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DRUG CLASS:

EphA2 receptor antagonist

6d
Identification of a novel diagnostic biomarker for osteoarthritis associated with chromatin regulators based on bioinformatics and experiments. (PubMed, J Orthop Surg Res)
Our findings suggest that AURKB serves as a crucial biomarker in the development and progression of OA and is significantly associated with immune infiltration, offering a novel perspective for elucidating the pathogenesis of OA.
Journal
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AURKB (Aurora Kinase B) • IL1B (Interleukin 1, beta)
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dasatinib
7d
Hpv-driven rewiring of the tumor immune microenvironment through single-cell profiling informs prognosis and therapy in HNSCC. (PubMed, Oral Oncol)
Our study leverages single-cell profiling to elucidate HPV-driven immunological remodeling in HNSCC. The derived prognostic signature effectively captures the essence of the TIME, serving as a reliable biomarker for predicting patient survival and informing precision therapy, potentially bridging the gap between HPV status and clinical decision-making.
Journal • Tumor mutational burden • PD(L)-1 Biomarker • IO biomarker
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TMB (Tumor Mutational Burden) • CD8 (cluster of differentiation 8) • PD-1 (Programmed cell death 1) • CD4 (CD4 Molecule) • BARD1 (BRCA1 Associated RING Domain 1)
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dasatinib
11d
Evaluation of antileukemic potentials of maslinic acid through targeting responsive proteins of human leukemia: a mechanistic perception on molecular modelling and dynamic stimulations. (PubMed, In Silico Pharmacol)
Maslinic acid (MA), a plant-derived pentacyclic triterpene, was compared to the FDA-approved drugs dasatinib (DAS) and doxorubicin (DOX) to determine its antileukemic potential. Thus, these results illustrate that MA may act as a natural scaffold with antileukemic properties and call for additional experimental confirmation. The online version contains supplementary material available at 10.1007/s40203-025-00478-3.
Journal
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FLT3 (Fms-related tyrosine kinase 3) • ABL1 (ABL proto-oncogene 1) • BCR (BCR Activator Of RhoGEF And GTPase)
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CBL mutation
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dasatinib • doxorubicin hydrochloride
17d
Study BT5528-100 in Patients With Advanced Solid Tumors Associated With EphA2 Expression (clinicaltrials.gov)
P1/2, N=288, Active, not recruiting, BicycleTx Limited | Recruiting --> Active, not recruiting | Trial completion date: Oct 2025 --> Jul 2027 | Trial primary completion date: Oct 2025 --> Jul 2026
Enrollment closed • Trial completion date • Trial primary completion date
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CD4 (CD4 Molecule) • EPHA2 (EPH receptor A2)
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Opdivo (nivolumab) • BT5528
18d
HLA diversity is associated with TKI response and treatment-free remission in chronic myeloid leukemia. (PubMed, Hemasphere)
Among 289 patients with clinical follow-up, HLA-DQB1*06:04 (aHR [95% CI] = 3.71 [1.57-8.77]) and DRB1*13:02 (aHR = 3.95 [1.77-8.81]) were associated with faster MR4 achievement in imatinib-treated patients (FDR < 0.01), while B*44:02 (aHR = 4.83 [1.62-14.41]) predicted favorable response to dasatinib (FDR < 0.05). Conversely, a higher HED score for HLA-C was associated with improved TFR in dasatinib-treated patients (P = 0.0067). These findings suggest that HLA genotype and class-specific HED may influence CML susceptibility and outcomes and could inform TKI selection and discontinuation strategies.
Journal
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HLA-DRB1 (Major Histocompatibility Complex, Class II, DR Beta 1) • HLA-DQB1 (Major Histocompatibility Complex, Class II, DQ Beta 1) • HLA-C (Major Histocompatibility Complex, Class I, C)
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dasatinib • imatinib
21d
PTEN Loss Promotes PI3Kβ Phosphorylation and EPHA2/SRC/p-PI3KβY962 Complex Assembly to Drive Tumorigenesis. (PubMed, Cancer Discov)
Dasatinib, an FDA-approved SRC/EPHA2 inhibitor, effectively reduced p-PI3KβY962 and inhibited tumor progression in PTEN-null but not PTEN-WT tumors. These findings establish p-PI3KβY962 as a druggable target and biomarker for developing targeted therapy in PTEN-deficient cancers beyond conventional PI3K kinase inhibition.
Journal
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MYC (V-myc avian myelocytomatosis viral oncogene homolog) • PTEN (Phosphatase and tensin homolog) • PIK3CB (Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit beta)
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dasatinib
25d
Case Report: Dual resistance to dasatinib/olverembatinib in accelerated-phase cml: identification of a novel SPECC1L-inserted e8a2 BCR::ABL1 transcript and ABL1 V379I mutation. (PubMed, Front Oncol)
She ultimately achieved Major Molecular Response (MMR) after haploidentical hematopoietic stem-cell transplantation (haplo-HSCT). This case highlights the importance of comprehensive molecular profiling at diagnosis and the need to develop alternative therapeutic strategies for rare BCR::ABL1 variants.
Journal
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ABL1 (ABL proto-oncogene 1) • SPECC1L (Sperm Antigen With Calponin Homology And Coiled-Coil Domains 1 Like)
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ABL1 fusion
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dasatinib • Nailike (olverembatinib)
28d
Machine learning-driven dissection of the obesity-ccRCC interface: FCGR2A emerges as a central coordinator of tumor-immune crosstalk. (PubMed, Front Oncol)
The optimized machine learning model (glmBoost+Stepglm) generated a parsimonious 14-gene signature demonstrating exceptional cross-cohort accuracy (mean AUC=0.991), while pharmacological screening prioritized kinase inhibitors (e.g., dasatinib, p=2.1×10⁻⁸) and immunomodulators as therapeutic candidates. Our study establishes FCGR2A-mediated myeloid reprogramming as a critical interface between metabolic dysfunction and ccRCC progression, serving as both a prognostic biomarker and therapeutic target. This dual-disease modeling paradigm provides actionable insights for precision management of obesity-associated malignancies.
Journal
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FCGR2A (Fc fragment of IgG receptor IIa)
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dasatinib
29d
Dual targeting of RET and SRC synergizes in RET fusion-positive cancer cells. (PubMed, Mol Oncol)
Our results show that the multitargeted SRC TKI dasatinib significantly enhanced the efficacy of RET TKIs in RET fusion-positive (RET+) NSCLC and PTC cells...Importantly, synergy was also observed with eCF506 (NXP900), a next-generation clinical SRC inhibitor. Finally, both SRC TKIs restored sensitivity in selpercatinib-resistant RET+ PTC cells. These results elucidate RET and SRC signaling crosstalk in RET+ NSCLC and PTC, suggesting that co-inhibiting SRC has clinical potential in TKI-naïve and -resistant RET+ cancers.
Journal
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RET (Ret Proto-Oncogene) • RPS6 (Ribosomal Protein S6)
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RET fusion • RET positive
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dasatinib • Retevmo (selpercatinib) • NXP900
1m
Identification of RCN3-positive cancer-associated fibroblasts as novel drivers of colorectal cancer through a TGF-β pathway-based risk signature. (PubMed, Int J Surg)
Comprehensive multi-omics mapping links heightened TGF-β activity and a distinct consensus-clustering subtype to unfavourable outcomes and immunotherapy resistance in CRC. The externally validated TGFRS offers a practical prognostic and predictive tool. RCN3⁺ CAFs constitute key stromal drivers, and dasatinib emerges as a repurposable agent to disrupt this axis, warranting clinical exploration.
Journal
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TGFB1 (Transforming Growth Factor Beta 1)
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dasatinib
1m
Trial completion date
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ABL1 (ABL proto-oncogene 1) • BCR (BCR Activator Of RhoGEF And GTPase) • RUNX1 (RUNX Family Transcription Factor 1) • KMT2A (Lysine Methyltransferase 2A) • ETV6 (ETS Variant Transcription Factor 6)
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MLL rearrangement
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dasatinib • cytarabine • doxorubicin hydrochloride • cyclophosphamide • etoposide IV • methotrexate • vincristine • daunorubicin • clofarabine • leucovorin calcium • Oncaspar liquid (pegaspargase) • mercaptopurine • thioguanine • Hemady (dexamethasone tablets) • Starasid (cytarabine ocfosfate)
1m
Cellular senescence in cancer: Unveiling dual roles, tumor microenvironment dynamics and therapeutic innovations (Review). (PubMed, Oncol Lett)
Recent advances in senotherapy, including senolytics such as dasatinib and quercetin, senomorphics and Traditional Chinese Medicine-derived agents such as resveratrol, aim to eliminate pathological senescence while preserving its beneficial roles...The primary aim of the present review is to systematically dissect the context-dependent mechanisms underlying cellular senescence in cancer-including the heterogeneity of the SASP and its cancer-type-specific roles and evaluate emerging senotherapeutic modalities, and discuss key challenges and future directions to guide precision oncology approaches. To further advance this aim, future research can leverage single-cell technologies to dissect senescence heterogeneity at the cellular and molecular levels; this will help distinguish protective senescent populations from pathogenic ones, thereby enabling the potential development of precision oncology approaches tailored to tumor-specific senescence landscapes.
Review • Journal • IO biomarker
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IL6 (Interleukin 6) • CXCL8 (Chemokine (C-X-C motif) ligand 8)
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dasatinib