Drug intelligence / Profile preview

LY2090314 + gemcitabine + nab-paclitaxel

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

Overview

This is a combination regimen of three agents: - **LY2090314** is a potent, selective small molecule inhibitor of glycogen synthase kinase-3 (GSK-3α and GSK-3β), which acts by inhibiting ATP binding. It stabilizes β-catenin, activates Wnt signaling, induces apoptosis, and inhibits proliferation in cancer cell lines including neuroblastoma and melanoma[1][2][4]. Its use aims to sensitize tumors to chemotherapy and enhance pro-apoptotic pathways. - **Gemcitabine** is a nucleoside analog that incorporates into DNA, inhibits DNA synthesis, and induces apoptosis, commonly used as an antineoplastic chemotherapeutic agent. - **Nab-paclitaxel** (nanoparticle albumin-bound paclitaxel; trade name Abraxane) is a taxane antineoplastic delivered as a nanoparticle albumin-bound formulation for improved delivery and reduced toxicity, promoting mitotic arrest by stabilizing microtubules. This combination has been investigated in metastatic pancreatic cancer, with LY2090314 serving as a chemo-sensitizer alongside standard cytotoxic chemotherapy[3][7].

Other names
nab-paclitaxelgemcitabine
02

Targets

GSK3 (Glycogen synthase kinase 3 beta)DNA polymerase family

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