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PubMed · 11816839

Cangrelor AstraZeneca.

S C Chattaraj
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Abstract

AstraZeneca is developing the P2T (P2YADP) purinoceptor antagonist and platelet aggregation inhibitor, cangrelor, for the potential treatment of unstable angina and as an ultrafast-acting intravenous antithrombotic agent. It is in phase IIb clinical trials [315723]. NDA and MAA applications are planned for after 2003 [275466], [314472]. It superseded the earlier compound, ARL-67085, which also reached phase II trials [328760]. In ex vivo samples of angina patients' blood, cangrelor inhibits platelet/monocyte conjugate development, which indicate the drug has some degree of disease-modifying activity [377418]. AstraZeneca is also developing derivatives of cangrelor. Removal of the triphosphate side chain, modification of the ribose to a carbocycle and the purine to a triazolopyridine resulted in a potent (IC50 = 4 nM) orally-active P2T/P2Y12 receptor antagonist. A lead compound was scheduled to enter trials as an antithrombotic agent in July 2000 [377666]. In March 1999, Lehman Brothers predicted a 30% probability that the drug would reach world markets and would be launched in 2002 [336599].

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Adenosine MonophosphateAnimalsClinical Trials, Phase I as TopicClinical Trials, Phase II as TopicClinical Trials, Phase III as TopicContraindicationsCoronary DiseaseHemodynamicsHumansPlatelet Aggregation InhibitorsReceptors, PurinergicStructure-Activity RelationshipJournal ArticleReview

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S C Chattaraj. 2001. Cangrelor AstraZeneca.. https://pubmed.ncbi.nlm.nih.gov/11816839/

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