First-in-Human Study of OKI-219 in Advanced Solid Tumors and Advanced Breast Cancer

Trial statusRecruiting
Trial phasePhase 1
Trial typeInterventional
Biological sexAll
Age18+
SponsorOnKure, Inc.

About this trial

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

This trial does not accept healthy volunteers

Qualifiers

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

Disqualifiers

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.

Trial design

Design model

Sequential

Treatments tested in this trial

  • OKI-219

    Drug

    Oral twice daily

  • Fulvestrant

    Drug

    Intramuscular injection

  • Trastuzumab

    Drug

    Intravenous (IV)

  • Tucatinib

    Drug

    Oral twice daily

  • Atirmociclib

    Drug

    Oral twice daily

  • Ribociclib

    Drug

    Oral once daily continuous for 21-days followed by 7 days off

Treatment groups

200 Participants
are divided into 9 treatment groups

9

Treatment groups

See each treatment group below.

Group A: Phase 1a: Part A Dose EscalationExperimental treatment 1 intervention
Group B: Phase 1b: Part B Dose EscalationExperimental treatment 2 interventions
Group C: Phase 1b: Part B Dose OptimizationExperimental treatment 2 interventions
Group D: Phase 1b: Part C Dose EscalationExperimental treatment 3 interventions
Group E: Phase 1b: Part C Dose ExpansionExperimental treatment 3 interventions
Group F: Phase 1b: Part D Dose EscalationExperimental treatment 3 interventions
Group G: Phase 1b: Part D Dose ExpansionExperimental treatment 3 interventions
Group H: Phase 1b: Part E Dose EscalationExperimental treatment 3 interventions
Group I: Phase 1b: Part E Dose ExpansionExperimental treatment 3 interventions

Trial outcomes

Primary outcomes

1

Identify maximum tolerated dose (MTD) of OKI-219 in monotherapy

Frequency of participants experiencing dose-limiting toxicities during the first 28-day cycle

Time frame
Cycle 1 (First 28 days on treatment)
2

Assess safety of OKI-219 as monotherapy or in combination with other anti-cancer therapies: incidence of SAEs

Number and type of SAEs experienced by participants during treatment and follow-up

Time frame
Through 30 days after last dose, an average of 1 year
3

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

Number of treatment-emergent adverse events (TEAEs) equal or greater than Grade 2 experienced during treatment and follow-up

Time frame
Through 30 days after last dose, an average of 1 year
4

Assess rate of dose modifications during treatment with OKI-219 as monotherapy or in combination with other anti-cancer therapies

rate of dose modifications

Time frame
Through last study dose, an average of 1 year

Secondary outcomes

1

Assess the plasma PK of OKI-219 following single and multiple doses as monotherapy or in combination with other anti-cancer therapies: maximum plasma concentration (Cmax)

PK of OKI-219: Cmax

Time frame
Through cycle 6 of treatment (up to 28 weeks)
2

Assess the plasma PK of OKI-219 following single and multiple doses as monotherapy or in combination with other anti-cancer therapies: time of maximum plasma concentration (Tmax)

PK of OKI-219: Tmax

Time frame
Through cycle 6 of treatment (up to 28 weeks)
3

Assess the plasma PK of OKI-219 following single and multiple doses as monotherapy or in combination with other anti-cancer therapies: area under the plasma concentration-time curve (AUC)

PK of OKI-219: AUC

Time frame
Through cycle 6 of treatment (up to 28 weeks)
4

Assess the plasma PK of OKI-219 following single and multiple doses as monotherapy or in combination with other anti-cancer therapies: terminal elimination half-life time (t1/2)

PK of OKI-219: t1/2

Time frame
Through cycle 6 of treatment (up to 28 weeks)

Other outcomes

Sponsors and contacts

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