Apalutamide API

CAS No.	956104-40-8
Therapeutic Category	Anti-Cancer/Oncology
Technology	Synthetic
Dosage Form	Oral Solids
Innovator Brand	Erleada(USA)
Registration Status	DMF
Polymorph	Form B; New form with own patent
GMP	FDA(USA)/NMPA(China)/MFDS (Korea) approved
EHS	ISO 14001 &45001 certificated

Product Description

Grade: Active Pharmaceutical Ingredient(API)
Chemical name: 4-[7-[6-cyano-5-(trifluoromethyl)pyrid in-3-yl]-8-oxo-6-sulfanylidene-5,7-diazaspiro[3.4]octan-5-yl]-2-fluoro-N-methylbenzamide
Molecular Formula: C21H15F4N5O2S
Molecular Weight: 477.43g/mol
Specification: Enterprise Standard established according to ChP/USP/EP
Appearance: White to light yellow powder
Total impurities: not more than 0.5%
Purity: not less than 99%
Residual Solvents: fully comply with ICH Q3C
Mutagenic impurities: fully comply with ICH M8
Nitrosamine assessment: available
Particle size: regular grade and micronized(D90＜10μm)
Storage: Room temperature
Production capacity: Commercial
Standard Package: 1kg/bag, 5kg/bag, or according to the customer’s requirement

Apalutamide is a potent androgen receptor (AR) antagonist that selectively binds to the ligand-binding domain of AR and blocks AR nuclear translocation or binding to androgen response elements. It has been used in trials studying the treatment of Prostate Cancer, Hepatic Impairment, Prostatic Neoplasms, Castration-Resistant Prostate Cancer, and Prostatic Neoplasms, Castration-Resistant, among others.
Exerting an antitumor action, Apalutamide blocks the effect of androgens that promote tumor growth. It targets the AR ligand-binding domain and prevents AR nuclear translocation, DNA binding, and transcription of AR gene targets in prostate tumors.
In mice bearing human CRPC xenograft models, Apalutamide treatment produced tumor regressions in a dose-dependent manner that was more effective than that of Bicalutamide or Enzalutamide. Unlike bicalutamide, Apalutamide antagonized AR-mediated signaling in AR overexpressing human CRPC cell lines.

Qingmu is an Apalutamide supplier, our Apalutamide has been filed in China(DMF filed and listed on CDE’s website), and DMF in CTD format is available and can be supported for registration worldwide.
Qingmu’s factory is established according to ICH/USFDA/EU/JAPAN/China regulations and current GMP, totally complies with environmental law in China, no risk to remove factory. Our new API factory is under design and is predicted to be put into use in 2025. So please rest assured to choose us.
Qingmu’s team has rich experience in patent challenges on crystalline form & synthesis processes and also synthetic route development and scale-up & quality research.
Qingmu’s lab is equipped with HPLC, GC, ICP-MS, GC-MS, CAD, microbalance, Malvern particle analyzer, etc. Qingmu passed the site inspection from NMPA(China), FDA(USA) and MFDS(Korea) and also customer audits from Europe, USA and Japan, etc.
As a China Apalutamide Manufacturer, Qingmu successfully exported products to more than 40 countries including Japan, USA, Germany, Spain, the Netherlands, Russia, South Korea, and Brazil.