General Information of the Drug (ID: M6APDG00066)
Name
Apixaban
Synonyms
Apixaban; Apixaban(BMS-562247-01); Eliquis; apixabanum; 1-(4-Methoxyphenyl)-7-oxo-6-[4-(2-oxopiperidin-1-yl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridine-3-carboxamide; 1-(4-methoxyphenyl)-7-oxo-6-(4-(2-oxopiperidin-1-yl)phenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridine-3-carboxamide; 3Z9Y7UWC1J; 503612-47-3; BMS 562247-01; BMS-562247; BMS-562247-01; BMS562247-01; CHEBI:72296; CHEMBL231779; UNII-3Z9Y7UWC1J
    Click to Show/Hide
Status
Approved
Structure
Formula
C25H25N5O4
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)
InChIKey
QNZCBYKSOIHPEH-UHFFFAOYSA-N
PubChem CID
10182969
VARIDT Drug ID
DR00211
INTEDE Drug ID
DR0122
Target Gene(s) and Their Upstream m6A Regulator, Together with the Effect of Target Gene(s) in Drug Response
The target genes involved in drug-target interaction (such as drug-metabolizing enzymes, drug transporters and therapeutic targets) and drug-mediated cell death signaling (including modulating DNA damage and repair capacity, escaping from drug-induced apoptosis, autophagy, cellular metabolic reprogramming, oncogenic bypass signaling, cell microenvironment, cell stemness, etc.) could be regulated by m6A regulator(s) and affected their corresponding drug response. You can browse detailed information on drug-related target gene(s) mediated by m6A regulators.
Breast cancer resistance protein (ABCG2)
Methyltransferase-like 3 (METTL3)
In total 1 mechanisms lead to this potential drug response
Response Summary Breast cancer resistance protein (ABCG2) is a therapeutic target for Apixaban. The Methyltransferase-like 3 (METTL3) has potential in affecting the response of Apixaban through regulating the expression of Breast cancer resistance protein (ABCG2). [1], [2]
Cytochrome P450 2C8 (CYP2C8)
Fat mass and obesity-associated protein (FTO)
In total 1 mechanisms lead to this potential drug response
Response Summary Cytochrome P450 2C8 (CYP2C8) is a therapeutic target for Apixaban. The Fat mass and obesity-associated protein (FTO) has potential in affecting the response of Apixaban through regulating the expression of Cytochrome P450 2C8 (CYP2C8). [3], [4]
Methyltransferase-like 14 (METTL14)
In total 1 mechanisms lead to this potential drug response
Response Summary Cytochrome P450 2C8 (CYP2C8) is a therapeutic target for Apixaban. The Methyltransferase-like 14 (METTL14) has potential in affecting the response of Apixaban through regulating the expression of Cytochrome P450 2C8 (CYP2C8). [3], [4]
Methyltransferase-like 3 (METTL3)
In total 1 mechanisms lead to this potential drug response
Response Summary Cytochrome P450 2C8 (CYP2C8) is a therapeutic target for Apixaban. The Methyltransferase-like 3 (METTL3) has potential in affecting the response of Apixaban through regulating the expression of Cytochrome P450 2C8 (CYP2C8). [3], [4]
YTH domain-containing protein 2 (YTHDC2)
In total 1 mechanisms lead to this potential drug response
Response Summary Cytochrome P450 2C8 (CYP2C8) is a therapeutic target for Apixaban. The YTH domain-containing protein 2 (YTHDC2) has potential in affecting the response of Apixaban through regulating the expression of Cytochrome P450 2C8 (CYP2C8). [3], [4]
P-glycoprotein 1 (ABCB1)
Insulin-like growth factor 2 mRNA-binding protein 3 (IGF2BP3)
In total 1 mechanisms lead to this potential drug response
Response Summary P-glycoprotein 1 (ABCB1) is a therapeutic target for Apixaban. The Insulin-like growth factor 2 mRNA-binding protein 3 (IGF2BP3) has potential in affecting the response of Apixaban through regulating the expression of P-glycoprotein 1 (ABCB1). [5], [6]
Methyltransferase-like 3 (METTL3)
In total 1 mechanisms lead to this potential drug response
Response Summary P-glycoprotein 1 (ABCB1) is a therapeutic target for Apixaban. The Methyltransferase-like 3 (METTL3) has potential in affecting the response of Apixaban through regulating the expression of P-glycoprotein 1 (ABCB1). [1], [6]
References
Ref 1 METTL3 promotes adriamycin resistance in MCF-7 breast cancer cells by accelerating pri-microRNA-221-3p maturation in a m6A-dependent manner. Exp Mol Med. 2021 Jan;53(1):91-102. doi: 10.1038/s12276-020-00510-w. Epub 2021 Jan 8.
Ref 2 Characterization of efflux transporters involved in distribution and disposition of apixaban. Drug Metab Dispos. 2013 Apr;41(4):827-35. doi: 10.1124/dmd.112.050260. Epub 2013 Feb 4.
Ref 3 Methylation of adenosine at the N(6) position post-transcriptionally regulates hepatic P450s expression. Biochem Pharmacol. 2020 Jan;171:113697. doi: 10.1016/j.bcp.2019.113697. Epub 2019 Nov 7.
Ref 4 Apixaban. Hosp Pharm. 2013 Jun;48(6):494-509. doi: 10.1310/hpj4806-494.
Ref 5 Binding of RNA m6A by IGF2BP3 triggers chemoresistance of HCT8 cells via upregulation of ABCB1. Am J Cancer Res. 2021 Apr 15;11(4):1428-1445. eCollection 2021.
Ref 6 Effect of Rifampin on the Pharmacokinetics of Apixaban, an Oral Direct Inhibitor of Factor Xa. Am J Cardiovasc Drugs. 2016 Apr;16(2):119-27. doi: 10.1007/s40256-015-0157-9.