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REFOCUS: A First-in-Human Study of Highly Selective FGFR2 Inhibitor, RLY-4008, in Patients With ICC and Other Advanced Solid Tumors

Phase 1
Active, not recruiting
Conditions
FGFR2 Gene Translocation
FGFR2 Gene Activation
Cholangiocarcinoma
Other Solid Tumors, Adult
FGFR2 Gene Mutation
FGFR2 Amplification
FGFR2 Gene Fusion/Rearrangement
Intrahepatic Cholangiocarcinoma
Interventions
Drug: RLY-4008
Registration Number
NCT04526106
Lead Sponsor
Relay Therapeutics, Inc.
Brief Summary

This is a Phase 1/2, open-label, FIH study designed to evaluate the safety, tolerability, pharmacokinetics (PK), pharmacodynamics (PDy), and antineoplastic activity of RLY-4008, a potent and highly selective FGFR2 inhibitor, in patients with unresectable or metastatic cholangiocarcinoma (CCA) and other solid tumors. The study consists of 3 parts: a dose escalation (Part 1), a dose expansion (Part 2), and an extension (Part 3).

Detailed Description

Not available

Recruitment & Eligibility

Status
ACTIVE_NOT_RECRUITING
Sex
All
Target Recruitment
540
Inclusion Criteria

Not provided

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Exclusion Criteria

Not provided

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Study & Design

Study Type
INTERVENTIONAL
Study Design
PARALLEL
Arm && Interventions
GroupInterventionDescription
Part 1: Dose EscalationRLY-4008Multiple doses of RLY-4008 for oral administration.
Part 2: Dose ExpansionRLY-4008Oral dose of RLY-4008 as determined during Part 1 Dose Escalation.
Part 3: ExtensionRLY-4008Oral dose of RLY-4008 as determined during Part 1 Dose Escalation.
Part 4: RolloverRLY-4008Oral dose of RLY-4008 as determined during Part 1 Dose Escalation.
Primary Outcome Measures
NameTimeMethod
Part 1 and Part 4: Number of patients with adverse events and serious adverse eventsEvery cycle (4-week cycles) until study discontinuation, approximately 24 months
Part 1: Determination of maximum tolerated dose (MTD) and recommended Phase 2 dose (RP2D) of RLY-4008Cycle 1 (4-week cycle) of treatment for MTD and at the end of every cycle (4-week cycles) for RP2D until study discontinuation, approximately 24 months
Part 2 and Part 3: Objective Response Rate (ORR) assessed by Independent Review Committee per RECIST v1.1Approximately every 8 weeks during treatment and every 12 weeks after the last dose in the absence of progressive disease, approximately 36 months
Part 4: Number of patients with dose interruptionsEvery 28-day cycle until end of treatment, approximately 24 months.
Part 4: Number of patients with dose reductionsEvery 28-day cycle until end of treatment, approximately 24 months.
Part 4: Number of patients with dose discontinuationsEvery 28-day cycle until end of treatment, approximately 24 months.
Secondary Outcome Measures
NameTimeMethod
Part 2 and Part 3:Dose intensityEvery 28-day cycle until end of treatment, approximately 24 months.
Part 2 and Part 3: Correlation between FGFR2 genotype by central tissue assessment and antitumor response, as measured by ORRApproximately every 8 weeks during treatment and every 12 weeks after the last dose in the absence of progressive disease, approximately 36 months
Part 1: Pharmacodynamic parameters including changes in carcinoembryonic antigen (CEA)Approximately every 2 weeks in Cycle 1 (4-week cycle) and every other cycle (4-week cycles) from Cycle 3, approximately 24 months
Part 2 and Part 3: Number of patients with dose interruptionsEvery 28-day cycle until end of treatment, approximately 24 months.
Part 2 and Part 3: Number of patients with dose reductionsEvery 28-day cycle until end of treatment, approximately 24 months.
Part 1: Duration of Response (DOR) assessed by Investigator per RECIST v1.1Approximately every 8 weeks during treatment and every 12 weeks after the last dose in the absence of progressive disease, approximately 36 months
Part 1: Pharmacodynamic parameters including changes in fibroblast growth factor 23 (FGF-23)Approximately every 2 weeks in Cycle 1 (4-week cycle) and every other cycle (4-week cycles) from Cycle 3, approximately 24 months
Part 1: Pharmacodynamic parameters including changes in cancer antigen 19-9 (CA 19-9)Approximately every 2 weeks in Cycle 1 (4-week cycle) and every other cycle (4-week cycles) from Cycle 3, approximately 24 months
Part 2 and Part 3: Number of patients with dose discontinuationsEvery 28-day cycle until end of treatment, approximately 24 months.
Part 1: FGFR2 gene status in plasma circulating tumor deoxyribonucleic acid (ctDNA) and tumor tissueEvery cycle (4-week cycles) through Cycle 3 and every other cycle thereafter until study discontinuation, approximately 24 months
Pharmacokinetic parameters including area under the plasma concentration versus time curve (AUC)Approximately every 2 weeks in Cycle 1 (4-week cycle) and every cycle through Cycle 4 (4-week cycles)
Pharmacokinetic parameters including half-life (t1/2)Approximately every 2 weeks in Cycle 1 (4-week cycle) and every cycle through Cycle 4 (4-week cycles)
Part 2 and Part 3: Duration of response (DOR) assessed by Investigator and Independent Review Committee per RECIST v1.1Approximately every 8 weeks during treatment and every 12 weeks after the last dose in the absence of progressive disease, approximately 36 months
Part 2 and Part 3: Progression-free survival (PFS) assessed by Investigator and Independent Review Committee per RECIST v1.1Approximately every 8 weeks during treatment and every 12 weeks after the last dose in the absence of progressive disease, approximately 36 months
Part 1: Disease Control Rate (DCR) as assessed by Investigator per RECIST v1.1Approximately every 8 weeks during treatment and every 12 weeks after the last dose in the absence of progressive disease, approximately 36 months
Part 1, Part 2, and Part 3: Objective Response Rate (ORR) as assessed by Investigator per RECIST v1.1Approximately every 8 weeks during treatment and every 12 weeks after the last dose in the absence of progressive disease, approximately 36 months
Pharmacokinetic parameters including maximum plasma drug concentration (Cmax)Approximately every 2 weeks in Cycle 1 (4-week cycle) and every cycle through Cycle 4 (4-week cycles)
Part 2 and Part 3: Disease control rate (DCR) assessed by Investigator and Independent Review Committee per RECIST v1.1Approximately every 8 weeks during treatment and every 12 weeks after the last dose in the absence of progressive disease, approximately 36 months
Part 2 and Part 3:Overall survival (OS)Up to approximately 36 months.
Part 2 and Part 3:Change from baseline in quality of life as assessed by EORTC QLQ-C30Approximately every 4 weeks during treatment, approximately 24 months

Trial Locations

Locations (48)

The University of Texas M.D. Anderson Cancer Center

🇺🇸

Houston, Texas, United States

The University of Alabama at Birmingham

🇺🇸

Birmingham, Alabama, United States

USC Norris Comprehensive Cancer Center

🇺🇸

Los Angeles, California, United States

Moffitt Cancer Center

🇺🇸

Tampa, Florida, United States

University of Chicago Medical Center

🇺🇸

Chicago, Illinois, United States

Winship Cancer Institute, Emory University

🇺🇸

Atlanta, Georgia, United States

University of Michigan

🇺🇸

Ann Arbor, Michigan, United States

Memorial Sloan Kettering Cancer Center

🇺🇸

New York, New York, United States

Taussig Cancer Institute Cleveland Clinic

🇺🇸

Cleveland, Ohio, United States

Fox Chase Cancer Center

🇺🇸

Philadelphia, Pennsylvania, United States

Texas Oncology

🇺🇸

Dallas, Texas, United States

St. Vincent's Hosptial Sydney

🇦🇺

Darlinghurst, Australia

Virginia Mason Medical Center

🇺🇸

Seattle, Washington, United States

Linear Clinical Research Ltd

🇦🇺

Nedlands, Australia

Icon Cancer Care South Brisbane

🇦🇺

South Brisbane,, Australia

Centre Leon Berard

🇫🇷

Lyon, France

Centre Antoine Lacassagne

🇫🇷

Nice, France

Gustave Roussy Cancer Campus

🇫🇷

Paris, France

Medizinische Hochschule Hannover

🇩🇪

Hannover, Germany

Universitätsklinikum Heidelberg

🇩🇪

Heidelberg, Germany

Queen Mary Hospital

🇭🇰

Hong Kong, Hong Kong

Seoul National University Hospital

🇰🇷

Seoul, Korea, Republic of

Asan Medical Center

🇰🇷

Seoul, Korea, Republic of

Samsung Medical Center

🇰🇷

Seoul, Korea, Republic of

Netherlands Cancer institute

🇳🇱

Amsterdam, Netherlands

National Cancer Center Singapore

🇸🇬

Singapore, Singapore

Hospital Universitari Vall d'Hebron

🇪🇸

Barcelona, Spain

START Barcelona-Hospital HM Nou Delfos

🇪🇸

Barcelona, Spain

Hospital Universitario Fundación Jiménez Díaz- START MADRID

🇪🇸

Madrid, Spain

Hospital Universitario HM Sanchinarro-START MADRID-CIOCC

🇪🇸

Madrid, Spain

Hospital Clínico Universitario de Valencia

🇪🇸

Valencia, Spain

Karolinska University Hospital

🇸🇪

Stockholm, Sweden

Clinica de Universidad de Navarra

🇪🇸

Pamplona, Spain

Sarah Cannon Research Institute UK

🇬🇧

London, United Kingdom

China Medical University Hospital

🇨🇳

Taichung, Taiwan

Huntsman Cancer Institute, University of Utah

🇺🇸

Salt Lake City, Utah, United States

UCSF Helen Diller Family Comprehensive Cancer Center

🇺🇸

San Francisco, California, United States

Mayo Clinic

🇺🇸

Rochester, Minnesota, United States

Istituto Europeo di Oncologia

🇮🇹

Milano, Italy

Istituto Nazionale Tumori Regina Elena

🇮🇹

Roma, Italy

Erasmus MC

🇳🇱

Rotterdam, Netherlands

Centre Georges François Leclerc

🇫🇷

Dijon, France

Institut Bergonie

🇫🇷

Bordeaux, France

University College London Hospitals NHS Foundation Trust

🇬🇧

London, United Kingdom

The Christie NHS Foundation Trust

🇬🇧

Manchester, United Kingdom

LMU Klinikum, Campus Grosshadern

🇩🇪

Munich, Germany

Massachusetts General Hospital

🇺🇸

Boston, Massachusetts, United States

Guy's Hospital

🇬🇧

London, United Kingdom

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