^
    5d
    AXL-Driven Stemness and Hedgehog Signaling in HER2-Positive Breast Cancer with Acquired Trastuzumab Resistance: Synergistic Potential of AXL and HER2 Co-Targeting. (PubMed, Life (Basel))
    These results emphasize the pivotal role of AXL in regulating both stemness and hedgehog signaling in HER2-positive breast cancer. The study suggests that targeting both AXL and HER2 could be a promising strategy to overcome trastuzumab resistance and improve treatment outcomes.
    Journal
    |
    HER-2 (Human epidermal growth factor receptor 2) • AXL (AXL Receptor Tyrosine Kinase) • PTCH1 (Patched 1) • GLI1 (GLI Family Zinc Finger 1) • SOX2 • POU5F1 (POU Class 5 Homeobox 1) • GAS6 (Growth arrest specific 6) • NANOG (Nanog Homeobox)
    |
    HER-2 positive
    |
    Herceptin (trastuzumab) • bemcentinib (BGB324)
    15d
    KC1036 in Combination With PD-1 Antibody and Platinum-based Chemotherapy for First-line Advanced Esophageal Cancer (clinicaltrials.gov)
    P2, N=60, Recruiting, Beijing Konruns Pharmaceutical Co., Ltd.
    New P2 trial
    |
    cisplatin • paclitaxel • Loqtorzi (toripalimab-tpzi) • KC1036
    19d
    COAXIN: Avelumab in Combination With AVB-S6-500 in Patients With Advanced Urothelial Carcinoma (clinicaltrials.gov)
    P1, N=19, Active, not recruiting, University of Oklahoma | Trial completion date: Feb 2026 --> Oct 2026
    Trial completion date
    |
    Bavencio (avelumab) • batiraxcept (AVB-500)
    20d
    ONO-7475-03: Study of ONO-7475 in Combination With Osimertinib in EGFR Gene Mutation-positive Non-small Cell Lung Cancer (clinicaltrials.gov)
    P1, N=78, Completed, Ono Pharmaceutical Co. Ltd | Active, not recruiting --> Completed | Trial completion date: Apr 2026 --> Jun 2025 | Trial primary completion date: Apr 2026 --> Jun 2025
    Trial completion • Trial completion date • Trial primary completion date
    |
    EGFR (Epidermal growth factor receptor)
    |
    EGFR mutation • EGFR L858R • EGFR exon 19 deletion
    |
    Tagrisso (osimertinib) • tamnorzatinib (ONO-7475)
    22d
    A Study of FC084CSA in Combination of Tislelizumab in Patients With Advanced Malignant Solid Tumors (clinicaltrials.gov)
    P1/2, N=33, Recruiting, FindCure Biosciences (ZhongShan) Co., Ltd. | Trial primary completion date: Feb 2026 --> Jul 2026
    Trial primary completion date
    |
    Tevimbra (tislelizumab-jsgr)
    27d
    Design, synthesis, and Lead optimization of novel Quinazoline-based FLT3 inhibitors with potent anti-acute myelogenous leukemia activity. (PubMed, Bioorg Med Chem Lett)
    Guided by a scaffold-hopping strategy based on G-749 (denfivontinib), a series of quinazoline-based derivatives was designed and synthesized to explore structure-activity relationships (SAR)...Mechanism studies indicated that W4 induced G0/G1 cell cycle arrest and apoptosis, accompanied by a reduction in intracellular reactive oxygen species levels and a loss of mitochondrial membrane potential. Collectively, these results identified W4 as a potent FLT3 inhibitor and provided valuable SAR insights for further scaffold optimization.
    Journal
    |
    FLT3 (Fms-related tyrosine kinase 3) • KIT (KIT proto-oncogene, receptor tyrosine kinase)
    |
    FLT3 mutation
    |
    denfivontinib (SKI-G-801)
    30d
    Postoperative Radiotherapy Combined With Nimotuzumab Followed by Bemcentinib in High-Risk Patients With Head and Neck Squamous Cell Carcinoma (clinicaltrials.gov)
    P3, N=370, Not yet recruiting, Shanghai Ninth People's Hospital Affiliated to Shanghai Jiao Tong University
    New P3 trial
    |
    EGFR (Epidermal growth factor receptor) • PD-L1 (Programmed death ligand 1)
    |
    cisplatin • bemcentinib (BGB324) • TheraCIM (nimotuzumab)
    1m
    Next-generation AI-assisted drug design against cancer: large language models meet conventional in silico methods. (PubMed, In Silico Pharmacol)
    AIC1 showed the highest binding affinity (- 10.079 kcal/mol), surpassing clinical-stage bemcentinib (- 8.234 kcal/mol)...This work pioneers LLM-driven in silico design of AXL inhibitors, offering a scalable blueprint for accelerated anticancer drug development. The online version contains supplementary material available at 10.1007/s40203-026-00582-y.
    Journal
    |
    GAS6 (Growth arrest specific 6)
    |
    bemcentinib (BGB324)
    1m
    KEYNOTE-D35: Oral Axl/Mer/CSF1R Selective Tyrosine Kinase Inhibitor Q702 in Combination With Pembrolizumab in Patients With Selected Advanced Solid Tumors (clinicaltrials.gov)
    P1/2, N=120, Active, not recruiting, Qurient Co., Ltd. | Recruiting --> Active, not recruiting | Trial completion date: Jun 2026 --> Mar 2028 | Trial primary completion date: Oct 2025 --> Dec 2027
    Enrollment closed • Trial completion date • Trial primary completion date
    |
    Keytruda (pembrolizumab) • adrixetinib (Q702)
    1m
    Super-Enhancer-Driven SOX4/SMAD3 Mediate Membrane Remodeling by Regulating Phospholipid Metabolism to Accelerate Leukemia Progression. (PubMed, Adv Sci (Weinh))
    Notably, the AXL inhibitor Bemcentinib effectively suppressed CML-BP progression in both in vivo and in vitro models. Collectively, our findings establish SE-driven SOX4 and SMAD3 as key regulators in CML-BP and identify Bemcentinib as a promising therapeutic strategy.
    Journal
    |
    ABL1 (ABL proto-oncogene 1) • BCR (BCR Activator Of RhoGEF And GTPase) • LPCAT1 (Lysophosphatidylcholine Acyltransferase 1) • SMAD3 (SMAD Family Member 3) • SOX4 (SRY-Box Transcription Factor 4)
    |
    bemcentinib (BGB324)
    1m
    QRNT-012: Study of Q702 in Subjects with Relapsed or Refractory Chronic Graft-versus-Host Disease (cGVHD) (2025-522680-14-00)
    P1, N=16, Recruiting, Qurient Co. Ltd.
    New P1 trial
    |
    adrixetinib (Q702)
    2ms
    ARC-27: A Study of AB801 Monotherapy and Combination Therapy in Participants With Advanced Malignancies (clinicaltrials.gov)
    P1, N=91, Active, not recruiting, Arcus Biosciences, Inc. | Recruiting --> Active, not recruiting
    Enrollment closed
    |
    EGFR (Epidermal growth factor receptor) • ALK (Anaplastic lymphoma kinase) • MET (MET proto-oncogene, receptor tyrosine kinase) • ROS1 (Proto-Oncogene Tyrosine-Protein Kinase ROS) • NTRK (Neurotrophic receptor tyrosine kinase)
    |
    EGFR mutation • ALK mutation • MET mutation
    |
    docetaxel