Drug intelligence / Profile preview

opevesostat + olaparib

Development stage
Unknown
Lead developer
Merck
Modality
Small Molecules
Administration
Oral
01

Overview

**Opevesostat + olaparib** is an investigational oral drug combination under clinical development for the treatment of metastatic castration-resistant prostate cancer (mCRPC)[3][5][7]. Opevesostat (MK-5684) is a small molecule with unknown detailed mechanism, being studied primarily as a targeted therapy for prostate cancer[3][7]. Olaparib is a small molecule poly(ADP-ribose) polymerase (PARP) inhibitor, approved for several cancers, and works by inhibiting PARP enzymes, impairing DNA repair in BRCA-mutated and homologous recombination-deficient cancers, enhancing cancer cell death[4][6][8]. The combination is intended to block parallel or complementary DNA repair/alive pathways in prostate cancer, potentially improving patient outcomes over single agent therapy.

Other names
opevesostat tosilate + olaparib
02

Targets

TNKS (Poly(ADP-ribose) Polymerase 5a)CYP11A1 (Cholesterol side chain cleavage enzyme)PARP2 (Poly (adp-ribose) polymerase 2)TNKS2 (Tankyrase 2)

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