Sch-351125 and Sch-350634. Schering-Plough.

Abstract

Schering-Plough is developing Sch-351125 (Sch-C), the lead in a series of CCR5 inhibitors, for the potential treatment of HIV infection. By March 2001, it had entered phase I studies in the US, however, by April 2001, these had been suspended based in part on observed QTc prolongation at the highest dose. By December 2001, a new phase I trial had been initiated in France. The company has continued to investigate a number of second-generation CCR5 receptor antagonists, including Sch-350634, for the potential treatment of HIV infection. Although it was reported at two separate meetings in early 2001 that Sch-350634 was in phase I/II trials, in April 2001, Schering-Plough confirmed that the compound was not in clinical development at that time and that a preclinical toxicology program was scheduled for late 2001. In December 2001, Morgan Stanley predicted a 2004 launch for a compound arising from the CCR5 inhibitor program, with sales of US$100 million in 2004, US$200 million in 2005, rising to US$300 million in 2006.

• Authors: José A Esté
• Journal: Current opinion in investigational drugs (London, England : 2000) (Curr Opin Investig Drugs) Vol. 3 Issue 3 Pg. 379-83 (Mar 2002) ISSN: 1472-4472 [Print] England
• PMID: 12054083 (Publication Type: Journal Article, Review)

Chemical References

• 1-((2,4-dimethyl-3-pyridinyl)carbonyl)-4-methyl-4-(3-methyl-4-(1-(4-(trifluoromethyl)phenyl)ethyl)-1-piperazinyl)piperidine N1-oxide
• Anti-HIV Agents
• CCR5 Receptor Antagonists
• Cyclic N-Oxides
• Oximes
• Piperazines
• Piperidines
• Pyridines
• Ancriviroc

Topics

• Anti-HIV Agents (adverse effects, chemical synthesis, metabolism, pharmacology, toxicity)
• CCR5 Receptor Antagonists
• Clinical Trials, Phase I as Topic
• Clinical Trials, Phase II as Topic
• Cyclic N-Oxides (adverse effects, chemical synthesis, metabolism, pharmacology, toxicity)
• HIV Infections (drug therapy)
• Humans
• Oximes
• Piperazines (adverse effects, chemical synthesis, metabolism, pharmacology, toxicity)
• Piperidines
• Pyridines (adverse effects, chemical synthesis, metabolism, pharmacology, toxicity)
• Structure-Activity Relationship