Drug intelligence / Profile preview

LY293111 + gemcitabine + cisplatin

Development stage
Unknown
Lead developer
Eli Lilly
Modality
Small Molecules
Administration
Oral (LY293111), Intravenous (gemcitabine, Cisplatin)
01

Overview

LY293111 + gemcitabine + cisplatin is a combination investigational regimen composed of three agents: LY293111, a small molecule originally developed as a potent **leukotriene B4 receptor antagonist** with additional activity as a **PPARγ agonist** and **5-lipoxygenase inhibitor**, gemcitabine, a nucleoside analog antimetabolite used as a chemotherapeutic agent, and cisplatin, a platinum-based DNA crosslinking agent. LY293111 has demonstrated **antiproliferative and pro-apoptotic effects** in various cancer cell types including pancreatic, breast, prostate, and colon cancers[1][2][3]. Mechanistically, it blocks LTB4-induced cellular growth by antagonizing the leukotriene B4 receptor and inhibits cancer growth through cell cycle arrest (S phase) and apoptosis via the mitochondrial pathway[1][3]. LY293111 also acts as a PPARγ agonist, with possible antidiabetic effects, and inhibits 5-lipoxygenase although with less potency. Combination of LY293111 with gemcitabine shows synergistic anticancer activity, offering improved efficacy in preclinical models of pancreatic cancer compared to either agent alone, and the combination has also been investigated with additional cytotoxic drugs like cisplatin in experimental settings[1].

Other names
LY293111LY-293111LY 293111gemcitabinecisplatin
02

Targets

PPARG (Peroxisome proliferator-activated receptor gamma)ALOX12 (Arachidonate 12-lipoxygenase, 12S type)DNALTB4R (Leukotriene B4 Receptor 1)

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