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    DRUG CLASS:

    PDGFR β inhibitor

    Related drugs:
    1m
    Study to Assess the Efficacy & Safety of KHK4951 in Patients With Neovascular Age-Related Macular Degeneration (clinicaltrials.gov)
    P2, N=180, Active, not recruiting, Kyowa Kirin Co., Ltd. | Recruiting --> Active, not recruiting
    Enrollment closed
    1m
    Study to Assess the Efficacy & Safety of KHK4951 in Patients With Diabetic Macular Edema (clinicaltrials.gov)
    P2, N=150, Active, not recruiting, Kyowa Kirin Co., Ltd. | Recruiting --> Active, not recruiting
    Enrollment closed
    2ms
    Selective EV Protein Sorting and Pathway Perturbation in AML Upon Synergistic FLT3 and Hedgehog Pathway Inhibition. (PubMed, J Extracell Vesicles)
    These findings were corroborated by comparative proteomics of EVs derived from AML patients and healthy donors. Ribosomal and ErbB signalling pathway proteins may play an important role in microenvironmental modulation by EVs, and Crenolanib treatment potentially acts by interfering with leukaemia niche formation.
    Journal
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    FLT3 (Fms-related tyrosine kinase 3) • RPS26 (Ribosomal Protein S26) • GAB1 (GRB2 Associated Binding Protein 1) • RPL27A (Ribosomal Protein L27a)
    |
    FLT3 mutation
    |
    crenolanib (ARO-002)
    6ms
    Study to Assess the Efficacy & Safety of KHK4951 in Patients With Neovascular Age-Related Macular Degeneration (clinicaltrials.gov)
    P2, N=180, Recruiting, Kyowa Kirin Co., Ltd. | Trial completion date: Dec 2025 --> Sep 2026 | Trial primary completion date: Nov 2025 --> Aug 2026
    Trial completion date • Trial primary completion date
    6ms
    Study to Assess the Efficacy & Safety of KHK4951 in Patients With Diabetic Macular Edema (clinicaltrials.gov)
    P2, N=150, Recruiting, Kyowa Kirin Co., Ltd. | Trial completion date: Dec 2025 --> Sep 2026 | Trial primary completion date: Nov 2025 --> Aug 2026
    Trial completion date • Trial primary completion date
    10ms
    Targeting ceramide transfer protein sensitizes AML to FLT3 inhibitors via a GRP78-ATF6-CHOP axis. (PubMed, Nat Commun)
    Additionally, co-treatment of HPA-12 and Crenolanib is effective in FLT3-ITD+ and FLT3-TKD+ AML patients. The synergistic effects are found to be mediated by the endoplasmic reticulum stress-GRP78/ATF6/CHOP axis and mitophagy. Our data provide an effective strategy to enhance the efficacy of FLT3 inhibitors in AML.
    Journal
    |
    FLT3 (Fms-related tyrosine kinase 3) • HSPA5 (Heat Shock Protein Family A (Hsp70) Member 5) • ATF6 (Activating Transcription Factor 6)
    |
    FLT3-ITD mutation
    |
    crenolanib (ARO-002)
    1year
    Targeting Myeloid Cells in Head and Neck Squamous Cell Carcinoma: A Kinase Inhibitor Library Screening Approach. (PubMed, Int J Mol Sci)
    Among the promising inhibitors tested, vatalanib, a VEGF-R inhibitor, demonstrated significant in vivo efficacy at inhibiting tumor growth and reducing tumor-associated myeloid cells, thereby underscoring its potential as a therapeutic agent. Our findings highlight specific kinase inhibitors with differential modulatory effects on HNSCC-associated myeloid subsets and caution the application of some as anti-cancer drugs. This experimental system may provide a robust platform for identifying new agents targeting tumor-associated myeloid cells in HNSCC and beyond, and for elucidating mechanistic insights into tumor-myeloid cell interaction.
    Journal
    |
    ITGAM (Integrin, alpha M)
    |
    vatalanib (PTK787)
    1year
    Discovery of key molecular signatures for diagnosis and therapies of glioblastoma by combining supervised and unsupervised learning approaches. (PubMed, Sci Rep)
    Finally, we recommended KGs-guided four repurposable drug molecules (Fluoxetine, Vatalanib, TGX221 and RO3306) against GBM through molecular docking, drug likeness, ADMET analyses and molecular dynamics simulation studies. Thus, the discoveries of this study could serve as valuable resources for wet-lab experiments in order to take a proper treatment plan against GBM.
    Journal
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    TOP2A (DNA topoisomerase 2-alpha) • RAD51 (RAD51 Homolog A) • AURKA (Aurora kinase A) • CHEK1 (Checkpoint kinase 1) • RAD51AP1 (RAD51 Associated Protein 1) • CCNB2 (Cyclin B2) • CDK1 (Cyclin-dependent kinase 1) • MCM10 (Minichromosome Maintenance 10 Replication Initiation Factor) • CDCA8 (Cell Division Cycle Associated 8)
    |
    TGX-221 • fluoxetine • vatalanib (PTK787)
    over1year
    The Comparative Metabolism of a Novel Hepatocellular Carcinoma Therapeutic Agent, 2,3-Diamino-N-(4-(benzo[d]thiazol-2-yl)phenyl)propanamide, in Human and Animal Hepatocytes. (PubMed, Metabolites)
    ETN101 remained stable in human CESs. In conclusion, this study provides comprehensive insights into the metabolic characteristics of ETN101, valuable for its toxicological and clinical development.
    Journal
    |
    CYP1A2 (Cytochrome P450, family 1, subfamily A, polypeptide 2)
    over1year
    A Study to Evaluate Safety, Tolerability and Pharmacokinetic of ND-003 Tablets in Healthy Adults (clinicaltrials.gov)
    P1, N=104, Enrolling by invitation, Shenzhen NewDEL Biotech, Co., Ltd | Not yet recruiting --> Enrolling by invitation
    Enrollment open
    over1year
    The relationships of platelet-derived growth factor, microvascular proliferation, and tumor cell proliferation in canine high-grade oligodendrogliomas: Immunohistochemistry of 45 tumors and an AFOB-01 xenograft mouse model. (PubMed, Vet Pathol)
    Crenolanib (a PDGFR inhibitor) inhibited AOFB-01 cell proliferation...Therefore, PDGF-A produced by microvascular proliferations and tumor cells may promote the proliferation of PDGFR-α-expressing tumor cells in canine HGOG. PDGFR-α signaling has potential as a therapeutic target.
    Preclinical • Journal • Tumor cell
    |
    PDGFRA (Platelet Derived Growth Factor Receptor Alpha)
    |
    crenolanib (ARO-002)
    over1year
    A Safety and Efficacy Study of Multiple Tyrosine Kinase Inhibitor Drug (ETN101) in Advanced Hepatocellular Carcinoma (clinicaltrials.gov)
    P1, N=50, Recruiting, Etnova Therapeutics Corp.
    New P1 trial • Metastases