PRUXELUTAMIDE

Details

Stereochemistry	ACHIRAL
Molecular Formula	C24H19F4N5O2S
Molecular Weight	517.499
Optical Activity	NONE
Defined Stereocenters	0 / 0
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

CC1(C)N(C(=S)N(C1=O)C2=C(F)C(=C(C=C2)C#N)C(F)(F)F)C3=CN=C(CCCC4=NC=CO4)C=C3

InChI

InChIKey=KCBJGVDOSBKVKP-UHFFFAOYSA-N

InChI=1S/C24H19F4N5O2S/c1-23(2)21(34)32(17-9-6-14(12-29)19(20(17)25)24(26,27)28)22(36)33(23)16-8-7-15(31-13-16)4-3-5-18-30-10-11-35-18/h6-11,13H,3-5H2,1-2H3

HIDE SMILES / InChI

Molecular Formula	C24H19F4N5O2S
Molecular Weight	517.499
Charge	0
Count

Stereochemistry	ACHIRAL
Additional Stereochemistry	No
Defined Stereocenters	0 / 0
E/Z Centers	0
Optical Activity	NONE

Description
Sources: http://www.kintor.us/2018/05/06/researchers-conference-of-proxalutamides-phase-iii-clinical-trial-held-successfully/ | https://clinicaltrials.gov/ct2/show/NCT03899467 | https://adisinsight.springer.com/drugs/800046361

Kintor Pharma is developing proxalutamide (developmental code GT-0918), an androgen receptor antagonist, for the treatment of metastatic castrate-resistant prostate cancer and AR-positive triple-negative breast cancer. Proxalutamide is involved in phase III clinical trials in China and in phase II in the USA for patients with metastatic castrate-resistant prostate cancer. In addition, the drug participates in phase I clinical trials for the treatment of AR-positive triple-negative breast cancer. Proxalutamide is expected to become a more effective, less toxic second-generation AR antagonist, which will have a bright prospect once it receives approval for coming on the market.

Originator

Approval Year

PubMed

Title	Date	PubMed
Microenvironmental pH-modified solid dispersions to enhance the dissolution and bioavailability of poorly water-soluble weakly basic GT0918, a developing anti-prostate cancer drug: preparation, characterization and evaluation in vivo.	2014 Nov 20	25171976
A comprehensive assay for nine major cytochrome P450 enzymes activities with 16 probe reactions on human liver microsomes by a single LC/MS/MS run to support reliable in vitro inhibitory drug-drug interaction evaluation.	2015	26007223

Patents

Sample Use Guides

In Vivo Use Guide

400mg/day of GT0918 (proxalutamide). All subjects will be randomized to take 400 mg or 500 mg of GT0918 by oral administration once daily on an empty stomach (2-3 hours after a meal) for initial treatment of 6 months

Route of Administration: Oral

Substance Class	Chemical Created by `admin` on `Sat Dec 16 10:30:09 GMT 2023` Edited by `admin` on `Sat Dec 16 10:30:09 GMT 2023`
Record UNII	QX6O64GP40
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

PRUXELUTAMIDE

Official Name

English

pruxelutamide [INN]

Common Name

English

GT-0918

Code

English

4-(4,4-DIMETHYL-3-(6-(3-(2-OXAZOLYL)PROPYL)-3-PYRIDINYL)-5-OXO-2-THIOXO-1-IMIDAZOLIDINYL)-3-FLUORO-2-(TRIFLUOROMETHYL)-BENZONITRILE

Systematic Name

English

GT0918

Code

English

PROXALUTAMIDE

Common Name

English

Proxalutamide [WHO-DD]

Common Name

English

Classification Tree Code System Code

NCI_THESAURUS

C146993