Drug intelligence / Profile preview

LY3499446 + erlotinib

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

Overview

LY3499446 + erlotinib is a combination therapy being evaluated for the treatment of advanced solid tumors, specifically targeting KRAS G12C-mutant non-small cell lung cancer (NSCLC) and other KRAS G12C-mutant tumors. LY3499446 is an experimental small molecule inhibitor developed to target mutant KRAS G12C, interfering with KRAS-mediated oncogenic signaling, while erlotinib is an approved small molecule inhibitor of the epidermal growth factor receptor (EGFR). The rationale behind the combination is that EGFR inhibition may enhance the anti-tumor activity of KRAS G12C inhibition. This combination is under clinical investigation in Phase 1/2 trials for its safety, pharmacokinetics, and efficacy in advanced solid tumors with KRAS G12C mutations, particularly NSCLC[1][2][3].

02

Targets

EGFR T790M (Epidermal growth factor receptor T790M mutant)KRASG12C (Kirsten rat sarcoma viral oncogene homolog G12C)

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