^
    3ms
    Oleandrin-mediated suppression of MELK induces apoptosis, autophagy, and ferroptosis in human non-small cell lung cancer cells. (PubMed, Phytomedicine)
    Oleandrin could potentially have therapeutic effects for NSCLC patients and possibly for other cancer types.
    Journal
    |
    MELK (Maternal Embryonic Leucine Zipper Kinase)
    |
    oleandrin (PBI-05204)
    5ms
    Rational Design and Identification of ISM7594 as a Tissue-Agnostic FGFR2/3 Inhibitor. (PubMed, J Med Chem)
    The compound demonstrated robust tumor growth suppression, favorable pharmacokinetic profile, and pharmacodynamic effects. This study supports the preclinical development of ISM7594 and demonstrates its potential in advancing tissue-agnostic therapy for advanced solid tumors with FGFR2/3 aberrations and mutation resistance.
    Journal • Pan tumor
    |
    FGFR2 (Fibroblast growth factor receptor 2) • FGFR1 (Fibroblast growth factor receptor 1)
    |
    FGFR2 mutation • FGFR2 fusion
    6ms
    Development of CPA-Catalyzed β-Selective Reductive Amination of Cardenolides for the Synthesis and Biological Evaluation of Hydrolytically Stable Analogs. (PubMed, Chemistry)
    The subsequent in vitro evaluation of digitoxigenin and oleandrin derivatives 13a, 13g, 15a, and 15gdemonstrated that these four analogs reduced steady-state ATP1A1 levels in T98G cells in the 12-96 nM range. Interestingly, only the oleandrin analog 15g also lowered also steady-state levels of the cellular prion protein (PrPC), the main therapeutic target for the treatment of prion diseases.
    Journal
    |
    ATP1A1 (ATPase Na+/K+ Transporting Subunit Alpha 1) • PRNP (Prion Protein)
    |
    oleandrin (PBI-05204)
    6ms
    A Study to Evaluate the Safety, Tolerability, and Pharmacokinetics of ABSK061 Mini-tablets in Healthy Adult Participants (clinicaltrials.gov)
    P1, N=42, Recruiting, Abbisko Therapeutics Co, Ltd
    New P1 trial
    |
    ABSK061
    6ms
    A Monotherapy in Subjects With Advanced Solid Tumors (clinicaltrials.gov)
    P1, N=42, Active, not recruiting, 3D Medicines (Beijing) Co., Ltd. | Trial completion date: Dec 2024 --> Dec 2026 | Trial primary completion date: Dec 2024 --> Dec 2025
    Trial completion date • Trial primary completion date
    |
    segigratinib (3D185)
    7ms
    Efficacy and Safety of 3D185 Monotherapy in Subjects With Previously Treated Locally Advanced or Metastatic Cholangiocarcinoma (clinicaltrials.gov)
    P2, N=50, Not yet recruiting, 3D Medicines (Beijing) Co., Ltd. | Trial completion date: Jun 2026 --> Jun 2028 | Trial primary completion date: Dec 2025 --> Dec 2027
    Trial completion date • Trial primary completion date
    |
    FGFR (Fibroblast Growth Factor Receptor)
    |
    segigratinib (3D185)
    7ms
    REFOCUS: A First-in-Human Study of Highly Selective FGFR2 Inhibitor, RLY-4008, in Patients With ICC and Other Advanced Solid Tumors (clinicaltrials.gov)
    P1/2, N=490, Active, not recruiting, Elevar Therapeutics | Trial primary completion date: Sep 2024 --> Sep 2025
    Trial primary completion date
    |
    FGFR2 (Fibroblast growth factor receptor 2) • FGF23 (Fibroblast Growth Factor 23) • CA 19-9 (Cancer antigen 19-9)
    |
    FGFR2 mutation • FGFR2 fusion
    |
    lirafugratinib (RLY-4008)
    7ms
    Novel Molecular Biomarkers to Guide Treatment Decision-making in Metastatic Urothelial Cancer-A Patient Cohort Analysis. (PubMed, Eur Urol Oncol)
    The molecular makeup of tumors, including molecular subtype, tumor microenvironment composition, and gene mutations, fusions, and amplifications, has previously been correlated with a response to immune checkpoint inhibitors, erdafitinib, or enfortumab vedotin (EV) monotherapy, and may withhold potential candidate biomarkers. Stratification of patients into subgroups based on these molecular features is possible. Our data challenge the concept of a one-treatment-fits-all paradigm and support the rationale for prospective clinical trials with biomarker-guided treatment selection of mUC patients.
    Journal • IO biomarker
    |
    FGFR2 (Fibroblast growth factor receptor 2) • NECTIN4 (Nectin Cell Adhesion Molecule 4)
    |
    FGFR2 mutation
    |
    Balversa (erdafitinib) • Padcev (enfortumab vedotin-ejfv)
    8ms
    Identification of Active Phytochemicals to Inhibit Signal Transducer and Activator of Transcription 5A (STAT5A) Dimerization for Prostate Cancer Therapy: An In Silico Approach. (PubMed, Anticancer Agents Med Chem)
    Pedunculagin demonstrated the strongest binding energy and stability, making it a promising candidate for further development as a novel lead compound to disrupt STAT5a/b dimerization in PCa therapy.
    Journal
    |
    STAT5A (Signal Transducer And Activator Of Transcription 5A)
    |
    oleandrin (PBI-05204)
    8ms
    THOR-2: A Study of Erdafitinib Versus Investigator Choice of Intravesical Chemotherapy in Participants Who Received Bacillus Calmette-Guérin (BCG) and Recurred With High Risk Non-Muscle-Invasive Bladder Cancer (NMIBC) (clinicaltrials.gov)
    P2, N=107, Completed, Janssen Research & Development, LLC | Active, not recruiting --> Completed
    Trial completion
    |
    FGFR (Fibroblast Growth Factor Receptor)
    |
    FGFR mutation • FGFR fusion
    |
    gemcitabine • Balversa (erdafitinib) • mitomycin
    9ms
    A Genome-Wide Synthetic Lethal Screen Identifies Spermidine Synthase as a Target to Enhance Erdafitinib Efficacy in FGFR-Mutant Bladder Cancer. (PubMed, Cancer Res)
    Notably, pharmacologic inhibition of SRM enhanced the efficacy of erdafitinib both in vitro and in vivo. Together, these results offer evidence that targeting SRM could attenuate the translation of HMGA2 and subsequently reduce EGFR transcription, thus enhancing the sensitivity of FGFR-mutant bladder cancer cells to erdafitinib treatment.
    Journal
    |
    EGFR (Epidermal growth factor receptor) • FGFR (Fibroblast Growth Factor Receptor) • HMGA2 (High mobility group AT-hook 2)
    |
    EGFR expression • FGFR mutation
    |
    Balversa (erdafitinib)