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rezvilutamide + leuprorelin
- Development stage
- Unknown
- Lead developer
- Hengrui Pharmaceutical
- Modality
- Peptides, Small Molecules
- Administration
- Oral, Subcutaneous
01
Overview
This combination therapy consists of rezvilutamide, a novel second-generation oral androgen receptor (AR) inhibitor, and leuprorelin, a luteinizing hormone-releasing hormone (LHRH) agonist. Rezvilutamide is designed with low blood-brain barrier permeability to minimize central nervous system side effects while maintaining potent antitumor activity by inhibiting AR nuclear translocation and DNA binding. Leuprorelin acts as androgen deprivation therapy (ADT) by causing pituitary desensitization, which suppresses testicular testosterone production. The combination is being evaluated by Fujian Medical University Union Hospital as an adjuvant intensive endocrine therapy for high-risk prostate cancer patients following radical prostatectomy to reduce the risk of biochemical recurrence and metastasis. This regimen is already established as a first-line standard for metastatic hormone-sensitive prostate cancer (mHSPC) in China.
- Brand names
- Jiangshida
- Other names
- SHR3680 + leuprorelin acetaterezvilutamide + leuprorelin acetate
02
Targets
GnRHR (Gonadotropin-releasing hormone receptor)AR (Adrenergic receptors)
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