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DRUG CLASS:

Tyrosine kinase inhibitor

1m
New P2 trial
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EGFR (Epidermal growth factor receptor)
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Zynyz (retifanlimab-dlwr) • zanzalintinib (XL092)
1m
NAPOLEON: Zanzalintinib in Men With Aggressive Variant Prostate Cancer (clinicaltrials.gov)
P2, N=30, Not yet recruiting, Deepak Kilari | Trial completion date: Dec 2027 --> Jul 2029 | Trial primary completion date: Dec 2026 --> Jul 2028
Trial completion date • Trial primary completion date
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CHGA (Chromogranin A)
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zanzalintinib (XL092)
1m
Zanzalintinib in Combination With Ipilimumab and Nivolumab in Patients With Metastatic Soft Tissue Sarcoma (clinicaltrials.gov)
P1, N=18, Recruiting, Washington University School of Medicine | Trial completion date: Jul 2031 --> Jan 2034 | Trial primary completion date: Aug 2026 --> Feb 2029
Trial completion date • Trial primary completion date
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Opdivo (nivolumab) • Yervoy (ipilimumab) • zanzalintinib (XL092)
2ms
Multiple binding modes of the tyrosine kinase inhibitor dovitinib to fibroblast growth factor receptor 1 characterized by surface plasmon resonance, 19F-NMR, and molecular dynamics simulations. (PubMed, J Biochem)
Furthermore, MD simulations introducing an additional dovitinib molecule to the FGFR1-dovitinib complex indicated the potential for weak and transient interactions in the preferred interaction regions on the FGFR1 surface. These findings highlight the multifaceted nature of kinase-inhibitor interactions and provide valuable biophysical insights that may contribute to future drug discovery efforts targeting receptor tyrosine kinases.
Journal
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FGFR1 (Fibroblast growth factor receptor 1)
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dovitinib (TKI258)
2ms
Enrollment change
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zanzalintinib (XL092)
2ms
Assessment of CD26+ Leukemic Stem Cells in Tunisian Patients with Chronic Myeloid Leukemia in the Era of Tyrosine Kinase Inhibitor Therapy. (PubMed, Indian J Hematol Blood Transfus)
CD26 + LSCs can be a useful marker in follow up of patients with CML. Despite promising findings, the limited sample size highlight the need for larger, prospective studies to validate these results and assess the predictive value of CD26 + LSCs for TKI discontinuation strategies.
Journal • IO biomarker
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ABL1 (ABL proto-oncogene 1) • BCR (BCR Activator Of RhoGEF And GTPase) • CD38 (CD38 Molecule) • CD34 (CD34 molecule) • PTPRC (Protein Tyrosine Phosphatase Receptor Type C) • DPP4 (Dipeptidyl Peptidase 4)
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PTPRC expression
2ms
Quantitation of Tucatinib, a Novel Tyrosine Kinase Inhibitor in Dried Blood Spot (DBS) With LC-ESI-MS/MS: Application to a Pharmacokinetic Study in Mice. (PubMed, Biomed Chromatogr)
This research aimed to create and validate a new rapid, sensitive, and specific LC-MS/MS technique for measuring tucatinib in dried blood spots (DBS) from mice, with afatinib serving as an internal standard (IS) following regulatory guidelines in the linearity range from 0.178 to 1009 ng/mL (r > 0.990). Tucatinib remained stable under various storage conditions. Comparison of DBS versus plasma samples concentrations showed a strong correlation, suggesting that DBS can serve as a valid alternative to plasma for pharmacokinetic evaluation.
PK/PD data • Preclinical • Journal
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HER-2 (Human epidermal growth factor receptor 2)
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HER-2 positive
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Gilotrif (afatinib) • Tukysa (tucatinib)
2ms
Enrollment change • Trial completion date
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zanzalintinib (XL092)
2ms
Attenuation of ABCG2-dependent drug efflux by befotertinib restores chemosensitivity in multidrug-resistant non-small cell lung cancer cells. (PubMed, Biomed Pharmacother)
Through this mechanism, befotertinib acts as a functional inhibitor of ABCG2, restoring intracellular drug accumulation and enhancing cytotoxic responses. Collectively, these findings indicate that befotertinib may serve as a chemosensitizing agent to overcome MDR in NSCLC with high ABCG2 expression, supporting further evaluation in combination therapeutic strategies.
Journal
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EGFR (Epidermal growth factor receptor) • ABCG2 (ATP Binding Cassette Subfamily G Member 2)
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Semena (befotertinib)
2ms
Pigmentary Changes Reported with Tyrosine Kinase Inhibitors: A Narrative Review of Mechanisms and Clinical Implications. (PubMed, Clin Drug Investig)
Larger multicenter studies, functional experimental models, and pharmacogenetic investigations are needed to elucidate predictive factors, clarify molecular mechanisms, and develop preventive or therapeutic strategies. Understanding these pigmentary changes may also provide valuable insights into drug activity and pave the way toward personalized medicine.
Review • Journal
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MITF (Melanocyte Inducing Transcription Factor)