Sch-351125 and Sch-350634. Schering-Plough

Curr Opin Investig Drugs. 2002 Mar;3(3):379-83.

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.

Publication types

  • Review

MeSH terms

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

Substances

  • 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