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Investigational Drug Details

Drug ID: D135
Drug Name: Lenalidomide
Synonyms:
Type: small molecule
DrugBank ID: DB00480
DrugBank Description: 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. FDA approved on December 27, 2005.
PubChem ID: 216326
CasNo: 191732-72-6
Repositioning for NAFLD: Yes
SMILES: NC1=CC=CC2=C1CN(C1CCC(=O)NC1=O)C2=O
Structure:
InChiKey: GOTYRUGSSMKFNF-UHFFFAOYSA-N
Molecular Weight: 259.2606
DrugBank Targets: Protein cereblon; Tumor necrosis factor ligand superfamily member 11; Cadherin-5; Prostaglandin G/H synthase 2
DrugBank MoA: 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
DrugBank Pharmacology: 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. Lenalidomide does not prolong the QTc interval.
DrugBank Indication: Lenalidomide is indicated for the treatment of multiple myeloma in combination with dexamethasone. It is also indicated for the treatment of patients with transfusion-dependent anemia due to low- or intermediate- risk myelodysplastic syndromes (MDS) associated with a deletion 5q cytogenetic abnormality with or without additional cytogenetic abnormalities.
Targets:
Therapeutic Category:
Clinical Trial Progress:
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