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PIPELINE > TRIAL OVERVIEW

Trial Information
Molecule Overview
Biomarker Testing
PI3Kα Inhibitor
LOXO-783
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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.4

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

  1. Gkeka P, et al. PLoS Comput Biol. 2014;10(10):e1003895.
  2. Karakas B, et al. Br J Cancer. 2006;94(4):455-459.
  3. Vasan N, et al. Ann Oncol. 2019;30(Suppl_10):x3–x11.
  4. 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.
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

  1. Gkeka P, et al. PLoS Comput Biol. 2014;10(10):e1003895.
  2. Karakas B, et al. Br J Cancer. 2006;94(4):455-459.
  3. Vasan N, et al. Ann Oncol. 2019;30(Suppl_10):x3–x11.
  4. 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.
For information on trial enrollment, locations, and more, call 1-800-545-5979.
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