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A Study to Evaluate KIN-2787 in Participants With BRAF and/or NRAS Mutation Positive Solid Tumors

Phase 1
Recruiting
Conditions
Solid Tumor, Adult
Non-small Cell Lung Cancer
Melanoma
Interventions
Registration Number
NCT04913285
Lead Sponsor
Pierre Fabre Medicament
Brief Summary

The purpose of this study is to evaluate the safety, tolerability, pharmacokinetics (PK), and preliminary efficacy of KIN-2787 in adults with BRAF/NRAS-mutated advanced or metastatic solid tumors.

Detailed Description

This is a two-part, open-label, multi-center, dose escalation and dose expansion study in participants with BRAF mutation-positive and/or NRAS mutation-positive tumors designed to evaluate the safety, tolerability, and pharmacokinetics (PK) of KIN-2787, a RAF small molecule kinase inhibitor, to determine a recommended Phase 2 dose (RP2D) of KIN-2787, and to assess the objective response to KIN-2787 therapy alone and in combination with binimetinib, a mitogen-activated protein kinase (MEK) inhibitor.

The dose expansion phase (Part B) will assess the safety and efficacy of KIN-2787 at the recommended dose and schedule in patients with cancers that contain BRAF Class I, II or III mutations, including lung cancer, melanoma, and other selected solid tumors.

Recruitment & Eligibility

Status
RECRUITING
Sex
All
Target Recruitment
400
Inclusion Criteria
  • Provide written informed consent prior to initiation of any study-specific procedures.
  • Metastatic or advanced stage solid tumor
  • Known BRAF Class I, Class II, or Class III alteration or melanoma with an NRAS mutation as confirmed by previous genomic analysis of tumor tissue or ctDNA.
  • Measurable (Part A and B) or evaluable (Part A only) disease by RECIST v1.1.
  • ECOG performance status 0-1
  • Adequate organ function, as measured by laboratory values (criteria listed in protocol).
  • Able to swallow, retain, and absorb oral medications.
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Exclusion Criteria
  • Known participants who have received local therapy with either surgery and/or radiation therapy (participants with asymptomatic untreated brain metastasis may be eligible if met with certain criteria)
  • In Part B Dose Expansion, previous treatment with any approved or in-development small molecule BRAF-, MEK-, or MAPK-directed inhibitor therapy.
  • GI tract disease causing an inability to take oral medication, malabsorption syndrome, requirement for intravenous alimentation, or uncontrolled inflammatory GI disease.
  • Active, uncontrolled bacterial, fungal, or viral infection.
  • Participant with a positive test result for SARS-CoV2 infection, is known to have asymptomatic infection or is suspected of having SARS-CoV2, is excluded
  • Women who are lactating or breastfeeding, or pregnant.
  • Participants with any other active treated malignancy within 3 years prior to enrollment

Complete inclusion and exclusion criteria are listed in the clinical study protocol.

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Study & Design

Study Type
INTERVENTIONAL
Study Design
SEQUENTIAL
Arm && Interventions
GroupInterventionDescription
Dose Escalation Combination therapy (Part A2)KIN-2787 and binimetinibDose escalation of KIN-2787 and binimetinib
Dose Escalation Combination therapy (Part B2)KIN-2787 and binimetinibDose expansion evaluating the recommended phase 2 dose (RP2D) of KIN-2787 and binimetinib
Dose Expansion Monotherapy (Part B1)KIN-2787Dose expansion evaluating the recommended phase 2 dose (RP2D) of KIN-2787
Dose Escalation Monotherapy (Part A1)KIN-2787Dose escalation of KIN-2787
Primary Outcome Measures
NameTimeMethod
Part A2 Dose Escalation: KIN-2787 + Binimetinib CombinationInitiation of study drug through 28 days after last dose (up to approximately 18 months)

To determine the safety and tolerability of oral administration of KIN-2787 + binimetinib including DLTs, and to identify the MTD and/or the appropriate dose for further clinical investigation.

In Part B (Dose Expansion) - duration of overall response (DOR).Initiation of study drug until disease progression (up to approximately 36 months)

Measure of clinical benefit, defined as the time from initial tumor response to documented tumor progression

Part A1 Dose escalation monotherapy:Initiation of study drug through 28 days after last dose (up to approximately 18 months)

To determine the safety and tolerability of oral administration of KIN-2787 including dose-limiting toxicities (DLTs), and to identify the maximum tolerated dose (MTD) and/or the appropriate dose for further clinical investigation in Part B Dose Expansion.

In Part B (Dose Expansion) - duration of stable disease.Initiation of study drug until disease progression (up to approximately 36 months)
In Part B (Dose Expansion) - disease control rate (DCR).Initiation of study drug until disease progression (up to approximately 36 months)
In Part B (Dose Expansion) - objective response rate (ORR) using RECIST v1.1.Initiation of study drug until disease progression (up to approximately 36 months)

To assess preliminary evidence of the anti-cancer activity of KIN-2787 and for (B2) KIN-2787 + binimetinib

Secondary Outcome Measures
NameTimeMethod
Part A1 Dose Escalation: Characterization of PK properties and effect of food on PK of KIN-2787 including, but not limited to Cmax.Initiation of study drug through Cycle 5, where each cycle is 28 days (up to approximately 4 months)
Part A1 Dose Escalation: Characterization of PK properties and effect of food on PK of KIN-2787 including, but not limited to AUC.Initiation of study drug through Cycle 5, where each cycle is 28 days (up to approximately 4 months)
Part B Dose Expansion: characterization of PK properties of KIN-2787, and for (B2) KIN-2787 + binimetinib including, but not limited to AUC.Initiation of study drug through Cycle 5, where each cycle is 28 days (up to approximately 4 months)
Part B Dose Expansion: characterization of PK properties of KIN-2787, and for (B2) KIN-2787 + binimetinib including, but not limited to tmax.Initiation of study drug through Cycle 5, where each cycle is 28 days (up to approximately 4 months)
Part A2 Dose Escalation: characterization of PK properties of KIN-2787 and binimetinib in combination including, but not limited to tmax.Initiation of study drug through Cycle 5, where each cycle is 28 days (up to approximately 4 months)
Part A1 Dose Escalation: Characterization of PK properties and effect of food on PK of KIN-2787 including, but not limited to tmax.Initiation of study drug through Cycle 5, where each cycle is 28 days (up to approximately 4 months)
Part A2 Dose Escalation: characterization of PK properties of KIN-2787 and binimetinib in combination including, but not limited to Cmax.Initiation of study drug through Cycle 5, where each cycle is 28 days (up to approximately 4 months)
Part A2 Dose Escalation: characterization of PK properties of KIN-2787 and binimetinib in combination including, but not limited to AUC.Initiation of study drug through Cycle 5, where each cycle is 28 days (up to approximately 4 months)
Part B Dose Expansion: characterization of PK properties of KIN-2787, and for (B2) KIN-2787 + binimetinib including, but not limited to Cmax.Initiation of study drug through Cycle 5, where each cycle is 28 days (up to approximately 4 months)

Trial Locations

Locations (43)

University of Southern California

🇺🇸

Los Angeles, California, United States

Fox Chase Cancer Center

🇺🇸

Philadelphia, Pennsylvania, United States

UCSD Moores Cancer Center

🇺🇸

La Jolla, California, United States

UCLA

🇺🇸

Los Angeles, California, United States

Providence Medical Foundation (St. Joseph's)

🇺🇸

Santa Rosa, California, United States

Stanford Cancer Center

🇺🇸

Stanford, California, United States

Thomas Jefferson

🇺🇸

Philadelphia, Pennsylvania, United States

NYU Langone

🇺🇸

New York, New York, United States

INCLIVA (Hospital Clinico de Valencia)

🇪🇸

Valencia, Spain

Union Hospital of Tongji Medical College of HUST

🇨🇳

Wuhan, Hubei, China

Beijing University Cancer Hospital

🇨🇳

Beijing, China

Linear Clinical Research

🇦🇺

Perth, Western Australia, Australia

Taipei Veterans General Hospital

🇨🇳

Taipei, Taiwan

Memorial Sloan Kettering Cancer Center

🇺🇸

New York, New York, United States

Providence

🇺🇸

Fullerton, California, United States

Decatur Memorial Hospital

🇺🇸

Decatur, Illinois, United States

Cleveland Clinic

🇺🇸

Cleveland, Ohio, United States

Virginia Cancer Specialists

🇺🇸

Fairfax, Virginia, United States

Northwest Medical Specialties

🇺🇸

Tacoma, Washington, United States

Melanoma Institute Australia

🇦🇺

Wollstonecraft, New South Wales, Australia

The Shanghai Pulmonary Hospital

🇨🇳

Shanghai, China

Linyi Cancer Hospital

🇨🇳

Linyi, Shandong, China

Institut Bergonie

🇫🇷

Bordeaux, France

Centre Leon Berard

🇫🇷

Lyon, France

APHM-CHU La Timone

🇫🇷

Marseille, France

Gustave Roussy

🇫🇷

Villejuif, France

CHU Nantes-Hotel Dieu

🇫🇷

Nantes, France

Seoul National University Hospital

🇰🇷

Seoul, Korea, Republic of

Samsung Medical Center

🇰🇷

Seoul, Korea, Republic of

Vall d'Hebron Institute of Oncology (VHIO)

🇪🇸

Barcelona, Spain

Netherlands Cancer Institute

🇳🇱

Amsterdam, Netherlands

Hospital Quiron Dexeus

🇪🇸

Barcelona, Spain

Hospital Universitario Insular de Gran Canaria

🇪🇸

Las Palmas De Gran Canaria, Spain

National Taiwan University Hospital

🇨🇳

Taipei, Taiwan

City of Hope

🇺🇸

Duarte, California, United States

Chungbuk National University Hospital

🇰🇷

Cheongju-si, Korea, Republic of

Hospital General Gregorio Marañón

🇪🇸

Madrid, Spain

UC Davis

🇺🇸

Sacramento, California, United States

Orlando Health Cancer Institute

🇺🇸

Orlando, Florida, United States

Sarah Cannon Research Institute - Lake Nona

🇺🇸

Orlando, Florida, United States

Moffitt Cancer Ceter

🇺🇸

Tampa, Florida, United States

Center for Cancer and Blood Disorders

🇺🇸

Bethesda, Maryland, United States

Sarah Cannon Research Institute

🇺🇸

Nashville, Tennessee, United States

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