Nilutamide is a synthetic non-steroidal antiandrogen active pharmaceutical ingredient (API) belonging to the androgen-receptor antagonist class. It is used in androgen-deprivation therapy and is primarily associated with the treatment of metastatic prostate cancer. Nilutamide works by blocking the action of androgens at the androgen receptor.
Nilutamide is a specialized oncology pharmaceutical API used in the development and manufacture of antiandrogen formulations and in pharmaceutical research.
The European Pharmacopoeia monograph identifies Nilutamide as 5,5-dimethyl-3-[4-nitro-3-(trifluoromethyl)phenyl]imidazolidine-2,4-dione and specifies a content of 98.0%–102.0% on the anhydrous substance.
CAS Number: 63612-50-0
Molecular Formula: C₁₂H₁₀F₃N₃O₄
Molecular Weight: 317.22 g/mol
Chemical Name: 5,5-Dimethyl-3-[4-nitro-3-(trifluoromethyl)phenyl]imidazolidine-2,4-dione
IUPAC Name: 5,5-Dimethyl-3-[4-nitro-3-(trifluoromethyl)phenyl]imidazolidine-2,4-dione
Drug Class: Non-Steroidal Antiandrogen
Therapeutic Class: Antiandrogen / Antineoplastic Agent
Therapeutic Area: Oncology / Prostate Cancer
Molecule Type: Synthetic Small Molecule
ATC Code: L02BB02
The molecular identity and physicochemical information are supported by IUPHAR/BPS and official/regulatory pharmaceutical sources.
Nilutamide is a non-steroidal androgen receptor antagonist. It competitively interferes with androgen binding to the androgen receptor, reducing androgen-dependent signaling.
Its pharmacological activity includes:
Nilutamide is used as part of androgen-deprivation treatment in prostate cancer.
Nilutamide API is relevant to:
Nilutamide has been used in combination with surgical castration for the treatment of metastatic prostate cancer. Its role is to inhibit androgen action at the receptor level after androgen deprivation.
Nilutamide binds to androgen receptors and prevents activation by endogenous androgens. This mechanism distinguishes it from steroidal antiandrogens and makes Nilutamide relevant to research involving androgen receptor signaling and prostate cancer biology.
Nilutamide is described as a white or almost white powder in the European Pharmacopoeia monograph. Regulatory information describes it as a microcrystalline, white to practically white powder.
Nilutamide has a molecular weight of approximately 317.22 g/mol.
Regulatory drug-substance information describes Nilutamide as:
A controlled Nilutamide API manufacturing process may involve:
Typical Nilutamide API quality control may include:
The European Pharmacopoeia monograph specifically establishes tests for related substances, water, sulfated ash and assay.
Store Nilutamide API protected from light in a tightly closed container under appropriate pharmaceutical storage conditions. The European Pharmacopoeia monograph specifically states protected from light.
Nilutamide is relevant to research involving:
| Parameter | Specification |
|---|---|
| Appearance | White crystalline powder or crystals |
| Identification | IR & HPLC compliant |
| Assay (HPLC) | 98.0% – 102.0% |
| Loss on Drying | NMT 0.5% |
| Residue on Ignition | NMT 0.1% |
| Heavy Metals | NMT 20 ppm |
| Individual Impurity | NMT 0.10% each |
| Total Impurities | NMT 0.30% |
| Water Content | NMT 0.5% |
| Melting Point | 153–156°C |