Rx00140 - Lenalidomide


Name:
Lenalidomide
Rx ID:
Rx00140
Validation Level:
Phenomic Similarity:
0.504
Reference ID:
DB00480
Primary Indications:
Multiple myeloma; low-1-risk myelodysplastic syndromes; intermediate-1-risk myelodysplastic syndromes; mantle cell lymphoma
Orphan Indications:
No annotated orphan indications.
Rare Indications:
Chronic lymphocytic leukemia; mantle cell lymphoma
Common Indications:
Multiple myeloma; transfusion dependant anemia; myelodysplastic syndromes; deletion 5 q cytogenetic abnormality; cytogenetic abnormalities
Pathways:
Integrated Pancreatic Cancer Pathway; Serotonergic synapse - Homo sapiens (human); Retrograde endocannabinoid signaling - Homo sapiens (human); Disease; Leishmaniasis - Homo sapiens (human); Selenium ...Click to show more
Drug Interactions:
Trastuzumab;
Food Interactions:
When given with a fatty meal, the extent of absorption is reduced.

Interactive 3D Model

Interactive Drug Target Network

Interactive Bipartite Drug Repurposing Graph

Rx00140
Primary Indication
Secondary Indication

Visualize Chemical Properties

Select x-axis

Select y-axis

Disease prevalence from Electronic Health Records

Click row to show all

Disease A Disease B A∩B A∩¬B B∩¬A Odds-Ratio P-Value Adjusted P-Value
low-1-risk myelodysplastic syndromes myelodysplastic syndromes 1504 4237 1504 952.307 0 0.0
intermediate-1-risk myelodysplastic syndromes myelodysplastic syndromes 1504 4237 1504 952.307 0 0.0
multiple myeloma anemia 1528 3327 109590 16.91 0 0.0
mantle cell lymphoma anemia 35 84 109590 15.341 1.11E-26 3.56e-23

Shared Genetic Architectures of Disease Pairs

Click row to show all

Disease A Disease B Adjusted P-Value Shared Gene IDs
MULTIPLE MYELOMA MYELODYSPLASTIC SYNDROMES 1.17e-45 ABCB1, CDKN2A, CEBPA, CSF3R, CTLA4, CXCL12, CYP1A1, CYP1B1, CYP2C19, CYP2D6, CYP3A4, CYP3A5, EPHX1, ERCC1, ERCC2, ERCC5, FAS, FCGR2A, FLT3, GSTM1, GSTP1, GSTT1, HFE, HLA-C, HLA-DPB1, HLA-DQB1, HLA-DRB1, HPSE, IFNG, IL10, IL12A, IL1A, IL1B, IL1R1, IL1RN, IL2, IL4, IL4R, IL6, IL6R, IL8, JAK1, JAK3, KIR2DS4, KIR2DS5, KRAS, LIG4, LTA, MEFV, MPO, MTHFR, MYD88, NAT2, NQO1, NRAS, PDGFRA, PLK2, TAP1, TAP2, TERC, TERT, TGFB1, TLR2, TLR4, TNF, TP53, TYMS, VDR, VEGFA, XPA, XRCC1, XRCC3, XRCC5

Chemical, Pharmacological and Biological Annotations


ATC Code:
L04AX04
Brands:
Ladevina; Lenangio
Category:
Antineoplastic Agents
ChEBI ID:
63791
PubChem ID:
216326
KEGG Drug ID:
D04687
SMILE:
NC1=CC=CC2=C1CN(C1CCC(=O)NC1=O)C2=O
InChI:
1S/C13H13N3O3/c14-9-3-1-2-7-8(9)6-16(13(7)19)10-4-5-11(17)15-12(10)18/h1-3,10H,4-6,14H2,(H,15,17,18)
Classification:
Kingdom:
Organic Compounds
Superclass:
Heterocyclic Compounds
Class:
Isoindoles and Derivatives
Subclass:
Isoindolines
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 syndro...
Click to show more...
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...
Click to show more...
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 therapeuti...
Click to show more...
Mechanism:
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 apopto...
Click to show more...

Adsorption, Distribution, Metabolism, Excretion and Toxicity


Human Intestinal Absorption:
+
Blood Brain Barrier:
+
Caco-2 permeable:
-
P-glycoprotein substrate:
Substrate
P-glycoprotein inhibitor I:
Inhibitor
P-glycoprotein inhibitor II:
Non-inhibitor
Renal organic cation transporter:
Non-inhibitor
CYP450 2C9 substrate:
Non-inhibitor
CYP450 2D6 substrate:
Non-inhibitor
CYP450 2C19 substrate:
Non-inhibitor
CYP450 inhibitory promiscuity:
Low CYP Inhibitory Promiscuity
Ames test:
Non AMES toxic
Carcinogenicity:
Non-carcinogens
Biodegradation:
Not ready biodegradable
Rat acute toxicity:
2.5145 LD50, mol/kg
hERG inhibition (predictor I):
Weak inhibitor
hERG inhibition (predictor II):
Non-inhibitor