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.
MeSH terms
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Anti-HIV Agents / adverse effects
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Anti-HIV Agents / chemical synthesis
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Anti-HIV Agents / metabolism
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Anti-HIV Agents / pharmacology*
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Anti-HIV Agents / toxicity
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CCR5 Receptor Antagonists*
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Clinical Trials, Phase I as Topic
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Clinical Trials, Phase II as Topic
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Cyclic N-Oxides / adverse effects
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Cyclic N-Oxides / chemical synthesis
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Cyclic N-Oxides / metabolism
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Cyclic N-Oxides / pharmacology*
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Cyclic N-Oxides / toxicity
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HIV Infections / drug therapy*
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Humans
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Oximes
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Piperazines / adverse effects
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Piperazines / chemical synthesis
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Piperazines / metabolism
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Piperazines / pharmacology*
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Piperazines / toxicity
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Piperidines*
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Pyridines / adverse effects
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Pyridines / chemical synthesis
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Pyridines / metabolism
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Pyridines / pharmacology*
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Pyridines / toxicity
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Structure-Activity Relationship
Substances
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1-((2,4-dimethyl-3-pyridinyl)carbonyl)-4-methyl-4-(3-methyl-4-(1-(4-(trifluoromethyl)phenyl)ethyl)-1-piperazinyl)piperidine N1-oxide
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Anti-HIV Agents
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CCR5 Receptor Antagonists
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Cyclic N-Oxides
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Oximes
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Piperazines
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Piperidines
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Pyridines
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Ancriviroc