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Study of IDE196 in Patients with Solid Tumors Harboring GNAQ/11 Mutations or PRKC Fusions

Phase 1
Recruiting
Conditions
Metastatic Uveal Melanoma
Colorectal Cancer
Cutaneous Melanoma
Other Solid Tumors
Interventions
Registration Number
NCT03947385
Lead Sponsor
IDEAYA Biosciences
Brief Summary

This is a Phase 1/2, multi-center, open-label basket study designed to evaluate the safety and anti-tumor activity of IDE196 in patients with solid tumors harboring GNAQ or GNA11 (GNAQ/11) mutations or PRKC fusions, including metastatic uveal melanoma (MUM), cutaneous melanoma, colorectal cancer, and other solid tumors.

Phase 1 (dose escalation - monotherapy) will assess safety, tolerability and pharmacokinetics of IDE196 via standard dose escalation scheme and determine the recommended Phase 2 dose. Safety and anti-tumor activity will be assessed in the Phase 2 (dose expansion) part of the study.

Phase 1 (dose escalation - binimetib combination) will assess safety, tolerability and pharmacokinetics of IDE196 and binimetinib via standard dose escalation scheme and determine the recommended Phase 2 dose. Safety and anti-tumor activity will be assessed in the Phase 2 (dose expansion) part of the study.

Phase 1 (dose escalation - crizotinib combination) will assess safety, tolerability and pharmacokinetics of IDE196 and crizotinib via standard dose escalation scheme and determine the recommended Phase 2 dose. Safety and anti-tumor activity will be assessed in the Phase 2 (dose expansion) part of the study. Evaluation of safety and efficacy across multiple doses may be explored in the dose optimization part of the study.

Crizotinib monotherapy with crossover to combination cohort may be assessed for safety and to show the contribution of each study drug to anti-tumor activity.

As of Protocol Amendment 10, Phase 1, Phase 2 dose expansion in IDE196 monotherapy, and Phase 2 dose expansion of IDE196 in combination with binimetinib have been fully enrolled. There were no patients enrolled in the crizotinib monotherapy cohorts.

Detailed Description

Not available

Recruitment & Eligibility

Status
RECRUITING
Sex
All
Target Recruitment
341
Inclusion Criteria
  • Patient must be ≥18 years of age and able to provide written informed consent

  • Diagnosis of the following:

    o MUM: Uveal melanoma with histological or cytological confirmed metastatic disease. Metastatic disease may be treatment naïve or have progressed on or after most recent therapy. If the most recent therapy was an immune-oncology agent, PD must be confirmed.

    • If a patient is treatment naïve and human leukocyte antigen (HLA)-A*02:01 positive***, documentation is required to provide rationale why treatment with tebentafusp is not the ideal firstline treatment approach or of the patient's intolerance to tebentafusp.

    ***To be enrolled in the HLA-A*02:01 positive cohort, HLA status must be documented by test results from a CAP/CLIA-certified laboratory.

  • Measurable disease per RECIST v1.1

  • Eastern Cooperative Oncology Group ≤1 and expected life expectancy of > 3 months

  • Adequate organ function at screening

  • Adequate contraceptive measures for non-sterilized male and female patients of childbearing potential

Crizotinib Combination Additional Inclusion Criteria:

  • Prior chemotherapy other therapies as applicable or major surgeries must have been completed at least 4 weeks prior to initiation of crizotinib
  • Patients with preexisting peripheral neuropathy can be included if it is Grade 1 or lower, prior to initiation of crizotinib Biopsy-eligible patients
  • Accessible lesion(s) that permit a total of at least two biopsies without unacceptable risk of a significant procedural complication.
Exclusion Criteria
  • Previous treatment with a PKC inhibitor
  • Known MSI-H/dMMR tumors who have not previously received immune checkpoint inhibitors
  • Known symptomatic brain metastases
  • Adverse events from prior anti-cancer therapy that have not resolved
  • Known acquired immunodeficiency syndrome (AIDS)-related illness, hepatitis B virus, or hepatitis C virus
  • Active infection requiring ongoing therapy
  • Recent surgery or radiotherapy
  • Prior gastrectomy or upper bowel removal or any other gastrointestinal disorder or defect
  • Females who are pregnant or breastfeeding
  • Impaired cardiac function
  • Treatment with prohibited medications that cannot be discontinued prior to study entry
  • For patients receiving IDE196 powder-in-capsule (PIC) formulation or crizotinib, allergy to mammalian meat products and gelatin

Crizotinib Combination Additional Exclusion Criteria:

  • Prior therapy directly targeting ALK, MET, or ROS1
  • Spinal cord compression
  • History of pneumonitis or interstitial lung disease
  • History of syncope
  • History of thromboembolic or cerebrovascular events ≤12 weeks prior to first dose of study treatment

PK Substudy (optional) with Pravastatin Additional Exclusion Criteria:

  • Taken any dose of statin or inhibitor of organic anion transporting polypeptide within 7 days prior to enrollment in the study and cannot refrain from them through C2D1
  • Taken drugs that interfere with the absorption, metabolism, or elimination of pravastatin
  • Any contraindication associated to the use of statins or hypersensitivity component of pravastatin
  • Active liver disease

Study & Design

Study Type
INTERVENTIONAL
Study Design
SEQUENTIAL
Arm && Interventions
GroupInterventionDescription
Dose Expansion MonotherapyIDE196RP2D in MUM and non-MUM tumors harboring GNAQ/11 mutations or PRKC fusions (cutaneous melanoma, CRC, other solid tumors)
Dose Escalation Binimetinib CombinationIDE196IDE196 dosed orally, twice daily (BID) for each 28-day cycle and Binimetinib dosed orally, twice daily (BID) for each 28-day cycle
Dose Expansion Binimetinib CombinationIDE196RP2D in MUM and non-MUM tumors harboring GNAQ/11 mutations (cutaneous melanoma, CRC, other solid tumors)
Dose Escalation Crizotinib CombinationIDE196IDE196 dosed orally, twice daily (BID) for each 28-day cycle and Crizotinib dosed orally, twice daily (BID) for each 28-day cycle
Dose Expansion Crizotinib CombinationIDE196RP2D in MUM and non-MUM tumors harboring GNAQ/11 mutations (cutaneous melanoma, CRC, other solid tumors) Previously treated MUM, Treatment naïve MUM, MUM patients with human leukocyte antigen (HLA)-A\*02:01 positive status
Dose Escalation MonotherapyIDE196IDE196 dosed orally, twice daily (BID) for each 28-day cycle
Dose Escalation Binimetinib CombinationBinimetinibIDE196 dosed orally, twice daily (BID) for each 28-day cycle and Binimetinib dosed orally, twice daily (BID) for each 28-day cycle
Dose Expansion Binimetinib CombinationBinimetinibRP2D in MUM and non-MUM tumors harboring GNAQ/11 mutations (cutaneous melanoma, CRC, other solid tumors)
Dose Escalation Crizotinib CombinationCrizotinibIDE196 dosed orally, twice daily (BID) for each 28-day cycle and Crizotinib dosed orally, twice daily (BID) for each 28-day cycle
Dose Expansion Crizotinib CombinationCrizotinibRP2D in MUM and non-MUM tumors harboring GNAQ/11 mutations (cutaneous melanoma, CRC, other solid tumors) Previously treated MUM, Treatment naïve MUM, MUM patients with human leukocyte antigen (HLA)-A\*02:01 positive status
Dose Optimization Crizotinib CombinationIDE196IDE196 dosed orally, twice daily (BID) for each 28-day cycle and Crizotinib dosed orally, twice daily (BID) for each 28-day cycle
Dose Optimization Crizotinib CombinationCrizotinibIDE196 dosed orally, twice daily (BID) for each 28-day cycle and Crizotinib dosed orally, twice daily (BID) for each 28-day cycle
Crizotinib Monotherapy with Crossover to CombinationIDE196Crizotinib dosed orally, twice daily (BID) for each 28-day cycle until disease progression then IDE196 added and dosed orally, twice daily (BID) for each 28-day cycle
Crizotinib Monotherapy with Crossover to CombinationCrizotinibCrizotinib dosed orally, twice daily (BID) for each 28-day cycle until disease progression then IDE196 added and dosed orally, twice daily (BID) for each 28-day cycle
PK Substudy with Pravastatin (OBTP1B1 Substrate)CrizotinibA PK substudy with approximately 18 patients will be nested within the IDE196 and crizotinib combination expansion cohort to evaluate the impact on the pravastatin PK profile by the steady state exposures of IDE196.
Primary Outcome Measures
NameTimeMethod
Recommended Phase 2 Dose (RP2D) as monotherapy, in combination with Binimetinib, or in combination with CrizotinibApprox. 6 months

Determine RP2D of IDE196 as monotherapy, in combination with Binimetinib, or in combination with Crizotinib

Duration of Response for combination with Binimetinib or in combination with Crizotinib Dose Expansion by Blinded Independent Review CommitteeApprox. 48 months

RECIST v1.1

Maximum Tolerated Dose (MTD)28 days following first dose of IDE196 as monotherapy, in combination with Binimetinib, or in combination with Crizotinib

Determine MTD of IDE196 as monotherapy, in combination with Binimetinib, or in combination with Crizotinib

Plasma Concentrations of Binimetinib administered in combination with IDE196Approx. 6 months

Pharmacokinetics of Binimetinib in combination with IDE196

Plasma Concentrations of Crizotinib administered in combination with IDE196Approx. 6 months

Pharmacokinetics of Crizotinib in combination with IDE196

Dose-limiting Toxicity (DLT)28 days following first dose of IDE196 as monotherapy, in combination with Binimetinib, or in combination with Crizotinib

Determine DLT of IDE196 as monotherapy, in combination with Binimetinib, or in combination with Crizotinib

Plasma Concentrations of IDE196 as monotherapy, in combination with Binimetinib, or in combination with CrizotinibApprox. 6 months

Pharmacokinetics of IDE196 as monotherapy, in combination with Binimetinib, or in combination with Crizotinib

Overall Response Rate (ORR) for combination with Binimetinib or in combination with Crizotinib Dose Expansion by Blinded Independent Review CommitteeApprox. 48 months

Response Evaluation Criteria in Solid Tumors (RECIST) version 1.1 (v1.1) criteria

Secondary Outcome Measures
NameTimeMethod
ORR by InvestigatorApprox. 48 months

RECIST v1.1

Duration of Response by InvestigatorApprox. 48 months

RECIST v1.1

Numbers of Participants with Adverse EventsApprox. 48 months

Safety and tolerability of IDE196 either as monotherapy, in combination with Binimetinib, or in combination with Crizotinib

Overall Response Rate (ORR) for combination with Binimetinib or in combination with Crizotinib in Dose Escalation and all combination cohorts by Blinded Independent Review CommitteeApprox. 48 months

Response Evaluation Criteria in Solid Tumors (RECIST) version 1.1 (v1.1) criteria

Duration of Response for combination with Binimetinib or in combination with Crizotinib in Dose Escalation and in all combination cohorts by Blinded Independent Review CommitteeApprox. 48 months

RECIST v1.1

Disease Control by InvestigatorApprox. 48 months

RECIST v1.1

Treatment-related pharmacodynamic effect in all patientsApprox. 48 months

Modulation of signaling proteins in PKC, MAPK, and MET pathways

Trial Locations

Locations (10)

UCLA Medical Center

🇺🇸

Los Angeles, California, United States

San Francisco Oncology Associates

🇺🇸

San Francisco, California, United States

Columbia University Medical Center - Herbert Irving Pavilion

🇺🇸

New York, New York, United States

Duke University Medical Center

🇺🇸

Durham, North Carolina, United States

University of Cincinnati Cancer Center

🇺🇸

Cincinnati, Ohio, United States

Sidney Kimmel Cancer Center at Thomas Jefferson University

🇺🇸

Philadelphia, Pennsylvania, United States

The Sarah Cannon Research Institute/Tennessee Oncology

🇺🇸

Nashville, Tennessee, United States

The University of Texas MD Anderson Cancer Center

🇺🇸

Houston, Texas, United States

Westmead Hospital

🇦🇺

Sydney, New South Wales, Australia

Princess Margaret Cancer Centre

🇨🇦

Toronto, Ontario, Canada

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