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A tyrosine kinase inhibitor (TKI) is a pharmaceutical drug that inhibits tyrosine kinases. Tyrosine kinases are enzymes responsible for the activation of many proteins by signal transduction cascades. The proteins are activated by adding a phosphate group to the protein (phosphorylation), a step that TKIs inhibit. TKIs are typically used as ...
Tyrosine kinase activity in the nucleus involves cell-cycle control and properties of transcription factors. [3] In this way, in fact, tyrosine kinase activity is involved in mitogenesis, or the induction of mitosis in a cell; proteins in the cytosol and proteins in the nucleus are phosphorylated at tyrosine residues during this process. [3]
It is not safe for use during pregnancy. [8] Nilotinib is a Bcr-Abl tyrosine kinase inhibitor and works by interfering with signalling within the cancer cell. [3] [8] Nilotinib was approved for medical use in the United States in 2007. [3] [8] It is on the World Health Organization's List of Essential Medicines. [9] It is approved as a generic ...
Bosutinib, sold under the brand name Bosulif, is a small molecule BCR-ABL and src tyrosine kinase inhibitor used for the treatment of chronic myelogenous leukemia. [2] Originally synthesized by Wyeth, it is being developed by Pfizer. [citation needed]
ALK inhibitors are anti-cancer drugs that act on tumours with variations of anaplastic lymphoma kinase (ALK) such as an EML4-ALK translocation. [1] They fall under the category of tyrosine kinase inhibitors , which work by inhibiting proteins involved in the abnormal growth of tumour cells.
Pazopanib, sold under the brand name Votrient, is an anti-cancer medication marketed worldwide by Novartis.It is a potent and selective multi-targeted receptor tyrosine kinase inhibitor that blocks tumour growth and inhibits angiogenesis.
It is a multi-targeted tyrosine-kinase inhibitor. [5] Some forms of chronic myeloid leukemia, those that have the T315I mutation, are resistant to current therapies such as imatinib. Ponatinib has been designed to be effective against these types of tumors. [6] Ponatinib was approved for medical use in the United States in December 2012. [7]
Remibrutinib is a small molecule drug that acts as a Bruton's tyrosine kinase (BTK) inhibitor. It is in development for the treatment of chronic spontaneous urticaria. [1] [2] In November 2023, Novartis announced that the compound "demonstrated clinically meaningful and statistically significant reduction in urticaria activity vs placebo" in a Phase III trial.