Jump to content

Lenvatinib

From Wikipedia, the free encyclopedia

This is an old revision of this page, as edited by Rod57 (talk | contribs) at 15:46, 29 January 2016 (top: PFS results). The present address (URL) is a permanent link to this revision, which may differ significantly from the current revision.

Lenvatinib
Clinical data
Trade namesLenvima
ATC code
Legal status
Legal status
  • In general: ℞ (Prescription only)
Identifiers
  • 4-[3-chloro-4-(cyclopropylcarbamoylamino)phenoxy]-7-methoxy-quinoline-6-carboxamide
CAS Number
PubChem CID
IUPHAR/BPS
ChemSpider
UNII
ChEBI
ChEMBL
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC21H19ClN4O4
Molar mass426.853 g/mol g·mol−1
3D model (JSmol)
  • C4CC4NC(=O)Nc3ccc(cc3Cl)Oc1ccnc(cc2OC)c1cc2C(=O)N
  • InChI=1S/C21H19ClN4O4/c1-29-19-10-17-13(9-14(19)20(23)27)18(6-7-24-17)30-12-4-5-16(15(22)8-12)26-21(28)25-11-2-3-11/h4-11H,2-3H2,1H3,(H2,23,27)(H2,25,26,28) checkY
  • Key:WOSKHXYHFSIKNG-UHFFFAOYSA-N checkY
 ☒NcheckY (what is this?)  (verify)

Lenvatinib (E7080; trade name Lenvima) is a multi-kinase inhibitor developed by Eisai Co. It inhibits both VEGFR2 and VEGFR3 kinases.[1]

Lenvatinib 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]

In February 2015, the FDA granted approval to lenvatinib for treatment of progressive, radioactive iodine (RAI)-refractory differentiated thyroid cancer (DTC).[3] In May 2015, EMA granted approval to lenvatinib for the same indication.[4]

Jan 2016: The US FDA have accepted it for Priority Review for the treatment of unresectable advanced or metastatic renal cell carcinoma (RCC) in combination with everolimus following one prior vascular endothelial growth factor (VEGF) targeted therapy.[5] This was after encouraging PFS results from a phase III trial.[5]

Clinical trials

A phase I clinical trial was performed in 2006.[6] A phase III trial started in March 2011.[7]

References

  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. ^ "Phase 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. ^ U.S. Food and Drug Administration. Hematology/Oncology (Cancer) Approvals & Safety Notifications. [1]
  4. ^ European Medicines Agency Summary of the European public assessment report (EPAR) for Lenvima [2]
  5. ^ a b New Combination Therapy for Treating Advanced RCC Receives FDA Priority Review - Jan 2016
  6. ^ Glen, H; D. Boss; T. R. Evans; M. Roelvink; et al. (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.
  7. ^ Clinical trial number NCT01321554 for "A Trial of E7080 in 131I-Refractory Differentiated Thyroid Cancer" at ClinicalTrials.gov