KRAS G12C Inhibitor

LY3537982

KRAS G12C Inhibitor

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

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

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

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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