounds (as CGP-73547) and evaluated against drug-resistant strains of HIV; the compounds in this series belong to a series of azadipeptide analogs and are bis(L-tert-leucine) derivatives that exhibit good antiviral activity and satisfactory pharmacokinetic profiles [297907]. Novartis subsequently discontinued evaluation of the compound in November 1999 [347827]. Phase II trials had already begun by July 1999 [334335] and BMS expects NDA filing to take place in 2001 [358937]. Use of BMS-232632 in combination with other antiretroviral agents has demonstrated that it may be used in combination with a variety of nucleoside analogs and protease inhibitors [298464]. It is thought to have a genotypic resistance profile that differs from that of other protease inhibitors [302157]. In February 1999, Lehman Brothers predicted the drug had a 30% probability of reaching market, with an estimated first launch date in 2001. The analysts predicted peak sales would occur in 2007, with sales of $500 million in the US and $300 million in the rest of the world at that time [319225].

UI MeSH Term Description Entries
D009842 Oligopeptides Peptides composed of between two and twelve amino acids. Oligopeptide
D011725 Pyridines Compounds with a six membered aromatic ring containing NITROGEN. The saturated version is PIPERIDINES.
D004353 Drug Evaluation, Preclinical Preclinical testing of drugs in experimental animals or in vitro for their biological and toxic effects and potential clinical applications. Drug Screening,Evaluation Studies, Drug, Pre-Clinical,Drug Evaluation Studies, Preclinical,Drug Evaluations, Preclinical,Evaluation Studies, Drug, Preclinical,Evaluation, Preclinical Drug,Evaluations, Preclinical Drug,Medicinal Plants Testing, Preclinical,Preclinical Drug Evaluation,Preclinical Drug Evaluations,Drug Screenings,Screening, Drug,Screenings, Drug
D005544 Forecasting The prediction or projection of the nature of future problems or existing conditions based upon the extrapolation or interpretation of existing scientific data or by the application of scientific methodology. Futurology,Projections and Predictions,Future,Predictions and Projections
D005767 Gastrointestinal Diseases Diseases in any segment of the GASTROINTESTINAL TRACT from ESOPHAGUS to RECTUM. Cholera Infantum,Gastrointestinal Disorders,Functional Gastrointestinal Disorders,Gastrointestinal Disorders, Functional,Disease, Gastrointestinal,Diseases, Gastrointestinal,Functional Gastrointestinal Disorder,Gastrointestinal Disease,Gastrointestinal Disorder,Gastrointestinal Disorder, Functional
D006261 Headache The symptom of PAIN in the cranial region. It may be an isolated benign occurrence or manifestation of a wide variety of HEADACHE DISORDERS. Cephalgia,Hemicrania,Bilateral Headache,Cephalalgia,Cephalodynia,Cranial Pain,Generalized Headache,Head Pain,Ocular Headache,Orthostatic Headache,Periorbital Headache,Retro-Ocular Headache,Sharp Headache,Throbbing Headache,Unilateral Headache,Vertex Headache,Bilateral Headaches,Cephalalgias,Cephalgias,Cephalodynias,Cranial Pains,Generalized Headaches,Head Pains,Headache, Bilateral,Headache, Generalized,Headache, Ocular,Headache, Orthostatic,Headache, Periorbital,Headache, Retro-Ocular,Headache, Sharp,Headache, Throbbing,Headache, Unilateral,Headache, Vertex,Headaches,Headaches, Bilateral,Headaches, Generalized,Headaches, Ocular,Headaches, Orthostatic,Headaches, Periorbital,Headaches, Retro-Ocular,Headaches, Sharp,Headaches, Throbbing,Headaches, Unilateral,Headaches, Vertex,Ocular Headaches,Orthostatic Headaches,Pain, Cranial,Pain, Head,Pains, Cranial,Pains, Head,Periorbital Headaches,Retro Ocular Headache,Retro-Ocular Headaches,Sharp Headaches,Throbbing Headaches,Unilateral Headaches,Vertex Headaches
D006801 Humans Members of the species Homo sapiens. Homo sapiens,Man (Taxonomy),Human,Man, Modern,Modern Man
D000069446 Atazanavir Sulfate An azapeptide and HIV-PROTEASE INHIBITOR that is used in the treatment of HIV INFECTIONS and AIDS in combination with other ANTI-HIV AGENTS. 3,12-bis(1,1-dimethylethyl)-8-hydroxy-4,11-dioxo-9-(phenylmethyl)-6-((4-(2-pyridinyl)phenyl)methyl)-2,5,6,10,13-pentaazatetradecanedioic acid dimethyl ester,Atazanavir,BMS 232632,BMS-232632,BMS-232632-05,BMS232632,CGP 73547,CGP 75136,CGP 75176,CGP 75355,CGP-73547,CGP-75136,CGP-75176,CGP-75355,CGP75136,CGP75176,CGP75355,Reyataz,232632, BMS,BMS 232632 05,BMS23263205,CGP73547
D000284 Administration, Oral The giving of drugs, chemicals, or other substances by mouth. Drug Administration, Oral,Administration, Oral Drug,Oral Administration,Oral Drug Administration,Administrations, Oral,Administrations, Oral Drug,Drug Administrations, Oral,Oral Administrations,Oral Drug Administrations
D000818 Animals Unicellular or multicellular, heterotrophic organisms, that have sensation and the power of voluntary movement. Under the older five kingdom paradigm, Animalia was one of the kingdoms. Under the modern three domain model, Animalia represents one of the many groups in the domain EUKARYOTA. Animal,Metazoa,Animalia

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