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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.
Sorafenib is a small molecule inhibitor of many tyrosine kinase receptors such as VEGFR-2. Side effects are in most cases mild to moderate such as rash, hand-foot skin reaction, diarrhea and dermatitis, and occur in about 33-38% patients using sorafenib. Other side effects are mild hypertension, leukopenia and bleeding. Uncommon side effects ...
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 ...
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.
Osimertinib, sold under the brand name Tagrisso, [6] is a medication used to treat non-small-cell lung carcinomas with specific mutations. [7] [8] It is a third-generation epidermal growth factor receptor tyrosine kinase inhibitor.
Entrectinib, sold under the brand name Rozlytrek, is an anti-cancer medication used to treat ROS1-positive non-small cell lung cancer and NTRK fusion-positive solid tumors. [5] It is a selective tyrosine kinase inhibitor (TKI), of the tropomyosin receptor kinases (TRK) A, B and C, C-ros oncogene 1 and anaplastic lymphoma kinase (ALK). [5]
This is strong motivation to perform research on tyrosine kinase inhibitors as potential targets in cancer treatment. Gefitinib, functioning as an epidermal growth factor receptor tyrosine kinase inhibitor, improved symptoms related to non-small cell lung cancer and resulted in radiographic tumor regressions. [15]
Regorafenib, sold under the brand name Stivarga among others, is an oral multi-kinase inhibitor developed by Bayer which targets angiogenic, stromal and oncogenic receptor tyrosine kinase (RTK). Regorafenib shows anti- angiogenic activity due to its dual targeted VEGFR2-TIE2 tyrosine kinase inhibition.