Lenvatinib

Lenvatinib Chemische Eigenschaften,Einsatz,Produktion Methoden

• Beschreibung

  Lenvatinib is an inhibitor of the receptor tyrosine kinases VEGF receptor 2 (VEGFR2) and VEGFR3 (IC₅₀s = 4 and 5.2 nM, respectively). It also inhibits the related kinases VEGFR1, FGFR1, PDGFRα, PDGFRβ and Kit (IC₅₀s = 22, 46, 51, 39, and 100 nM, respectively). Lenvatinib (30 mg/kg, twice per day) reduces tumor growth in an H146 small cell lung cancer mouse xenograft model and induces tumor regression when administered at a dose of 100 mg/kg twice per day. Formulations containing lenvatinib have been used in the treatment of differentiated thyroid cancer, renal cell carcinoma, and hepatocellular carcinoma.

• Verwenden

  Lenvatinib is an orally active inhibitor of multiple receptor tyrosine kinases including VEGF, FGF and SCF receptors.

• Verwenden

  E7080 (Lenvatinib) is a multi-target inhibitor of VEGFR2 and VEGFR3 with IC50 of 4 nM and 5.2 nM, respectively.

• Definition

  ChEBI: A member of the class of quinolines that is the carboxamide of 4-{3-chloro-4-[(cyclopropylcarbamoyl)amino]phenoxy}-7-methoxyquinoline-6-carboxylic acid. A multi-kinase inhibitor and orphan drug used (as its mesylate salt) for the treatment of various types of thyroid cancer that do not respond to radioiodine.

• Mechanism of action

  Lenvatinib exerts its mechanism of action via inhibition of multiple receptors of tyrosine kinases: VEGFR-1 (FLT1), VEGFR-2( KDR), VEGFR-3 (FLT4), FGFR-1, FGFR-2, FGFR-3, FGFR-4, PDGFRa, RET, and c-KIT. Tumor growth is dependent on the development and proliferation of new blood vessels (neovascularization). Tumor growth and angiogenesis occur when the ligands bind to their respective tyrosine kinase receptors in the cellular membrane, initiating an intracellular signal transduction phosphorylation cascade promoting angiogenesis and cell proliferation. The inhibition of the VEGF receptors prevents tumor angiogenesis, and the inhibition of FGFR, RET, PDGFRα, and KIT prevents the further proliferation of malignant cells. The concurrent inhibition of both receptor pathways results in the inhibition of nuclear signal transduction and concomitant suppression of the activity of factors involved in tumor growth[5]. It inhibits vascular endothelial growth factor receptor family , fibroblast growth factor receptor family (FGFR1–4), platelet-derived growth factor receptor–alpha (PDGFRα), tyrosine-kinase receptor (KIT) and rearranged during transfection receptor (RET).
  

• Nebenwirkungen

  The most common side effects of LENVIMA (lenvatinib) in people treated for thyroid cancer include tiredness; joint and muscle pain; decreased appetite; weight loss; nausea; mouth sores; headache; vomiting; rash, redness, itching, or peeling of your skin on your hands and feet; stomach (abdomen) pain; and hoarseness.
  The most common side effects of LENVIMA when given with everolimus in people treated for kidney cancer include tiredness; joint and muscle pain; decreased appetite; vomiting; nausea; mouth sores; swelling in your arms and legs; cough; stomach (abdomen) pain; trouble breathing; rash; weight loss; and bleeding.
  The most common side effects of LENVIMA in people treated for liver cancer include tiredness; decreased appetite; joint and muscle pain; weight loss; stomach (abdomen) pain; rash, redness, itching, or peeling of your skin on your hands and feet; hoarseness; bleeding; change in thyroid hormone levels; nausea.

• target

  VEGFR-1

• Einzelnachweise

  1) Matsui et al. (2008), E7080, a novel inhibitor that targets multiple kinases, has potent antitumor activities against stem cell factor producing human small cell lung cancer H146, based on angiogenesis inhibition; Int. J. Cancer, 122 664 2) Matsui et al. (2008), Multi-kinase inhibitor E7080 suppresses lymph node and lung metastases of human mammary breast tumor MDA-MB-231 via inhibition of vascular endothelial growth factor-receptor (VEGF-R)2 and VEGF-R3 kinase; Clin. Cancer Res., 14 5459 3) Glen et al. (2011), E7080, a multi-targeted tyrosine kinase inhibitor suppresses tumor cell migration and invasion; BMC Cancer, 11 309 4) Yamamoto et al. (2014), Lenvatinib, an angiogenesis inhibitor targeting VEGFR/FGFR, shows broad antitumor activity in human tumor xenograft models associated with microvessel density and pericyte coverage; Vasc. Cell, 6 18
  [5] Capozzi M, et al. Lenvatinib, a molecule with versatile application: from preclinical evidence to future development in anti-cancer treatment. Cancer Management and Research, 2019; 11: 3847–3860.

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