Drug intelligence / Profile preview

enzalutamide + abiraterone acetate + prednisone

Development stage
Unknown
Lead developer
Astellas Pharma
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
Administration
Oral
01

Overview

This is a **combination therapy** comprising three pharmaceuticals: enzalutamide, abiraterone acetate, and prednisone. The regimen has been evaluated in clinical trials for the treatment of metastatic castration-resistant prostate cancer (mCRPC). - **Enzalutamide** is an androgen receptor inhibitor that blocks the effects of a`ndrogens at the receptor level, thereby inhibiting tumor growth driven by androgen receptor signaling. - **Abiraterone acetate** is a prodrug of abiraterone, a selective inhibitor of androgen biosynthesis through irreversible inhibition of the enzyme CYP17A1 (17α-hydroxylase/C17,20-lyase), reducing testosterone production. - **Prednisone** is a synthetic glucocorticoid corticosteroid, included primarily to mitigate mineralocorticoid excess side effects of abiraterone. This combination aims to simultaneously inhibit androgen receptor signaling and androgen production in prostate cancer cells. Despite theoretical potential for overcoming resistance mechanisms, large clinical trials found no significant overall survival advantage compared to enzalutamide alone, and toxicity rates were higher[1][2][4][5]. Primarily indicated for metastatic castration-resistant prostate cancer.

02

Targets

GR (Glucocorticoid receptor)CYP17A1 (Steroid 17-alpha-hydroxylase/C17,20 lyase)AR (Adrenergic receptors)

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