In this chapter, we discuss the new tyrosine kinase inhibitors that inhibit more than only HER-2 and discuss some ongoing clinical trials in this area. In so doing, we hope to provide information for overcoming tyrosine kinase drug resistance and to identify the ideal settings for these ...
TKIs can competitively bind to the kinase structural domains to prevent downstream pathway activation and inhibit tumor growth. Kinase inhibitors, including TKIs, are often classified
Inhibition of mutant FLT3 receptors in leukemia cells by the small molecule tyrosine kinase inhibitor PKC412. Cancer Cell 2002; 1: 433–443. 61 Chu SH, Small D. Mechanisms of resistance to FLT3 inhibitors. Drug Resist Updat 2009; 12: 8–16. This work is licensed under a Creative Commons ...
In AML, the main TKs mutations are produced in Fms-like tyrosine kinase 3 (FLT3), KIT and Janus kinase (JAK) genes, and with less frequency in BCR-ABL. The striking results with TK Inhibitors (TKIs) therapy in BCR-ABL1 chronic myeloid leukemias has paved the way for its clinical ...
Protein kinase inhibitors: the tyrosine specific protein kinases. Pharmacol Ther 1998; 77(2): 81–114 PubMed CAS Google Scholar Shawver L. Tyrosine kinase inhibitors: from the emergence of targets to their clinical development. In: Perry MC, editor. American Society of Clinical Oncology ...
KIT tyrosine kinase inhibitors have been approved for advanced SM, and avapritinib has also been recently approved as the first such inhibitor for indolent systemic mastocytosis. Other TKIs are currently in clinical trials for patients with non-advanced SM who have persistent and severe symptoms ...
Bruton tyrosine kinase inhibitors (BTKi) have transformed the treatment of B-cell malignancies, but intolerance has often led to their discontinuation. The phase I/II BRUIN study evaluated pirtobrutinib, a highly selective non-covalent (reversible) BTKi, in patients with relapsed / refractory B-...
AM PDX models had variable responses to rationally selected non-FGFR/VEGFR kinase inhibitors In parallel with the RTK inhibitor drug study, several other narrow-spectrum kinase or enzyme inhibitors were screened with small PDX tumor cohorts based on promising literature findings. Figure S3 shows all ...
Background BCR::ABL1-positive patients with chronic myeloid leukemia (CML) are treated with tyrosine kinase inhibitors (TKIs) to reduce the transcript copy-number, achieving a major molecular response (MMR). However, genetic alterations in ABL1 and other genes may be associated with resistance, ...
Imatinib, one of the first tyrosine kinase inhibitors (TKIs) to be approved, revolutionized the treatment of chronic myelogenous leukaemia. Other compounds with different spectra of kinase inhibition are currently used to treat renal cell carcinoma, non-small-cell lung cancer and colon cancer. More ...