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    DRUG CLASS:

    c-Abl tyrosine kinase inhibitor

    Related drugs:
    16d
    IkT-148009-201: A Randomized, Double-Blind, Placebo-Controlled Trial of IkT-148009 in Untreated Parkinson's Disease (clinicaltrials.gov)
    P2, N=137, Completed, ABLi Therapeutics, Inc. | Active, not recruiting --> Completed
    Trial completion
    6ms
    Identification of alkynyl nicotinamide HSN748 as a RET solvent-front mutant inhibitor with intracranial efficacy. (PubMed, RSC Med Chem)
    RET solvent-front G810C/R/S mutations confer resistance to the currently approved RET protein tyrosine kinase inhibitors (TKIs) selpercatinib and pralsetinib. Among three compounds (HSN748, HSND19, and HSN608) evaluated for B/KR(G810C) brain tumors, HSN748 exhibited significant intracranial tumor inhibition. PK analysis indicated that HSN748 has a brain/plasma partition coefficient (K p) of 0.4, demonstrating its capability to penetrate the central nervous system (CNS).
    Journal
    |
    RET (Ret Proto-Oncogene) • KIF5B (Kinesin Family Member 5B) • CCDC6 (Coiled-Coil Domain Containing 6)
    |
    RET fusion • RET mutation • CCDC6-RET fusion • RET positive
    |
    Retevmo (selpercatinib) • Gavreto (pralsetinib) • HSN608
    1year
    A Phase 1, SAD and MAD Study to Evaluate the Safety and Tolerability of FB418 (clinicaltrials.gov)
    P1, N=64, Recruiting, 1ST Biotherapeutics, Inc. | Not yet recruiting --> Recruiting | Trial primary completion date: Sep 2024 --> Dec 2024
    Enrollment open • Trial primary completion date
    1year
    A PK Study of IkT-148009 in Older and Elderly Healthy Subjects (clinicaltrials.gov)
    P1, N=8, Completed, Inhibikase Therapeutics, Inc.
    New P1 trial
    |
    itraconazole
    1year
    A Phase I 7-Day Dosing Study of IkT-148009. (clinicaltrials.gov)
    P1, N=6, Completed, Inhibikase Therapeutics, Inc.
    New P1 trial
    over1year
    IkT-148009-201: A Randomized, Double-Blind, Placebo-Controlled Trial of IkT-148009 in Untreated Parkinson's Disease (clinicaltrials.gov)
    P2, N=120, Active, not recruiting, Inhibikase Therapeutics, Inc. | Trial primary completion date: Jun 2024 --> Sep 2024
    Trial primary completion date
    over1year
    PROSEEK: A Phase 2 Study In Early Parkinson's Disease Patients Evaluating The Safety And Efficacy Of Abl Tyrosine Kinase Inhibition Using K0706 (clinicaltrials.gov)
    P2, N=513, Terminated, Sun Pharma Advanced Research Company Limited | Trial completion date: Mar 2024 --> Jun 2024 | Active, not recruiting --> Terminated; Terminated based on study outcomes
    Trial completion date • Trial termination
    over1year
    A Randomized, Double-Blind, Placebo-Controlled Trial of IkT-148009 in Untreated Parkinson's Disease (clinicaltrials.gov)
    P2, N=120, Active, not recruiting, Inhibikase Therapeutics, Inc. | Recruiting --> Active, not recruiting
    Enrollment closed
    2years
    Effect of asciminib and vitamin K2 on Abelson tyrosine-kinase-inhibitor-resistant chronic myelogenous leukemia cells. (PubMed, BMC Cancer)
    Asciminib and VK2 are suggested as a novel treatment for ABL-TKI-resistant cells since they increase treatment efficacy. Additionally, this treatment option has intriguing clinical relevance for patients who are resistant to ABL TKIs.
    Journal
    |
    ABL1 (ABL proto-oncogene 1) • BCR (BCR Activator Of RhoGEF And GTPase) • CASP3 (Caspase 3) • CASP7 (Caspase 7)
    |
    imatinib • Iclusig (ponatinib) • Scemblix (asciminib)
    over2years
    Fluid retention-associated adverse events in patients treated with BCR::ABL1 inhibitors based on FDA Adverse Event Reporting System (FAERS): a retrospective pharmacovigilance study. (PubMed, BMJ Open)
    This pharmacovigilance study serves as a clinical reminder to physicians to be more vigilant for fluid retention-associated AEs with BCR::ABL inhibitors.
    Retrospective data • Journal • Adverse events
    |
    dasatinib • imatinib • Iclusig (ponatinib) • Tasigna (nilotinib) • bosutinib
    almost3years
    Synthesis and biological evaluation of novel aromatic amide derivatives as potential BCR-ABL inhibitors. (PubMed, Bioorg Med Chem Lett)
    Biological studies showed that compared with Imatinib, these compounds showed significant proliferation inhibitory activities of HL-60 and K562 in cell activity assay...Compounds 4g and 4j, as potential BCR-ABL1 inhibitors, inhibit the phosphorylation of ABL1 and CRKL in a dose-dependent manner. Therefore, compounds 4g and 4j can be used as a starting point for further optimization.
    Journal
    |
    ABL1 (ABL proto-oncogene 1) • BCR (BCR Activator Of RhoGEF And GTPase) • CRKL (CRK Like Proto-Oncogene, Adaptor Protein)
    |
    imatinib