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lenalidomide

L04AX04

Forms & Strengths

Capsules: 2.5 mg, 5 mg, 10 mg, 15 mg, 20 mg, 25 mg

Adult Dosing

Multiple Myeloma: 25 mg orally once daily on Days 1-21 of repeated 28-day cycles (in combination with dexamethasone)
Myelodysplastic Syndrome (MDS): 10 mg orally once daily
Follicular Lymphoma / Marginal Zone Lymphoma: 20 mg orally once daily on Days 1-21 of repeated 28-day cycles (in combination with rituximab)

Pediatric Dosing

Safety and efficacy in pediatric patients have not been established

Indications

Multiple myeloma in combination with dexamethasone
Transfusion-dependent anemia due to low- or intermediate-1-risk myelodysplastic syndromes associated with a deletion 5q cytogenetic abnormality
Follicular lymphoma or marginal zone lymphoma, in combination with rituximab, after prior therapy

Mechanism of Action

Immunomodulatory agent that binds to cereblon, a component of the cullin-RING E3 ubiquitin ligase complex
Promotes ubiquitination and degradation of specific transcription factors (Ikaros and Aiolos), leading to direct anti-myeloma and immunomodulatory effects
Inhibits angiogenesis and induces apoptosis of malignant plasma cells and B-cell lymphomas

Contraindications

Pregnancy (teratogenic, structural and neurodevelopmental toxicities)
Severe hypersensitivity to lenalidomide

Adverse Reactions

Neutropenia, thrombocytopenia, and anemia
Venous thromboembolism (deep vein thrombosis and pulmonary embolism)
Fatigue, asthenia, and peripheral edema
Diarrhea, constipation, and nausea
Increased risk of second primary malignancies (e.g., AML, MDS)

Drug Interactions

Erythropoietin-stimulating agents may increase the risk of thrombosis
Concomitant use with strong CYP3A4 inducers or inhibitors generally does not significantly alter pharmacokinetics, but monitor closely
Anticoagulants or antiplatelet agents increase bleeding risk when co-administered with lenalidomide-induced thrombocytopenia

Curated Content: Needs Vetting Before Put to Clinical Use