Product Name

Apixaban

CAS Number

503612-47-3

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Product Name:
Apixaban
CAS Number:
503612-47-3
Indication:
Apixaban is to reduce the risk of stroke and systemic embolism in patients with nonvalvular atrial fibrillation. It has also been used to lower the risk of developing venous thrombosis post-orthopedic surgical procedures.
Mode of Action:

Apixaban acts by directly inhibiting, in a reversible manner, free and clot-bound factor Xa to inhibit coagulation.

Pharmacodynamics:

Apixaban acts by inhibiting coagulation, and thus prevents development of blood clots. As a result of FXa inhibition, apixaban prolongs clotting tests such as prothrombin time (PT), INR, and activated partial thromboplastin time (aPTT). Changes observed in these clotting tests at the expected therapeutic dose, however, are small, subject to a high degree of variability, and not useful in monitoring the anticoagulation effect of apixaban. The Rotachrom® Heparin chromogenic assay is not recommended for assessing the anticoagulant effect of apixaban.

Metabolism:

Apixaban mainly undergoes o-demethylation and hydroxylation to metabolites. The major site of biotransformation is at the 3-oxopiperidinyl moiety. The main enzyme responsible for metabolism is CYP3A4/5 while CYP1A2, 2C8, 2C9, 2C19, and 2J2 are minor metabolic enzymes. There are no active metabolites and unchanged apixaban is the primary circulating entity.

Toxicity:

Major bleeding events.

IUPAC:
1-(4-methoxyphenyl)-7-oxo-6-[4-(2-oxopiperidin-1-yl)phenyl]-4, 5-dihydropyrazolo[5, 4-c]pyridine-3-carboxamide
ATC:
B01AF02
PubChem:
10182969
DrugBank:
DB06605
Formula:
C25H25N5O4
Molecular Mass:
459.497
Synonyms:
BMS-562247
SMILES:
COC1=CC=C(C=C1)N1N=C(C(N)=O)C2=C1C(=O)N(CC2)C1=CC=C(C=C1)N1CCCCC1=O
AHFS Code:
20:12.04.14
InChi:
InChI=1S/C25H25N5O4/c1-34-19-11-9-18(10-12-19)30-23-20(22(27-30)24(26)32)13-15-29(25(23)33)17-7-5-16(6-8-17)28-14-3-2-4-21(28)31/h5-12H,2-4,13-15H2,1H3,(H2,26,32)
General Reference:
General Reference:

 

  1. Granger CB, Alexander JH, McMurray JJ, Lopes RD, Hylek EM, Hanna M, Al-Khalidi HR, Ansell J, Atar D, Avezum A, Bahit MC, Diaz R, Easton JD, Ezekowitz JA, Flaker G, Garcia D, Geraldes M, Gersh BJ, Golitsyn S, Goto S, Hermosillo AG, Hohnloser SH, Horowitz J, Mohan P, Jansky P, Lewis BS, Lopez-Sendon JL, Pais P, Parkhomenko A, Verheugt FW, Zhu J, Wallentin L: Apixaban versus warfarin in patients with atrial fibrillation. N Engl J Med. 2011 Sep 15;365(11):981-92. doi: 10.1056/NEJMoa1107039. Epub 2011 Aug 27. Pubmed
  2. de Souza Brito F, Lopes RD, Alexander JH: The safety and efficacy of apixaban : where do we stand in 2013? Expert Opin Drug Saf. 2013 May 10. Pubmed

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