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

General Information of Drug (ID: DMFORDT)

Drug Name

Afimoxifene Drug Info

Synonyms

4-Hydroxytamoxifen; Afimoxifene; (Z)-4-Hydroxytamoxifen; Hydroxytamoxifen; 4-Monohydroxytamoxifen; Tamogel; 68047-06-3; trans-4-Hydroxytamoxifen; Ici 79280; 68392-35-8; 65213-48-1; 4-OH-TAM; (Z)-4-(1-(4-(2-(Dimethylamino)ethoxy)phenyl)-2-phenylbut-1-en-1-yl)phenol; Z-4-hydroxytamoxifen; UNII-95K54647BZ; CHEMBL489; ICI 79,280; TAMOXIFEN, 4-HYDROXY-, (Z)-; BRN 4910749; (E/Z)-4-Hydroxy Tamoxifen; MLS000069742; C26H29NO2; CHEBI:44616; 95K54647BZ; SMR000058939; 4-(1-(4-(2-(Dimethylamino)ethoxy)phenyl)-2-phenylbut-1-enyl)phenol

Indication

Disease Entry	ICD 11	Status	REF
Breast cancer	2C60-2C65	Phase 2	[1]
Ductal carcinoma	2E65.2	Phase 2	[2]

Cross-matching ID

PubChem CID: 449459
ChEBI ID: CHEBI:44616
CAS Number: CAS 68047-06-3
TTD Drug ID: DMFORDT
VARIDT Drug ID: DR01487
INTEDE Drug ID: DR1944

Molecule(s) Related to This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Estrogen receptor (ESR)	TTZAYWL	ESR1_HUMAN	Modulator	[3]

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Drug Transporter (DTP)

DTP Name	DTP ID	UniProt ID	Highest Status	REF
P-glycoprotein 1 (ABCB1)	DTUGYRD	MDR1_HUMAN	Phase 3	[4]

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Drug-Metabolizing Enzyme (DME)

DME Name	DME ID	UniProt ID	Highest Status	REF
UDP-glucuronosyltransferase 1A1 (UGT1A1)	DEYGVN4	UD11_HUMAN	Phase 2	[5]
UDP-glucuronosyltransferase 1A8 (UGT1A8)	DE2GB8N	UD18_HUMAN	Phase 2	[5]

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

Molecule	Molecule Type	Gene Name	Liver	Colon	Kidney	Small Intestine
Estrogen receptor (ESR)	DTT	ESR1	3.728	3.17	4.897	4.505
P-glycoprotein 1 (ABCB1)	DTP	P-GP	7.009	6.988	7.442	8.135

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

Breast cancer

ICD Disease Classification

2C60-2C65

Molecule Name	Molecule Type	Gene Name	p-value	Fold-Change	Z-score
P-glycoprotein 1 (ABCB1)	DTP	P-GP	7.23E-01	-8.20E-02	-3.22E-01
UDP-glucuronosyltransferase 1A1 (UGT1A1)	DME	UGT1A1	7.69E-01	1.91E-02	5.45E-02

Molecular Expression Atlas between Disease Section and Healthy Individual Tissue

References

1	ClinicalTrials.gov (NCT00272714) Study of Afimoxifene Gel to Treat Cyclic Mastalgia in Premenopausal Women. U.S. National Institutes of Health.
2	Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
3	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).
4	Antiestrogens and steroid hormones: substrates of the human P-glycoprotein. Biochem Pharmacol. 1994 Jul 19;48(2):287-92.
5	Glucuronidation of active tamoxifen metabolites by the human UDP glucuronosyltransferases. Drug Metab Dispos. 2007 Nov;35(11):2006-14.