^
    7ms
    A Phase 1 Study of KIN-3248, an irreversible small molecule pan-FGFR inhibitor, in Patients with Advanced FGFR 2/3 Driven Solid Tumors. (PubMed, Cancer Res Commun)
    The trial was terminated early for commercial considerations; therefore, RP2D was not established. Preliminary clinical data suggest that KIN-3248 is a safe, oral FGFR1-4 inhibitor with favorable PK parameters, though further dose escalation was required to nominate the MTD/RP2D.
    P1 data • Journal • Metastases
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    FGFR2 (Fibroblast growth factor receptor 2) • FGFR3 (Fibroblast growth factor receptor 3)
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    FGFR mutation
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    KIN-3248
    9ms
    The irreversible FGFR inhibitor KIN-3248 overcomes FGFR2 kinase domain mutations. (PubMed, Clin Cancer Res)
    Thus, KIN-3248 is a novel FGFR1-4 inhibitor whose distinct activity profile against FGFR kinase domain mutations highlights its potential for the treatment of ICC and other FGFR-driven cancers.
    Journal
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    FGFR2 (Fibroblast growth factor receptor 2) • FGFR3 (Fibroblast growth factor receptor 3)
    |
    FGFR2 mutation • FGFR2 fusion • FGFR mutation • FGFR3 fusion • FGFR3 V555M
    |
    KIN-3248
    10ms
    Discovery of KIN-3248, An Irreversible, Next Generation FGFR Inhibitor for the Treatment of Advanced Tumors Harboring FGFR2 and/or FGFR3 Gene Alterations. (PubMed, J Med Chem)
    Herein, we describe how structure-based drug design (SBDD) was used to enable the discovery of the potent and kinome selective pan-FGFR inhibitor KIN-3248, which is active against many acquired resistance mutations. KIN-3248 is currently in phase I clinical development for the treatment of advanced tumors harboring FGFR2 and/or FGFR3 gene alterations.
    Journal • Metastases
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    FGFR2 (Fibroblast growth factor receptor 2) • FGFR3 (Fibroblast growth factor receptor 3)
    |
    FGFR2 mutation
    |
    KIN-3248
    12ms
    A Study to Evaluate KIN-3248 in Participants With Advanced Tumors Harboring FGFR2 and//or FGFR3 Gene Alterations (clinicaltrials.gov)
    P1, N=54, Active, not recruiting, Kinnate Biopharma | Recruiting --> Active, not recruiting | N=120 --> 54
    Enrollment closed • Enrollment change • Metastases
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    FGFR2 (Fibroblast growth factor receptor 2)
    |
    KIN-3248
    over1year
    Phase I study evaluating KIN-3248, a next-generation, irreversible pan-FGFR inhibitor, in patients with advanced cholangiocarcinoma, urothelial carcinoma and other solid tumors harboring FGFR2 and/or FGFR3 gene alterations (ESMO 2023)
    Secondary objectives include pharmacokinetic and pharmacodynamic assessments including measures of FGFR pathway modulation. Planned sample size is 140 pts and the study is enrolling patients in the US, EU and globally.
    Clinical • P1 data • Metastases
    |
    FGFR2 (Fibroblast growth factor receptor 2) • FGFR3 (Fibroblast growth factor receptor 3)
    |
    FGFR2 mutation
    |
    KIN-3248
    over1year
    Phase 1/1b study evaluating KIN-3248, a next-generation, irreversible pan-FGFR inhibitor (FGFRi), in patients (pts) with advanced cholangiocarcinoma (CCA) and other solid tumors harboring FGFR2 and/or FGFR3 gene alterations (ESMO-GI 2023)
    Reversible FGFRi are approved for the treatment of pts with locally advanced or metastatic CCA harboring FGFR2 gene fusions or rearrangements (pemigatinib and infigratinib) or metastatic urothelial carcinoma (UC) with susceptible FGFR2 or FGFR3 genetic alterations (erdafitinib). Secondary objectives include pharmacokinetic and pharmacodynamic assessments including measures of FGFR pathway modulation. The study is actively enrolling patients in the US and globally.Clinical trial identification: NCT05242822.Legal entity responsible for the study: Kinnate Biopharma.
    Clinical • P1 data • Metastases
    |
    FGFR2 (Fibroblast growth factor receptor 2) • FGFR3 (Fibroblast growth factor receptor 3)
    |
    FGFR2 mutation • FGFR2 fusion • FGFR3 fusion
    |
    Balversa (erdafitinib) • Truseltiq (infigratinib) • Pemazyre (pemigatinib) • KIN-3248
    over1year
    First in human (FIH) Phase 1/1b study evaluating KIN-3248, a next-generation, irreversible pan-FGFR inhibitor (FGFRi), in patients (pts) with advanced cholangiocarcinoma (CCA) and other solid tumors harboring FGFR2 and/or FGFR3 gene alterations (CCF 2023)
    No abstract available
    Clinical • P1 data • Metastases
    |
    FGFR2 (Fibroblast growth factor receptor 2) • FGFR3 (Fibroblast growth factor receptor 3)
    |
    KIN-3248
    almost2years
    First in human (FIH) phase 1/1b study evaluating KIN-3248, a next-generation, irreversible pan-FGFR inhibitor (FGFRi), in patients (pts) with advanced urothelial carcinoma (UC) and other solid tumors harboring FGFR2 and/or FGFR3 gene alterations. (ASCO-GU 2023)
    Reversible FGFRi are approved for the treatment of pts with locally advanced or metastatic urothelial carcinoma (UC) with susceptible FGFR2 or FGFR3 genetic alterations (erdafitinib) or metastatic CCA harboring FGFR2 gene fusions or rearrangements (pemigatinib and infigratinib). The study is actively enrolling patients in the US and globally. Clinical trial information: NCT05242822.
    Clinical • P1 data • Metastases
    |
    FGFR2 (Fibroblast growth factor receptor 2) • FGFR3 (Fibroblast growth factor receptor 3) • FGFR1 (Fibroblast growth factor receptor 1)
    |
    FGFR2 mutation • FGFR2 fusion
    |
    Balversa (erdafitinib) • Truseltiq (infigratinib) • Pemazyre (pemigatinib) • KIN-3248
    almost2years
    First in human (FIH) phase 1/1b study evaluating KIN-3248, a next-generation, irreversible pan-FGFR inhibitor (FGFRi), in patients (pts) with advanced cholangiocarcinoma (CCA) and other solid tumors harboring FGFR2 and/or FGFR3 gene alterations. (ASCO-GI 2023)
    Reversible FGFRi are approved for the treatment of pts with locally advanced or metastatic CCA harboring FGFR2 gene fusions or rearrangements (pemigatinib and infigratinib) or metastatic urothelial carcinoma (UC) with susceptible FGFR2 or FGFR3 genetic alterations (erdafitinib). The study is actively enrolling patients in the US and globally. Clinical trial information: NCT05242822.
    Clinical • P1 data • Metastases
    |
    FGFR2 (Fibroblast growth factor receptor 2) • FGFR3 (Fibroblast growth factor receptor 3)
    |
    FGFR2 mutation • FGFR2 fusion • FGFR3 fusion
    |
    Balversa (erdafitinib) • Truseltiq (infigratinib) • Pemazyre (pemigatinib) • KIN-3248
    over2years
    Design and rationale of a first-in-human (FIH) phase 1/1b study evaluating KIN-3248, a next-generation, irreversible (irrev), pan-FGFR inhibitor (FGFRi), in adult patients with solid tumors harboring FGFR2 and/or FGFR3 gene alterations (NCT05242822). (ASCO 2022)
    There are currently 3 FDA-approved, reversible FGFRi for treatment of patients w/previously treated, locally advanced or metastatic (met) cholangiocarcinoma (CCA) harboring FGFR2 gene fusions/rearrangements (pemigatinib and infigratinib) or met urothelial carcinoma (UC) w/susceptible FGFR2 or FGFR3 genetic alterations (erdafitinib). Secondary objectives include pharmacokinetic and pharmacodynamic assessments including measures of FGFR pathway modulation. Enrollment is expected to commence in April 2022.
    Clinical • P1 data
    |
    FGFR2 (Fibroblast growth factor receptor 2) • FGFR3 (Fibroblast growth factor receptor 3) • FGFR1 (Fibroblast growth factor receptor 1)
    |
    FGFR2 mutation • FGFR2 fusion • FGFR3 fusion
    |
    Balversa (erdafitinib) • Truseltiq (infigratinib) • Pemazyre (pemigatinib) • KIN-3248
    over2years
    A Study to Evaluate KIN-3248 in Participants With Advanced Tumors Harboring FGFR2 and//or FGFR3 Gene Alterations (clinicaltrials.gov)
    P1, N=120, Recruiting, Kinnate Biopharma | Not yet recruiting --> Recruiting
    Enrollment open
    |
    FGFR2 (Fibroblast growth factor receptor 2)
    |
    KIN-3248
    almost3years
    A Study to Evaluate KIN-3248 in Participants With Advanced Tumors Harboring FGFR2 and//or FGFR3 Gene Alterations (clinicaltrials.gov)
    P1, N=120, Not yet recruiting, Kinnate Biopharma
    New P1 trial
    |
    FGFR2 (Fibroblast growth factor receptor 2)
    |
    KIN-3248