Lenalidomide

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Lenalidomide
3-(4-amino-1,3-dihydro- 1-oxo-2H-isoindol-2-yl)- 2,6-piperidinedione
CAS number 191732-72-6	ATC code L04AX0?
Chemical formula	C₁₃H₁₃N₃O₃
Molecular weight	259.264
Bioavailability	?
Metabolism	?
Elimination half-life	?
Excretion	?
Pregnancy category	X
Legal status	FDA approved 2005
Routes of administration	Oral

Lenalidomide (initially known as CC-5013 and marketed as Revlimid® by Celgene) is a derivative of thalidomide introduced in 2004. It was initially intended as a treatment for multiple myeloma, for which thalidomide is an accepted therapeutic modality, but has also shown efficacy in the hematological disorders known as the myelodysplastic syndromes.

The exact mechanism of the immunomodulatory drugs (i.e. thalidomide, CC-4047/Actimid and lenalidomide) is not known. Apart from interfering with the immune system, they are also thought to act on angiogenesis.

Lenalidomide and bortezomib are considered therapeutic breakthroughs in myeloma, which generally carries a poor prognosis.

With myelodysplastic syndrome, the best results of lenalidomide were obtained in patients with the 5q- syndrome (List et al 2005).

It was approved by the FDA on December 27, 2005 for patients with low or intermediate-1 risk MDS with 5q- with or without additional cytogenetic abnormalities.

Contents

1 Mechanism of action
2 Risks
3 References
4 External links

Mechanism of action

The exact mechanism by which Lenalidomide acts as an immunomodulatory agent is unknown. However, recent evidence suggests that it enhances ligand-dependent expansion of a subset of T cell, the Natural killer T cell, that responds to lipid antigens and is thought to be involved in immune tolerance, tumor immunosurveilance, modulation of autoimmunity, and protection from infection.

Risks

Lenalidomide is related to thalidomide, and considered to be teratogenic. It has the pregnancy category X and cannot be prescribed for women who are pregnant or who might be conceiving. For this reason is the drug only available through a restricted distribution system called RevAssistSM.

Other potential side effects are thrombosis, pulmonary embolus, and hepatotoxicity, as well as bone marrow toxicity resulting in neutropenia and thrombocytopenia.

References

List A, Kurtin S, Roe DJ, Buresh A, Mahadevan D, Fuchs D, Rimsza L, Heaton R, Knight R, Zeldis JB. Efficacy of lenalidomide in myelodysplastic syndromes. N Engl J Med 2005;352:549-57. PMID 15703420.
Chang DH, Liu N, Klimek V, Hassoun H, Mazumder A, Numer SD, Jagannath S, Dhodapkar MV. Enhancement of ligand dependent activation of human natural killer T cells by lenalidomide: therapeutic implications. Blood 2006;epub ahead of print. PMID 16569772.
Anderson KC. Lenalidomide and thalidomide: mechanisms of action--similarities and differences. Semin Hematol 2005;42(4 Suppl 4):S3-8. PMID 16344099.

External links

[Prescribing Information]
[IMiDs] Immunomodulatory Drugs are a group of oral drugs that are chemically similar to thalidomide"
[Medical News]

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