Lenvatinib

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Lenvatinib
Lenvatinib skeletal.svg
Systematic (IUPAC) name
4-[3-chloro-4-(cyclopropylcarbamoylamino)phenoxy]-7-methoxy-quinoline-6-carboxamide
Clinical data
Legal status
  • Prescription only
Identifiers
CAS number 417716-92-8 N
ATC code None
PubChem CID 9823820
ChemSpider 7999567 YesY
UNII EE083865G2 YesY
ChEBI CHEBI:816009 N
ChEMBL CHEMBL1289601 N
Chemical data
Formula C21H19ClN4O4 
Mol. mass 426.853 g/mol
 N (what is this?)  (verify)

Lenvatinib (E7080) is a multi-kinase inhibitor that is being investigated for the treatment of various types of cancer by Eisai Co. It inhibits both VEGFR2 and VEGFR3 kinases.[1]

The substance was granted orphan drug status for the treatment of various types of thyroid cancer that do not respond to radioiodine; in the US and Japan in 2012 and in Europe in 2013.[2]

Clinical trials[edit]

Lenvatinib has had promising results from a phase I clinical trial in 2006[3] and is being tested in several phase II trials as of October 2011, for example against hepatocellular carcinoma.[4] After a phase II trial testing the treatment of thyroid cancer has been completed with modestly encouraging results,[5] the manufacturer launched a phase III trial in March 2011.[6]

References[edit]

  1. ^ Matsui, J.; Funahashi, Y.; Uenaka, T.; Watanabe, T.; Tsuruoka, A.; Asada, M. (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". Clinical Cancer Research 14 (17): 5459–65. doi:10.1158/1078-0432.CCR-07-5270. PMID 18765537. 
  2. ^ "Phae III trial shows lenvatinib meets primary endpoint of progression free surival benefit in treatment of radioiodine-refactory differentiated thyroid cancer". Eisai. 3 February 2014. 
  3. ^ Glen, H; D. Boss; T. R. Evans; M. Roelvink; J. M. Saro; P. Bezodis; W. Copalu; A. Das; G. Crosswell; J. H. Schellens (2007). "A phase I dose finding study of E7080 in patients (pts) with advanced malignancies". Journal of Clinical Oncology, ASCO Annual Meeting Proceedings Part I 25 (18S): 14073. 
  4. ^ ClinicalTrials.gov NCT00946153 Study of E7080 in Patients With Advanced Hepatocellular Carcinoma (HCC)
  5. ^ Gild, M. L.; Bullock, M.; Robinson, B. G.; Clifton-Bligh, R. (2011). "Multikinase inhibitors: A new option for the treatment of thyroid cancer". Nature Reviews Endocrinology 7 (10): 617–624. doi:10.1038/nrendo.2011.141. PMID 21862995.  edit
  6. ^ ClinicalTrials.gov NCT01321554 A Trial of E7080 in 131I-Refractory Differentiated Thyroid Cancer