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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 ...
Sorafenib, sold under the brand name Nexavar, [3] is a kinase inhibitor drug approved for the treatment of primary kidney cancer (advanced renal cell carcinoma), advanced primary liver cancer (hepatocellular carcinoma), FLT3-ITD positive AML and radioactive iodine resistant advanced thyroid carcinoma.
Other serious side effects may include QT prolongation, sudden death, pancreatitis, and liver problems. [8] 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.
It is an oral VEGF receptor tyrosine kinase inhibitor. [3] The most common side effects include fatigue (tiredness), hypertension (high blood pressure), diarrhea, decreased appetite, nausea, dysphonia (voice changes), hypothyroidism, cough, and stomatitis. [4] [3] [5]
Like many small molecule tyrosine kinase inhibitors, lapatinib is regarded as well tolerated. The most common side effects reported are diarrhea, fatigue, nausea and rashes. [4] [15] Of note, lapatinib related rash is associated with improved outcome. [16] In clinical studies elevated liver enzymes have been reported.
Repotrectinib is an inhibitor of proto-oncogene tyrosine-protein kinase ROS1 (ROS1) and of the tropomyosin receptor tyrosine kinases (TRKs) TRKA, TRKB, and TRKC. [1] The most common adverse reactions include dizziness, dysgeusia, peripheral neuropathy, constipation, dyspnea, ataxia, fatigue, cognitive disorders, and muscular weakness. [2]
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.
Ibrutinib is a potent, irreversible inhibitor of Bruton's tyrosine kinase (BTK). The acrylamide group of ibrutinib forms a covalent bond with the cysteine residue C481 in the BTK active site, leading to sustained inhibition of BTK enzymatic activity. BTK is an important signalling molecule of the B-cell antigen receptor (BCR) pathway, which ...
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