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.

PI3Kα Inhibitor

LOXO-783

Gkeka P, et al¹; Karakas B, et al²; Vasan N, et al³

Target

Phosphoinositide 3-kinase alpha (PI3Kα) H1047R mutations are activating oncogenic events that occur in ~15% of breast cancers and less commonly in other cancers.⁴

Molecule

LOXO-783 is a potent, highly mutant-selective, brain-penetrant, allosteric small molecule PI3Kα H1047R inhibitor. LOXO-783 has shown preclinical activity without on-target wild-type PI3Kα mediated toxicity.⁵

Clinical Development

LOXO-783 is being investigated in an open-label, multicenter, phase 1a/1b study in patients with PIK3CA H1047R-mutant advanced breast cancer and other solid tumors.

References

Gkeka P, et al. PLoS Comput Biol. 2014;10(10):e1003895.
Karakas B, et al. Br J Cancer. 2006;94(4):455-459.
Vasan N, et al. Ann Oncol. 2019;30(Suppl_10):x3–x11.
Samuels Y, et al. Science. 2004;304(5670):554.
Klippel A, et al. Preclinical characterization of LOXO-783 (LOX-22783), a highly potent, mutant-selective, and brain-penetrant allosteric PI3Kα H1047R inhibitor. Presented at AACR-NCI-EORTC Virtual Meeting 2021; October 7, 2021.

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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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