Revlimid

Multiple myeloma — in combination with dexamethasone; as maintenance therapy after autologous HSCT; Myelodysplastic syndromes (MDS) — transfusion-dependent anemia with deletion 5q with or without additional cytogenetic abnormalities; Mantle cell lymphoma (MCL) — relapsed or progressed after two prior therapies, one of which included bortezomib; Follicular lymphoma (FL) — in combination with rituximab, relapsed/refractory after at least two prior systemic therapies; Marginal zone lymphoma (MZL) — in combination with rituximab, relapsed/refractory after at least two prior systemic therapies

Multiple myeloma (with dexamethasone): 25 mg orally Days 1-21 of 28-day cycle
MM maintenance after ASCT: 10 mg daily continuously on 28-day cycles, may increase to 15 mg after 3 cycles if tolerated
MDS del(5q): 10 mg daily
MCL: 25 mg daily Days 1-21 of 28-day cycle
FL/MZL (with rituximab): 20 mg daily Days 1-21 of 28-day cycle for up to 12 cycles

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

Pregnancy — lenalidomide is an analogue of thalidomide and is contraindicated in pregnancy.

• Embryo-Fetal Toxicity: REMS program required. Two forms of contraception required for females of reproductive potential.
• Hematologic Toxicity: Grade 3-4 neutropenia in 33-59%, thrombocytopenia in 22-62% depending on indication.
• Venous/Arterial Thromboembolism: DVT (7-10%), PE (4-6%). Prophylaxis with aspirin or anticoagulants recommended.
• Increased Mortality in CLL: Not indicated for CLL outside of clinical trials.
• Second Primary Malignancies: Including AML/MDS (3-5% cumulative incidence) and solid tumors.
• Hepatotoxicity: Including fatal hepatic failure.
• Severe Cutaneous Reactions: Including SJS, TEN. Discontinue permanently.
• Tumor Lysis Syndrome: Monitor in patients with high tumor burden.
• Tumor Flare Reaction: In MCL and CLL patients.

Neutropenia (42%), thrombocytopenia (36%), diarrhea (30%), fatigue (28%), constipation (24%), nausea (22%), muscle cramp (18%), rash (16%), anemia (12%), pyrexia (15%)

Consult the complete prescribing information for a comprehensive list of adverse reactions and their frequencies.

Consult the complete prescribing information for drug interactions, including effects on CYP enzymes, transporters, and concomitant medications that may require dose adjustments or monitoring.

Consult the full prescribing information for pregnancy-related considerations.

Refer to prescribing information for lactation guidance.

Pediatric safety and efficacy information is detailed in the full label.

Dose modifications for organ impairment are specified in the complete prescribing information.

Lenalidomide is an immunomodulatory agent with antineoplastic, anti-angiogenic, pro-erythropoietic, and immunomodulatory properties. It binds to cereblon, a substrate receptor of the CRL4-CRBN E3 ubiquitin ligase, leading to ubiquitination and proteasomal degradation of Ikaros (IKZF1) and Aiolos (IKZF3) transcription factors. This results in direct anti-tumor effects, enhanced T-cell and natural killer cell-mediated immunity against tumor cells, and inhibition of angiogenesis.

Tmax: 0.5-6 hours. Half-life: approximately 3 hours. Minimal protein binding (<30%). Not extensively metabolized; 82% excreted unchanged in urine. Dose adjust for renal impairment.

Clinical efficacy and safety data supporting the approval are available in the full prescribing information and from the clinical trials listed below.

• MM-009 — Lenalidomide + dexamethasone vs. placebo + dex in relapsed/refractory MM. Phase III, n=353.
  🔬 NCT00056160 ↗ 📄 Primary Publication ↗
• MM-010 — Lenalidomide + dexamethasone vs. placebo + dex in relapsed/refractory MM (international). Phase III, n=351.
  🔬 NCT00424047 ↗ 📄 Primary Publication ↗

Revlimid has FDA-approved indications across the following cancer types covered on PipelineEvidence: