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Lenvatinib

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Information about Lenvatinib

Lenvatinib is orally available multi-kinase inhibitor and antineoplastic agent that is used in treatment of advanced, metastatic medullary thyroid cancer and refractory renal cell carcinoma.

Liver safety of Lenvatinib

Lenvatinib is associated with a modest rate of serum enzyme elevations during treatment and has been implicated to rare instances of clinically apparent, acute liver injury some of which have been fatal. 

Mechanism of action of Lenvatinib

Lenvatinib (len va' ti nib) is an orally available, small molecule, multi-kinase inhibitor with activity against vascular endothelial growth factor receptor (VEGFR) 1, 2 and 3 as well as fibroblast growth factor (FGF) 1, 2, 3 and 4, platelet derived growth factor receptor (PDGFR) alpha, cKit and the RET proto-oncogene.  Several of these receptors are overexpressed in cancer cells and can cause unregulated cell growth.  Lenvatinib has been evaluated as therapy of several forms of advanced and metastatic carcinomas and has shown efficacy in thyroid and renal cell carcinoma. 

FDA approval information for Lenvatinib

Lenvatinib received accelerated approval for use in the United States in 2015 for therapy of metastatic, refractory thyroid cancer after failure of other therapies.  Indications were expanded in 2016 to include advanced, refractory renal cell carcinoma. 

Dosage and administration for Lenvatinib

Lenvatinib is available as capsules of 4 and 10 mg under the brand name Lenvima.  The recommended dose for thyroid cancer is 24 mg orally once daily and for renal cell cancer is 18 mg (in combination with 5 mg of everolimus) orally once daily. 

Side effects of Lenvatinib

Side effects are common and can include hypertension, fatigue, diarrhea, nausea, vomiting, anorexia, weight loss, abdominal pain, stomatitis, headache, joint and muscle pain, peripheral edema, cough, dyspnea, rash, hemorrhagic events and proteinuria.  Other uncommon, but potentially severe side effects include severe hypertension, heart failure, arterial thrombotic events, proteinuria, severe diarrhea, renal impairment, gastrointestinal perforation or fistulae, prolongation of the QTc interval, hypocalcemia, reversible posterior leukoencephalopathy and embryo-fetal toxicity.

 


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