Product Name

Lenalidomide

CAS Number

191732-72-6

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Product Name:
Lenalidomide
CAS Number:
191732-72-6
Indication:
For the treatment of patients with transfusion-dependent anemia due to low- or intermediate- risk myelodysplastic syndromes associated with a deletion 5q cytogenetic abnormality with or without additional cytogenetic abnormalities.
Mode of Action:

The mechanism of action of lenalidomide remains to be fully characterized, however it has been demonstrated that lenalidomide inhibits the expression of cyclooxygenase-2 (COX-2), but not COX-1, in vitro. In vivo it induces tumor cell apoptosis directly and indirectly by inhibition of bone marrow stromal cell support, by anti-angiogenic and anti-osteoclastogenic effects, and by immunomodulatory activity

Pharmacodynamics:

Lenalidomide, a thalidomide analogue, is an immunomodulatory agent possessing immunomodulatory and antiangiogenic properties. Lenalidomide inhibits the secretion of pro-inflammatory cytokines and increases the secretion of anti-inflammatory cytokines from peripheral blood mononuclear cells. Lenalidomide inhibits cell proliferation with varying effectiveness (IC50s) in some but not all cell lines. Lenalidomide is effective in inhibiting growth of Namalwa cells (a human B cell lymphoma cell line with a deletion of one chromosome 5) but is much less effective in inhibiting growth of KG-1 cells (human myeloblastic cell line, also with a deletion of one chromosome 5) and other cell lines without chromosome 5 deletions.

Metabolism:

The metabolic profile of lenalidomide in humans has not been studied. In healthy volunteers, approximately two-thirds of lenalidomide is eliminated unchanged through urinary excretion. The process exceeds the glomerular filtration rate and therefore is partially or entirely active.

Toxicity:

The most frequently reported adverse events were related to blood and lymphatic system disorders, skin and subcutaneous tissue disorders, gastrointestinal disorders, and general disorders and administrative site conditions.

IUPAC:
3-(4-amino-1-oxo-2, 3-dihydro-1H-isoindol-2-yl)piperidine-2, 6-dione
ATC:
L04AX04
PubChem:
216326
DrugBank:
DB00480 (APRD01303)
Formula:
C21H28O2
Molecular Mass:
259.2606
Synonyms:
CC-5013 CDC 501 IMiD3
SMILES:
NC1=CC=CC2=C1CN(C1CCC(=O)NC1=O)C2=O
InChi:
GOTYRUGSSMKFNF-UHFFFAOYSA-N
General Reference:
General Reference:

 

  1. 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 Feb 10;352(6):549-57. Pubmed
  2. Chang DH, Liu N, Klimek V, Hassoun H, Mazumder A, Nimer SD, Jagannath S, Dhodapkar MV: Enhancement of ligand-dependent activation of human natural killer T cells by lenalidomide: therapeutic implications. Blood. 2006 Jul 15;108(2):618-21. Epub 2006 Mar 28. Pubmed
  3. Anderson KC: Lenalidomide and thalidomide: mechanisms of actionãsimilarities and differences. Semin Hematol. 2005 Oct;42(4 Suppl 4):S3-8. Pubmed

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