Cangrelor

Cangrelor
Clinical data
Trade names	Kengreal, Kengrexal
Other names	AR-C69931MX
AHFS/Drugs.com	Monograph
License data	US DailyMed: Cangrelor;
Routes of; administration	Intravenous
ATC code	B01AC25 (WHO) ;
Legal status
Legal status	CA: ℞-only; US: ℞-only; EU: Rx-only;
Pharmacokinetic data
Bioavailability	100% (IV)
Protein binding	~97–98%.
Metabolism	Rapid deactivation in the circulation (independent of CYP system)
Elimination half-life	~3–6 minutes
Excretion	Kidney (58%), Bile duct (35%)
Identifiers
	IUPAC name [dichloro-[[[(2R,3S,4R,5R)-3,4-dihydroxy-5-[6-(2-methylsulfanylethylamino)-2-(3,3,3-trifluoropropylsulfanyl)purin-9-yl]oxolan-2-yl]methoxy-hydroxyphosphoryl]oxy-hydroxyphosphoryl]methyl]phosphonic acid;
CAS Number	163706-06-7 ;
PubChem CID	9854012;
IUPHAR/BPS	1776;
DrugBank	DB06441 ;
ChemSpider	8029718 ;
UNII	6AQ1Y404U7;
KEGG	D03359 ; as salt: D03361 ;
ChEBI	CHEBI:90841 ;
ChEMBL	ChEMBL1097279 ;
CompTox Dashboard (EPA)	DTXSID90167651 ;
Chemical and physical data
Formula	C17H25Cl2F3N5O12P3S2
Molar mass	776.35 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES CSCCNC1=NC(=NC2=C1N=CN2[C@H]3[C@@H]([C@@H]([C@H](O3)COP(=O)(O)OP(=O)(C(P(=O)(O)O)(Cl)Cl)O)O)O)SCCC(F)(F)F;
	InChI InChI=1S/C17H25Cl2F3N5O12P3S2/c1-43-5-3-23-12-9-13(26-15(25-12)44-4-2-16(20,21)22)27(7-24-9)14-11(29)10(28)8(38-14)6-37-42(35,36)39-41(33,34)17(18,19)40(30,31)32/h7-8,10-11,14,28-29H,2-6H2,1H3,(H,33,34)(H,35,36)(H,23,25,26)(H2,30,31,32)/t8-,10-,11-,14-/m1/s1 ; Key:PAEBIVWUMLRPSK-IDTAVKCVSA-N ;

Cangrelor, sold under the brand name Kengreal among others, is a P2Y₁₂ inhibitor FDA approved as of June 2015 as an antiplatelet drug for intravenous application. Some P2Y₁₂ inhibitors are used clinically as effective inhibitors of adenosine diphosphate-mediated platelet activation and aggregation. Unlike clopidogrel (Plavix), which is a prodrug, cangrelor is an active drug not requiring metabolic conversion.

Poor interim results led to the abandonment of the two CHAMPION clinical trials in mid-2009. The BRIDGE study, for short term use prior to surgery, continues. The CHAMPION PHOENIX trial was a randomized study of over 11,000 patients published in 2013. It found usefulness of cangrelor in patients getting cardiac stents. Compared with clopidogrel given around the time of stenting, intravenous ADP-receptor blockade with cangrelor significantly reduced the rate of stent thrombosis and myocardial infarction. Reviewers have questioned the methodology of the trial.