- |||||||||| Journal: A Network-Driven Framework for Drug Response Precision Prediction of Acute Myeloid Leukemia. (Pubmed Central) - Jul 11, 2025
For instance, the co-expression of C19ORF59 and FLT3 is associated with resistance to FLT3 inhibitors. In summary, NetAML offers a powerful strategy for personalized AML treatment by constructing drug-specific models, identifying clinically actionable biomarkers, and supporting the development of optimized, patient-specific therapeutic regimens.
- |||||||||| emavusertib (CA-4948) / Curis, Dr. Reddy's
Journal: Discovery of pyrrolo[2,3-d]pyrimidine derivatives as novel FLT3/IRAK4 inhibitors. (Pubmed Central) - Jul 10, 2025
In summary, NetAML offers a powerful strategy for personalized AML treatment by constructing drug-specific models, identifying clinically actionable biomarkers, and supporting the development of optimized, patient-specific therapeutic regimens. Among them, HB-29 had the remarkable activity towards FLT3-WT (IC50
- |||||||||| midostaurin / Generic mfg., Vanflyta (quizartinib) / Daiichi Sankyo
Journal: Novel water-soluble and highly efficient dual type I/II next generation inhibitors of FMS-like tyrosine kinase 3 (FLT3). (Pubmed Central) - Jul 10, 2025
Additionally, good water solubility and consequently biological availability was achieved by attaching amine functions to appropriate scaffold positions, suggested by modeling of inhibitor binding at inactive and active FLT3 states. Subsequent formation of different salts led to very promising results in in vivo studies and improvements compared to midostaurin (1b), Quizartinib (7), Marbotinib 10 and its carbamate 11c.
- |||||||||| Avastin (bevacizumab) / Roche, nintedanib / Generic mfg.
Preclinical, Journal: Impact of Nintedanib on tumor angiogenesis and vascular normalization in a mouse model of colorectal cancer. (Pubmed Central) - Jul 10, 2025
In xenograft mouse model of colorectal cancer Nintedanib revealed anti-tumoral effects and induced vascular normalization. Our findings indicate that the treatment with Nintedanib could be able to improve intratumoral oxygen and thereby drug delivery to potentially enhance the efficacy of preexisting oncological therapies such as chemotherapy and radiation.
- |||||||||| EO-3021 / Concentra Biosciences
Trial completion date, Trial termination, Trial primary completion date: ELVCAP-002-01: Study of EO-3021 in Adult Patients With Solid Tumors Likely to Express CLDN18.2 (clinicaltrials.gov) - Jul 2, 2025
P1, N=88, Terminated,
Establishing an appropriate treatment strategy for HCC patients with AVF is imperative, highlighting the need for tailored therapeutic approaches based on individual vascular profiles. Trial completion date: Dec 2028 --> Jun 2025 | Recruiting --> Terminated | Trial primary completion date: Sep 2028 --> May 2025; Business Decision
- |||||||||| Xospata (gilteritinib) / Astellas
FL Derived From Erythrocytes Mediates Cancer-Induced Bone Pain by Activating its Receptor Flt3 in Sensory Neurons (Discovery Hall) - Jul 1, 2025 - Abstract #ASBMR2025ASBMR_1260;
FL-induced sprouting was abolished by Gilteritinib, a Flt3 inhibitor, without inducing significant neuronal toxicity...This suggests that KCNC4 is downstream of the FL/Flt3 axis in DRGs. These findings suggest that bone metastatic cancer cells inducing FL expression in erythrocytes in the marrow which may mediate CIBP through the Flt3/KCNC4 pathway in DRGs.
- |||||||||| Xospata (gilteritinib) / Astellas
FL Derived From Erythrocytes Mediates Cancer-Induced Bone Pain by Activating its Receptor Flt3 in Sensory Neurons (Discovery Hall) - Jul 1, 2025 - Abstract #ASBMR2025ASBMR_577;
FL-induced sprouting was abolished by Gilteritinib, a Flt3 inhibitor, without inducing significant neuronal toxicity...This suggests that KCNC4 is downstream of the FL/Flt3 axis in DRGs. These findings suggest that bone metastatic cancer cells inducing FL expression in erythrocytes in the marrow which may mediate CIBP through the Flt3/KCNC4 pathway in DRGs.
- |||||||||| Inlyta (axitinib) / Pfizer, Lenvima (lenvatinib) / Eisai, Merck (MSD)
FROM LIPS TO LUNGS: RECURRENT ADENOID CYSTIC CARCINOMA MANIFESTING AS LUNG MASS (McCormick Place - Lakeside Center Exhibit Hall Poster Area 4) - Jun 30, 2025 - Abstract #CHEST2025CHEST_3004;
ACC is rare, highly metastatic to lungs with poor prognosis. Any patient with ACC, even with curative surgery, who presents with pulmonary nodules/masses, should be evaluated for recurrence.
- |||||||||| SAR131675 / Sanofi
Proffered Paper: Reshaping Tumor-Vascular-Immune Crosstalk by VEGFR-3 Modulation in Breast Cancer Brain Metastases (Auditorium II; Poster Board No EACR25-1283) - Jun 29, 2025 - Abstract #EACR2025EACR_2025;
Cell tolerance to VEGFR-3 inhibitor (VEGFR-3i), SAR131675, was evaluated in vitro using increasing compound concentrations... These findings suggest that normalizing lymphatic vasculature through VEGFR3 modulation can reshape the tumor-immune-lymphatic landscape, fostering a more effective anti-tumor immune response and potentially enhancing immunotherapy efficacy.
- |||||||||| Venclexta (venetoclax) / Roche, AbbVie
C/EBP? coordinates key metabolic pathways driving the resistance to targeted therapies in FLT3-mutated acute myeloid leukemia (Poster and Exhibition Hall; Poster Board No EACR25-1525) - Jun 29, 2025 - Abstract #EACR2025EACR_1878;
in regulating both lipid and amino acid metabolism, affecting therapeutic response in FLT3-mutant AML. By identifying lipid biosynthesis enzymes and mitochondrial transaminases as key metabolic drivers of FLT3 inhibitors or VEN/AZA resistance, respectively, our study highlights promising targets to enhance treatment efficacy in this high-risk patient subgroup.
- |||||||||| Fruzaqla (fruquintinib) / Takeda
PK/PD data, Journal: Population Pharmacokinetics of Fruquintinib, a Selective Oral Inhibitor of VEGFR -1, -2, and -3, in Patients with Refractory Metastatic Colorectal Cancer. (Pubmed Central) - Jun 26, 2025
Age (18.0-82.0 years), sex, race (Asian, Black, and White), ethnicity (Hispanic vs non-Hispanic), Eastern Cooperative Oncology Group performance status score, tumor type, mild or moderate renal impairment, and mild hepatic impairment had no clinically meaningful impact on fruquintinib or M11 PK. This analysis supports the same fruquintinib starting dosage, without need for adjustments, for these patient-specific factors.
- |||||||||| Stivarga (regorafenib) / Bayer, Cabometyx (cabozantinib tablet) / Exelixis
Journal, Adverse events: Corneal Perforation as a Possible Ocular Adverse Event Caused by Cabozantinib: A Clinical Case and Brief Review. (Pubmed Central) - Jun 26, 2025
In this regard, one case of corneal perforation during treatment with a VEGFR-TKI, Regorafenib, has been reported, while there are no data about Cabozantinib...Therefore, particular importance should be placed on ophthalmologic surveillance during treatment with these drugs in patients who develop ocular symptoms. Further in vitro and in vivo studies are necessary to deepen the knowledge about VEGFR-TKI-mediated ocular AEs.
- |||||||||| Journal: A Modified FLT3 PCR Assay Using a TapeStation Readout. (Pubmed Central) - Jun 26, 2025
Given the widespread use of TapeStation instruments in molecular diagnostics laboratories as part of next-generation sequencing (NGS) workflows, this modified assay is well-suited as a companion test for rapid NGS platforms to detect larger FLT3-ITDs, which are NGS often miscalledor under-called by the NGS bioinformatics algorithms. However, it is not suitable for use as a standalone assay, as it is unable to reliably detect very short FLT3-ITDs.
- |||||||||| erlotinib / Generic mfg.
Journal, IO biomarker: Design, synthesis, and antiproliferative activity of new 5-ethylsulfonyl-indazole-3-carbohydrazides as dual EGFR/VEGFR-2 kinases inhibitors. (Pubmed Central) - Jun 25, 2025
Apoptotic markers assay results showed that increased levels of p53 and Bax proteins, along with lower levels of antiapoptotic Bcl-2, govern the apoptosis process in these new compounds. Computational analyses, encompassing molecular docking, molecular dynamics (MD) simulations, and density functional theory (DFT) computations, elucidated the binding interactions of these drugs with EGFR and VEGFR-2.
- |||||||||| FH-2001 / Fosun Pharma
Journal, PD(L)-1 Biomarker, IO biomarker: FH-2001 is a novel FGFR/VEGFR dual inhibitor with immune-modulating activity. (Pubmed Central) - Jun 24, 2025
Mechanistically, FH-2001 treatment dramatically reduced c-Myc and PD-L1 mRNA and protein levels in a dose-dependent manner in vitro. Taken together, FH-2001 is a promising dual-target inhibitor of FGFR and VEGFR and also modulates cancer immunity, while its robust antitumor activity positions it as a potentially class-leading anticancer agent.
- |||||||||| Legalon (silibinin) / Viatris
Journal: Synthesis and antitumor activity of silibinin derivatives targeting VEGFR. (Pubmed Central) - Jun 18, 2025
Their structures were confirmed by MS, 1H NMR, and 13C NMR. In vitro activity assay showed that these compounds can inhibit cell proliferation of A549 and SGC7901 cells, especially compounds I3 and I8 showed better inhibitory activity on these tumor cells, and similar to the positive control drug lapatinib, which may be potential candidate compounds for tumor therapy.
- |||||||||| Biomarker, Journal: Case Report WIN-MTB-2023001 WIN International Molecular Tumor Board A 62-year-old male with metastatic colorectal cancer with 5 prior lines of treatment. (Pubmed Central) - Jun 17, 2025
We present a 62-year-old male with mCRC harboring BRAF, MET, APC, TP53 and NRAS alterations, following FOLFOX and FOLFIRI, dabrafenib plus panitumumab, and a BRAF inhibitor clinical trial, each leading to initial responses followed by disease progression...Personalized combinations suggested included amivantamab-vmjw (anti-MET/EGFR antibody) (one-third standard dose) (for MET amplification and due to prior response to anti-EGFR antibody), trametinib, 1 mg po daily (MEK inhibitor for BRAF V600E mutation), and regorafenib (may have WNT inhibitor activity relevant to APC mutation; VEGFR activity relevant since TP53 alterations upregulate VEGF/VEGFR axis) starting at 40 mg po daily three weeks on, one week off. Another option was trametinib at 1 mg daily, cetuximab (EGFR antibody), 250 mg/m
- |||||||||| Journal: Single-Cell RNA Sequencing Reveals Macrophage-Endothelial Cell Crosstalk in Viral Myocarditis. (Pubmed Central) - Jun 17, 2025
Moreover, inhibition of VEGFR exacerbated cardiac dysfunction, highlighting the protective role of angiogenesis in myocarditis progression. In summary, these results elucidated a cardioprotective role of macrophage-driven angiogenesis via vascular endothelial growth factor signaling during viral myocarditis, providing new insights into therapeutic strategies for inflammatory heart diseases.
- |||||||||| Unveiling the impact of VEGFR2/KDR modulation on pulmonary microvascular endothelial cells in COPD/emphysema (PS-6; Board Number: 14) - Jun 11, 2025 - Abstract #ERS2025ERS_1187;
10q thus might be an efficient and potent FLT3 inhibitor with the capacity for overcoming multiple FLT3 mutations. VEGFR2 signaling via pY1175-VEGFR2/ERK is crucial for endothelial integrity, affecting cell morphology and barrier function through integrin ?3, underscoring VEGFR2's significance in MVEC structure and pointing to its therapeutic potential in COPD/emphysema.
- |||||||||| Journal: Epigollatecatechin gallate alleviates rheumatoid arthritis through PI3K-Akt pathway by inhibiting FLT1. (Pubmed Central) - Jun 9, 2025
However, optimizing the ADMET profile through structural modifications and nanocarrier delivery, along with in vivo and in vitro experimental validation, will enhance its therapeutic potential. EGCG, a key component of ELP, has significant therapeutic effects on RA by suppressing the PI3K/AKT signaling pathway and downregulating FLT1 gene expression, thereby exhibiting anti-inflammatory effects.
- |||||||||| Venclexta (venetoclax) / Roche, AbbVie, cytarabine / Generic mfg.
Review, Journal: SOHO State of the Art Updates and Next Questions Acute Myeloid Leukemia: Current Status and Next Questions. (Pubmed Central) - Jun 8, 2025
Allogeneic stem cell transplant is the most effective treatment for residual leukemia in resistant AML but is limited by toxicity and donor availability. Immune-based strategies, including antibodies and bispecific molecules, show promise in early trials, and safer cellular therapies could expand treatment options.
- |||||||||| Journal: DLL4/VEGF bispecific molecularly imprinted nanomissile for robust tumor therapy. (Pubmed Central) - Jun 5, 2025
This study pioneers the construction of the first bsMINM with inherent, enhanced anti-angiogenic effects achieved through dual blockades. The platform's bispecific recognition capability opens a new avenue for tumor treatment and shows significant promise in addressing issues caused by signaling pathway compensation.
- |||||||||| tivozanib eye drops (KHK4951) / Kyowa Kirin
Trial completion date, Trial primary completion date: Study to Assess the Efficacy & Safety of KHK4951 in Patients With Neovascular Age-Related Macular Degeneration (clinicaltrials.gov) - Jun 5, 2025
P2, N=180, Recruiting,
The platform's bispecific recognition capability opens a new avenue for tumor treatment and shows significant promise in addressing issues caused by signaling pathway compensation. Trial completion date: Dec 2025 --> Sep 2026 | Trial primary completion date: Nov 2025 --> Aug 2026
- |||||||||| tivozanib eye drops (KHK4951) / Kyowa Kirin
Trial completion date, Trial primary completion date: Study to Assess the Efficacy & Safety of KHK4951 in Patients With Diabetic Macular Edema (clinicaltrials.gov) - Jun 5, 2025
P2, N=150, Recruiting,
Trial completion date: Dec 2025 --> Sep 2026 | Trial primary completion date: Nov 2025 --> Aug 2026 Trial completion date: Dec 2025 --> Sep 2026 | Trial primary completion date: Nov 2025 --> Aug 2026
- |||||||||| Xpovio (selinexor) / Karyopharm
Review, Journal: Selinexor in acute myeloid leukemia: therapeutic applications and current challenges. (Pubmed Central) - Jun 4, 2025
Although selinexor has shown potential, its resistance and adverse reactions still need further research and control. Future research directions include exploring the best medication schemes, clarifying the appropriate population, and developing new combination treatment plans to improve treatment effects and overcome drug resistance issues.
- |||||||||| sunitinib / Generic mfg.
Journal: Design, synthesis, molecular modeling, and antiproliferative evaluation of new 2-oxoindolin-3-ylidene thiazole derivatives. (Pubmed Central) - Jun 4, 2025
A series of novel 2-oxoindolin-3-ylidene thiazole derivatives were designed and synthesized, inspired by the pharmacophoric features of the VEGFR-2 inhibitor sunitinib...Molecular docking studies confirmed strong binding interactions within the VEGFR-2 active site, while in silico ADME and DFT analyses supported favourable pharmacokinetic properties and reactivity. These findings position compound 4c as a promising lead for the development of anticancer agents.
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