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18d
Medicinal chemistry perspective on quinazoline derivatives: Sustainable synthetic routes, anticancer evaluation, and SAR analysis. (PubMed, Eur J Med Chem)
FDA-approved drugs like Gefitinib, Erlotinib, Afatinib, Dacomitinib, and Vandetanib validate the therapeutic significance of the quinazoline framework in modulating different cancer pathways. Structure activity relationship (SAR) analyses reveal that adding halogen, methoxy, or heteroaryl groups at specific ring positions enhance kinase affinity and cytotoxic efficacy. Overall, this review highlights recent progress linking synthetic design, molecular docking, and biological response, establishing quinazoline derivatives as promising multitargeted scaffolds for the design of next-generation anticancer agents.
Review • Journal
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EGFR (Epidermal growth factor receptor) • HER-2 (Human epidermal growth factor receptor 2) • BRAF (B-raf proto-oncogene) • PARP1 (Poly(ADP-Ribose) Polymerase 1)
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erlotinib • Gilotrif (afatinib) • gefitinib • Vizimpro (dacomitinib) • Caprelsa (vandetanib)
21d
Can We Develop Glioma Subtype-Specific Precision Medicines? An Integrative Machine Learning Pipeline for Biomarker Discovery and Drug Repurposing for Glioblastoma and Low-Grade Glioma. (PubMed, OMICS)
Repurposed drug candidates were then predicted via signature-based prioritization and evaluated using molecular docking simulations, revealing six promising compounds for GBM (vandetanib, capecitabine, melatonin, agomelatine, ramelteon, and tasimelteon) and one for LGG (ambroxol). This study demonstrates the utility of combining class-balancing, feature selection, and drug repurposing pipelines to uncover clinically relevant glioma biomarkers and therapeutic candidates, thus providing a computational foundation for future experimental and translational validation in these brain cancers and neuro-oncology.
Journal
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ANK3 (Ankyrin 3)
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capecitabine • Caprelsa (vandetanib)
21d
A phase 2 study of GI-6207 in patients with recurrent medullary thyroid cancer. (PubMed, Oncologist)
The immunotherapy was well tolerated, but did not have an impact on tumor growth rate at 6 months as measured by calcitonin kinetics.
P2 data • Journal
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CEACAM5 (CEA Cell Adhesion Molecule 5) • CD4 (CD4 Molecule)
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Cabometyx (cabozantinib tablet) • Retevmo (selpercatinib) • Caprelsa (vandetanib) • GI-6207
21d
Cutaneous Adverse Events of Tyrosine Kinase Inhibitors in Endocrine Tumors: Clinical Features, Mechanisms, and Management Strategies. (PubMed, Biomedicines)
Grade-based algorithms combining topical corticosteroids/antibiotics, dose interruptions or reductions, and short systemic courses (e.g., doxycycline, antihistamines) enable symptom control while maintaining anticancer intensity... Dermatologic toxicities are predictable, mechanism-linked, and manageable with proactive, multidisciplinary care. Standardized prevention and treatment pathways tailored to specific TKIs-particularly lenvatinib, vandetanib, and cabozantinib-can preserve dose intensity, optimize quality of life, and sustain antineoplastic efficacy.
Review • Journal • Adverse events
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RET (Ret Proto-Oncogene)
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Lenvima (lenvatinib) • Cabometyx (cabozantinib tablet) • Caprelsa (vandetanib)
29d
Single-Cell Multi-Omics Reveals B2M-Mediated Myeloid Reprogramming and Constructs a Predictive Model for Early Hepatocellular Carcinoma Recurrence. (PubMed, FASEB J)
Drug sensitivity analyses further suggested that vandetanib may have the potential to inhibit recurrence by targeting B2M-related pathways. These findings provide evidence that B2M may contribute to remodeling of the immune microenvironment in recurrent HCC. Our integrative single-cell multi-omics approach highlights a possible mechanism of early recurrence and offers a preliminary predictive tool with therapeutic implications.
Journal
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PD-L1 (Programmed death ligand 1) • IFNG (Interferon, gamma) • B2M (Beta-2-microglobulin) • CASP3 (Caspase 3) • GAS6 (Growth arrest specific 6) • CDK1 (Cyclin-dependent kinase 1)
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Caprelsa (vandetanib)
2ms
Selpercatinib plus cemiplimab in RET positive medullary thyroid cancer patient with skin cancers. (PubMed, Tumori)
The combination of selpercatinib and cemiplimab was possible, with no new safety signals observed.
Journal • PD(L)-1 Biomarker
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RET (Ret Proto-Oncogene)
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RET mutation • RET positive
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Retevmo (selpercatinib) • Libtayo (cemiplimab-rwlc) • Caprelsa (vandetanib)
3ms
Vandetanib and Everolimus in Treating Patients With Advanced or Metastatic Cancer (clinicaltrials.gov)
P1, N=151, Completed, M.D. Anderson Cancer Center | Active, not recruiting --> Completed | Trial completion date: May 2026 --> Oct 2025 | Trial primary completion date: May 2026 --> Oct 2025
Trial completion • Trial completion date • Trial primary completion date
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everolimus • Caprelsa (vandetanib)
3ms
Vascular endothelial cells and angiogenesis. (PubMed, Pharmacol Res)
Ponatinib, regorafenib, and vandetanib are FDA-approved VEGFR, Tie2, and Ephrin receptor blockers used in the treatment of various malignancies. Other disorders characterized by aberrant angiogenesis include diabetic retinopathies and neovascular age-related macular degeneration.
Review • Journal
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MET (MET proto-oncogene, receptor tyrosine kinase) • HGF (Hepatocyte growth factor) • FLT1 (Fms-related tyrosine kinase 1) • NRP1 (Neuropilin 1) • EFNA1 (Ephrin A1)
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Iclusig (ponatinib) • Stivarga (regorafenib) • Caprelsa (vandetanib)
4ms
Design, synthesis, anticancer evaluation, biological screening, and computational study of novel 6,7-dimethoxyquinazoline derivatives as VEGFR-2 inhibitors and apoptotic inducers. (PubMed, Eur J Med Chem)
Moreover, the MTT viability test for compounds 9a, 9b, and 9c demonstrated less cytotoxicity against normal fibroblast cells (WI38), revealing enhanced safety profiles with IC50 values of 28.04, 219.79, and 43.77 μM, respectively, compared to Sorafenib (IC50 = 26 μM). Enzyme inhibition assays revealed that compounds 9a-c effectively inhibited EGFR and VEGFR-2, confirming the multi-targeting potential of this series of compounds.
Journal
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EGFR (Epidermal growth factor receptor) • BCL2 (B-cell CLL/lymphoma 2) • KDR (Kinase insert domain receptor) • CASP3 (Caspase 3)
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sorafenib • Caprelsa (vandetanib) • Fruzaqla (fruquintinib)
4ms
DFT Structural and UV-Vis Spectral Insights into Photosensitivity of Vandetanib: A Dual EGFR/SARS-CoV-2 Mpro Inhibitor. (PubMed, Pharmaceuticals (Basel))
This study provides molecular-level insights into the structural and photophysical origins of vandetanib's photosensitivity. The findings improve understanding of its adverse effects and can inform the safer design of EGFR-targeting drugs with reduced phototoxic risks.
Journal
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EGFR (Epidermal growth factor receptor)
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Caprelsa (vandetanib)
4ms
Thyroid cancer: From molecular insights to therapy (Review). (PubMed, Oncol Lett)
Molecularly targeted therapies constitute the cornerstone of current strategies, with vemurafenib inhibiting BRAF/MEK in PTC, sorafenib acting as a multikinase suppressor in FTC, vandetanib blocking RET in MTC and berberine-doxorubicin combinations overcoming chemoresistance in ATC. Metabolic interventions, including metformin for glucose modulation in PTC and novel delivery systems such as micelle-encapsulated AB3 for MTC, demonstrate translational potential. The present review summarizes molecular mechanisms, diagnostic tools and emerging therapies while emphasizing the necessity of subtype-specific approaches to improve clinical outcomes in thyroid oncology.
Review • Journal • PD(L)-1 Biomarker • IO biomarker
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PD-L1 (Programmed death ligand 1) • BRAF (B-raf proto-oncogene) • TP53 (Tumor protein P53) • RET (Ret Proto-Oncogene) • TERT (Telomerase Reverse Transcriptase) • PD-1 (Programmed cell death 1) • MALAT1 (Metastasis associated lung adenocarcinoma transcript 1) • CREB3L1 (CAMP Responsive Element Binding Protein 3 Like 1) • STC1 (Stanniocalcin 1) • STMN1 (Stathmin 1)
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TP53 mutation • BRAF V600E • BRAF V600 • RAS mutation
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Zelboraf (vemurafenib) • sorafenib • doxorubicin hydrochloride • Caprelsa (vandetanib) • metformin
4ms
A real-world pharmacovigilance assessment of drug-related carcinoembryonic antigen increase. (PubMed, Medicine (Baltimore))
And dacomitinib, regorafenib, fruquintinib, vandetanib, and panitumumab were the top 5 drugs with high risk. Non-antitumor drugs were all moderate risk, involving atorvastatin, zoledronic acid, amiodarone hydrochloride, lithium, and teduglutide...The number of related adverse event reports increased year by year. The results of this study provided the relevant basis for pharmacovigilance, and provided the basis for strengthening drug safety and making correct drug decision in clinical practice.
Journal • Adverse events • Real-world evidence
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CEACAM5 (CEA Cell Adhesion Molecule 5)
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Vectibix (panitumumab) • Stivarga (regorafenib) • Vizimpro (dacomitinib) • Caprelsa (vandetanib) • Fruzaqla (fruquintinib) • zoledronic acid • atorvastatin