Enzalutamide
![Enzalutamide Structure](CAS/GIF/915087-33-1.gif)
- CAS No.
- 915087-33-1
- Chemical Name:
- Enzalutamide
- Synonyms
- CS-355;101095;MDV-3100;Mr Amine;Ezalutamide;EnzalutaMide;Enzalutamide API;Enzalutamide, >=99%;brand name: Xtandi.;ENZALUTAMIDE;MDV-3100
- CBNumber:
- CB62500946
- Molecular Formula:
- C21H16F4N4O2S
- Molecular Weight:
- 464.44
- MOL File:
- 915087-33-1.mol
- Modify Date:
- 2024/5/13 18:00:15
SAFETY
Risk and Safety Statements
Symbol(GHS) | ![]() GHS07 |
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Signal word | Warning | |||||||||
Hazard statements | H315-H319-H227 | |||||||||
Precautionary statements | P501-P210-P264-P280-P302+P352-P370+P378-P337+P313-P305+P351+P338-P362+P364-P332+P313-P403+P235 | |||||||||
HS Code | 29339900 | |||||||||
NFPA 704 |
|
Enzalutamide Chemical Properties,Uses,Production
Description
In August 2012, the US FDA approved enzalutamide for the treatment of metastatic castration-resistant prostate cancer (mCRPC) in patients who have previously been treated with docetaxel. Synthesis of enzalutamide was achieved by a triply convergent route that employed a Strecker condensation, followed by isothiocyanate condensation and hydrolysis to form the thiohydantoin moiety. In LNCaP/AR cells with high expression of AR, enzalutamide demonstrated potent inhibition of 16b-[18F]-5α-dihydrotestosterone binding (IC50=21 nM compared with bicalutamide IC50=160 nM), and inhibited AR translocation to the nucleus more potently than bicalutamide.The primary metabolite is the result of CYP2C8-mediated N-demethylation; enzalutamide is primarily eliminated by hepatic metabolism.
Chemical Properties
White Solid
Uses
MDV3100, known as Enzalutamide, is a second-generation androgen receptor (AR) signaling inhibitor. It is able to inhibit binding of androgens to the AR, AR nuclear translocation, and the association of the AR with DNA.
Definition
ChEBI: A benzamide obtained by formal condensation of the carboxy group of 4-{3-[4-cyano-3-(trifluoromethyl)phenyl]-5,5-dimethyl-4-oxo-2-thioxoimidazolidin-1-yl}-2-fluorobenzoic acid with methylamine. Used for the treatment of of metastatic castration-resistant p ostate cancer.
Clinical Use
In August 2012, the FDA approved enzalutamide, marketed by Medivation and Astellas Pharma US for the treatment of metastatic castration-resistant prostate cancer (CRPC), specifically for those patients who had previously received docetaxel. Enzalutamide is an inhibitor of androgen receptors (AR)— whose increased expression has been closely linked with castration-resistant prostate cancer (CRPC),thus, AR inhibitors have seen increased recent attention from the medicinal chemistry community. Phase I/II trials were particularly promising for enzalutamide, as 43% of patients showed >50% sustained suppression of a key serum biomarker.
Enzalutamide Preparation Products And Raw materials
Raw materials
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chevron_rightPreparation Products
Supplier | Tel | Country | ProdList | Advantage | Inquiry |
---|---|---|---|---|---|
GLR Innovations | +91 9891111994 | New Delhi, India | 4542 | 58 | Inquiry |
AVD pharmaceuticals Pvt Ltd | +919860835260 | Pune, India | 102 | 58 | Inquiry |
Dr. Reddy's Laboratories Ltd | +91-4049002900 +91-4049002900 | Hyderabad, India | 165 | 58 | Inquiry |
J S LABS | +91-7330612784 +91-7330612784 | Tamil Nadu, India | 160 | 58 | Inquiry |
Gonane Pharma | +91-9819380043 +91-9819380043 | NaviMumbai, India | 192 | 58 | Inquiry |
CDYMAX | +91-9019317788 +91-9019317788 | Bangalore, India | 28 | 58 | Inquiry |
Shilpa Medicare Limited (SML) | +91-8532238704 +91-9320649838 | Karnataka, India | 61 | 58 | Inquiry |
Crams Technologies | 0129-4011068 | New Delhi, India | 39 | 58 | Inquiry |
Basil Drugs AND Pharmaceuticals Pvt Ltd | +91-2249700250 +91-9619320820 | Mumbai, India | 108 | 58 | Inquiry |
Zydus Lifesciences Ltd. | +91-0265-2315243 +91-6358895661 | Gujarat, India | 89 | 58 | Inquiry |
Supplier | Advantage |
---|---|
GLR Innovations | 58 |
AVD pharmaceuticals Pvt Ltd | 58 |
Dr. Reddy's Laboratories Ltd | 58 |
J S LABS | 58 |
Gonane Pharma | 58 |
CDYMAX | 58 |
Shilpa Medicare Limited (SML) | 58 |
Crams Technologies | 58 |
Basil Drugs AND Pharmaceuticals Pvt Ltd | 58 |
Zydus Lifesciences Ltd. | 58 |
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