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First-in-Human Study of OKI-219 in Advanced Solid Tumors and Advanced Breast Cancer
NCT06239467 · OnKure, Inc.
In plain English
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Official title
PIKture-01: First-in-Human Study of the PI3KαH1047R Mutant-Selective Inhibitor OKI-219 as Monotherapy in Participants With Advanced Solid Tumors and as Part of Combination Therapy in Participants With Advanced Breast Cancer
About this study
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 other anti-cancer drugs. 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 fulvestrant (Part B), trastuzumab and tucatinib (Part C), atirmociclib (Part D), and ribociclib and fulvestrant (Part E). Participants will continue to receive study treatment until disease progression, intolerable toxicity, or other study treatment withdrawal criteria are met.
Eligibility criteria
Key Inclusion Criteria:
* Participants with advanced solid tumors with documented evidence of a PI3KαH1047R mutation in tumor tissue and/or blood (ie, ctDNA).
* Eastern Cooperative Oncology Group (ECOG) Performance status score of to 1.
* Life expectancy \> 12 weeks for Part A and \> 6 months for Parts B, C, D, and E in the opinion of the Investigator.
* Adequate organ and bone marrow function
* Have adequate archival tumor tissue sample available or be approved by the Sponsor for enrollment if no tumor sample is available.
* At least 1 measurable lesion based on RECIST version 1.1.
Additional Cohort-specific key inclusion criteria:
Part A
* Participants with HR+/HER2- locally advanced, unresectable or metastatic breast cancer, must have received at least 1 prior line of hormonal therapy and at least 1 prior line of CDK4/6-inhibitor in the advanced or metastatic setting.
* Participants with HER2+ locally advanced, unresectable or metastatic breast cancer, must have received prior taxane, trastuzumab, pertuzumab, and tucatinib. Prior trastuzumab deruxtecan is allowed but not required.
* Participants with HER2-low breast cancer must have received prior trastuzumab deruxtecan.
* Participants with colorectal cancer must have KRAS wild-type disease.
Part B
* Participants with locally advanced, unresectable or metastatic HR+/HER2- breast cancer must have received at least 1 prior line of hormonal therapy in the advanced or metastatic setting and at least 1 prior CDK4/6-inhibitor.
* Participants with HER2-low breast cancer should have received prior trastuzumab deruxtecan
Part C ● Participants with HR±/HER2+ locally advanced, unresectable or metastatic breast cancer must have received prior taxane, trastuzumab, and pertuzumab unless unavailable in the region or contraindicated. Prior trastuzumab deruxtecan is allowed but not required.
Part D
● Participants must have HR+/HER2- locally advanced, unresectable or metastatic breast cancer
Part E ● Participants must have HR+/HER2- locally advanced, unresectable or metastatic breast cancer.
Key Exclusion Criteria:
* Treatment with any investigational product or other anticancer therapy within 28 days or 5 half-lives, whichever is shorter, of the start of treatment
* Participants with a known KRAS mutation.
* Participants with a known deleterious mutation in phosphatase and tensin homolog (PTEN) or negative for PTEN protein expression by IHC.
* Major surgery or wide-field radiation within 28 days or limited field palliative radiation within 7 days prior to the first dose of study drug.
* Known active central nervous system metastasis, including leptomeningeal disease.
* Uncontrolled Type 1 or Type 2 diabetes as defined by HbA1C ≥ 8%.
* Concomitant active malignancy or previous malignancy within 2 years of the time of enrollment.
* Impaired cardiovascular function or clinically significant cardiovascular disease,
* History of symptomatic drug-induced pneumonitis.
* Participants with active HIV, Hepatitis B, and Hepatitis C viral infections
Additional Cohort-specific key exclusion criteria:
Part C:
* Grade 2 or higher diarrhea at study entry.
* History of chronic liver disease.
Part E:
● History of interstitial lung disease.
Study design
Enrollment target: 200 participants
Allocation: randomized
Masking: none
Age groups: adult, older_adult
Timeline
Starts: 2024-02-26
Estimated completion: 2027-08-01
Last updated: 2025-09-09
Interventions
Drug: OKI-219Drug: FulvestrantDrug: TrastuzumabDrug: TucatinibDrug: AtirmociclibDrug: Ribociclib
Primary outcomes
- • Identify maximum tolerated dose (MTD) of OKI-219 in monotherapy (Cycle 1 (First 28 days on treatment))
- • Assess safety of OKI-219 as monotherapy or in combination with other anti-cancer therapies: incidence of SAEs (Through 30 days after last dose, an average of 1 year)
- • Assess safety of OKI-219 as monotherapy or in combination with other anti-cancer therapies: incidence of Grade 2 or greater treatment emergent adverse events (Through 30 days after last dose, an average of 1 year)
Sponsor
OnKure, Inc. · industry
Contacts & investigators
ContactOnKure, Inc. · contact · info@onkure.com · 720-307-2892
All locations (34)
California Cancer Associates for Research and ExcellenceRecruiting
Encinitas, California, United States
University of California San Diego UCSDRecruiting
La Jolla, California, United States
UCLA Jonsson Comprehensive Cancer CenterRecruiting
Los Angeles, California, United States
Hoag - Huntington BeachRecruiting
Newport Beach, California, United States
Regents of the University of ColoradoRecruiting
Aurora, Colorado, United States
Sarah Cannon Research Institute at HealthONERecruiting
Denver, Colorado, United States
Massachusetts General HospitalRecruiting
Boston, Massachusetts, United States
Karmanos Cancer InsituteWithdrawn
Detroit, Michigan, United States
Comprehensive Cancer Centers of NevadaRecruiting
Las Vegas, Nevada, United States
Stony Brook UniversityRecruiting
Stony Brook, New York, United States
SCRI Oncology Partners - NashvilleRecruiting
Nashville, Tennessee, United States
NEXT Oncology VirginiaRecruiting
Fairfax, Virginia, United States
Fred Hutchinson Cancer CenterRecruiting
Seattle, Washington, United States
Institut Jules BordetRecruiting
Anderlecht, Belgium
UZ Leuven - Campus GasthuisbergRecruiting
Leuven, Belgium
GZA Hopsitals Campus Sint-AugustinusRecruiting
Wilrijk, Belgium
Centre de Lutte Contre le Cancer CLCC - Centre Georges Francois Leclerc (CGFL)Recruiting
Dijon, France
Centre Oscar LambretRecruiting
Lille, France
Centre Leon BerardRecruiting
Lyon, France
Centre Antoine LacassagneRecruiting
Nice, France
Hopital Lyon SudRecruiting
Pierre-Bénite, France
Institut Gustave RoussyRecruiting
Villejuif, France
Ospedale San RaffaeleRecruiting
Milan, Italy
Ospedale San Gerardo-ASST MonzaRecruiting
Monza, Italy
Istituto Clinico HumanitasRecruiting
Rozzano, Italy
Gachon University Gil Medical CenterRecruiting
Incheon, South Korea
Seoul National University HospitalRecruiting
Seoul, South Korea
Severance HospitalRecruiting
Seoul, South Korea
Asan Medical CenterRecruiting
Seoul, South Korea
Samsung Medical CenterRecruiting
Seoul, South Korea
NEXT Oncology Phase I Unit / IOB- Hospital Quironsalud BarcelonaRecruiting
Barcelona, Spain
Hospital Beata Maria AnaRecruiting
Madrid, Spain
Hospital Universitario 12 de OctubreRecruiting
Madrid, Spain
START - MadridRecruiting
Madrid, Spain