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idetrexed + olaparib (Algok Bio)

Development stage: Unknown
Lead developer: Algok Bio
Modality: Small Molecules
Administration: Oral, Intravenous

Overview

Idetrexed + olaparib is a combination therapy currently being evaluated in the Phase I/Ib IDOL clinical trial for the treatment of alpha-folate receptor (FRα) overexpressing high-grade serous ovarian cancer. Idetrexed (formerly BTG945) is a small-molecule, FRα-targeted thymidylate synthase inhibitor that selectively enters cancer cells overexpressing the receptor, where it inhibits thymidylate synthase to disrupt DNA synthesis. Olaparib is an approved PARP inhibitor that blocks DNA damage repair mechanisms. The combination is designed to synergistically increase DNA damage and induce apoptosis in cancer cells, particularly in platinum-resistant cases, by combining targeted cytotoxic delivery with the inhibition of DNA repair pathways.

Brand names: Lynparza
Other names: dose level-Institute of Cancer Research, United Kingdom-high grade serous ovarian cancerIdetrexed and Olaparib in Ovarian Cancer

Targets

PARP3 (Poly(adp-ribose) polymerase 3)TS (Thymidylate synthase)FOLR1 (FRα)PARP2 (Poly (adp-ribose) polymerase 2)

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