Drug intelligence / Profile preview

OKN4395 + pembrolizumab

Development stage
Phase 1
Lead developer
Owkin
Modality
Monoclonal Antibodies → Antibody-Based Therapeutics, Small Molecules
Administration
Oral, Intravenous
01

Overview

The combination of **OKN4395** and **pembrolizumab** is being evaluated for the treatment of advanced solid tumors. OKN4395 is a first-in-class, highly selective small-molecule inhibitor of the **EP2**, **EP4**, and **DP1** prostaglandin receptors, developed to disrupt immune evasion mechanisms exploited by cancer cells. Pembrolizumab is a monoclonal antibody and a programmed cell death protein 1 (**PD-1**) checkpoint inhibitor that enhances anti-tumor immune responses by blocking the PD-1 pathway. The rationale of this combination is that OKN4395 may restore immune recognition of tumor cells, potentially synergizing with pembrolizumab's checkpoint blockade for enhanced anti-tumor activity in cancers less responsive to checkpoint inhibition alone. The combination is under investigation in a Phase 1 clinical trial for safety, tolerability, pharmacokinetics, and preliminary anti-tumor activity in multiple solid tumors, including non-small cell lung cancer, colorectal cancer, head and neck squamous cell carcinoma, sarcoma, pancreatic adenocarcinoma, and mesothelioma[1][2][3][4][6][7][9].

02

Targets

PDCD1 (Programmed cell death protein 1 receptor)PTGDR (Prostanoid DP1 receptor)PTGER2 (Prostaglandin E2 receptor EP2)PTGER4 (Prostaglandin E2 receptor EP4 subtype)

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