Drug intelligence / Profile preview

IDE-161 + pembrolizumab

Development stage
Unknown
Lead developer
IDEAYA Biosciences
Modality
Monoclonal Antibodies → Antibody-Based Therapeutics, Small Molecules
Administration
Oral, Intravenous
01

Overview

**IDE-161 + pembrolizumab** is a combination of two investigational and approved oncology drugs: IDE-161, a small molecule inhibitor of Poly(ADP-ribose) glycohydrolase (PARG), and pembrolizumab, a monoclonal antibody that targets programmed cell death protein 1 (PD-1). IDE-161 is designed to disrupt DNA repair by inhibiting PARG, leading to enhanced DNA damage and cancer cell death, particularly in tumors with homologous recombination deficiency (HRD). Pembrolizumab is an immune checkpoint inhibitor that enhances anti-tumor immunity by blocking PD-1, thereby restoring T-cell activity against tumor cells. This combination is currently being investigated for advanced or metastatic endometrial cancer, including both microsatellite instability-high (MSI-high) and microsatellite stable (MSS) subtypes[1][3][5][7][9]. The rationale is to target both DNA repair and the immune microenvironment for a synergistic anti-tumor effect.

Other names
IDE-161IDE161IDE 161IDEAYA IDE161
02

Targets

PARG (Poly(ADP-ribose) glycohydrolase)PDCD1 (Programmed cell death protein 1 receptor)

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