Drug intelligence / Profile preview

LY2090314 + pemetrexed + carboplatin

Development stage
Phase 1
Lead developer
Eli Lilly
Modality
Small Molecules
Administration
Intravenous
01

Overview

**LY2090314 + pemetrexed + carboplatin** is a combination regimen composed of LY2090314 (a potent, selective small molecule inhibitor of glycogen synthase kinase-3, GSK-3), pemetrexed (an antifolate chemotherapy agent), and carboplatin (a platinum-based chemotherapy agent). LY2090314 inhibits GSK-3 by blocking ATP binding, leading to stabilization of β-catenin and activation of Wnt/β-catenin signaling, and induces apoptosis in tumor cells[1][4][6]. Pemetrexed inhibits thymidylate synthase and other folate-dependent enzymes, blocking DNA and RNA synthesis. Carboplatin forms DNA crosslinks, leading to apoptosis in cancer cells. This combination is investigated primarily in advanced solid tumors, notably non-small cell lung cancer and mesothelioma[1][5].

02

Targets

DNAGSK3 (Glycogen synthase kinase 3 beta)TS (Thymidylate synthase)

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