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PIPELINE > TRIAL OVERVIEW

Molecule Overview
KRAS G12D Inhibitor
LY3962673
KRAS G12D MoA

Gong X, et al1; Iyer C, et al2

Target

KRAS is one of the most commonly mutated oncogenes across all tumor types. KRAS G12D represents a KRAS mutation that is identified in patients with pancreatic cancer (37.0%), colorectal cancer (12.5%), and non-small cell lung cancer (4.9%).3

Molecule
LY3962673 is a potent, oral, KRAS G12D inhibitor; in preclinical models, it has demonstrated dose-dependent tumor growth inhibition as monotherapy and in combination.1 LY3962673 is highly selective against HRAS, NRAS, KRAS, and other non-G12D-mutant KRAS. In a 133-molecule off-target panel screen, there were no off-target activities at biologically meaningful exposures.2
Clinical Development

LY3962673 preclinical data support further evaluation in clinical trials.

References

  1. Gong X, et al. LY3962673, an oral, highly potent, mutant-selective, and non-covalent KRAS G12D inhibitor demonstrates robust anti-tumor activity in KRAS G12D models. Presented at: AACR Annual Meeting; April 5-10, 2024; San Diego, CA.
  2. Iyer C, et al. Preclinical characterization of LY3962673, B115 an orally bioavailable, highly potent, and selective KRAS G12D inhibitor. Presented at: AACR-NCI-EORTC Annual Meeting; October 11-15, 2023; Boston, MA.
  3. Hofmann MH, et al. Cancer Discov. 2022;12(4):924-937.
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