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Lapatinib , used in the form of lapatinib ditosylate (trade names Tykerb and Tyverb marketed by Novartis) is an orally active drug for breast cancer and other solid tumours. [3] It is a dual tyrosine kinase inhibitor which interrupts the HER2/neu and epidermal growth factor receptor (EGFR) pathways. [4]
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 ...
HER2-positive breast cancer, gastric cancer, pancreatic cancer (orphan) and gastro-oesophageal junction cancer. Cardiac dysfunction, infusion-related reactions, peripheral neuropathy and pulmonary toxicity (rare). 2.2 Tyrosine kinase inhibitor: Afatinib: PO: EGFR, HER2 and HER4 inhibitor. Non-small cell lung cancer.
Intedanib is a multiple tyrosine kinase inhibitor and is the first drug to treat idiopathic pulmonary fibrosis. [4] Indol derivatives with 1-NH of 2-indolinone motif that is an H-bond donor, and 2-carbonyl oxygen that acts as an H-bond acceptor, bind with Glu915 and Cys917, respectively.
Neratinib (), sold under the brand name Nerlynx, is a tyrosine kinase inhibitor anti-cancer medication used for the treatment of breast cancer. [3] [4]The most common side effect is diarrhea, which affects nearly all patients. [4]
Bcr-Abl tyrosine-kinase inhibitors (TKI) are the first-line therapy for most patients with chronic myelogenous leukemia (CML). More than 90% of CML cases are caused by a chromosomal abnormality that results in the formation of a so-called Philadelphia chromosome .
Tucatinib is a kinase inhibitor indicated in combination with trastuzumab and capecitabine for the treatment of adults with advanced unresectable or metastatic HER2-positive breast cancer, including those with brain metastases, who have received one or more prior anti-HER2-based regimens in the metastatic setting. [3]
Axitinib, sold under the brand name Inlyta, is a small molecule tyrosine kinase inhibitor developed by Pfizer.It has been shown to significantly inhibit growth of breast cancer in animal models [4] and has shown partial responses in clinical trials with renal cell carcinoma (RCC) [5] and several other tumour types.
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