Drug intelligence / Profile preview

opevesostat + cabazitaxel

Development stage
Unknown
Lead developer
Merck
Modality
Classical Binding Small Molecules → Small Molecules, Covalent Small Molecules → Small Molecules, Nucleic Acid-Directed Small Molecules → Small Molecules
Administration
Oral, Intravenous
01

Overview

Opevesostat + cabazitaxel is an experimental combination therapy under investigation for the treatment of metastatic castration-resistant prostate cancer (mCRPC). Opevesostat (code name MK-5684) is a novel oral agent purported to act as an androgen receptor pathway inhibitor, targeting androgen signaling pathways central to prostate cancer progression. Cabazitaxel is a second-generation taxane chemotherapy approved for mCRPC, which works by inhibiting microtubule dynamics, thus blocking mitosis and inducing apoptosis in cancer cells. The combination aims to enhance antitumor efficacy by targeting both the androgen axis (opevesostat) and cell division processes (cabazitaxel). This strategy is being tested in clinical trials for patients who have progressed on prior hormone therapies and chemotherapy.[3][5]

02

Targets

CYP11A1 (Cholesterol side chain cleavage enzyme)TUBB (Tubulin (alpha and beta subunits))AR (Adrenergic receptors)

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