Oncology Pipeline

Loxo@Lilly aims to create medicines that make life better for all those affected by cancer around the world. Bringing together the focus and spirit of a biotech with the scale, resources, and heritage of Lilly, our team is focused on rapidly delivering impactful new medicines for people with cancer. Our approach centers on creating oncology medicines that unequivocally show early signs of clinical activity and will matter to patients.

KRAS G12C Inhibitor

LY3537982

Janes MR, et al¹; Kano Y, et al²

Target

KRAS is the most common oncogene across all tumor types. KRAS G12C represents a KRAS mutation in patients with non-small cell lung cancer (12% to 15%) and colorectal cancer (3%), and also occurs in patients with other solid tumors such as pancreatic cancer and endometrial cancer (1% to 2%).^3,4

Molecule

LY3537982 is a selective covalent inhibitor of KRAS G12C; it demonstrates activity as monotherapy and in combination with other anticancer therapies in preclinical models. It has competitive pharmacokinetic properties supporting its advancement into clinical testing. LY3537982 has been shown in vitro to target a KRAS G12C mutation, thereby inhibiting mutant KRAS-dependent signaling.⁵

Clinical Development

LY3537982 is being studied in a clinical trial in patients with non-small cell lung cancer, colorectal cancer, or other advanced solid tumors.

References

Janes MR, et al. Cell. 2018;172(3):578-589.
Kano Y, et al. Nat Commun. 2019;10(1):224.
Dogan S, et al. Clin Cancer Res. 2012;18(22):6169-6177.
Jones RP, et al. Br J Cancer. 2017;116(7):923-929.
Peng SB, et al. Cancer Res. 2021;81(suppl 13):1259.

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The safety and efficacy of the agents under investigation have not been established. There is no guarantee that the agents will receive regulatory approval and become commercially available for the uses being investigated.

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