lenalidomide
Revlimid (lenalidomide) is an oral immunomodulatory drug from Bristol-Myers Squibb. It redirects the cell's protein-degradation machinery against specific cancer-supporting proteins and is a backbone of multiple myeloma therapy, alone or in combination.
This page is based on FDA prescribing information and the EMA medicine record for lenalidomide, cross-checked with MedlinePlus and the National Cancer Institute dictionary; the mechanism is explained in plain language, and analogies are used only where they stay accurate.
How it works
Explains what the medicine does in the body, not dosing, side effects, or safety.
An analogy
The cell has a shredder for unneeded proteins, and cereblon is the clerk deciding what gets fed in. Lenalidomide hands the clerk a forged work order naming two proteins myeloma cells rely on, Ikaros and Aiolos. The shredder destroys them, and the cancer cells lose the support they need to survive.
In simple terms
Lenalidomide changes how the cell's protein-recycling system works. It binds a protein called cereblon and redirects the machinery to break down certain proteins, including ones myeloma cells need to grow. It also stimulates immune cells that attack the cancer and reduces the blood supply tumours rely on. In a specific myelodysplastic syndrome with deletion 5q it helps restore normal red blood cell production.
In depth
Lenalidomide is a thalidomide analogue that binds cereblon, the substrate receptor of the CRL4 ubiquitin ligase complex, altering its specificity to recruit the transcription factors Ikaros and Aiolos for proteasomal degradation. Their loss is toxic to myeloma cells and derepresses immune activation. It also inhibits angiogenesis and TNF-alpha production. Because of thalidomide-class teratogenicity, prescribing is restricted under pregnancy prevention programs.
See it in motion
A schematic animation of the mechanism — simplified for clarity, not drawn to scale.
How cereblon modulators reprogram protein tagging
- Cereblon is part of an E3 ubiquitin ligase that tags proteins for destruction.
- Lenalidomide binds cereblon and redirects the machinery to break down certain proteins, including ones myeloma cells need to grow.
- Those tagged proteins are sent to the cell's disposal machinery.
- The shredder destroys them, and the myeloma cells lose the support they need to survive.
Target: Cereblon (CRBN) component of the E3 ubiquitin ligase complex
Part of the cell's protein-recycling machinery; lenalidomide binds cereblon and retargets the machinery to destroy specific proteins that myeloma cells depend on.
Approved uses
Approved uses differ by country and change over time. Always follow your local prescribing information.
Approved uses in United States
FDA- With dexamethasone, for the treatment of multiple myeloma in adults
- Maintenance treatment of multiple myeloma following autologous hematopoietic stem cell transplantation
- Treatment of transfusion-dependent anemia due to low- or intermediate-1-risk myelodysplastic syndromes associated with a deletion 5q cytogenetic abnormality
Approved uses in European Union
EMA- As monotherapy, for maintenance treatment of newly diagnosed multiple myeloma in adults who have undergone autologous stem cell transplantation
Official sources
The statements on this page trace back to these records.
- Revlimid (lenalidomide) — Summary of product characteristics and package leaflet, English version
European Medicines Agency
- U.S. Food and Drug Administration: lenalidomide prescribing information
U.S. Food and Drug Administration
- MedlinePlus: lenalidomide
MedlinePlus, U.S. National Library of Medicine
- National Cancer Institute: lenalidomide
National Cancer Institute
This page explains how the medicine works — it isn’t the patient leaflet. For anything that applies to you, read the leaflet that came with your medicine or ask your pharmacist.
MedUnfold provides educational content and is not medical advice. Always follow your local prescribing information and healthcare professional.