title: Cangrelor AstraZeneca.
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 It superseded the earlier compound, ARL-67085, which also reached phase II trials [328760].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].
authors.affiliation: Mylan Pharmaceuticals Inc, Morgantown, WV 26504-4310, USA. sarat_c82@hotmail.com
authors.forename: S C
authors.initials: SC
authors.lastname: Chattaraj
mesh_terms: D000249:Adenosine Monophosphate / Q000009:adverse effects / Q000031:analogs & derivatives / Q000494:pharmacology* / Q000627:therapeutic use; D000818:Animals; D017321:Clinical Trials, Phase I as Topic; D017322:Clinical Trials, Phase II as Topic; D017326:Clinical Trials, Phase III as Topic; D000075202:Contraindications; D003327:Coronary Disease / Q000188:drug therapy*; D006439:Hemodynamics / Q000187:drug effects; D006801:Humans; D010975:Platelet Aggregation Inhibitors / Q000009:adverse effects / Q000494:pharmacology* / Q000627:therapeutic use; D011983:Receptors, Purinergic / Q000187:drug effects*; D013329:Structure-Activity Relationship
chemical_list: D010975:Platelet Aggregation Inhibitors; D011983:Receptors, Purinergic; D000249:Adenosine Monophosphate; C117446:cangrelor