Advanced renal cell carcinoma (RCC) - first-line treatment in combination with pembrolizumab

Active Ingredient: Lenvatinib

Indication for Lenvatinib

Population group: only adults (18 years old or older)
Therapeutic intent: Curative procedure

Lenvatinib is indicated for the treatment of adults with advanced renal cell carcinoma (RCC) in combination with pembrolizumab, as first-line treatment.

For this indication, competent medicine agencies globally authorize below treatments:

20 mg once daily

For:

Dosage regimens

Oral, 20 milligrams lenvatinib, once daily.

Detailed description

The recommended dose of lenvatinib is 20 mg orally once daily in combination with pembrolizumab either 200 mg every 3 weeks or 400 mg every 6 weeks administered as an intravenous infusion over 30 minutes. The daily dose of lenvatinib is to be modified as needed according to the dose/toxicity management plan. Lenvatinib treatment should continue until disease progression or unacceptable toxicity. Pembrolizumab should be continued until disease progression, unacceptable toxicity or the maximum duration of therapy as specified for pembrolizumab.

See the Summary of Product Characteristics (SmPC) for pembrolizumab for full pembrolizumab dosing information.

Dose adjustment and discontinuation for lenvatinib

Management of adverse reactions may require dose interruption, adjustment, or discontinuation of lenvatinib therapy. Mild to moderate adverse reactions (e.g., Grade 1 or 2) generally do not warrant interruption of lenvatinib unless intolerable to the patient despite optimal management. Severe (e.g., Grade 3) or intolerable adverse reactions require interruption of lenvatinib until improvement of the reaction to Grade 0 to 1 or baseline.

Optimal medical management (i.e., treatment or therapy) for nausea, vomiting, and diarrhoea should be initiated prior to any lenvatinib therapy interruption or dose reduction; gastrointestinal toxicity should be actively treated in order to reduce the risk of development of renal impairment or renal failure.

For toxicities thought to be related to lenvatinib (see Table 2), upon resolution/improvement of an adverse reaction to Grade 0 to 1 or baseline, treatment should be resumed at a reduced dose of lenvatinib as suggested in Table 1.

Table 1. Dose modifications from recommended lenvatinib daily dosea:

 Lenvatinib dose in combination with
pembrolizumab
Recommended
daily dose
20 mg orally once daily
First dose reduction14 mg orally once daily
Second dose
reduction
10 mg orally once daily
Third dose
reduction
8 mg orally once daily

a Limited data are available for doses below 8 mg

When used in combination with pembrolizumab, one or both medicines should be interrupted as appropriate. Lenvatinib should be withheld, dose reduced, or discontinued as appropriate. Withhold or discontinue pembrolizumab in accordance with the instructions in the SmPC for pembrolizumab. No dose reductions are recommended for pembrolizumab.

All treatments should be discontinued in case of life-threatening reactions (e.g., Grade 4) with the exception of laboratory abnormalities judged to be non-life-threatening, in which case they should be managed as severe reactions (e.g., Grade 3).

Grades are based on the National Cancer Institute (NCI) Common Terminology Criteria for Adverse Events (CTCAE).

Table 2. Adverse reactions requiring dose modification of lenvatinib:

Adverse reactionSeverityActionDose reduce and
resume lenvatinib
HypertensionGrade 3
(despite optimal
antihypertensive therapy)
InterruptResolves to Grade 0, 1 or 2.
Grade 4DiscontinueDo not resume
Proteinuria≥2 gm/24 hoursInterruptResolves to less than 2 gm/
24 hours.
Nephrotic syndrome-------DiscontinueDo not resume
Renal impairment or failureGrade 3InterruptResolves to Grade 0-1 or
baseline.
Grade 4*DiscontinueDo not resume
Cardiac dysfunctionGrade 3InterruptResolves to Grade 0-1 or
baseline.
Grade 4DiscontinueDo not resume
PRES/RPLSAny gradeInterruptConsider resuming at reduced
dose if resolves to Grade 0-1.
HepatotoxicityGrade 3InterruptResolves to Grade 0-1 or
baseline.
Grade 4*DiscontinueDo not resume
Arterial thromboembolismsAny gradeDiscontinueDo not resume
HaemorrhageGrade 3InterruptResolves to Grade 0-1.
Grade 4DiscontinueDo not resume
GI perforation or fistulaGrade 3InterruptResolves to Grade 0-1 or
baseline.
Grade 4DiscontinueDo not resume
Non-GI fistulaGrade 4DiscontinueDo not resume
QT interval prolongation>500 msInterruptResolves to <480 ms or
baseline
DiarrhoeaGrade 3InterruptResolves to Grade 0-1 or
baseline.
Grade 4 (despite medical
management)
DiscontinueDo not resume

* Grade 4 laboratory abnormalities judged to be non-life-threatening, may be managed as severe reactions (e.g., Grade 3)

Dosage considerations

Lenvatinib should be taken at about the same time each day.

Active ingredient

Lenvatinib

Lenvatinib is a receptor tyrosine kinase (RTK) inhibitor that selectively inhibits the kinase activities of vascular endothelial growth factor (VEGF) receptors VEGFR1 (FLT1), VEGFR2 (KDR), and VEGFR3 (FLT4), in addition to other proangiogenic and oncogenic pathway-related RTKs including fibroblast growth factor (FGF) receptors FGFR1, 2, 3, and 4, the platelet derived growth factor (PDGF) receptor PDGFRα, KIT, and RET.

Read more about Lenvatinib

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