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 Registry Number 417716-92-8 N
ATC code None
PubChem CID: 9823820
IUPHAR/BPS 7426
ChemSpider 7999567 YesY
UNII EE083865G2 YesY
ChEBI CHEBI:85994 YesY
ChEMBL CHEMBL1289601 N
Chemical data
Formula C21H19ClN4O4
Molecular 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 showed promising results in 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 was completed with modestly encouraging results,[5] the manufacturer launched a phase III trial in March 2011.[6]The FDA has granted approval to lenvatinib (Lenvima) as a treatment for patients with progressive, radioactive iodine (RAI)-refractory differentiated thyroid cancer (DTC).

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" (PDF). 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. ^ Clinical trial number NCT00946153 for "Study of E7080 in Patients With Advanced Hepatocellular Carcinoma (HCC)" at ClinicalTrials.gov
  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. ^ Clinical trial number NCT01321554 for "A Trial of E7080 in 131I-Refractory Differentiated Thyroid Cancer" at ClinicalTrials.gov