Participate in Research at CU Anschutz

OKI-219-101 is a Phase 1a/1b, open-label, multicenter, dose-escalation study designed to evaluate the safety, tolerability, pharmacokinetics (PK), pharmacodynamics (PDx), and efficacy of OKI-219 as monotherapy and in combination with fulvestrant or trastuzumab. Phase 1a (Part A) will investigate escalating doses of OKI-219 monotherapy, and Phase 1b will investigate OKI-219 (at a tolerated dose determined in Part A) in combination with standard dose fulvestrant (Part B) or standard dose trastuzumab (Part C). Participants will continue to receive study treatment until disease progression, intolerable toxicity, or other study treatment withdrawal criteria are met.

You are being asked to be in this research study because you have an advanced tumor with the PI3KαH1047R mutation or breast cancer with the PI3KαH1047R mutation. OnKure has begun a study of an investigational drug called OKI-219 as a possible treatment for people who have cancer due to a mutation in a gene (made up of DNA) called PI3Kα. An investigational drug is one that has not been approved by regulatory agencies, such as the United States (US) Food and Drug Administration (FDA), European Union (EU) European Medicines Agency (EMA), Taiwan FDA (TFDA), South Korea Ministry of Food and Drug Safety (MFDS), or others. This is the first human study of OKI-219. One of the most commonly found mutations (a change in the gene) in cancer is a mutation in the PI3Kα gene. Mutations in PI3Kα lead to activation of a cellular pathway which can result in an increase in cell growth and increased survival of these cells, leading to the formation of tumors. It can also make these cells resistant to therapies to reduce, stop or kill the cells (anticancer therapies). Because of this pathway’s role in cancer/tumor growth, it is an attractive pathway for new cancer therapies. H1047R is a specific part of the PI3Kα gene that can be mutated. OKI-219 is an inhibitor of PI3KαH1047R and will bind to the mutated part and stop the action of the mutated pathway. This may help slow the cancer growth or make it more responsive to other anticancer therapies. This study plans to learn more about: how well OKI-219 works, how safe OKI-219 is, and to learn what is the best dose of OKI-219 either alone or in combination with other anticancer drugs that have been approved by regulatory agencies.