Drug intelligence / Profile preview

enzalutamide + leuprolide + dutasteride

Development stage
Unknown
Lead developer
Astellas Pharma
Modality
Small Molecules
Administration
Oral, Intramuscular, Subcutaneous
01

Overview

This is a combination regimen of **enzalutamide**, **leuprolide**, and **dutasteride** administered as neoadjuvant or adjuvant therapy in prostate cancer, most often in high-risk, non-metastatic prostate cancer. **Enzalutamide** is a second-generation androgen receptor inhibitor that blocks androgen receptor signaling. **Leuprolide** is a GnRH (gonadotropin-releasing hormone) agonist that suppresses testicular androgen production, providing androgen deprivation therapy (ADT). **Dutasteride** is a 5-alpha-reductase inhibitor that blocks conversion of testosterone to dihydrotestosterone (DHT), a more potent androgen. In combination, these agents provide *maximal androgen blockade* through three mechanisms: inhibition of receptor signaling, suppression of gonadal androgen synthesis, and reduced peripheral conversion to DHT. Typically, this regimen is used in investigational contexts for high-risk or locally advanced prostate cancer, with some evidence supporting improved pathologic response compared to monotherapy[1].

02

Targets

SRD5A1 (Steroid 5-alpha-reductase type 1)SRD5A2 (Steroid 5-alpha-reductase type II)GnRHR (Gonadotropin-releasing hormone receptor)AR (Adrenergic receptors)

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