Description

The first new frontline treatment option for HCC approved in Japan Lenvanix (Lenvatinib) is a multikinase inhibitor that interrupts the pathways of VEGFR1, VEGFR2 and VEGFR3. It is used in the treatment of differentiated thyroid cancer (DTC), renal Cell Carcinoma and Hepatocellular Carcinoma (HCC).

 

Indications

Lenvatinib is a kinase inhibitor that is indicated:

• For the treatment of patients with locally recurrent or metastatic, progressive, radioactive iodine-refractory differentiated thyroid cancer (DTC).
• In combination with everolimus, for the treatment of patients with advanced renal cell carcinoma (RCC) following one prior antiangiogenic therapy.
• For the first-line treatment of patients with unrespectable hepatocellular carcinoma (HCC).

 

Pharmacology of Lenvanix

Based on x-ray crystallography and kinetic interaction studies, Lenvanix binds to the adenosine 5′-triphosphate binding site of VEGFR2 and to a neighboring region via a cyclopropane ring and thereby inhibits tyrosine kinase activity and associated signaling pathways.

Lenvatinib is a receptor tyrosine kinase (RTK) inhibitor that inhibits the kinase activities of vascular endothelial growth factor (VEGF) receptors VEGFR1 (FLT1), VEGFR2 (KDR), and VEGFR3 (FLT4). Lenvanix inhibits other RTKs that implicated in pathogenic angiogenesis, tumor growth, and cancer progression in addition to their normal cellular functions, including fibroblast growth factor (FGF) receptors FGFR1, 2, 3, and 4; the platelet-derived growth factor receptor alpha (PDGFRα), KIT, and RET.

 

Dosage & Administration

Differentiated thyroid cancer (DTC): The recommended dosage is 24 mg orally once daily.

Renal cell carcinoma (RCC): The recommended dosage is 18 mg orally once daily with everolimus 5 mg orally once daily.

Hepatocellular carcinoma (HCC): The recommended dosage is based on actual body weight:

• 12 mg orally once daily for patients greater than or equal to 60 kg
• 8 mg orally once daily for patients less than 60 kg.

Modify the recommended daily dose for certain patients with renal or hepatic impairment.

 

Side Effects of Lenvanix

For DTC, adverse reactions (incidence ≥30%) are hypertension, fatigue, diarrhea, arthralgia/myalgia, decreased appetite, decreased weight, nausea, stomatitis, headache, vomiting, proteinuria, palmarplantar erythrodysesthesia syndrome, abdominal pain, and dysphonia.

In RCC, the common adverse reactions (incidence ≥30%) for Lenvatinib and everolimus are diarrhea, fatigue, arthralgia/myalgia, decreased appetite, vomiting, nausea, stomatitis/oral inflammation, hypertension, peripheral edema, cough, abdominal pain, dyspnea, rash, decreased weight, hemorrhagic events, and proteinuria.

For HCC, the most common adverse reactions (incidence ≥20%) are hypertension, fatigue, diarrhea, decreased appetite, arthralgia/myalgia, decreased weight, abdominal pain, palmar-plantar erythrodysesthesia syndrome, proteinuria, dysphonia, hemorrhagic events, hypothyroidism, and nausea.

 

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