Rezvilutamide is an orally active, nonsteroidal androgen receptor (AR) antagonist developed for the treatment of advanced prostate cancer. It is also known by the development code SHR-3680. Rezvilutamide competitively binds to the androgen receptor and inhibits androgen-dependent receptor signaling, thereby suppressing transcription of androgen-responsive genes involved in prostate cancer growth. It was approved in China in 2022.
Rezvilutamide has the molecular formula C22H20F3N3O4S, molecular weight 479.47 g/mol, and CAS Number 1572045-62-5. FDA GSRS identifies the substance under UNII 70FJN2AW22.
Rezvilutamide is a selective nonsteroidal antiandrogen with a defined (S)-configuration in its dihydroxypropoxy side chain. Its chemical structure contains trifluoromethyl, benzonitrile, thiohydantoin/imide and dihydroxypropoxy structural features.
The API is currently commercially available as a research and pharmaceutical-development compound. Current analytical references describe it as a white to off-white solid.
| Parameter | Rezvilutamide |
|---|---|
| Product Name | Rezvilutamide |
| Synonym | SHR-3680 / SHR3680 |
| CAS Number | 1572045-62-5 |
| Molecular Formula | C22H20F3N3O4S |
| Molecular Weight | 479.47 g/mol |
| API Type | Synthetic small molecule |
| Drug Class | Nonsteroidal antiandrogen |
| Pharmacological Class | Androgen receptor antagonist |
| Development Code | SHR-3680 |
| Physical Form | Solid |
| Appearance | White to off-white |
| Defined Stereocenters | 1 |
| Hydrogen Bond Donors | 2 |
| Hydrogen Bond Acceptors | 7 |
| Rotatable Bonds | 7 |
| Topological Polar Surface Area | 129.12 Ų |
| XLogP | 1.41 |
The molecular and physicochemical values are supported by PubChem and IUPHAR/BPS.
Rezvilutamide is an androgen receptor antagonist used in oncology research and prostate-cancer drug development. It is approved in China and has been evaluated in metastatic prostate cancer, including metastatic castration-resistant prostate cancer.
Applications include:
Rezvilutamide API quality control should focus on identity, assay, related substances, stereochemical purity, residual solvents and other process-related impurities.
Because Rezvilutamide contains one defined stereocenter, stereochemical purity is an important analytical consideration. PubChem confirms one defined atom stereocenter in the molecular structure.
Appropriate analytical characterization can include:
Commercial analytical material is currently reported at ≥98% purity, but this should be regarded as a commercial/reference value rather than a universal pharmacopoeial API release specification.
A quality-focused Rezvilutamide API manufacturing process should control chemical purity and stereochemical integrity while maintaining consistent physical characteristics.
Important manufacturing controls include:
Rezvilutamide API should be packed in a suitable, tightly closed pharmaceutical container and protected from moisture, contamination and excessive environmental exposure.
Current commercial analytical material is listed as a solid and one reference recommends −20°C storage for long-term research-material stability. This commercial research-storage condition should not automatically be interpreted as a universal pharmaceutical API storage requirement.
Typical Rezvilutamide API documentation can include:
Rezvilutamide is a structurally complex, stereochemically defined androgen receptor antagonist. Reliable API quality therefore requires control of both chemical purity and stereochemical characteristics. FDA GSRS and PubChem confirm the defined molecular identity and stereochemical structure.
A quality-oriented manufacturing program should emphasize:
| Parameter | Specification |
|---|---|
| Appearance | white to off-white crystalline powder |
| Identification | IR & HPLC compliant |
| Assay (HPLC) | 98.0% – 102.0% |