Drug intelligence / Profile preview

MK-8776 + gemcitabine

Development stage
Unknown
Lead developer
Merck
Modality
Small Molecules
Administration
Intravenous
01

Overview

MK-8776 + gemcitabine is an investigational combination therapy involving MK-8776, a potent and selective small molecule checkpoint kinase 1 (Chk1) inhibitor, together with gemcitabine, a deoxycytidine nucleoside analog and ribonucleotide reductase inhibitor. MK-8776 blocks Chk1, disrupting the DNA damage checkpoint, especially during S/G2 phase, thereby sensitizing cancer cells to gemcitabine-induced DNA damage by preventing homologous recombination repair of double-strand breaks[1][3][5]. Gemcitabine acts by inhibiting DNA synthesis and function, causing cell cycle arrest. The combination is designed to enhance cytotoxicity and apoptotic cell death in tumors, especially in advanced solid and hematologic malignancies. MK-8776 has been developed by Merck.

Other names
MK-8776 + gemcitabine
02

Targets

CHEK2 (Checkpoint kinase 2)CDK2 (Cyclin-dependent kinase 2)RNR (Ribonucleotide reductase)CHEK1 (Checkpoint kinase 1)DNA

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