Drug intelligence / Profile preview

pemigatinib + gemcitabine + cisplatin

Development stage
Preclinical
Lead developer
Incyte
Modality
Small Molecules
Administration
Oral (pemigatinib), Intravenous (gemcitabine, Cisplatin)
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Overview

Pemigatinib + gemcitabine + cisplatin is a combination of three pharmaceutical drugs, each with a distinct mechanism of action, mainly investigated for the treatment of advanced or metastatic cholangiocarcinoma and other biliary tract cancers. Pemigatinib is a small molecule inhibitor targeting fibroblast growth factor receptors, particularly FGFR2, and is developed as a targeted therapy for tumors harboring FGFR2 rearrangements. Gemcitabine is a nucleoside analog that interferes with DNA synthesis, resulting in inhibition of cell proliferation, while cisplatin is a platinum-containing compound that disrupts DNA function by inducing DNA crosslinks and apoptosis. The combination is the subject of clinical research, but as of now is not recognized as a standard triple regimen; rather, pemigatinib is compared as a monotherapy against the standard gemcitabine plus cisplatin in clinical trials for the first-line treatment of unresectable or metastatic cholangiocarcinoma with FGFR2 rearrangements[1][2][4][5]. There are limited or no data supporting the use of all three agents concurrently in clinical practice.

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Targets

FGFR4 (Fibroblast growth factor receptor 4)VEGFR2 (Vascular endothelial growth factor receptor 2)RNR (Ribonucleotide reductase)DNA polymerase familyFGFR3 (Fibroblast growth factor receptor 3)KIT (c-KIT proto-oncogene receptor tyrosine kinase)DNAFGFR2 (Keratinocyte growth factor receptor)FGFR1 (Fibroblast growth factor receptor 1)

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