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Where is pemetinib produced? Pemetinib was developed by Incyte, and Pemazyre belongs to a class of drugs called kinase inhibitors. It works by blocking the action of abnormal proteins that signal cancer cells to multiply. This helps to stop or slow the spread of cancer cells and is suitable for: cholangiocarcinoma that has metastasized (spread to other parts of the body) or is locally advanced and cannot be treated with surgery, and for the treatment of cholangiocarcinoma patients with FGFR2 gene fusions or other changes in the structure of the FGFR2 gene.
Pemetinib is a small molecule kinase inhibitor targeting FGFR1, 2 and 3 with an IC50 value of less than 2nM. Pemetinib also inhibits FGFR4 in vitro at approximately 100-fold higher concentrations than FGFR1, 2, and 3. Pemetinib leads to constitutive activation of FGFR by activating FGFR amplification and fusion, thereby inhibiting FGFR1-3 phosphorylation and signaling and reducing cell viability.
Constitutive FGFR signaling can support the proliferation and survival of malignant cells. Pemetinib exhibits antitumor activity in mouse xenograft models of human tumors with alterations in FGFR1, FGFR2, or FGFR3, resulting in constitutive FGFR activation, including cholangiocarcinoma xenograft models in patients expressing oncogenic FGFR2-Transformer-2 beta homolog (TRA2b) fusion proteins.
The recommended dose of pemetinib is 13.5 mg orally daily for 14 days, followed by 7 days off in a 21-day cycle. Continue treatment until disease progression or unacceptable toxicity. Swallow the tablets whole, with or without food. Common side effects are diarrhea, nausea, change in taste, vomiting, loss of appetite, weight loss, constipation, stomach pain, mouth sores, dry mouth and/or dry skin; decreased urine output; or rapid heartbeat. Nailitis, hair loss, headache, fatigue, joint pain, painful urination, swelling and pain in limbs or joints. Blurred vision, eye floaters, seeing flashes of light or other vision changes, muscle cramps, numbness, or dry mouth.
Note: The above information comes from the Internet and is compiled and edited by Medical Companion Travel (please correct me if there are any errors or omissions). It is only to provide information on the latest drugs on the market in the world and help Chinese patients understand the latest international new drug trends. It is only for internal discussion among medical staff and does not serve as any basis for medication. For specific medication guidelines, please consult the attending physician.
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