ODM-201

China [CN]

Mechanism of Action

It potently binds to the AR ligand-binding domain, blocking AR nuclear translocation and DNA binding, inhibiting AR-mediated gene transcription, and reducing androgen signaling pathway activity.

It has inhibitory effects on AR mutants (such as T878A and L702H), overcoming resistance to some second-generation antiandrogen drugs.

It has extremely low blood-brain barrier penetration, resulting in a low risk of central nervous system toxicity.

Clinical Application

Indications: Used in combination with androgen deprivation therapy (ADT) for the treatment of non-metastatic castration-resistant prostate cancer (nmCRPC).

Dosage and Administration: Adults: 600 mg twice daily, taken with food.

Dosage Form: Film-coated tablets, 300 mg.

Pharmacokinetics

It is well absorbed orally, has high plasma protein binding, is primarily metabolized by CYP3A4, has a half-life of approximately 14 hours, and its metabolites are inactive. No dose adjustment is required for patients with hepatic impairment, but monitoring is necessary for patients with renal impairment.

It hardly penetrates the blood-brain barrier, and there are no reports of central nervous system adverse reactions such as seizures.

Safety

Common adverse reactions: fatigue, limb pain, rash, diarrhea, etc., mostly mild to moderate.

Contraindications: Contraindicated in patients allergic to this product.

Precautions: Avoid concomitant use with strong CYP3A4 inducers/inhibitors; may cause fetal harm, contraindicated in pregnant women.

Clinical Efficacy