Generic
Lenalidomide
4 brands available in the market
At a glance
Lenalidomide is used for the treatment of multiple myeloma, myelodysplastic syndromes (MDS), mantle cell lymphoma (MCL), follicular lymphoma (FL), and marginal zone lymphoma (MZL). It has immunomodulatory, antiangiogenic, and antineoplastic properties.
Description
Lenalidomide is an analogue of thalidomide with immunomodulatory, antiangiogenic, and antineoplastic properties. It acts through cereblon, a component of a cullin ring E3 ubiquitin ligase enzyme complex. In the presence of drug, substrate proteins (Aiolos, Ikaros, and CK1α) are targeted for ubiquitination and degradation, leading to direct cytotoxic and immunomodulatory effects. Lenalidomide inhibits proliferation and induces apoptosis of certain hematopoietic tumor cells including MM, MCL, and del(5q) MDS.
Indications
- Multiple myeloma (in combination with Dexamethasone; maintenance therapy after auto-HSCT)
- Myelodysplastic syndromes (MDS) - transfusion-dependent anemia with deletion 5q cytogenetic abnormality
- Mantle cell lymphoma (MCL) - relapsed or progressed after 2 prior therapies including Bortezomib
- Follicular lymphoma (FL) - in combination with Rituximab for previously treated patients
- Marginal zone lymphoma (MZL) - in combination with Rituximab for previously treated patients
Therapeutic class
Cytotoxic Chemotherapy
Pharmacological class
Immunomodulatory Drug
Pharmacology
Lenalidomide acts through cereblon to cause ubiquitination and degradation of Aiolos, Ikaros, and CK1α proteins, increasing T cell and NK cell number and activation, increasing IL-2 and interferon-γ secretion, and inhibiting pro-inflammatory cytokines (TNF-α and IL-6).
Mechanism of action
Enhances the immune system, inhibits angiogenesis, and prevents cancer cell growth.
Dosage
Multiple Myeloma: 25 mg PO daily, Days 1-21 (28-day cycles) + Dexamethasone
MDS: 10 mg PO daily
MCL: 25 mg/day, Days 1-21 (28-day cycles)
FL/MZL: 20 mg PO daily, Days 1-21 + Rituximab
Renal Impairment: Dose adjustment needed in moderate-severe cases
Administration
- Swallow capsules whole with water; do not open, break, or chew
- Take at about the same time each day
- Can be taken with or without food
Missed dose
If you miss a dose, take it as soon as you remember. If it's almost time for your next dose, skip the missed dose and continue with your regular schedule. Do not double the dose.
Side effects
Common Side Effects:
- Headache, weakness, nausea, rash, dizziness, drowsiness
- Edema, loss of appetite, decreased white blood cell count, decreased calcium, weight gain
- Muscle weakness, fatigue, fever, anxiety, blood clots, dry skin
- Weight loss, confusion, decreased neutrophils, neuropathy, constipation, tremor
Precautions & warnings
- Embryo-fetal toxicity - absolutely contraindicated in pregnancy
- Hematologic toxicity - monitor CBC regularly
- Venous and arterial thromboembolism - thromboprophylaxis recommended
- Hepatotoxicity - monitor liver enzymes
- Severe cutaneous reactions - angioedema, SJS, TEN, DRESS
- Monitor for tumor lysis syndrome and tumor flare reaction
Contraindications
- Pregnancy (absolutely contraindicated)
- Lactation
- Sexually active women of childbearing potential not using 2 forms of contraception
- Severe hypersensitivity (angioedema, Stevens-Johnson syndrome, toxic epidermal necrolysis)
Drug interactions
- Erythropoietic agents: Increased risk of thrombosis
- Digoxin, ketoconazole, itraconazole, cyclosporine, verapamil, quinidine, clarithromycin: Increased plasma concentration
Food interactions
Safety with alcohol is not known; consult your doctor.
Use in pregnancy
Use in Pregnancy: Lenalidomide is highly unsafe during pregnancy (FDA Category X). Can cause severe fetal harm. Absolutely contraindicated.
Pregnancy Category: X — always consult a doctor before taking during pregnancy.
Use in lactation
Use in Lactation: Lenalidomide is probably unsafe during breastfeeding; may pass into breast milk and harm the baby. Do not breastfeed during treatment.
Pediatric use
Safety and effectiveness not established in pediatric patients (under 18 years).
Geriatric use
No dosage adjustment needed in elderly patients.
Renal / hepatic impairment
Renal Impairment: Dose adjustment needed in moderate-severe kidney disease.
Hepatic Impairment: Use with caution; dose adjustment may be needed.
Overdose effects
No specific experience in overdose management; symptomatic and supportive measures should be employed.
Storage conditions
Store below 30°C in a dry place, protected from light; keep out of reach of children.
Chemical structure
Lenalidomide