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LY2603618 + gemcitabine

Development stage: Unknown
Lead developer: Eli Lilly
Modality: Small Molecules
Administration: Intravenous

Overview

LY2603618 + gemcitabine is a combination therapy consisting of LY2603618, a selective inhibitor of checkpoint kinase 1 (CHK1), and gemcitabine, an antimetabolite chemotherapy agent. LY2603618 inhibits CHK1, a key regulator of the DNA damage checkpoint, which may enhance the effects of antimetabolites like gemcitabine. The combination was investigated for its potential to improve treatment outcomes in various cancers, particularly pancreatic cancer. In clinical studies, LY2603618 inhibited CHK1 autophosphorylation (S296) and increased DNA damage-mediated CHK1 phosphorylation (S345), while gemcitabine acts as an irreversible inhibitor of ribonucleotide reductase (RNR).

Targets

CHEK1 (Checkpoint kinase 1)DNA polymerase familyRNR (Ribonucleotide reductase)

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