Drug intelligence / Profile preview

gemcitabine + dasatinib + erlotinib

Development stage
Unknown
Lead developer
National Cancer Institute
Modality
Small Molecules
Administration
Intravenous, Oral
01

Overview

This combination therapy involves the co-administration of gemcitabine, dasatinib, and erlotinib for the treatment of advanced pancreatic adenocarcinoma. Gemcitabine is a pyrimidine nucleoside analog that functions as a chemotherapy agent by inhibiting DNA synthesis and ribonucleoside reductase. Dasatinib is a potent, multi-targeted small molecule inhibitor of Src family kinases and BCR-ABL. Erlotinib is a small molecule tyrosine kinase inhibitor targeting the epidermal growth factor receptor (EGFR). This specific triple combination was evaluated in a Phase I dose-escalation study (NCT01660971) sponsored by the National Cancer Institute (NCI) to investigate whether dual inhibition of the Src and EGFR pathways could enhance the efficacy of gemcitabine in patients with locally advanced or metastatic pancreatic cancer. The study aimed to determine the maximum tolerated dose and safety profile of this regimen based on preclinical data showing cooperative attenuation of tumor growth.

Other names
Gemcitabine, Dasatinib and Erlotinib
02

Targets

SFK (SRC family kinases)EGFR T790M (Epidermal growth factor receptor T790M mutant)DNARNR (Ribonucleotide reductase)

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