Drug intelligence / Profile preview

LY3499446

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

Overview

LY3499446 is an orally available small molecule inhibitor specifically targeting the KRAS G12C mutation. It covalently binds to cysteine 12 within the switch II pocket of GDP-bound KRAS G12C protein. This binding inhibits mutant KRAS-dependent signaling pathways that drive tumor cell growth and proliferation in cancers harboring this mutation. The drug was developed for potential antineoplastic activity in advanced solid tumors with a focus on non-small cell lung cancer (NSCLC), colorectal cancer (CRC), and other solid tumors with confirmed KRAS G12C mutations. Developed by Eli Lilly and Company, it reached phase I/II clinical trials but development was terminated before completion[1][3][5][9].

Other names
LY3499446LY-3499446LY 3499446
02

Targets

KRASG12C (Kirsten rat sarcoma viral oncogene homolog G12C)

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