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    DRUG CLASS:

    Kinase inhibitor

    Related drugs:
    5d
    Pharmacogenomic and Circulating Biomarkers for CDK4/6 Inhibitors (clinicaltrials.gov)
    P=N/A, N=100, Enrolling by invitation, London Health Sciences Centre Research Institute OR Lawson Research Institute of St. Joseph's | Not yet recruiting --> Enrolling by invitation
    Enrollment open
    29d
    Regorafenib in Combination With Venetoclax and Azacitidine for the Treatment of Patients With Relapsed or Refractory Acute Myeloid Leukemia (clinicaltrials.gov)
    P1, N=20, Suspended, City of Hope Medical Center | Recruiting --> Suspended
    Trial suspension
    |
    BCL2 (B-cell CLL/lymphoma 2)
    |
    Venclexta (venetoclax) • azacitidine • Stivarga (regorafenib)
    1m
    Identification and Verification of Immune Metabolism-Related Biomarkers and Immune Infiltration Landscape for Pediatric Opsoclonus Myoclonus Ataxia Syndrome in Neuroblastoma. (PubMed, CNS Neurosci Ther)
    Four immune metabolism-associated diagnostic genes were identified, including TRAF3IP2, RIPK1, KEAP1, and DPP4 for OMAS.
    Journal
    |
    KEAP1 (Kelch Like ECH Associated Protein 1) • RIPK1 (Receptor Interacting Serine/Threonine Kinase 1)
    2ms
    Development of a leucine aminopeptidase-activatable co-prodrug from CDDO-Me and ligustrazine for synergistic treatment of liver injury. (PubMed, Bioorg Chem)
    Furthermore, CHL reduced p-p65 expression by 5-fold, indicating its effective inhibition of NF-κB transcriptional activity and thereby alleviating inflammatory responses. Therefore, the LAP-activable co-prodrug CHL holds promising potential as a candidate for the synergistic treatment of liver injury.
    Journal
    |
    NQO1 (NAD(P)H dehydrogenase, quinone 1) • RELA (RELA Proto-Oncogene)
    2ms
    Vandetanib and Everolimus in Treating Patients With Advanced or Metastatic Cancer (clinicaltrials.gov)
    P1, N=151, Completed, M.D. Anderson Cancer Center | Active, not recruiting --> Completed | Trial completion date: May 2026 --> Oct 2025 | Trial primary completion date: May 2026 --> Oct 2025
    Trial completion • Trial completion date • Trial primary completion date
    |
    everolimus • Caprelsa (vandetanib)
    2ms
    A Clinical Study of Neflamapimod in Patients With Dementia With Lewy Bodies (clinicaltrials.gov)
    P2, N=25, Active, not recruiting, EIP Pharma Inc | Recruiting --> Active, not recruiting
    Enrollment closed
    3ms
    Design, Synthesis, and 2D QSAR Analysis of Some Novel Pyrazolo[1,5-a]pyrimidine Derivatives as Pim-1 Kinase Inhibitors for the Treatment of MCF-7 Breast Cancer. (PubMed, Drug Dev Res)
    Compound 4d exhibited a 1.5-fold increased cytotoxic activity compared to doxorubicin against the MCF-7 cell line, whereas compound 9a showed an analogous activity to doxorubicin...Besides, docking of the desired compounds into Pim-1 ATP binding site showed a noteworthy binding mode for the enzyme inhibition. Additionally, a 2D QSAR identified the potential structural features controlling the Pim-1 inhibitory activity attained via the targeted pyrazolo[1,5-a]pyrimidines.
    Journal
    |
    TP53 (Tumor protein P53) • PIM1 (Pim-1 Proto-Oncogene)
    |
    doxorubicin hydrochloride
    3ms
    Stereotactic Body Radiotherapy and Focal Adhesion Kinase Inhibitor in Advanced Pancreas Adenocarcinoma (clinicaltrials.gov)
    P2, N=42, Active, not recruiting, Washington University School of Medicine | Trial primary completion date: Sep 2025 --> Dec 2025
    Trial primary completion date
    |
    Fakzynja (defactinib)
    3ms
    Design and synthesis of new Thieno[2,3-d]pyrimidine-based derivatives as anti-breast cancer: Biological evaluation, PIM-1 kinase inhibition, and in silico studies. (PubMed, Bioorg Chem)
    Compound 15 demonstrated the strongest anticancer activity, with IC50 value of 34.49 ± 1.32 μM, compared to doxorubicin (IC50 = 34.20 ± 0.28 μM)...Additionally, the binding relationships produced between compound 15 and the PIM-1 kinase active site were investigated using molecular docking experiments, providing insights into their inhibitory potential. Finally, to further assess the stability of the compound 15-PIM-1 kinase complex and validate the docking results, molecular dynamics (MD) simulations were performed.
    Journal • IO biomarker
    |
    BCL2 (B-cell CLL/lymphoma 2) • BAX (BCL2-associated X protein) • CASP3 (Caspase 3) • PIM1 (Pim-1 Proto-Oncogene)
    |
    doxorubicin hydrochloride
    3ms
    KC1036, a multi-kinase inhibitor with anti-angiogenic activity, can effectively suppress the tumor growth of Ewing sarcoma. (PubMed, Angiogenesis)
    The novel anti-angiogenic inhibitor, KC1036, is effective in treating ES in the preclinical models.
    Journal
    |
    FGFR (Fibroblast Growth Factor Receptor) • AXL (AXL Receptor Tyrosine Kinase) • KDR (Kinase insert domain receptor) • FLT1 (Fms-related tyrosine kinase 1) • NPY1R (Neuropeptide Y Receptor Y1)
    |
    doxorubicin hydrochloride • pazopanib • Cabometyx (cabozantinib tablet) • KC1036
    3ms
    ACCRU-GI-2008: Atezolizumab in Combination With a Multi-Kinase Inhibitor for the Treatment of Unresectable, Locally Advanced, or Metastatic Liver Cancer (clinicaltrials.gov)
    P2, N=122, Recruiting, Academic and Community Cancer Research United | Trial primary completion date: Dec 2024 --> Dec 2025
    Trial primary completion date
    |
    Avastin (bevacizumab) • Tecentriq (atezolizumab) • Lenvima (lenvatinib) • Cabometyx (cabozantinib tablet)
    3ms
    CA209-8LC: Study of PI3Kinase Inhibition (Copanlisib) and Anti-PD-1 Antibody Nivolumab in Relapsed/Refractory Solid Tumors With Expansions in Mismatch-repair Proficient (MSS) Colorectal Cancer (clinicaltrials.gov)
    P1/2, N=48, Completed, Sidney Kimmel Comprehensive Cancer Center at Johns Hopkins | Active, not recruiting --> Completed
    Trial completion • Mismatch repair • pMMR
    |
    KRAS (KRAS proto-oncogene GTPase) • BRAF (B-raf proto-oncogene)
    |
    KRAS wild-type • BRAF wild-type • NRAS wild-type
    |
    Opdivo (nivolumab) • Aliqopa (copanlisib)