Lenvatinib
VEGFR multikinase inhibitors
VEGFR multikinase inhibitorsHigh alert
An error with this medicine can cause serious harm: double checks and protocols are used.Pregnancy: avoid
Avoid in pregnancy. Can harm the fetus: a pregnancy test is done before starting, effective contraception is used during treatment and for a time afterwards (by women and by men…
A broad multikinase inhibitor (VEGFR, FGFR, PDGFR, KIT, RET) for thyroid, liver, kidney and endometrial cancer. Watch BP, QT and liver.
Also called: lenvatinib mesylate
Quick facts
- Group
- VEGFR multikinase inhibitors
- Target
- VEGFR1-3, FGFR, PDGFR, KIT and RET tyrosine kinases
- Used for
- Unresectable hepatocellular carcinoma
- Key effects
- Hypertension · Fatigue · Diarrhoea
- Monitor
- Blood pressure regularly · ECG and electrolytes
- ATC
- L01EX08
No doses: the clinician sets them by the current guideline.
Mechanism of action
The figure shows lenvatinib in the ATP pocket of the human VEGFR2 (KDR) kinase domain.
Lenvatinib blocks the kinases of VEGFR1-3 and FGFR, which drive angiogenesis, and of PDGFR, KIT and RET, which drive tumour growth. Combined with pembrolizumab it adds anti-angiogenic action to immune checkpoint blockade in endometrial and kidney cancer.
- Blocks VEGFR1-3 and FGFR: angiogenesis stops
- Blocks PDGFR, KIT and RET: tumour growth signals stop
- Paired with pembrolizumab or everolimus in some cancers
Indications
- Recurrent or metastatic differentiated thyroid cancer that no longer responds to radioactive iodine. Thyroid cancer (papillary) →
- Unresectable hepatocellular carcinoma, as first treatment. Hepatocellular carcinoma →
- Advanced renal cell carcinoma: first line with pembrolizumab, or with everolimus after anti-angiogenic therapy. Renal cell carcinoma →
- Advanced endometrial carcinoma that is not MSI-high or mismatch repair-deficient, after systemic therapy, with pembrolizumab. Endometrial cancer →
Adverse effects
Common
- Hypertension
- Fatigue, decreased appetite, weight loss
- Diarrhoea, nausea, mouth sores
- Hand-foot skin reaction (red, painful, peeling palms and soles)
- Hoarseness, joint and muscle pain, headache
Contraindications
- No absolute contraindications in the label apart from hypersensitivity; see the warnings
Key interactions
- Other QT-prolonging drugs (some antiarrhythmics, macrolides, antipsychotics)
- Additive risk of QT prolongation and arrhythmia.
- Bisphosphonates or denosumab (osteoporosis drugs)
- Higher risk of osteonecrosis of the jaw.
- Anticoagulants and antiplatelet drugs
- Add to its bleeding risk.
What is monitored
- Blood pressure regularly
- ECG and electrolytes
- Liver tests and other laboratory tests
- Dental examination before starting
Administration and safety
- Oral capsules swallowed whole; if swallowing is hard, the label describes dissolving them in water or apple juice, and giving them by feeding tube.
- Stopped before planned surgery or dental surgery and restarted only when the wound has healed, as the doctor directs.
Pregnancy and breastfeeding
Avoid in pregnancy. Can harm the fetus: a pregnancy test is done before starting, effective contraception is used during treatment and for a time afterwards (by women and by men with partners who could conceive), and breastfeeding is avoided.
Nursing care
- Measure blood pressure at every visit and teach home monitoring if ordered.
- Review the medication list for QT-prolonging drugs and osteoporosis drugs.
- Teach to report bleeding, black stools, vomiting blood, severe abdominal pain, chest pain or stroke symptoms at once.
- Advise a dental check before starting and to tell any dentist or surgeon about the drug.
Pharmacokinetics
- Absorption
- Oral capsules, once daily, with or without food.
- Metabolism
- Liver, CYP3A.
- Half-life
- About 28 hours.
Test yourself
Think of the answer, then tap the question to see it.
Which thyroid cancers are treated with lenvatinib?
Recurrent or metastatic differentiated thyroid cancer that no longer responds to radioactive iodine.
Which immunotherapy is combined with lenvatinib in endometrial cancer?
Pembrolizumab.
Which jaw complication is a warning for lenvatinib?
Osteonecrosis of the jaw, more likely with dental procedures and osteoporosis drugs.
Connections
← Back to the class: VEGFR multikinase inhibitors
Educational content on how drugs work; not a prescribing guide and no substitute for a health professional's advice. No doses are given.
Sources: Lenvatinib: MedlinePlus Drug Information (MedlinePlus (U.S. National Library of Medicine), 2023); Lenvatinib Mesylate - NCI (National Cancer Institute, 2023); ATCDDD - ATC/DDD Index (WHO Collaborating Centre for Drug Statistics Methodology, 2026).
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Representative model, for educational purposes only.