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eprenetapopt + pembrolizumab
- Development stage
- Unknown
- Lead developer
- Aprea Therapeutics
- Modality
- Monoclonal Antibodies → Antibody-Based Therapeutics, Small Molecules
- Administration
- Intravenous
01
Overview
Eprenetapopt (APR-246) is a small molecule that restores the function of mutant and wild-type p53 protein by stabilizing its folded structure, leading to activation of p53-dependent tumor suppression pathways and induction of apoptosis in tumor cells. It also affects cellular redox homeostasis. Pembrolizumab is a humanized monoclonal antibody that targets the programmed cell death protein 1 (PD‑1) receptor on lymphocytes, blocking its interaction with PD-L1/PD-L2 ligands and thereby enhancing T-cell mediated immune responses against tumors. The combination has been studied in phase I/II trials for advanced/metastatic solid tumors, including non-small cell lung cancer (NSCLC), urothelial cancer, and gastric/gastroesophageal junction cancers. Eprenetapopt is developed by Aprea Therapeutics; pembrolizumab is developed by Merck & Co[1][3][5][6].
- Other names
- eprenetapoptAPR-246APR246APR 246pembrolizumabKeytruda
02
Targets
PDCD1 (Programmed cell death protein 1 receptor)TP53 (Cellular Tumor Antigen p53 R175H)
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