Drug intelligence / Profile preview

LY3039478 + cisplatin + gemcitabine

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

Overview

This is a **combination regimen** of three drugs: **LY3039478 (crenigacestat)**, **cisplatin**, and **gemcitabine**. LY3039478 is an orally bioavailable, potent, and selective small-molecule inhibitor of the gamma-secretase complex, leading to inhibition of **Notch signaling** (Notch1-4 receptors), a pathway implicated in several malignancies[1][2][4][5]. Cisplatin is a platinum-based chemotherapy that forms DNA crosslinks and induces apoptosis in rapidly dividing cells. Gemcitabine is a nucleoside analog (antimetabolite) that inhibits DNA synthesis. This combination is being investigated as an antineoplastic treatment in clinical trials for advanced or metastatic solid tumors, including cholangiocarcinoma and other cancers with aberrant Notch signaling[3].

Other names
crenigacestat + cisplatin + gemcitabine
02

Targets

DNADNA polymerase familyNOTCH (Neurogenic locus notch homolog protein 3)GSEC (Gamma-Secretase Complex)RNR (Ribonucleotide reductase)

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