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palupiprant

Development stage: Phase 1
Lead developer: Adlai Nortye
Modality: Small Molecules
Administration: Oral

Overview

Palupiprant is a small molecule, orally bioavailable, and selective antagonist of the prostaglandin E2 (PGE2) receptor type 4 (EP4). It is designed to modulate the tumor microenvironment by inhibiting PGE2-mediated activation of immunosuppressive tumor-associated myeloid cells (TAMCs), thereby reducing immunosuppression and tumor cell proliferation. This mechanism promotes CD8+ T-cell-mediated tumor clearance and enhances the efficacy of immune checkpoint inhibitors. Palupiprant shows promise in solid tumors with high PGE2 expression and is being investigated in combination with radiotherapy/chemoradiotherapy for various cancers.

Other names: Palupiprantum

Targets

PTGER4 (Prostaglandin E2 receptor EP4 subtype)

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