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

General Information of Drug (ID: DMAT2XH)

Drug Name
Nabumetone Drug Info
Synonyms NNB-001; NNB-004; NNB-005; Nabumetone (oral); Nabumetone (oral), Nobex; 6-MNA (oral), Nobex
Indication
Disease Entry ICD 11 Status REF
Osteoarthritis FA00-FA05 Approved [1]
Pain MG30-MG3Z Approved [2]
Cross-matching ID
PubChem CID
4409
ChEBI ID
CHEBI:7443
CAS Number
CAS 42924-53-8
TTD Drug ID
DMAT2XH
INTEDE Drug ID
DR1122
ACDINA Drug ID
D00451

Molecule(s) Related to This Drug


Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
Prostaglandin G/H synthase 2 (COX-2) TTVKILB PGH2_HUMAN Inhibitor [3]

Drug-Metabolizing Enzyme (DME)
DME Name DME ID UniProt ID Highest Status REF
Cytochrome P450 2C9 (CYP2C9) DE5IED8 CP2C9_HUMAN Approved [4]
Cytochrome P450 1A2 (CYP1A2) DEJGDUW CP1A2_HUMAN Approved [5]
Aldo-keto reductase 1C1 (AKR1C1) DE7P2FB AK1C1_HUMAN Approved [6]
Aldo-keto reductase 1C4 (AKR1C4) DEAJN47 AK1C4_HUMAN Approved [6]
Corticosteroid 11-beta-dehydrogenase 1 (HSD11B1) DEZDRQO DHI1_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
Corticosteroid 11-beta-dehydrogenase 1 (HSD11B1) DME HSD11B1 10.967 5.178 5.865 6.377
Cytochrome P450 1A2 (CYP1A2) DME CYP1A2 10.036 5.779 6.508 6.481
Aldo-keto reductase 1C4 (AKR1C4) DME AKR1C4 8.442 2.511 3.138 1
Aldo-keto reductase 1C1 (AKR1C1) DME AKR1C1 10.667 8.55 9.706 8.77
Cytochrome P450 2C9 (CYP2C9) DME CYP2C9 11.76 5.931 6.164 9.423
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 Osteoarthritis
ICD Disease Classification FA00-FA05
Molecule Name Molecule Type Gene Name p-value Fold-Change Z-score
Prostaglandin G/H synthase 2 (COX-2) DTT PTGS2 7.93E-04 -0.29 -0.34
Corticosteroid 11-beta-dehydrogenase 1 (HSD11B1) DME HSD11B1 1.64E-01 1.14E-01 1.66E-01
Cytochrome P450 1A2 (CYP1A2) DME CYP1A2 7.36E-01 1.62E-02 1.08E-01
Aldo-keto reductase 1C4 (AKR1C4) DME AKR1C4 4.05E-01 3.23E-02 2.28E-01
Aldo-keto reductase 1C1 (AKR1C1) DME AKR1C1 7.03E-02 6.23E-02 2.87E-01
Cytochrome P450 2C9 (CYP2C9) DME CYP2C9 1.90E-01 -9.81E-03 -5.96E-02
Molecular Expression Atlas between Disease Section and Healthy Individual Tissue

References

1 Nabumetone FDA Label
2 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: 7245).
3 Renal effects of nabumetone, a COX-2 antagonist: impairment of function in isolated perfused rat kidneys contrasts with preserved renal function in vivo. Exp Nephrol. 2001;9(6):387-96.
4 In vitro characterization of the cytochrome P450 isoforms involved in the metabolism of 6-methoxy-2-napthylacetic acid, an active metabolite of the prodrug nabumetone. Biol Pharm Bull. 2011;34(5):734-9.
5 A predominate role of CYP1A2 for the metabolism of nabumetone to the active metabolite, 6-methoxy-2-naphthylacetic acid, in human liver microsomes. Drug Metab Dispos. 2009 May;37(5):1017-24.
6 Reductive metabolism of nabumetone by human liver microsomal and cytosolic fractions: exploratory prediction using inhibitors and substrates as marker probes. Eur J Drug Metab Pharmacokinet. 2015 Jun;40(2):127-35.