Must-read for patients: Overview of basic information in the Chinese instructions for lenvatinib/lenvatinib

1. Generic name: Lenvatinib, Lenvatinib

Product name:Lenvima, Lenvima

Other names: Lenvatinib, E7080

2. Who can take lenvatinib? Indications?

Lenvatinib is indicated for the treatment of:

1. Differentiated thyroid cancer (DTC): It is suitable for the treatment of adult patients with locally recurrent or metastatic, progressive, and radioactive iodine-refractory differentiated cancer.

2. Renal cell carcinoma (RCC): It can be used in combination with pembrolizumab for the first-line treatment of adult patients with advanced renal cell carcinoma; it can also be combined with everolimus for adult patients with advanced renal cell carcinoma who have received one anti-angiogenic treatment in the past.

3. Hepatocellular carcinoma (HCC): Suitable for first-line treatment of patients with unresectable hepatocellular carcinoma.

4. Endometrial cancer (EC): It can be used in combination with pembrolizumab to treat patients with advanced endometrial cancer who, according to testing, are mismatch repair proficient (pMMR) patients or non-microsatellite instability high (MSI-H) patients. These patients have disease progression after previous systemic therapy in any case and are not suitable for therapeutic surgery or radiotherapy.

3. What are the side effects of lenvatinib?

Clinically, the most common side effects of lenvatinib are fatigue, joint and muscle pain, loss of appetite, weight loss, nausea, oral ulcers, headache, vomiting, rash, palmoplantar erythrodysesthesia syndrome (PPE; rash and numbness on the palms and soles), hoarseness, stomach pain, etc. Adverse events such as pancreatitis, impaired wound healing, cholecystitis, nephrotic syndrome, arterial (including aortic) aneurysms, dissection, and rupture have also occurred after the drug was marketed.

4. How should you take lenvatinib?

1. Drug dosage:

(1)Differentiated thyroid cancer (DTC)Patients: The recommended dose of lenvatinib is24 mg orally once daily until disease progression or unacceptable toxicity.

(2) Patients with renal cell carcinoma (RCC); the recommended dose of the drug for first-line treatment is 20 mg once a day, combined with 200 mg pembrolizumab by intravenous infusion for 30 minutes every 3 weeks, until disease progression or unacceptable toxicity occurs, or for up to 2 years. After completing 2 years of combination therapy, lenvatinib can be administered as a single agent until disease progression or unacceptable toxicity. The recommended dose for previously treated RCC patients is 18 mg, taken orally in combination with 5 mg of everolimus, once daily until disease progression or unacceptable toxicity occurs.

(3) Hepatocellular carcinoma (HCC) Patients: The recommended dose is based on actual body weight: patients ≥60kg take 12mg; patients <60kg take 8mg; take orally once a day until disease progression or unacceptable toxicity occurs.

(4) Endometrial cancer (EC) patients: The recommended dose of lenvatinib is 20 mg once daily, similarly combined with 200 mg pembrolizumab intravenously, 30 minutes every 3 weeks, until unacceptable toxicity or disease progression occurs.

2. Medication management: Lenvatinib is provided in the form of capsule preparations and should be taken once a day at the same time every day, regardless of eating or not. Do not crush or chew lenvatinib capsules. If a dose is missed and cannot be taken within 12 hours, skip the dose and take the next dose at the normal dosing time.

For patients who cannot swallow the capsule, they need to dissolve it in water or apple juice to make a suspension. The specific operation is as follows: Put up to 5 capsules into a 20mL container or syringe, keeping the capsules intact without breaking or crushing. Add 3mL of liquid and let it sit for 10 minutes to allow the capsule shell to disintegrate, then stir or shake for 3 minutes until it is completely disintegrated and take it. Rinse with 2 mL of liquid and take again, repeat until no residue remains. If 6 capsules are needed, take it in two batches, 3 capsules each time. If the suspension is not used immediately, it can be stored in a refrigerator at 2-8°C in a covered container for up to 24 hours and then discarded.

5. How to store lenvatinib?

LenvatinibStorage temperature20°C to 25°C (68°F to 77°F); tolerance to 15°C to 30°C (59°F to 86°F).

6. How does lenvatinib work?

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

7. What will happen if you overdose on lenvatinib?

Due to high plasma protein binding, lenvatinib is not expected to be dialyzable. One patient who received a single oral dose of lenvatinib120 mg died due to multiple organ dysfunction.