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- Title
A review on regorafenib as multikinase inhibitor.
- Authors
Hemalatha, C. N.; Haripriya, A.; Sharmili, P.; Harikrishnan, N.
- Abstract
Combating with cancer is one of the key medical challenges of our society. Conversely, existing chemotherapeutic advances are not adequate to maintain a life expectancy of cancer affected sufferers. Therefore, translational research can pave the novel prospect to treat cancer in a fundamental way. In that connection, the present study on regorafenib a multikinase inhibitor, this is having a great impact on colorectal cancer (CRC) treatment. Regorafenib a new molecular entity kinase inhibitor, which inhibits multiple membrane-bound and intracellular kinase involved in a wide range of normal cellular functions and in pathological processes such as oncogenesis, tumor angiogenesis, and maintenance of the tumor microenvironment. They are used in the treatment of metastatic colon cancer. Regorafenib inhibited Hep 3B, PLC/ PRF/5, and Hep G2 cells and showed reduced cell growth at a concentration of 1-5 μM. It also inhibited cell migration in RJ 345, RJ 348 MCF 7, and MDAMB-231 at a concentration of 0.5/5 μM; cell apoptosis action in HT-15, HT-29, DLD-1, and HCT-116 cells at a concentration of 1-10 μM; and proliferation action in other CRC cell lines and markedly slowed tumor activity. The activity of regorafenib in multiple kinases such as vascular endothelial growth factor receptors-1, 2, and 3, TIE2, fibroblast growth factor receptor 1 inhibits at a concentration of 4-311 nM; and oncogenic receptor tyrosine kinases (RTKs), KIT, RET, and mutant forms of BRAF at an IC50 value 1.5-28 nM thereby its pharmacological activity with respective biological targets was evaluated. It displays antimetastatic activity, which may contribute to its efficacy in patients with metastatic CRC.
- Subjects
FIBROBLAST growth factor receptors; VASCULAR endothelial growth factors; FIBROBLAST growth factors; IRINOTECAN; CELL migration
- Publication
Drug Invention Today, 2020, Vol 13, Issue 1, p19
- ISSN
0975-7619
- Publication type
Article