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

General Information of Drug (ID: DM8SMD1)

Drug Name

Tazarotene Drug Info

Synonyms

Avage; Suretin; Tazaroteno; Tazarotenum; Tazorac; Tazoral; Zorac; AGN 190168; AGN-190168; Avage (TN); Tazarotene [USAN:INN]; Tazorac (TN); Zorac (TN); Tazarotene (JAN/USAN/INN); Tazorac, Avage, Zora, Tazarotene; Ethyl 6-((4,4-dimethylthiochroman-6-yl)ethynyl)nicotinate; Ethyl 6-(2-(4,4-dimethylthiochroman-6-yl)ethynyl)nicotinate; Ethyl 6-[(4,4-dimethyl-3,4-dihydro-2H-thiochromen-6-yl)ethynyl]nicotinate; Ethyl 6-[2-(4,4-dimethyl-2,3-dihydrothiochromen-6-yl)ethynyl]pyridine-3-carboxylate; 3-Pyridinecarboxylic acid, 6-((3,4-dihydro-4,4-dimethyl-2H-1-benzothiopyran-6-yl)ethynyl)-, ethyl ester; 3-Pyridinecarboxylic acid, 6-((3,4-dihydro-4,4-dimethyl-2H-1-benzothiopyran-6-yl)ethynyl)-,ethyl ester

Indication

Disease Entry	ICD 11	Status	REF
Acne vulgaris	ED80	Approved	[1]
Psoriasis	EA90	Approved	[1]
Psoriasis vulgaris	EA90	Approved	[2]

Therapeutic Class

Dermatologic Agents

Cross-matching ID

PubChem CID: 5381
ChEBI ID: CHEMBL32184
CAS Number: CAS 118292-40-3
TTD Drug ID: DM8SMD1
INTEDE Drug ID: DR1536

Molecule-Related Drug Atlas

Molecule Type:

DTT

DME

Drug Status:

Approved Drug(s)

Patented Agent(s)

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Drug(s) Targeting Retinoic acid receptor gamma (RARG)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Tretinoin	DM49DUI	Acne vulgaris	ED80	Approved	[5]
Alitretinoin	DMME8LH	Kaposi sarcoma	2B57	Approved	[6]
Trifarotene	DMOL793	Acne vulgaris	ED80	Approved	[7]
Palovarotene	DMAD2OZ	Fibrodysplasia ossificans progressiva	FB31.1	Approved	[8]
PMID27336223-Compound-13	DMSZLYD	N. A.	N. A.	Patented	[9]
PMID27336223-Compound-12	DMT4P7K	N. A.	N. A.	Patented	[9]
PMID27336223-Compound-14	DMC41MA	N. A.	N. A.	Patented	[9]
PMID27336223-Compound-11	DMBN6KU	N. A.	N. A.	Patented	[9]
PMID27336223-Compound-15	DMIYCFE	N. A.	N. A.	Patented	[9]
PMID27336223-Compound-9	DM6V13W	N. A.	N. A.	Patented	[9]
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Drug(s) Metabolized By Cytochrome P450 2C8 (CYP2C8)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Fluorouracil	DMUM7HZ	Adenocarcinoma	2D40	Approved	[10]
Estradiol	DMUNTE3	Acne vulgaris	ED80	Approved	[11]
Imatinib	DM7RJXL	Acute lymphoblastic leukaemia	2A85	Approved	[11]
Zidovudine	DM4KI7O	Human immunodeficiency virus infection	1C62	Approved	[12]
Verapamil	DMA7PEW	Angina pectoris	BA40	Approved	[13]
Diclofenac	DMPIHLS	Chronic renal failure	GB61.Z	Approved	[14]
Sorafenib	DMS8IFC	Adenocarcinoma	2D40	Approved	[15]
Quinine	DMSWYF5	Malaria	1F40-1F45	Approved	[11]
Mycophenolate mofetil	DMPQAGE	Hepatosplenic T-cell lymphoma		Approved	[16]
Propofol	DMB4OLE	Anaesthesia	9A78.6	Approved	[17]
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Molecular Interaction Atlas of This Drug

Molecular Interaction Atlas

Download the Complete Interaction Atlas for Visualization in Cytoscape

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Retinoic acid receptor gamma (RARG)	TT1Q3IE	RARG_HUMAN	Binder	[3]

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Drug-Metabolizing Enzyme (DME)

DME Name	DME ID	UniProt ID	MOA	REF
Cytochrome P450 2C8 (CYP2C8)^{Main DME}	DES5XRU	CP2C8_HUMAN	Substrate	[4]

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References

1	Tazarotene 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: 6952).
3	Recent developments in receptor-selective retinoids. Curr Pharm Des. 2000 Jun;6(9):919-31.
4	Cytochrome P450 2C8 and flavin-containing monooxygenases are involved in the metabolism of tazarotenic acid in humans. Drug Metab Dispos. 2003 Apr;31(4):476-81.
5	Targacept active conformation search: a new method for predicting the conformation of a ligand bound to its protein target. J Med Chem. 2004 Dec 30;47(27):6831-9.
6	Retinoic acid receptors and retinoid X receptors: interactions with endogenous retinoic acids. Proc Natl Acad Sci U S A. 1993 Jan 1;90(1):30-4.
7	Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2019
8	Randomised controlled trial for emphysema with a selective agonist of the gamma-type retinoic acid receptor. Eur Respir J. 2012 Aug;40(2):306-12.
9	Therapeutic use of selective synthetic ligands for retinoic acid receptors: a patent review.Expert Opin Ther Pat. 2016 Aug;26(8):957-71.
10	Roles of cytochromes P450 1A2, 2A6, and 2C8 in 5-fluorouracil formation from tegafur, an anticancer prodrug, in human liver microsomes. Drug Metab Dispos. 2000 Dec;28(12):1457-63.
11	Role of cytochrome P450 2C8 in drug metabolism and interactions. Pharmacol Rev. 2016 Jan;68(1):168-241.
12	Summary of information on human CYP enzymes: human P450 metabolism data. Drug Metab Rev. 2002 Feb-May;34(1-2):83-448.
13	Differential expression and function of CYP2C isoforms in human intestine and liver. Pharmacogenetics. 2003 Sep;13(9):565-75.
14	Analysis of human cytochrome P450 2C8 substrate specificity using a substrate pharmacophore and site-directed mutants. Biochemistry. 2004 Dec 14;43(49):15379-92.
15	Interaction of sorafenib and cytochrome P450 isoenzymes in patients with advanced melanoma: a phase I/II pharmacokinetic interaction study. Cancer Chemother Pharmacol. 2011 Nov;68(5):1111-8.
16	PharmGKB summary: mycophenolic acid pathway. Pharmacogenet Genomics. 2014 Jan;24(1):73-9.
17	Possible involvement of multiple human cytochrome P450 isoforms in the liver metabolism of propofol. Br J Anaesth. 1998 Jun;80(6):788-95.