Lenvatinib

Lenvatinib

Clinical data
Trade names	Lenvima
AHFS/Drugs.com	lenvima
Routes of administration	Oral
ATC code	L01XE29 (WHO)
Legal status
Legal status	US: ℞-only
Pharmacokinetic data
Bioavailability	85% (estimated)
Protein binding	98–99%
Metabolism	CYP3A4, aldehyde oxidase, non-enzymatic
Metabolites	Desmethyl-lenvatinib (M2) and others
Biological half-life	28 hours
Excretion	~65% feces, 25% urine
Identifiers
IUPAC name 4-[3-Chloro-4-(cyclopropylcarbamoylamino)phenoxy]-7-methoxy-quinoline-6-carboxamide
Synonyms	E7080
CAS Number	417716-92-8 N
PubChem CID	9823820
IUPHAR/BPS	7426
DrugBank	DB09078 N
ChemSpider	7999567 Y
UNII	EE083865G2
KEGG	D09919 N
ChEBI	CHEBI:85994 N
ChEMBL	CHEMBL1289601 N
Chemical and physical data
Formula	C21H19ClN4O4
Molar mass	426.853 g/mol
3D model (Jmol)	Interactive image
SMILES C4CC4NC(=O)Nc3ccc(cc3Cl)Oc1ccnc(cc2OC)c1cc2C(=O)N
InChI 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) Y Key:WOSKHXYHFSIKNG-UHFFFAOYSA-N Y
NY (what is this?)

Lenvatinib (trade name Lenvima) is an anti-cancer drug for the treatment of certain kinds of thyroid cancer, and potentially for other cancers as well. It was developed by Eisai Co. and acts as a multiple kinase inhibitor against the VEGFR1, VEGFR2 and VEGFR3 kinases.

Lenvatinib is approved (since 2015) for the treatment of differentiated thyroid cancer that is either locally recurrent or metastatic, progressive, and did not respond to treatment with radioactive iodine (radioiodine).

In May 2016, the US FDA approved it (in combination with everolimus) for the treatment of advanced renal cell carcinoma following one prior anti-angiogenic therapy.

Hypertension (high blood pressure) was the most common side effect in studies (73% of patients, versus 16% in the placebo group), followed by diarrhoea (67% vs. 17%) and fatigue (67% vs. 35%). Other common side effects included decreased appetite, hypotension (low blood pressure), thrombocytopenia (low blood platelet count), nausea, muscle and bone pain.

As lenvatinib moderately prolongs QT time, addition of other drugs with this property could increase the risk of a type of abnormal heart rhythm, namely torsades de pointes. No relevant interactions with enzyme inhibitors and inducers are expected.