Drug intelligence / Profile preview

LY3143921

Development stage
Phase 1
Lead developer
Cancer Research UK
Modality
Small Molecules
Administration
Oral
01

Overview

LY3143921 is an orally bioavailable small molecule inhibitor of cell division cycle 7 (CDC7) kinase, developed for the treatment of advanced solid tumors. CDC7 is a protein kinase involved in regulating DNA replication and cell-cycle progression, and it is often overexpressed in malignant cells, particularly those with TP53 mutations. By inhibiting CDC7 activity, LY3143921 aims to block cancer cell proliferation and induce cancer cell death while sparing normal cells that express lower levels of CDC7. Preclinical studies have shown promising anti-cancer activity in models of colorectal cancer and squamous non-small cell lung cancer, especially those harboring TP53 mutations. The drug has been evaluated in phase 1 clinical trials to determine its safety, tolerability, pharmacokinetics, and preliminary efficacy in patients with advanced or refractory solid tumors[2][3][4][8].

Other names
CDC7 kinase inhibitor LY3143921 hydrateCDC-7 kinase inhibitor LY3143921 hydrateCDC 7 kinase inhibitor LY3143921 hydrate
02

Targets

CDC7 (Cell division cycle 7-related protein kinase)

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