Tyrosine Kinase Inhibitors (TKI)
The success of Gleevec in the treatment of early CML led us and others to hope (rather naively) that our pioneering work on EGFR and Bcr-Abl kinase inhibitors, would set the foundation for the cure of other cancers - Alexander Levitzk
HWN Suggests
Kinase drug discovery 20 years after imatinib: progress and future directions
Protein kinases regulate nearly all aspects of cell life, and alterations in their expression, or mutations in their genes, cause cancer and other diseases. Here, we review the remarkable progress made over the past 20 years in improving the potency and specificity of small-molecule inhibitors of protein and lipid kinases, resulting in the approval of more than 70 new drugs since imatinib was approved in 2001. These compounds have had a significant impact on the way in which we now treat cancers and non-cancerous conditions. We discuss how the challenge of drug resistance to kinase inhibitors is being met and the future of kinase drug discovery.
Articles of Interest
Targeted Therapy with Tyrosine Kinase Inhibitors
Tyrosine kinases are a family of proteins that contribute to the development of cancer. Anticancer drug development has recently taken aim at these receptors. The tyrosine kinase inhibitors (TKIs) are a class of small-molecule, orally administered agents with a unique mechanism of action. Since these drugs are administered orally, they can be dispensed in any practice setting. The purpose of this article is to provide an overview of TKIs and review important considerations for dispensing these agents.
Emerging Importance of Tyrosine Kinase Inhibitors against Cancer: Quo Vadis to Cure?
Receptor tyrosine kinases (RTKs) are crucial intermediaries of the several cellular pathways and carcinogenesis that directly affect the prognosis and survival of higher tumor grade patients. Tyrosine kinase inhibitors (TKIs) are efficacious drugs for targeted therapy of various cancers. Therefore, RTKs have become a promising therapeutic target to cure cancer.
Role of Tyrosine Kinase Inhibitors in Cancer Therapy
Cancer chemotherapy has been one of the major medical advances in the last few decades. However, the drugs used for this therapy have a narrow therapeutic index, and often the responses produced are only just palliative as well as unpredictable. In contrast, targeted therapy that has been introduced in recent years is directed against cancer-specific molecules and signaling pathways and thus has more limited nonspecific toxicities. Tyrosine kinases are an especially important target because they play an important role in the modulation of growth factor signaling.
Smart drugs: Tyrosine kinase inhibitors in cancer therapy
Cancer therapy directed at specific, frequently occurring molecular alterations in signaling pathways of cancer cells has been validated through the clinical development and regulatory approval of agents such as Herceptin for the treatment of advanced breast cancer and Gleevec for chronic myelogenous leukemia and gastrointestinal stromal tumors. While most novel, target-directed cancer drugs have pregenomic origins, one can anticipate a postgenomic wave of sophisticated “smart drugs” to fundamentally change the treatment of all cancers.
Tyrosine kinase inhibitor Therapy
Tyrosine kinase inhibitors (TKIs) are a type of targeted therapy. TKIs come as pills, taken orally. A targeted therapy identifies and attacks specific types of cancer cells while causing less damage to normal cells. In CML, TKIs target the abnormal BCR::ABL1 protein that causes uncontrolled CML cell growth and block its function, causing the CML cells to die.
Tyrosine kinase inhibitors (TKI) for chronic myeloid leukaemia (CML)
The main treatment for chronic myeloid leukaemia (CML) is with drugs called tyrosine kinase inhibitors (TKIs). TKIs are a type of targeted therapy. They work by switching off (inhibiting) the tyrosine kinase that is made by the BCR-ABL1 gene in the leukaemia cells. This stops or slows the bone marrow from making abnormal white blood cells. It also allows the leukaemia cells to mature and die..
Tyrosine Kinase Inhibitors in Cancer: Breakthrough and Challenges of Targeted Therapy
To conclude, the best achievement of RTKIs in cancer treatment concerns chronic myeloid leukemia (CML), since the survival rate of patients treated with imatinib at 10 years is 83.3%. There are some evolutionary explanations to CML exception.
Resources
StatPearls
Tyrosine kinase inhibitors (TKI) are a group of pharmacologic agents that disrupt the signal transduction pathways of protein kinases by several modes of inhibition.
