Products
Lenvatinib was approved in many countries in 2015 in capsule form (Lenvima). In 2017, Kisplyx capsules were also approved.
Structure and properties
Lenvatinib (C21H19ClN4O4, Mr = 426.9 g/mol) is present in the drug as lenvatinib mesilate, a white to pale reddish-yellow powder that is sparingly soluble in water. It is a quinoline and carboxamide derivative.
Effects
Lenvatinib has antitumor, antiproliferative, and antiangiogenic properties. The effects are based on the inhibition of various kinases, especially VEGFR (vascular endothelial growth factor). In addition, lenvatinib also inhibits FGFR, PDGFRα, KIT and RET. It has a long half-life of 28 hours.
Indications
- For the treatment of patients with radioiodine-refractory, locally advanced or metastatic, progressive, differentiated thyroid carcinoma (Lenvima).
- In combination with everolimus for the treatment of adult patients with advanced renal cell carcinoma (RCC) after prior vascular endothelial growth factor (VEGF)-targeted treatment (Kisplyx).
Dosage
According to the professional information. The capsules are taken once a day, regardless of meals.
Contraindications
- Hypersensitivity
- Pregnancy and lactation
Full precautions can be found in the drug label.
Interactions
Lenvatinib is a substrate of P-glycoprotein, BCRP, and CYP3A.
Adverse effects
The most common potential adverse effects include hypertension, fatigue, diarrhea, joint pain, muscle pain, lack of appetite, weight loss, nausea, oral mucositis, headache, vomiting, proteinuria, hand-foot syndrome, abdominal pain, and voice disorders.
