Details of the Drug-Related molecule(s) Expression Atlas

General Information of Drug (ID: DM89JLN)

• Drug Name: Apixaban Drug Info
• Synonyms: GG2; BMS 562247-01; BMS-562247; Eliquis (TN); BMS-562247-01; Apixaban (JAN/USAN/INN); BMS-562247-01, Apixaban; Ro-1H-pyrazolo[3,4-c]pyridine-3-carboxylic acid amide; 1-(4-Methoxyphenyl)-7-oxo-6-[4-(2-oxopiperidin-1-yl)phenyl]-4,5,6,7-tetrahyd

Indication

Disease Entry	ICD 11	Status	REF
Thrombosis	DB61-GB90	Approved	[1]

• Cross-matching ID:
  PubChem CID: 10182969
  ChEBI ID: CHEBI:72296
  CAS Number: CAS 503612-47-3
  TTD Drug ID: DM89JLN
  VARIDT Drug ID: DR00211
  INTEDE Drug ID: DR0122
  ACDINA Drug ID: D00040

Molecule(s) Related to This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Coagulation factor Xa (F10)	TTCIHJA	FA10_HUMAN	Inhibitor	[2]

Drug Transporter (DTP)

DTP Name	DTP ID	UniProt ID	Highest Status	REF
Breast cancer resistance protein (ABCG2)	DTI7UX6	ABCG2_HUMAN	Approved	[3]
P-glycoprotein 1 (ABCB1)	DTUGYRD	MDR1_HUMAN	Approved	[4]

Drug-Metabolizing Enzyme (DME)

DME Name	DME ID	UniProt ID	Highest Status	REF
Cytochrome P450 3A4 (CYP3A4)	DE4LYSA	CP3A4_HUMAN	Approved	[5]
Cytochrome P450 2C9 (CYP2C9)	DE5IED8	CP2C9_HUMAN	Approved	[6]
Mephenytoin 4-hydroxylase (CYP2C19)	DEGTFWK	CP2CJ_HUMAN	Approved	[6]
Cytochrome P450 1A2 (CYP1A2)	DEJGDUW	CP1A2_HUMAN	Approved	[6]
Cytochrome P450 3A5 (CYP3A5)	DEIBDNY	CP3A5_HUMAN	Approved	[7]
Cytochrome P450 2C8 (CYP2C8)	DES5XRU	CP2C8_HUMAN	Approved	[6]

The Expression Level of Molecule(s) in Normal Tissue of Major ADME-Related Organs

Molecule	Molecule Type	Gene Name	Liver	Colon	Kidney	Small Intestine
Coagulation factor Xa (F10)	DTT	F10	7.763	4.672	3.248	4.609
P-glycoprotein 1 (ABCB1)	DTP	P-GP	7.009	6.988	7.442	8.135
Breast cancer resistance protein (ABCG2)	DTP	BCRP	6.732	7.513	6.326	9.277
Cytochrome P450 2C8 (CYP2C8)	DME	CYP2C8	9.791	3.744	3.413	1.609
Cytochrome P450 1A2 (CYP1A2)	DME	CYP1A2	10.036	5.779	6.508	6.481
Cytochrome P450 3A5 (CYP3A5)	DME	CYP3A5	10.08	7.207	5.403	9.211
Mephenytoin 4-hydroxylase (CYP2C19)	DME	CYP2C19	7.867	5.142	5.52	7.08
Cytochrome P450 2C9 (CYP2C9)	DME	CYP2C9	11.76	5.931	6.164	9.423
Cytochrome P450 3A4 (CYP3A4)	DME	CYP3A4	11.692	6.58	4.984	9.089

The Expression Level of Molecule(s) between Disease Section and Healthy Individual Tissue

• The Studied Disease: Thrombosis
• ICD Disease Classification: DB61-GB90

Molecule Name	Molecule Type	Gene Name	p-value	Fold-Change	Z-score
Coagulation factor Xa (F10)	DTT	F10	4.84E-02	-0.28	-0.9
P-glycoprotein 1 (ABCB1)	DTP	P-GP	2.04E-02	-1.13E+00	-1.00E+00
Breast cancer resistance protein (ABCG2)	DTP	BCRP	2.10E-01	3.71E-01	7.59E-01
Cytochrome P450 2C8 (CYP2C8)	DME	CYP2C8	1.73E-04	1.53E-01	7.44E-01
Cytochrome P450 1A2 (CYP1A2)	DME	CYP1A2	1.44E-01	-3.59E-01	-1.14E+00
Cytochrome P450 3A5 (CYP3A5)	DME	CYP3A5	3.51E-02	1.53E+00	1.16E+00
Mephenytoin 4-hydroxylase (CYP2C19)	DME	CYP2C19	1.02E-01	-2.84E-01	-7.34E-01
Cytochrome P450 2C9 (CYP2C9)	DME	CYP2C9	1.62E-02	-4.23E-01	-1.25E+00
Cytochrome P450 3A4 (CYP3A4)	DME	CYP3A4	5.84E-01	-1.61E-01	-3.61E-01

References

• [1] URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 6390).
• [2] Pfizer. Product Development Pipeline. March 31 2009.
• [3] Characterization of efflux transporters involved in distribution and disposition of apixaban. Drug Metab Dispos. 2013 Apr;41(4):827-35.
• [4] 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.
• [5] In vitro assessment of metabolic drug-drug interaction potential of apixaban through cytochrome P450 phenotyping, inhibition, and induction studies. Drug Metab Dispos. 2010 Mar;38(3):448-58.
• [6] Apixaban. Hosp Pharm. 2013 Jun;48(6):494-509.
• [7] Apixaban. After hip or knee replacement: LMWH remains the standard treatment. Prescrire Int. 2012 Sep;21(130):201-2, 204.