Drug intelligence / Profile preview

abiraterone decanoate + dexamethasone + enzalutamide

Development stage
Preclinical
Lead developer
Astellas Pharma
Modality
Small Molecules
Administration
Oral
01

Overview

A combination therapy consisting of **abiraterone decanoate**, **dexamethasone**, and **enzalutamide**. All three agents target the androgen signaling axis and are used in the treatment of advanced prostate cancer, mainly metastatic castration-resistant prostate cancer (mCRPC). **Abiraterone decanoate** is an esterified long-acting formulation of abiraterone, a CYP17A1 inhibitor that suppresses androgen synthesis; **dexamethasone** is a synthetic glucocorticoid often included to mitigate mineralocorticoid excess from abiraterone; and **enzalutamide** is an androgen receptor (AR) inhibitor that blocks AR signaling at multiple steps. This combination aims to provide dual blockade of androgen biosynthesis and AR pathway signaling, in addition to corticosteroid mitigation. While clinical studies have evaluated the combination of abiraterone acetate plus prednisone and enzalutamide in mCRPC, these trials found no meaningful efficacy advantage over single-agent therapy, and the combination increased toxicity (hypertension, liver enzyme elevations) and altered abiraterone pharmacokinetics. Abiraterone decanoate is an investigational long-acting preparation of abiraterone, designed for less frequent dosing; however, clinical trials for this exact three-drug combination are not reported in the available literature, and evidence is instead derived from the use of abiraterone acetate + steroid + enzalutamide[1][2][3].

02

Targets

CYP2D6 (Cytochrome P450 2D6)CYP3A4 (Cytochrome P450 3A4)GR (Glucocorticoid receptor)AR (Adrenergic receptors)CYP17A1 (Steroid 17-alpha-hydroxylase/C17,20 lyase)

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