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

General Information of Drug (ID: DMZMSPF)

Drug Name

Bicalutamide Drug Info

Synonyms

Casodex; Cosudex; Propanamide; Raffolutil; Astra brand of bicalutamide; AstraZeneca brand of bicalutamide; Zeneca brand of bicalutamide; Calutide (TN); Casodex (TN); Cosudex (TN); KS-1161; Kalumid (TN); Bicalutamide [USAN:INN:BAN]; Bicalutamide (JAN/USP/INN); Casodex, Cosudex, Calutide, Kalumid, Bicalutamide; N-[4-cyano-3-(trifluoromethyl)phenyl]-3-(4-fluorophenyl)sulfonyl-2-hydroxy-2-methylpropanamide; (+-)-4'-Cyano-alpha,alpha,alpha-trifluoro-3-((p-fluorophenyl)sulfonyl)-2-methyl-m-lactotoluidide; 4'-cyano-3-(4-fluorophenylsulfonyl)-2-hydroxy-2-methyl-3'-(trifluoromethyl)propionanilide

Indication

Disease Entry	ICD 11	Status	REF
Prostate cancer	2C82.0	Approved	[1]
Castration-resistant prostate carcinoma		Investigative	[2]
Metastatic prostate carcinoma		Investigative	[2]

Therapeutic Class

Anticancer Agents

Cross-matching ID

PubChem CID: 2375
ChEBI ID: CHEBI:91617
CAS Number: CAS 90357-06-5
TTD Drug ID: DMZMSPF
VARIDT Drug ID: DR00795
INTEDE Drug ID: DR0210
ACDINA Drug ID: D00069

Molecule(s) Related to This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Androgen receptor (AR)	TTS64P2	ANDR_HUMAN	Antagonist	[3]

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Drug Transporter (DTP)

DTP Name	DTP ID	UniProt ID	Highest Status	REF
Breast cancer resistance protein (ABCG2)	DTI7UX6	ABCG2_HUMAN	Approved	[4]
P-glycoprotein 1 (ABCB1)	DTUGYRD	MDR1_HUMAN	Approved	[4]

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Drug-Metabolizing Enzyme (DME)

DME Name	DME ID	UniProt ID	Highest Status	REF
Cytochrome P450 3A4 (CYP3A4)	DE4LYSA	CP3A4_HUMAN	Approved	[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
Androgen receptor (AR)	DTT	AR	5.955	4.868	5.902	5.567
P-glycoprotein 1 (ABCB1)	DTP	P-GP	7.009	6.988	7.442	8.135
Breast cancer resistance protein (ABCG2)	DTP	BCRP	6.732	7.513	6.326	9.277
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

Prostate cancer

ICD Disease Classification

2C82.0

Molecule Name	Molecule Type	Gene Name	p-value	Fold-Change	Z-score
Androgen receptor (AR)	DTT	AR	2.13E-01	-0.07	-0.11
P-glycoprotein 1 (ABCB1)	DTP	P-GP	2.80E-02	-1.36E-01	-1.05E+00
Breast cancer resistance protein (ABCG2)	DTP	BCRP	1.91E-02	2.50E-01	1.01E+00
Cytochrome P450 3A4 (CYP3A4)	DME	CYP3A4	7.93E-02	-8.20E-02	-8.93E-01

Molecular Expression Atlas between Disease Section and Healthy Individual Tissue

References

1	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: 2863).
2	Bicalutamide FDA Label
3	Androgen receptor overexpression induces tamoxifen resistance in human breast cancer cells. Breast Cancer Res Treat. 2010 May;121(1):1-11.
4	Effects of the ABCG2 and ABCB1 drug transporter polymorphisms on the pharmacokinetics of bicalutamide in humans. Clin Chim Acta. 2015 Jan 1;438:7-11.
5	Bicalutamide: clinical pharmacokinetics and metabolism. Clin Pharmacokinet. 2004;43(13):855-78.