Axitinib: Mechanism, Applications, and Stability in Targeted Cancer Therapy
Nov 18,2024
Introduce
Axitinib is a multi-target small molecule inhibitor, mainly targeting VEGFR, Kit, PDGFR, and RET. The currently approved indication for marketing is second-line treatment for advanced renal cell carcinoma, which means that Axitinib can be chosen for the treatment of advanced renal cell carcinoma after the failure of Sotan treatment. In addition to kidney cancer, this drug has also been tried by patients for solid tumors such as liver cancer, sarcoma, and neuroendocrine tumors, which are recognized to be sensitive to anti-angiogenic drugs and have abundant tumor blood supply. It also has certain therapeutic effects.
Figure 1 Characteristics of Axitinib
Indication
Axitinib is a multi-target small molecule inhibitor, mainly targeting VEGFR, Kit, and PDGFR (multi-target, anti-angiogenic small molecule inhibitors, with some also inhibiting MET, such as cabozantinib). The currently approved indication for marketing is second-line treatment for advanced renal cell carcinoma, which means that Axitinib can be chosen for the treatment of advanced renal cell carcinoma after the failure of Sotan treatment. In addition to kidney cancer, this drug has also been tried by patients for solid tumors such as liver cancer, sarcoma, and neuroendocrine tumors, which are recognized to be sensitive to anti-angiogenic drugs and have abundant tumor blood supply. It also has certain therapeutic effects.
The role of Axitinib
1. The angiogenesis inhibitory effect of Axitinib
Axitinib, as a targeted angiogenesis inhibitor, blocks the interaction between tumor cells and vascular endothelial cells by inhibiting some important signaling pathways, such as the vascular endothelial growth factor receptor (VEGFR) signaling pathway. This mechanism prevents tumor cells from obtaining sufficient blood supply and nutrients, thereby reducing the growth rate of tumors.
2. The therapeutic effect of Axitinib on renal cancer
Axitinib is widely used in the treatment of advanced or metastatic renal cell carcinoma. Clinical trials have shown that the use of Axitinib can prolong patient survival and reduce the risk of tumor progression. Compared with traditional chemotherapy drugs, Axitinib has fewer toxic side effects and better tolerability, making it an important treatment option for kidney cancer patients.
3. Treatment strategy and dosage of Axitinib
Axitinib is generally recommended to be taken after meals and taken according to the doctor's guidance. The general starting dose is 4-5 milligrams orally per day, and the dose can be gradually increased according to the patient's tolerance and efficacy. However, it should be noted that the dosage should not be changed Axitinib should not be discontinued on its own, and adjustments must be made under the guidance of a doctor.
Usage and dosage
Only doctors with experience in tumor treatment can use Axitinib for treatment. (1) The starting dose is 5mg orally twice a day. Axitinib instructions can adjust the dosage based on individual safety and tolerability. (2) Administer the INLYTA dose approximately every 12 hours. (3) INLYTA should be swallowed whole with a glass of water. (4) If a strong CYP3A4/5 inhibitor is required, Axitinib will be priced at a reduced dose of INLYTA by approximately half (5) For patients with moderate liver damage, Axitinib is priced at a reduced starting dose of about half the dose.
Side effects of Axitinib
Axitinib is a targeted therapy drug used to treat advanced renal cell carcinoma. As a targeted therapy drug, its use reduces damage to normal cells to some extent, but it may also have some side effects. Common side effects of Axitinib include hypertension, fatigue, diarrhea, decreased appetite, nausea, hoarseness, hand-foot syndrome (HFS), weight loss, vomiting, and constipation. Monitoring blood pressure and complete blood count is recommended during treatment. Axitinib is a small-molecule tyrosine kinase inhibitor. It shows partial response to multiple tumor types and is used for the treatment of renal cell carcinoma (RCC). The therapeutic effect is as follows: 1. Inhibit tumor growth. 2. Extend the progression survival of patients with renal cell carcinoma. Axitinib is also used to treat patients with recurrent renal cell carcinoma after surgery. This drug has shown excellent performance in treating related diseases, with significant therapeutic effects and high safety.
Reference
[1] Chen Y, Tortorici M A, Garrett M, et al. Clinical pharmacology of axitinib[J]. Clinical pharmacokinetics, 2013, 52: 713-725.
[2] Kelly R J, Rixe O. Axitinib (AG-013736)[J]. Small molecules in oncology, 2010: 33-44.
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xitinib is an oral inhibitor of the VEGF, PDGF and colony stimulating factor-1 receptor tyrosine kinases and is currently in development for the potential treatment.
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