Drug intelligence / Profile preview

LY2603618 + cisplatin + pemetrexed

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

Overview

LY2603618 is a selective, small molecule inhibitor of checkpoint kinase 1 (CHK1), a key regulator of the DNA damage response and cell cycle checkpoints. By inhibiting CHK1, LY2603618 disrupts the ability of cancer cells to repair DNA damage induced by chemotherapy agents such as cisplatin and pemetrexed. Cisplatin is a platinum-based chemotherapeutic agent that induces DNA cross-links, while pemetrexed is an antimetabolite that inhibits folate-dependent enzymes essential for DNA synthesis. The combination of these drugs aims to enhance anticancer efficacy by simultaneously damaging tumor DNA and blocking its repair mechanisms[2][3][6].

02

Targets

PDK (Pyruvate dehydrogenase kinase isoform 1)CHEK1 (Checkpoint kinase 1)DNADHFR (Dihydrofolate reductase)GART (GAR transformylase)TS (Thymidylate synthase)

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