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

General Information of Drug (ID: DMPMDTH)

Drug Name

AZD9496 Drug Info

Synonyms

DFBDRVGWBHBJNR-BBNFHIFMSA-N; 1639042-08-2; UNII-DA9P7LN909; DA9P7LN909; CHEMBL3623004; AZD-9496; (E)-3-(3,5-difluoro-4-((1R,3R)-2-(2-fluoro-2-methylpropyl)-3-methyl-2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indol-1-yl)phenyl)acrylic acid; (E)-3-(3,5-Difluoro-4-((1R,3R)-2-(2-fluoro-2-methylpropyl)-3-methyl-2,3,4,9-tetrahydro-1H-pyrido(3,4-b)indol-1-yl)phenyl)acrylic acid; SCHEMBL16266273; SCHEMBL16266275; MolPort-044-560-384; EX-A1326; s8372; BDBM50125052; ZINC219669733; AKOS030526632; AC-29011; HY-12870; Selective estrogen

Indication

Disease Entry	ICD 11	Status	REF
Breast cancer	2C60-2C65	Phase 1	[1]

Cross-matching ID

PubChem CID: 86287635
CAS Number: CAS 1639042-08-2
TTD Drug ID: DMPMDTH
INTEDE Drug ID: DR1801

Molecule-Related Drug Atlas

Molecule Type:

DTT

DME

Drug Status:

Approved Drug(s)

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Drug(s) Targeting Estrogen receptor (ESR)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Tamoxifen	DMLB0EZ	Breast cancer	2C60-2C65	Approved	[3]
Estradiol	DMUNTE3	Acne vulgaris	ED80	Approved	[4]
Estrone	DM5T6US	Acne vulgaris	ED80	Approved	[4]
Estradiol Valerate	DM8MC6O	Hormone replacement therapy	8E01	Approved	[5]
Estradiol Acetate	DM07U2A	Hormone replacement therapy	8E01	Approved	[5]
Estradiol Cypionate	DM27Z5T	Hormone replacement therapy	8E01	Approved	[5]
Ethinyl Estradiol	DMODJ40	Acne vulgaris	ED80	Approved	[6]
Raloxifene	DMDKF3M	Osteoporosis	FB83.0	Approved	[7]
Ospemifene	DMC4GEI	Dyspareunia	GA12	Approved	[8]
Toremifene	DMQYUWG	Breast cancer	2C60-2C65	Approved	[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

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Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Estrogen receptor (ESR)	TTZAYWL	ESR1_HUMAN	Antagonist	[1]

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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	[2]

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References

1	Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
2	Complete substrate inhibition of cytochrome P450 2C8 by AZD9496, an oral selective estrogen receptor degrader. Drug Metab Dispos. 2018 Sep;46(9):1268-1276.
3	Modulators of vascular sex hormone receptors and their effects in estrogen-deficiency states associated with menopause. Recent Pat Cardiovasc Drug Discov. 2008 Nov;3(3):165-86.
4	Reprint of Are all estrogens the same Maturitas. 2008 Sep-Oct;61(1-2):195-201.
5	Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
6	17alpha-Ethinylestradiol hinders nucleotide excision repair in zebrafish liver cells. Aquat Toxicol. 2009 Dec 13;95(4):273-8.
7	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. (Target id: 620).
8	Clinical pipeline report, company report or official report of Shionogi (2011).
9	Effect of selective estrogen receptor modulators on cell proliferation and estrogen receptor activities in normal human prostate stromal and epithe... Prostate Cancer Prostatic Dis. 2009;12(4):375-81.
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.