Drug Information

Drug (ID: DG00247) and It's Reported Resistant Information

Name	Enzalutamide
Synonyms	MDV3100; Enzalutamide (AR inhibitor) Click to Show/Hide
Indication	In total 1 Indication(s) Prostate cancer [ICD-11: 2C82] Approved [1]
Structure
Drug Resistance Disease(s)	Disease(s) with Clinically Reported Resistance for This Drug (1 diseases) Prostate cancer [ICD-11: 2C82] [1]
Target	Androgen receptor (AR)	ANDR_HUMAN	[1]
Click to Show/Hide the Molecular Information and External Link(s) of This Drug
Formula	C21H16F4N4O2S
IsoSMILES	CC1(C(=O)N(C(=S)N1C2=CC(=C(C=C2)C(=O)NC)F)C3=CC(=C(C=C3)C#N)C(F)(F)F)C
InChI	1S/C21H16F4N4O2S/c1-20(2)18(31)28(12-5-4-11(10-26)15(8-12)21(23,24)25)19(32)29(20)13-6-7-14(16(22)9-13)17(30)27-3/h4-9H,1-3H3,(H,27,30)
InChIKey	WXCXUHSOUPDCQV-UHFFFAOYSA-N
PubChem CID	15951529
ChEBI ID	CHEBI:68534
TTD Drug ID	D0QK5X
INTEDE ID	DR0583
DrugBank ID	DB08899

Type(s) of Resistant Mechanism of This Drug

ADTT: Aberration of the Drug's Therapeutic Target

Drug Resistance Data Categorized by Their Corresponding Diseases

ICD-02: Benign/in-situ/malignant neoplasm

Click to Show/Hide the Resistance Disease of This Class

Prostate cancer [ICD-11: 2C82]

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Drug Resistance Data Categorized by Their Corresponding Mechanisms
Aberration of the Drug's Therapeutic Target (ADTT)		Click to Show/Hide
Key Molecule: Androgen receptor (AR)			[1]
Molecule Alteration	Structural variation	Copy number gain	Molecule Info
Resistant Disease	Prostate cancer [ICD-11: 2C82.0]		Disease Info
Experimental Note	Identified from the Human Clinical Data
Experiment for Molecule Alteration	Whole genome sequencing assay; Exome sequencing assay
Mechanism Description	Accordingly, AR amplification was detected in circulating cell-free DNA and was shown to be associated with enzalutamide and abiraterone treatment resistance in a cohort of 62 CRPC patients.
Key Molecule: Androgen receptor (AR)			[1]
Molecule Alteration	Structural variation	Copy number gain	Molecule Info
Resistant Disease	Primary prostate cancer [ICD-11: 2C82.Z]		Disease Info
Experimental Note	Identified from the Human Clinical Data
Experiment for Molecule Alteration	Whole genome sequencing assay; Exome sequencing assay
Mechanism Description	Accordingly, AR amplification was detected in circulating cell-free DNA and was shown to be associated with enzalutamide and abiraterone treatment resistance in a cohort of 62 CRPC patients.

References

Ref 1	Clonal origin and spread of metastatic prostate cancer. Endocr Relat Cancer. 2016 Apr;23(4):R207-17. doi: 10.1530/ERC-16-0049. Epub 2016 Mar 21.