Oncology Pipeline

For more than 50 years, Lilly has been dedicated to delivering life-changing medicines and support to people living with cancer and those who care for them. Lilly is determined to build on this heritage and continue making life better for all those affected by cancer around the world. In 2019 Lilly created Loxo Oncology at Lilly, with the goal of rapidly delivering impactful new medicines for people with cancer. Our approach centers on creating new medicines that work in early clinical development and will matter to patients.

BTK Inhibitor

Pirtobrutinib, LOXO-305

BTK Inhibitor

Wu J, et al1; Singh SP, et al2

Target
Bruton tyrosine kinase (BTK) inhibitors represent a major therapeutic advance in the treatment of patients with chronic lymphocytic leukemia (CLL), mantle cell lymphoma (MCL), and B-cell malignancies by inducing durable responses.3-8  BTK is critical for the propagation of B-cell receptor signaling and is upregulated in many B-cell malignancies as compared with normal B cells. BTK inhibition, both in vitro and in vivo, decreases proliferation and survival signals.3
Molecule
Pirtobrutinib (LOXO-305) is an investigational, oral, highly selective, noncovalent BTK inhibitor. It possesses nanomolar potency independent of BTK C481 status in enzyme and cell-based assays. Pirtobrutinib has been shown in preclinical studies to reversibly bind BTK, deliver consistently high target coverage regardless of BTK turnover rate, preserve activity in the presence of the C481 acquired resistance mutations, and avoid off-target kinases.9
Clinical Development
Pirtobrutinib is being investigated in clinical trials in patients with chronic lymphocytic leukemia/small lymphocytic lymphoma, mantle cell lymphoma, or non-Hodgkin’s lymphoma.

References

  1. Wu J, et al. J Hematol Oncol. 2016;9(1):80.
  2. Singh SP, et al. Mol Cancer. 2018;17(1):57.
  3. Woyach JA, et al. J Clin Oncol. 2017;35(13):1437-1443.
  4. Mato AR, et al. Blood. 2016;128(18):2199-2205.
  5. Byrd JC, et al. N Eng J Med. 2016;374(4):323-332.
  6. Rule S, et al. Haematologica. 2019;104(5):e211-e214.
  7. Wang M, et al. Leukemia. 2019;33(11):2762-2766.
  8. Noy A, et al. Blood. 2017;129(16):2224-2232.
  9. Gomez EB, et al. Blood. 2019;134(suppl 1):4644.

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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