General Information of Drug (ID: DMQMBZ1)

Drug Name
Rivaroxaban Drug Info
Synonyms XARELTO (TN)
Indication
Disease Entry ICD 11 Status REF
Deep vein thrombosis BD71 Approved [1]
Heparin-induced thrombocytopenia 3B64.12 Approved [2]
Coronavirus Disease 2019 (COVID-19) 1D6Y Phase 3 [3]
Cross-matching ID
PubChem CID
9875401
ChEBI ID
CHEBI:68579
CAS Number
CAS 366789-02-8
TTD Drug ID
DMQMBZ1
VARIDT Drug ID
DR00227
INTEDE Drug ID
DR1431
ACDINA Drug ID
D00601

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 Modulator [4]

Drug Transporter (DTP)
DTP Name DTP ID UniProt ID Highest Status REF
Breast cancer resistance protein (ABCG2) DTI7UX6 ABCG2_HUMAN Approved [5]
P-glycoprotein 1 (ABCB1) DTUGYRD MDR1_HUMAN Approved [6]

Drug-Metabolizing Enzyme (DME)
DME Name DME ID UniProt ID Highest Status REF
Cytochrome P450 3A4 (CYP3A4) DE4LYSA CP3A4_HUMAN Approved [7]
Cytochrome P450 3A5 (CYP3A5) DEIBDNY CP3A5_HUMAN Approved [8]
Cytochrome P450 2J2 (CYP2J2) DERSX5P CP2J2_HUMAN Approved [7]

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 2J2 (CYP2J2) DME CYP2J2 7.706 6.315 4.621 7.65
Cytochrome P450 3A5 (CYP3A5) DME CYP3A5 10.08 7.207 5.403 9.211
Cytochrome P450 3A4 (CYP3A4) DME CYP3A4 11.692 6.58 4.984 9.089
Molecule Expression Atlas in Normal Tissue of Major ADME-related organs

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

The Studied Disease Deep vein thrombosis
ICD Disease Classification BD71
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 2J2 (CYP2J2) DME CYP2J2 1.81E-19 1.37E+00 4.29E+00
Cytochrome P450 3A5 (CYP3A5) DME CYP3A5 3.51E-02 1.53E+00 1.16E+00
Cytochrome P450 3A4 (CYP3A4) DME CYP3A4 5.84E-01 -1.61E-01 -3.61E-01
Molecular Expression Atlas between Disease Section and Healthy Individual Tissue

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: 6388).
2 Rivaroxaban FDA Label
3 Effect of Anticoagulation Therapy on Clinical Outcomes in COVID-19 (COVID-PREVENT)
4 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
5 Absence of both MDR1 (ABCB1) and breast cancer resistance protein (ABCG2) transporters significantly alters rivaroxaban disposition and central nervous system entry. Basic Clin Pharmacol Toxicol. 2013 Mar;112(3):164-70.
6 Downregulation of ABCB1 gene in patients with total hip or knee arthroplasty influences pharmacokinetics of rivaroxaban: a population pharmacokinetic-pharmacodynamic study. Eur J Clin Pharmacol. 2019 Feb 6.
7 Comparative efficacy and safety of the novel oral anticoagulants dabigatran, rivaroxaban and apixaban in preclinical and clinical development. Thromb Haemost. 2010 Mar;103(3):572-85.
8 Pharmacology of the new target-specific oral anticoagulants. J Thromb Thrombolysis. 2013 Aug;36(2):133-40.