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PIPELINE > TRIAL OVERVIEW

Trial Information
Molecule Overview
RET Inhibitor
Selpercatinib
RET_Inhibitor

Mulligan LM1

Target

Rearranged during transfection (RET) fusions have been identified in approximately 2% of non-small cell lung cancer,2,3 approximately 10% of papillary thyroid cancer,4,5 and less than 1% in other solid tumors including pancreatic and colorectal cancer.6-8  RET point mutations account for approximately 60% of medullary thyroid cancer.9-11 Cancers that harbor activating RET fusions or RET mutations depend primarily on this single constitutively activated kinase for their proliferation and survival. This dependency renders such tumors highly susceptible to small-molecule inhibitors targeting RET.

Molecule

Selpercatinib is a selective, potent, CNS-active small-molecule inhibitor of RET. Selpercatinib possesses nanomolar potency against diverse RET alterations, including RET fusions, activating RET point mutations, and acquired resistance mutations. Selpercatinib has been shown in vitro and in vivo to exhibit specificity for RET, with limited activity against other tyrosine kinases.12,13

Clinical Development

Selpercatinib is being investigated in clinical trials in patients with RET-associated medullary thyroid cancer, non-small cell lung cancer, papillary thyroid carcinoma, pediatric cancers, and other solid tumors.

References

  1. Mulligan LM. Nat Rev Cancer. 2014;14:173-186.
  2. Lipson D, et al. Nat Med. 2012;18(3):382-384.
  3. Takeuchi K, et al. Nat Med. 2012;18(3):378-381.
  4. Drilon A, et al. Nat Rev Clin Oncol. 2018;15(3):151-167.
  5. Parimi V, et al. NPJ Precis Oncol. 2023;7(1):10.
  6. Yang SR, et al. Clin Cancer Res. 2021;27(5):1316-1328.
  7. Kohno T, et al. Carcinogenesis. 2020;41(2):123-129.
  8. Li AY, et al. Cancer Treat Rev. 2019;81:101911.
  9. Hofstra RM, et al. Nature. 1994;367(6461):375-376.
  10. Agrawal N, et al. J Clin Endocrinol Metab. 2013;98(2):E364-E369.
  11. Taccaliti A, et al. Curr Genomics. 2011;12(8):618-625.
  12. Subbiah V, et al. Ann Oncol. 2018;29:1869-1876.
  13. Drilon A, et al. LIBRETTO-001: A phase 1 study of LOXO-292, a potent and highly selective RET inhibitor, in patients with RET-altered cancers. Presented at: ASCO Annual Meeting; June 1-5, 2018; Chicago, IL.
For information on trial enrollment, locations, and more, call 1-800-545-5979.
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