General Information of Drug (ID: DME5Y64)

Drug Name
Tranilast Drug Info
Synonyms
tranilast; 53902-12-8; Rizaben; trans-Tranilast; Tranilastum; 70806-55-2; MK 341; N-(3,4-Dimethoxycinnamoyl)anthranilic acid; Tranilastum [INN-Latin]; Tranilast [USAN:INN:JAN]; Tranpro; UNII-HVF50SMY6E; SB-252218; MK-341; Tranilast (SB 252218); 3,4-DAA; n-(3',4'-dimethoxycinnamoyl) anthranilic acid; HVF50SMY6E; MLS000028468; CHEBI:77572; C18H17NO5; Anthranilic acid, N-(3,4-dimethoxycinnamoyl)-; NZHGWWWHIYHZNX-CSKARUKUSA-N; 2-((3-(3,4-Dimethoxyphenyl)-1-oxo-2-propenyl)amino)benzoic acid; MFCD00864787; T 0318; NU-3450; Rizaben (TN); Tranilast (JAN/USAN/INN); Rizaben, SB 252218, MK 341, Tranpro ,Tranilast; N-(3',4'-dimethoxycinnamoyl) anthranilic acid; N-(3′ -Dimethoxycinnamoyl)anthranilic Acid; 2-({(2E)-3-[3,4-bis(methyloxy)phenyl]prop-2-enoyl}amino)benzoic acid; 2-[[(E)-3-(3,4-dimethoxyphenyl)prop-2-enoyl]amino]benzoic acid; 2-[[3-(3,4-Dimethoxyphenyl)-1-oxo-2-propenyl]amino] benzoic acid; Molecule 20
Indication
Disease Entry ICD 11 Status REF
Allergic rhinitis CA08.0 Approved [1]
Ocular allergy 4A81 Approved [2]
Asthma CA23 Investigative [3]
Keloid EE60 Investigative [4]
Cross-matching ID
PubChem CID
5282230
ChEBI ID
CHEBI:77572
CAS Number
CAS 53902-12-8
TTD Drug ID
DME5Y64
INTEDE Drug ID
DR1628

Molecule(s) Related to This Drug


Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
Histamine H1 receptor (H1R) TTTIBOJ HRH1_HUMAN Antagonist [5]
Steryl-sulfatase (STS) TTHM0R1 STS_HUMAN Inhibitor [6]

Drug-Metabolizing Enzyme (DME)
DME Name DME ID UniProt ID Highest Status REF
Cytochrome P450 3A4 (CYP3A4) DE4LYSA CP3A4_HUMAN Phase 4 [7]
Cytochrome P450 2C9 (CYP2C9) DE5IED8 CP2C9_HUMAN Phase 4 [8]

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

Molecule Molecule Type Gene Name Liver Colon Kidney Small Intestine
Histamine H1 receptor (H1R) DTT HRH1 5.972 5.7 5.816 6.002
Steryl-sulfatase (STS) DTT STS 4.722 6.048 5.125 4.768
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
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 Allergic rhinitis
ICD Disease Classification CA08.0
Molecule Name Molecule Type Gene Name p-value Fold-Change Z-score
Steryl-sulfatase (STS) DTT STS 1.80E-38 -0.79 -1.15
Cytochrome P450 2C9 (CYP2C9) DME CYP2C9 1.07E-11 -1.16E-01 -2.53E-01
Cytochrome P450 3A4 (CYP3A4) DME CYP3A4 1.87E-03 -6.67E-02 -2.12E-01
Molecular Expression Atlas between Disease Section and Healthy Individual Tissue

References

1 Seasonal facial erythema in a patient with allergic rhinitis treated using a combination of tranilast and roxithromycin. Immunopharmacol Immunotoxicol. 2023 Dec;45(4):508-510.
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: 6326).
3 Tranilast: a review of its therapeutic applications. Pharmacol Res. 2015 Jan;91:15-28.
4 Treatment of keloid and hypertrophic scars by iontophoretic transdermal delivery of tranilast. Scand J Plast Reconstr Surg Hand Surg. 1997 Jun;31(2):151-8.
5 Emerging drugs for ocular allergy. Expert Opin Emerg Drugs. 2005 Aug;10(3):505-20.
6 Review of estrone sulfatase and its inhibitors--an important new target against hormone dependent breast cancer. Curr Med Chem. 2002 Jan;9(2):263-73.
7 Integrated analysis on the physicochemical properties of dihydropyridine calcium channel blockers in grapefruit juice interactions. Curr Pharm Biotechnol. 2012 Jul;13(9):1705-17.
8 Glucuronidation of antiallergic drug, Tranilast: identification of human UDP-glucuronosyltransferase isoforms and effect of its phase I metabolite. Drug Metab Dispos. 2007 Apr;35(4):583-9.