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IdentificationPharmacologyInteractionsReferencesTrialsEconomicsPropertiesSpectraTaxonomyLenalidomide
Identification
- Name
- Lenalidomide
- Accession Number
- DB00480 (APRD01303)
- Type
- Small Molecule
- Groups
- Approved
- 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. [Wikipedia] FDA approved on December 27, 2005.
- Structure
Structure for DB00480 (Lenalidomide)
- Synonyms
- 1-oxo-2-(2,6-Dioxopiperidin-3-yl)-4-aminoisoindoline
- 3-(4-Amino-1-oxoisoindolin-2-yl)piperidine-2,6-dione
- CC-5013
- CDC 501
- IMid-1
- IMiD3
- Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Revlimid Capsule 15 mg/1 Oral Celgene 2006-06-29 Not applicable US 
Revlimid Capsule 5 mg Oral Celgene Europe Limited 2007-06-14 Not applicable EU 
Revlimid Capsule 2.5 mg Oral Celgene 2016-12-20 Not applicable Canada 
Revlimid Capsule 20 mg Oral Celgene Europe Limited 2007-06-14 Not applicable EU Revlimid Capsule 25 mg Oral Celgene Europe Limited 2007-06-14 Not applicable EU Revlimid Capsule 10 mg/1 Oral Celgene 2005-12-27 Not applicable US Revlimid Capsule 5 mg Oral Celgene 2008-02-19 Not applicable Canada Revlimid Capsule 25 mg Oral Celgene 2008-10-10 Not applicable Canada Revlimid Capsule 2.5 mg Oral Celgene Europe Limited 2007-06-14 Not applicable EU Revlimid Capsule 2.5 mg/1 Oral Celgene 2012-04-16 Not applicable US - International/Other Brands
- Ladevina / Lenangio / Revlimid
- Categories
- Acids, Carbocyclic
- Angiogenesis Inhibitors
- Angiogenesis Modulating Agents
- Antineoplastic Agents
- Antineoplastic and Immunomodulating Agents
- Growth Inhibitors
- Growth Substances
- Imides
- Immunologic Factors
- Immunosuppressive Agents
- Isoindoles
- Myelosuppressive Agents
- P-glycoprotein/ABCB1 Substrates
- Phthalic Acids
- Phthalimides
- Piperidines
- Piperidones
- UNII
- F0P408N6V4
- CAS number
- 191732-72-6
- Weight
- Average: 259.2606
Monoisotopic: 259.095691297 - Chemical Formula
- C13H13N3O3
- InChI Key
- GOTYRUGSSMKFNF-UHFFFAOYSA-N
- InChI
- 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)
- IUPAC Name
- 3-(4-amino-1-oxo-2,3-dihydro-1H-isoindol-2-yl)piperidine-2,6-dione
- SMILES
- NC1=CC=CC2=C1CN(C1CCC(=O)NC1=O)C2=O
Pharmacology
- 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.
- Structured Indications
- 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. Lenalidomide does not prolong the QTc interval.
- Mechanism 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
Target Actions Organism AProtein cereblon inhibitorHuman ATumor necrosis factor ligand superfamily member 11 inhibitorHuman UCadherin-5 antagonistHuman UProstaglandin G/H synthase 2 negative modulatorHuman - Absorption
Rapidly absorbed following oral administration, with maximum plasma concentrations occurring between 0.625 and 1.5 hours post-dose. Co-administration with food does not alter the extent of absorption (AUC) but does reduce the maximal plasma concentration (Cmax) by 36%. The pharmacokinetic disposition of lenalidomide is linear. Accumulation does not occur following multiple doses.
- Volume of distribution
- Not Available
- Protein binding
30% protein bound.
- Metabolism
Lenalidomide undergoes limited metabolism. Unchanged lenalidomide is the predominant circulating component in humans. Two identified metabolites are hydroxy-lenalidomide and N-acetyl-lenalidomide; each constitutes less than 5% of parent levels in circulation. The cytochrome P450 enzyme system is not involved with the metabolism of lenalidomide.
- Route of elimination
Elimination is primarily renal. When a single oral dose of 25 mg is given healthy subjects, 90% and 4% of the dose is eliminated in urine and feces, respectively. Hydroxy-lenalidomide and N-acetyl-lenalidomide represent 4.59% and 1.83% of the excreted dose, respectively.
- Half life
Healthy subjects = 3 hours; Multiple myeloma or MDS patients = 3 - 5 hours.
- Clearance
The renal clearance of lenalidomide exceeds the glomerular filtration rate.
- 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.
- Affected organisms
- Humans and other mammals
- Pathways
- Not Available
- Pharmacogenomic Effects/ADRs
- Not Available
Interactions
- Drug Interactions
Drug Interaction Drug group Acetaminophen The serum concentration of Lenalidomide can be increased when it is combined with Acetaminophen. Approved Acetyldigitoxin Acetyldigitoxin may decrease the cardiotoxic activities of Lenalidomide. Approved Acetyldigoxin Acetyldigoxin may decrease the cardiotoxic activities of Lenalidomide. Experimental Afatinib The serum concentration of Lenalidomide can be increased when it is combined with Afatinib. Approved Albendazole The serum concentration of Lenalidomide can be increased when it is combined with Albendazole. Approved, Vet Approved Aldosterone The serum concentration of Lenalidomide can be decreased when it is combined with Aldosterone. Experimental Alectinib The serum concentration of Lenalidomide can be increased when it is combined with Alectinib. Approved Alfentanil The serum concentration of Lenalidomide can be increased when it is combined with Alfentanil. Approved, Illicit Amantadine The serum concentration of Lenalidomide can be increased when it is combined with Amantadine. Approved Aminohippuric acid The serum concentration of Lenalidomide can be increased when it is combined with Aminohippuric acid. Approved Amiodarone The serum concentration of Lenalidomide can be decreased when it is combined with Amiodarone. Approved, Investigational Amitriptyline The serum concentration of Lenalidomide can be increased when it is combined with Amitriptyline. Approved Amlodipine The serum concentration of Lenalidomide can be increased when it is combined with Amlodipine. Approved Amprenavir The serum concentration of Lenalidomide can be decreased when it is combined with Amprenavir. Approved Amsacrine The serum concentration of Lenalidomide can be increased when it is combined with Amsacrine. Approved Astemizole The serum concentration of Lenalidomide can be increased when it is combined with Astemizole. Approved, Withdrawn Atazanavir The serum concentration of Lenalidomide can be increased when it is combined with Atazanavir. Approved, Investigational Atenolol The serum concentration of Lenalidomide can be increased when it is combined with Atenolol. Approved Atorvastatin The serum concentration of Lenalidomide can be increased when it is combined with Atorvastatin. Approved Azelastine The serum concentration of Lenalidomide can be increased when it is combined with Azelastine. Approved Azithromycin The serum concentration of Lenalidomide can be increased when it is combined with Azithromycin. Approved BCG vaccine The therapeutic efficacy of BCG vaccine can be decreased when used in combination with Lenalidomide. Investigational Benzocaine The serum concentration of Lenalidomide can be increased when it is combined with Benzocaine. Approved Bepridil The serum concentration of Lenalidomide can be increased when it is combined with Bepridil. Approved, Withdrawn Bevacizumab Bevacizumab may increase the cardiotoxic activities of Lenalidomide. Approved, Investigational Biperiden The serum concentration of Lenalidomide can be increased when it is combined with Biperiden. Approved Boceprevir The serum concentration of Lenalidomide can be increased when it is combined with Boceprevir. Withdrawn Bosutinib The serum concentration of Lenalidomide can be increased when it is combined with Bosutinib. Approved Bromocriptine The serum concentration of Lenalidomide can be increased when it is combined with Bromocriptine. Approved, Investigational Buprenorphine The serum concentration of Lenalidomide can be increased when it is combined with Buprenorphine. Approved, Illicit, Investigational, Vet Approved Buspirone The serum concentration of Lenalidomide can be increased when it is combined with Buspirone. Approved, Investigational Cabazitaxel The risk or severity of adverse effects can be increased when Cabazitaxel is combined with Lenalidomide. Approved Caffeine The serum concentration of Lenalidomide can be increased when it is combined with Caffeine. Approved Canagliflozin The serum concentration of Lenalidomide can be increased when it is combined with Canagliflozin. Approved Candesartan cilexetil The serum concentration of Lenalidomide can be increased when it is combined with Candesartan. Approved Captopril The serum concentration of Lenalidomide can be increased when it is combined with Captopril. Approved Carbamazepine The serum concentration of Lenalidomide can be decreased when it is combined with Carbamazepine. Approved, Investigational Carvedilol The serum concentration of Lenalidomide can be increased when it is combined with Carvedilol. Approved, Investigational Caspofungin The serum concentration of Lenalidomide can be increased when it is combined with Caspofungin. Approved Chloroquine The serum concentration of Lenalidomide can be increased when it is combined with Chloroquine. Approved, Vet Approved Chlorotrianisene Chlorotrianisene may increase the thrombogenic activities of Lenalidomide. Withdrawn Chlorpromazine The serum concentration of Lenalidomide can be increased when it is combined with Chlorpromazine. Approved, Vet Approved Chlorpropamide The serum concentration of Lenalidomide can be increased when it is combined with Chlorpropamide. Approved Chlorprothixene The serum concentration of Lenalidomide can be increased when it is combined with Chlorprothixene. Approved, Withdrawn Cholesterol The serum concentration of Lenalidomide can be increased when it is combined with Cholesterol. Experimental Cholic Acid The serum concentration of Lenalidomide can be decreased when it is combined with Cholic Acid. Approved Cilazapril The serum concentration of Lenalidomide can be increased when it is combined with Cilazapril. Approved Cimetidine The serum concentration of Lenalidomide can be decreased when it is combined with Cimetidine. Approved Ciprofloxacin The serum concentration of Lenalidomide can be increased when it is combined with Ciprofloxacin. Approved, Investigational Citalopram The serum concentration of Lenalidomide can be increased when it is combined with Citalopram. Approved Clarithromycin The serum concentration of Lenalidomide can be increased when it is combined with Clarithromycin. Approved Clofazimine The serum concentration of Lenalidomide can be increased when it is combined with Clofazimine. Approved, Investigational Clomipramine The serum concentration of Lenalidomide can be increased when it is combined with Clomipramine. Approved, Vet Approved Clostridium tetani toxoid antigen (formaldehyde inactivated) The therapeutic efficacy of Clostridium tetani toxoid antigen (formaldehyde inactivated) can be decreased when used in combination with Lenalidomide. Approved Clotrimazole The serum concentration of Lenalidomide can be decreased when it is combined with Clotrimazole. Approved, Vet Approved Clozapine The risk or severity of adverse effects can be increased when Lenalidomide is combined with Clozapine. Approved Cobicistat The serum concentration of Lenalidomide can be increased when it is combined with Cobicistat. Approved Colchicine The serum concentration of Lenalidomide can be increased when it is combined with Colchicine. Approved Colforsin The serum concentration of Lenalidomide can be increased when it is combined with Colforsin. Experimental Conjugated estrogens Conjugated estrogens may increase the thrombogenic activities of Lenalidomide. Approved Corynebacterium diphtheriae toxoid antigen (formaldehyde inactivated) The therapeutic efficacy of Corynebacterium diphtheriae toxoid antigen (formaldehyde inactivated) can be decreased when used in combination with Lenalidomide. Approved Crizotinib The serum concentration of Lenalidomide can be increased when it is combined with Crizotinib. Approved Cyclophosphamide Cyclophosphamide may increase the cardiotoxic activities of Lenalidomide. Approved, Investigational Cyclosporine The serum concentration of Lenalidomide can be decreased when it is combined with Cyclosporine. Approved, Investigational, Vet Approved Cymarin Cymarin may decrease the cardiotoxic activities of Lenalidomide. Experimental Daclatasvir The serum concentration of Lenalidomide can be increased when it is combined with Daclatasvir. Approved Dactinomycin The serum concentration of Lenalidomide can be increased when it is combined with Dactinomycin. Approved Daidzein Daidzein may increase the thrombogenic activities of Lenalidomide. Experimental Darbepoetin alfa Darbepoetin alfa may increase the thrombogenic activities of Lenalidomide. Approved, Investigational Dasatinib The serum concentration of Lenalidomide can be increased when it is combined with Dasatinib. Approved, Investigational Daunorubicin The serum concentration of Lenalidomide can be decreased when it is combined with Daunorubicin. Approved Denosumab The risk or severity of adverse effects can be increased when Denosumab is combined with Lenalidomide. Approved Desipramine The serum concentration of Lenalidomide can be increased when it is combined with Desipramine. Approved Deslanoside Deslanoside may decrease the cardiotoxic activities of Lenalidomide. Approved Desloratadine The serum concentration of Lenalidomide can be increased when it is combined with Desloratadine. Approved, Investigational Dexamethasone Dexamethasone may increase the thrombogenic activities of Lenalidomide. Approved, Investigational, Vet Approved Dextromethorphan The serum concentration of Lenalidomide can be increased when it is combined with Dextromethorphan. Approved Diclofenac The serum concentration of Lenalidomide can be increased when it is combined with Diclofenac. Approved, Vet Approved Dienestrol Dienestrol may increase the thrombogenic activities of Lenalidomide. Approved Diethylstilbestrol Diethylstilbestrol may increase the thrombogenic activities of Lenalidomide. Approved Digitoxin Digitoxin may decrease the cardiotoxic activities of Lenalidomide. Approved Digoxin The serum concentration of Digoxin can be increased when it is combined with Lenalidomide. Approved Dihydroergotamine The serum concentration of Lenalidomide can be increased when it is combined with Dihydroergotamine. Approved Diltiazem The serum concentration of Lenalidomide can be increased when it is combined with Diltiazem. Approved Dipyridamole The serum concentration of Lenalidomide can be increased when it is combined with Dipyridamole. Approved Docetaxel The risk or severity of adverse effects can be increased when Docetaxel is combined with Lenalidomide. Approved, Investigational Doxazosin The serum concentration of Lenalidomide can be increased when it is combined with Doxazosin. Approved Doxepin The serum concentration of Lenalidomide can be increased when it is combined with Doxepin. Approved Doxorubicin The serum concentration of Lenalidomide can be decreased when it is combined with Doxorubicin. Approved, Investigational Dronabinol The serum concentration of Lenalidomide can be increased when it is combined with Dronabinol. Approved, Illicit Dronedarone The serum concentration of Lenalidomide can be increased when it is combined with Dronedarone. Approved Elbasvir The serum concentration of Lenalidomide can be increased when it is combined with Elbasvir. Approved Enalapril The serum concentration of Lenalidomide can be increased when it is combined with Enalapril. Approved, Vet Approved Enasidenib The serum concentration of Lenalidomide can be increased when it is combined with Enasidenib. Approved Enzalutamide The serum concentration of Lenalidomide can be increased when it is combined with Enzalutamide. Approved Epimestrol Epimestrol may increase the thrombogenic activities of Lenalidomide. Experimental Equol Equol may increase the thrombogenic activities of Lenalidomide. Investigational Ergonovine The serum concentration of Lenalidomide can be increased when it is combined with Ergonovine. Approved Ergotamine The serum concentration of Lenalidomide can be increased when it is combined with Ergotamine. Approved Erythromycin The serum concentration of Lenalidomide can be decreased when it is combined with Erythromycin. Approved, Vet Approved Erythropoietin Erythropoietin may increase the thrombogenic activities of Lenalidomide. Approved Estradiol Estradiol may increase the thrombogenic activities of Lenalidomide. Approved, Investigational, Vet Approved Estramustine The serum concentration of Lenalidomide can be increased when it is combined with Estramustine. Approved Estriol Estriol may increase the thrombogenic activities of Lenalidomide. Approved, Vet Approved Estrone Estrone may increase the thrombogenic activities of Lenalidomide. Approved Ethinyl Estradiol Ethinyl Estradiol may increase the thrombogenic activities of Lenalidomide. Approved Etoposide The serum concentration of Lenalidomide can be increased when it is combined with Etoposide. Approved Etravirine The serum concentration of Lenalidomide can be increased when it is combined with Etravirine. Approved Felodipine The serum concentration of Lenalidomide can be increased when it is combined with Felodipine. Approved, Investigational Fentanyl The serum concentration of Lenalidomide can be increased when it is combined with Fentanyl. Approved, Illicit, Investigational, Vet Approved Fexofenadine The serum concentration of Lenalidomide can be increased when it is combined with Fexofenadine. Approved Fidaxomicin The serum concentration of Lenalidomide can be increased when it is combined with Fidaxomicin. Approved Fingolimod Lenalidomide may increase the immunosuppressive activities of Fingolimod. Approved, Investigational Fluconazole The serum concentration of Lenalidomide can be increased when it is combined with Fluconazole. Approved Fluoxetine The serum concentration of Lenalidomide can be increased when it is combined with Fluoxetine. Approved, Vet Approved Flupentixol The serum concentration of Lenalidomide can be increased when it is combined with Flupentixol. Approved, Withdrawn Fluphenazine The serum concentration of Lenalidomide can be increased when it is combined with Fluphenazine. Approved Flurazepam The serum concentration of Lenalidomide can be increased when it is combined with Flurazepam. Approved, Illicit Fluvoxamine The serum concentration of Lenalidomide can be increased when it is combined with Fluvoxamine. Approved, Investigational G17DT The therapeutic efficacy of G17DT can be decreased when used in combination with Lenalidomide. Investigational Gefitinib The serum concentration of Lenalidomide can be increased when it is combined with Gefitinib. Approved, Investigational Genistein Genistein may increase the thrombogenic activities of Lenalidomide. Investigational GI-5005 The therapeutic efficacy of GI-5005 can be decreased when used in combination with Lenalidomide. Investigational Gitoformate Gitoformate may decrease the cardiotoxic activities of Lenalidomide. Experimental Glecaprevir The serum concentration of Lenalidomide can be increased when it is combined with Glecaprevir. Approved Glyburide The serum concentration of Lenalidomide can be increased when it is combined with Glyburide. Approved Glycerin The serum concentration of Lenalidomide can be increased when it is combined with Glycerin. Approved, Investigational Gramicidin D The serum concentration of Lenalidomide can be increased when it is combined with Gramicidin D. Approved Grepafloxacin The serum concentration of Lenalidomide can be increased when it is combined with Grepafloxacin. Withdrawn Haloperidol The serum concentration of Lenalidomide can be increased when it is combined with Haloperidol. Approved Hexestrol Hexestrol may increase the thrombogenic activities of Lenalidomide. Withdrawn Hydrocortisone The serum concentration of Lenalidomide can be increased when it is combined with Hydrocortisone. Approved, Vet Approved Idelalisib The serum concentration of Lenalidomide can be increased when it is combined with Idelalisib. Approved Imatinib The serum concentration of Lenalidomide can be increased when it is combined with Imatinib. Approved Imipramine The serum concentration of Lenalidomide can be increased when it is combined with Imipramine. Approved Indinavir The serum concentration of Lenalidomide can be decreased when it is combined with Indinavir. Approved Indomethacin The serum concentration of Lenalidomide can be increased when it is combined with Indomethacin. Approved, Investigational INGN 201 The therapeutic efficacy of INGN 201 can be decreased when used in combination with Lenalidomide. Investigational INGN 225 The therapeutic efficacy of INGN 225 can be decreased when used in combination with Lenalidomide. Investigational Isavuconazonium The serum concentration of Lenalidomide can be increased when it is combined with Isavuconazonium. Approved, Investigational Itraconazole The serum concentration of Lenalidomide can be increased when it is combined with Itraconazole. Approved, Investigational Ivacaftor The serum concentration of Lenalidomide can be increased when it is combined with Ivacaftor. Approved Ivermectin The serum concentration of Lenalidomide can be increased when it is combined with Ivermectin. Approved, Vet Approved Ketamine The serum concentration of Lenalidomide can be increased when it is combined with Ketamine. Approved, Vet Approved Ketoconazole The serum concentration of Lenalidomide can be increased when it is combined with Ketoconazole. Approved, Investigational Lanatoside C Lanatoside C may decrease the cardiotoxic activities of Lenalidomide. Experimental Lansoprazole The serum concentration of Lenalidomide can be increased when it is combined with Lansoprazole. Approved, Investigational Lapatinib The serum concentration of Lenalidomide can be increased when it is combined with Lapatinib. Approved, Investigational Leflunomide The risk or severity of adverse effects can be increased when Lenalidomide is combined with Leflunomide. Approved, Investigational Levofloxacin The serum concentration of Lenalidomide can be increased when it is combined with Levofloxacin. Approved, Investigational Levothyroxine The serum concentration of Lenalidomide can be decreased when it is combined with Levothyroxine. Approved Lidocaine The serum concentration of Lenalidomide can be increased when it is combined with Lidocaine. Approved, Vet Approved Liothyronine The serum concentration of Lenalidomide can be decreased when it is combined with Liothyronine. Approved, Vet Approved Liotrix The serum concentration of Lenalidomide can be decreased when it is combined with Liotrix. Approved Lisinopril The serum concentration of Lenalidomide can be increased when it is combined with Lisinopril. Approved, Investigational Lomitapide The serum concentration of Lenalidomide can be increased when it is combined with Lomitapide. Approved Loperamide The serum concentration of Lenalidomide can be increased when it is combined with Loperamide. Approved Lopinavir The serum concentration of Lenalidomide can be increased when it is combined with Lopinavir. Approved Loratadine The serum concentration of Lenalidomide can be increased when it is combined with Loratadine. Approved Losartan The serum concentration of Lenalidomide can be increased when it is combined with Losartan. Approved Lovastatin The serum concentration of Lenalidomide can be increased when it is combined with Lovastatin. Approved, Investigational Lumacaftor The serum concentration of Lenalidomide can be decreased when it is combined with Lumacaftor. Approved Maprotiline The serum concentration of Lenalidomide can be increased when it is combined with Maprotiline. Approved Mebendazole The serum concentration of Lenalidomide can be increased when it is combined with Mebendazole. Approved, Vet Approved Mefloquine The serum concentration of Lenalidomide can be increased when it is combined with Mefloquine. Approved Megestrol acetate The serum concentration of Lenalidomide can be increased when it is combined with Megestrol acetate. Approved, Vet Approved Meprobamate The serum concentration of Lenalidomide can be increased when it is combined with Meprobamate. Approved, Illicit Mestranol Mestranol may increase the thrombogenic activities of Lenalidomide. Approved Metamizole The risk or severity of adverse effects can be increased when Metamizole is combined with Lenalidomide. Withdrawn Methadone The serum concentration of Lenalidomide can be increased when it is combined with Methadone. Approved Methallenestril Methallenestril may increase the thrombogenic activities of Lenalidomide. Experimental Methoxy polyethylene glycol-epoetin beta Methoxy polyethylene glycol-epoetin beta may increase the thrombogenic activities of Lenalidomide. Approved Metildigoxin Metildigoxin may decrease the cardiotoxic activities of Lenalidomide. Experimental Metoprolol The serum concentration of Lenalidomide can be increased when it is combined with Metoprolol. Approved, Investigational Mibefradil The serum concentration of Lenalidomide can be increased when it is combined with Mibefradil. Withdrawn Miconazole The serum concentration of Lenalidomide can be increased when it is combined with Miconazole. Approved, Investigational, Vet Approved Midazolam The serum concentration of Lenalidomide can be decreased when it is combined with Midazolam. Approved, Illicit Mifepristone The serum concentration of Lenalidomide can be decreased when it is combined with Mifepristone. Approved, Investigational Mitomycin The serum concentration of Lenalidomide can be increased when it is combined with Mitomycin. Approved Mitoxantrone The serum concentration of Lenalidomide can be decreased when it is combined with Mitoxantrone. Approved, Investigational Morphine The serum concentration of Lenalidomide can be increased when it is combined with Morphine. Approved, Investigational Moxestrol Moxestrol may increase the thrombogenic activities of Lenalidomide. Experimental Naltrexone The serum concentration of Lenalidomide can be increased when it is combined with Naltrexone. Approved, Investigational, Vet Approved Naringenin The serum concentration of Lenalidomide can be increased when it is combined with Naringenin. Experimental Natalizumab The risk or severity of adverse effects can be increased when Lenalidomide is combined with Natalizumab. Approved, Investigational Nefazodone The serum concentration of Lenalidomide can be decreased when it is combined with Nefazodone. Approved, Withdrawn Nelfinavir The serum concentration of Lenalidomide can be decreased when it is combined with Nelfinavir. Approved Neostigmine The serum concentration of Lenalidomide can be increased when it is combined with Neostigmine. Approved, Vet Approved Nicardipine The serum concentration of Lenalidomide can be increased when it is combined with Nicardipine. Approved Nifedipine The serum concentration of Lenalidomide can be decreased when it is combined with Nifedipine. Approved Nilotinib The serum concentration of Lenalidomide can be increased when it is combined with Nilotinib. Approved, Investigational Nisoldipine The serum concentration of Lenalidomide can be increased when it is combined with Nisoldipine. Approved Nitrazepam The serum concentration of Lenalidomide can be increased when it is combined with Nitrazepam. Approved Nitrendipine The serum concentration of Lenalidomide can be increased when it is combined with Nitrendipine. Approved Norethisterone The serum concentration of Lenalidomide can be decreased when it is combined with Norethisterone. Approved Oleandrin Oleandrin may decrease the cardiotoxic activities of Lenalidomide. Experimental Omeprazole The serum concentration of Lenalidomide can be increased when it is combined with Omeprazole. Approved, Investigational, Vet Approved Ouabain Ouabain may decrease the cardiotoxic activities of Lenalidomide. Approved P-Nitrophenol The serum concentration of Lenalidomide can be increased when it is combined with P-Nitrophenol. Experimental Paclitaxel The risk or severity of adverse effects can be increased when Paclitaxel is combined with Lenalidomide. Approved, Vet Approved Palmitic Acid The serum concentration of Lenalidomide can be increased when it is combined with Palmitic Acid. Experimental Pantoprazole The serum concentration of Lenalidomide can be increased when it is combined with Pantoprazole. Approved Paroxetine The serum concentration of Lenalidomide can be increased when it is combined with Paroxetine. Approved, Investigational Perindopril The serum concentration of Lenalidomide can be increased when it is combined with Perindopril. Approved Peruvoside Peruvoside may decrease the cardiotoxic activities of Lenalidomide. Experimental Phenobarbital The serum concentration of Lenalidomide can be decreased when it is combined with Phenobarbital. Approved Pibrentasvir The serum concentration of Lenalidomide can be increased when it is combined with Pibrentasvir. Approved Pimecrolimus The risk or severity of adverse effects can be increased when Pimecrolimus is combined with Lenalidomide. Approved, Investigational Pimozide The serum concentration of Lenalidomide can be increased when it is combined with Pimozide. Approved Platelet Activating Factor The serum concentration of Lenalidomide can be decreased when it is combined with Platelet Activating Factor. Experimental Polyestradiol phosphate Polyestradiol phosphate may increase the thrombogenic activities of Lenalidomide. Approved Ponatinib The serum concentration of Lenalidomide can be increased when it is combined with Ponatinib. Approved Posaconazole The serum concentration of Lenalidomide can be increased when it is combined with Posaconazole. Approved, Investigational, Vet Approved Pravastatin The serum concentration of Lenalidomide can be increased when it is combined with Pravastatin. Approved Prazosin The serum concentration of Lenalidomide can be increased when it is combined with Prazosin. Approved Prednisone The serum concentration of Lenalidomide can be increased when it is combined with Prednisone. Approved, Vet Approved Probenecid The serum concentration of Lenalidomide can be increased when it is combined with Probenecid. Approved Progesterone The serum concentration of Lenalidomide can be decreased when it is combined with Progesterone. Approved, Vet Approved Promestriene Promestriene may increase the thrombogenic activities of Lenalidomide. Investigational Promethazine The serum concentration of Lenalidomide can be increased when it is combined with Promethazine. Approved Propafenone The serum concentration of Lenalidomide can be increased when it is combined with Propafenone. Approved Propranolol The serum concentration of Lenalidomide can be increased when it is combined with Propranolol. Approved, Investigational Proscillaridin Proscillaridin may decrease the cardiotoxic activities of Lenalidomide. Experimental Protriptyline The serum concentration of Lenalidomide can be increased when it is combined with Protriptyline. Approved Quercetin The serum concentration of Lenalidomide can be increased when it is combined with Quercetin. Experimental Quinacrine The serum concentration of Lenalidomide can be increased when it is combined with Quinacrine. Approved Quinestrol Quinestrol may increase the thrombogenic activities of Lenalidomide. Approved Quinidine The serum concentration of Lenalidomide can be increased when it is combined with Quinidine. Approved Quinine The serum concentration of Lenalidomide can be increased when it is combined with Quinine. Approved Rabies virus inactivated antigen, A The risk or severity of adverse effects can be increased when Lenalidomide is combined with Rabies virus inactivated antigen, A. Approved Rabies virus inactivated antigen, A The therapeutic efficacy of Rabies virus inactivated antigen, A can be decreased when used in combination with Lenalidomide. Approved Ranitidine The serum concentration of Lenalidomide can be increased when it is combined with Ranitidine. Approved Ranolazine The serum concentration of Lenalidomide can be increased when it is combined with Ranolazine. Approved, Investigational Reboxetine The serum concentration of Lenalidomide can be increased when it is combined with Reboxetine. Approved, Investigational Regorafenib The serum concentration of Lenalidomide can be increased when it is combined with Regorafenib. Approved Reserpine The serum concentration of Lenalidomide can be decreased when it is combined with Reserpine. Approved Rifampicin The serum concentration of Lenalidomide can be decreased when it is combined with Rifampicin. Approved Rilpivirine The serum concentration of Lenalidomide can be increased when it is combined with Rilpivirine. Approved Rindopepimut The therapeutic efficacy of Rindopepimut can be decreased when used in combination with Lenalidomide. Investigational Ritonavir The serum concentration of Lenalidomide can be decreased when it is combined with Ritonavir. Approved, Investigational Roflumilast Roflumilast may increase the immunosuppressive activities of Lenalidomide. Approved Rolapitant The serum concentration of Lenalidomide can be increased when it is combined with Rolapitant. Approved Rotavirus Vaccine The therapeutic efficacy of Rotavirus Vaccine can be decreased when used in combination with Lenalidomide. Approved Rubella virus vaccine The therapeutic efficacy of Rubella virus vaccine can be decreased when used in combination with Lenalidomide. Approved Saquinavir The serum concentration of Lenalidomide can be decreased when it is combined with Saquinavir. Approved, Investigational Scopolamine The serum concentration of Lenalidomide can be increased when it is combined with Scopolamine. Approved Secoisolariciresinol Secoisolariciresinol may increase the thrombogenic activities of Lenalidomide. Investigational Selegiline The serum concentration of Lenalidomide can be increased when it is combined with Selegiline. Approved, Investigational, Vet Approved Sertraline The serum concentration of Lenalidomide can be increased when it is combined with Sertraline. Approved Simeprevir The serum concentration of Lenalidomide can be increased when it is combined with Simeprevir. Approved Simvastatin The serum concentration of Lenalidomide can be increased when it is combined with Simvastatin. Approved Sipuleucel-T The therapeutic efficacy of Sipuleucel-T can be decreased when used in combination with Lenalidomide. Approved Sirolimus The serum concentration of Lenalidomide can be decreased when it is combined with Sirolimus. Approved, Investigational Sorafenib The serum concentration of Lenalidomide can be increased when it is combined with Sorafenib. Approved, Investigational Spironolactone The serum concentration of Lenalidomide can be increased when it is combined with Spironolactone. Approved SRP 299 The therapeutic efficacy of SRP 299 can be decreased when used in combination with Lenalidomide. Investigational St. John's Wort The serum concentration of Lenalidomide can be decreased when it is combined with St. John's Wort. Nutraceutical Staurosporine The serum concentration of Lenalidomide can be increased when it is combined with Staurosporine. Experimental Streptozocin The serum concentration of Lenalidomide can be decreased when it is combined with Streptozocin. Approved Sulfinpyrazone The serum concentration of Lenalidomide can be increased when it is combined with Sulfinpyrazone. Approved Sumatriptan The serum concentration of Lenalidomide can be increased when it is combined with Sumatriptan. Approved, Investigational Sunitinib The serum concentration of Lenalidomide can be increased when it is combined with Sunitinib. Approved, Investigational Synthetic Conjugated Estrogens, A Synthetic Conjugated Estrogens, A may increase the thrombogenic activities of Lenalidomide. Approved Synthetic Conjugated Estrogens, B Synthetic Conjugated Estrogens, B may increase the thrombogenic activities of Lenalidomide. Approved Tacrine The serum concentration of Lenalidomide can be increased when it is combined with Tacrine. Withdrawn Tacrolimus The risk or severity of adverse effects can be increased when Tacrolimus is combined with Lenalidomide. Approved, Investigational Tamoxifen The serum concentration of Lenalidomide can be decreased when it is combined with Tamoxifen. Approved Taurocholic Acid The serum concentration of Lenalidomide can be increased when it is combined with Taurocholic Acid. Experimental Tecemotide The therapeutic efficacy of Tecemotide can be decreased when used in combination with Lenalidomide. Investigational Telaprevir The serum concentration of Lenalidomide can be increased when it is combined with Telaprevir. Withdrawn Telmisartan The serum concentration of Lenalidomide can be increased when it is combined with Telmisartan. Approved, Investigational Temsirolimus The serum concentration of Lenalidomide can be increased when it is combined with Temsirolimus. Approved Terazosin The serum concentration of Lenalidomide can be increased when it is combined with Terazosin. Approved Terfenadine The serum concentration of Lenalidomide can be increased when it is combined with Terfenadine. Withdrawn Tesmilifene The serum concentration of Lenalidomide can be decreased when it is combined with Tesmilifene. Investigational Testosterone The serum concentration of Lenalidomide can be increased when it is combined with Testosterone. Approved, Investigational TG4010 The therapeutic efficacy of TG4010 can be decreased when used in combination with Lenalidomide. Investigational Tibolone Tibolone may increase the thrombogenic activities of Lenalidomide. Approved Ticagrelor The serum concentration of Lenalidomide can be increased when it is combined with Ticagrelor. Approved Tofacitinib Lenalidomide may increase the immunosuppressive activities of Tofacitinib. Approved, Investigational Tolvaptan The serum concentration of Lenalidomide can be increased when it is combined with Tolvaptan. Approved Trastuzumab Trastuzumab may increase the cardiotoxic activities of Lenalidomide. Approved, Investigational Trazodone The serum concentration of Lenalidomide can be decreased when it is combined with Trazodone. Approved, Investigational Trifluoperazine The serum concentration of Lenalidomide can be increased when it is combined with Trifluoperazine. Approved Triflupromazine The serum concentration of Lenalidomide can be increased when it is combined with Triflupromazine. Approved, Vet Approved Trimethoprim The serum concentration of Lenalidomide can be decreased when it is combined with Trimethoprim. Approved, Vet Approved Trimipramine The serum concentration of Lenalidomide can be increased when it is combined with Trimipramine. Approved Troleandomycin The serum concentration of Lenalidomide can be increased when it is combined with Troleandomycin. Approved Velpatasvir The serum concentration of Lenalidomide can be increased when it is combined with Velpatasvir. Approved Venlafaxine The serum concentration of Lenalidomide can be increased when it is combined with Venlafaxine. Approved Verapamil The serum concentration of Lenalidomide can be decreased when it is combined with Verapamil. Approved Vinblastine The serum concentration of Lenalidomide can be decreased when it is combined with Vinblastine. Approved Vincristine The serum concentration of Lenalidomide can be decreased when it is combined with Vincristine. Approved, Investigational Vinorelbine The serum concentration of Lenalidomide can be increased when it is combined with Vinorelbine. Approved, Investigational Voxilaprevir The serum concentration of Lenalidomide can be increased when it is combined with Voxilaprevir. Approved Yellow fever vaccine The therapeutic efficacy of Yellow fever vaccine can be decreased when used in combination with Lenalidomide. Approved Zeranol Zeranol may increase the thrombogenic activities of Lenalidomide. Vet Approved Zimelidine The serum concentration of Lenalidomide can be increased when it is combined with Zimelidine. Withdrawn Zoster vaccine The therapeutic efficacy of Zoster vaccine can be decreased when used in combination with Lenalidomide. Approved - Food Interactions
- When given with a fatty meal, the extent of absorption is reduced.
References
- Synthesis Reference
Surya Narayana Devarakonda, Sesha Reddy Yarraguntla, Vamsi Krishna Mudapaka, Rajasekhar Kadaboina, Veerender Murki, Amarendhar Manda, Venkata Rao Badisa, Naresh Vemula, Rama Seshagiri Rao Pulla, Venu Nalivela, "PREPARATION OF LENALIDOMIDE." U.S. Patent US20110021567, issued January 27, 2011.
US20110021567- General 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 Feb 10;352(6):549-57. [PubMed:15703420]
- 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:16569772]
- Anderson KC: Lenalidomide and thalidomide: mechanisms of action--similarities and differences. Semin Hematol. 2005 Oct;42(4 Suppl 4):S3-8. [PubMed:16344099]
- External Links
- Human Metabolome Database
- HMDB14623
- KEGG Drug
- D04687
- PubChem Compound
- 216326
- PubChem Substance
- 46505725
- ChemSpider
- 187515
- BindingDB
- 50078323
- ChEBI
- 63791
- ChEMBL
- CHEMBL848
- Therapeutic Targets Database
- DAP001255
- PharmGKB
- PA162363968
- RxList
- RxList Drug Page
- Drugs.com
- Drugs.com Drug Page
- Wikipedia
- Lenalidomide
- ATC Codes
- L04AX04 — Lenalidomide
- AHFS Codes
- 10:00.00 — Antineoplastic Agents
- FDA label
- Download (400 KB)
- MSDS
- Download (225 KB)
Clinical Trials
- Clinical Trials
Pharmacoeconomics
- Manufacturers
- Celgene corp
- Celgene Corporation
- Packagers
- Dosage forms
Form Route Strength Capsule Oral 10 mg/1 Capsule Oral 10 mg Capsule Oral 15 mg/1 Capsule Oral 15 mg Capsule Oral 2.5 mg/1 Capsule Oral 2.5 mg Capsule Oral 20 mg/1 Capsule Oral 20 mg Capsule Oral 25 mg Capsule Oral 25 mg/1 Capsule Oral 5 mg Capsule Oral 5 mg/1 Capsule Oral 7.5 mg - Prices
Unit description Cost Unit Revlimid 25 mg capsule 411.71USD capsule Revlimid 15 mg capsule 407.7USD capsule Revlimid 10 mg capsule 406.05USD capsule Revlimid 5 mg capsule 388.0USD capsule DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.- Patents
Patent Number Pediatric Extension Approved Expires (estimated) CA2477301 No 2009-09-01 2023-04-13 Canada CA2342974 No 2005-08-16 2014-02-24 Canada US6045501 No 1998-08-28 2018-08-28 US US6315720 No 2000-10-23 2020-10-23 US US6561976 No 1998-08-28 2018-08-28 US US6561977 No 2000-10-23 2020-10-23 US US6755784 No 2000-10-23 2020-10-23 US US6908432 No 1998-08-28 2018-08-28 US US8204763 No 1998-08-28 2018-08-28 US US8315886 No 2000-10-23 2020-10-23 US US8626531 No 2000-10-23 2020-10-23 US US8589188 No 1998-08-28 2018-08-28 US US7468363 No 2003-10-07 2023-10-07 US US6281230 No 1996-07-24 2016-07-24 US US8530498 No 2003-05-15 2023-05-15 US US6555554 No 1996-07-24 2016-07-24 US US7189740 No 2003-04-11 2023-04-11 US US7968569 No 2003-10-07 2023-10-07 US US8404717 No 2003-04-11 2023-04-11 US US8648095 No 2003-05-15 2023-05-15 US US8741929 No 2008-03-08 2028-03-08 US US9101622 No 2003-05-15 2023-05-15 US US9101621 No 2003-05-15 2023-05-15 US US9056120 No 2003-04-11 2023-04-11 US US5635517 No 1999-10-04 2019-10-04 US US7119106 No 1996-07-24 2016-07-24 US US7465800 No 2007-04-27 2027-04-27 US US7855217 No 2004-11-24 2024-11-24 US US8288415 No 1996-07-24 2016-07-24 US
Properties
- State
- Solid
- Experimental Properties
Property Value Source water solubility Soluble in organic solvent/water mixtures, and buffered aqueous solvents. Lenalidomide is more soluble in organic solvents and low pH solutions. Solubility was significantly lower in less acidic buffers, ranging from about 0.4 to 0.5 mg/mL. Not Available logP -0.4 Not Available - Predicted Properties
Property Value Source Water Solubility 2.33 mg/mL ALOGPS logP -0.43 ALOGPS logP -0.71 ChemAxon logS -2 ALOGPS pKa (Strongest Acidic) 11.61 ChemAxon pKa (Strongest Basic) 2.31 ChemAxon Physiological Charge 0 ChemAxon Hydrogen Acceptor Count 4 ChemAxon Hydrogen Donor Count 2 ChemAxon Polar Surface Area 92.5 Å2 ChemAxon Rotatable Bond Count 1 ChemAxon Refractivity 68.3 m3·mol-1 ChemAxon Polarizability 25.55 Å3 ChemAxon Number of Rings 3 ChemAxon Bioavailability 1 ChemAxon Rule of Five Yes ChemAxon Ghose Filter No ChemAxon Veber's Rule No ChemAxon MDDR-like Rule No ChemAxon - Predicted ADMET features
Property Value Probability Human Intestinal Absorption + 0.9958 Blood Brain Barrier + 0.9372 Caco-2 permeable - 0.5981 P-glycoprotein substrate Substrate 0.6845 P-glycoprotein inhibitor I Inhibitor 0.6012 P-glycoprotein inhibitor II Non-inhibitor 0.8927 Renal organic cation transporter Non-inhibitor 0.726 CYP450 2C9 substrate Non-substrate 0.8861 CYP450 2D6 substrate Non-substrate 0.7878 CYP450 3A4 substrate Substrate 0.5855 CYP450 1A2 substrate Non-inhibitor 0.8746 CYP450 2C9 inhibitor Non-inhibitor 0.8405 CYP450 2D6 inhibitor Non-inhibitor 0.8806 CYP450 2C19 inhibitor Non-inhibitor 0.78 CYP450 3A4 inhibitor Non-inhibitor 0.7469 CYP450 inhibitory promiscuity Low CYP Inhibitory Promiscuity 0.843 Ames test Non AMES toxic 0.8268 Carcinogenicity Non-carcinogens 0.9068 Biodegradation Not ready biodegradable 0.9967 Rat acute toxicity 2.5145 LD50, mol/kg Not applicable hERG inhibition (predictor I) Weak inhibitor 0.9803 hERG inhibition (predictor II) Non-inhibitor 0.5098
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
Spectrum Spectrum Type Splash Key Predicted GC-MS Spectrum - GC-MS Predicted GC-MS Not Available Predicted MS/MS Spectrum - 10V, Positive (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 20V, Positive (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 40V, Positive (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 10V, Negative (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 20V, Negative (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 40V, Negative (Annotated) Predicted LC-MS/MS Not Available LC-MS/MS Spectrum - LC-ESI-qTof , Positive LC-MS/MS Not Available MS/MS Spectrum - , positive LC-MS/MS splash10-0002-1920000000-c10c48acd9b8123e3505
Taxonomy
- Description
- This compound belongs to the class of organic compounds known as isoindolones. These are aromatic polycyclic compounds that an isoindole bearing a ketone.
- Kingdom
- Organic compounds
- Super Class
- Organoheterocyclic compounds
- Class
- Isoindoles and derivatives
- Sub Class
- Isoindolines
- Direct Parent
- Isoindolones
- Alternative Parents
- Alpha amino acids and derivatives / Isoindoles / Piperidinediones / Delta lactams / Benzenoids / Tertiary carboxylic acid amides / N-unsubstituted carboxylic acid imides / Dicarboximides / Azacyclic compounds / Primary amines show 4 more
- Substituents
- Alpha-amino acid or derivatives / Isoindolone / Isoindole / Piperidinedione / Delta-lactam / Piperidinone / Piperidine / Benzenoid / Carboxylic acid imide / Dicarboximide show 18 more
- Molecular Framework
- Aromatic heteropolycyclic compounds
- External Descriptors
- dicarboximide, aromatic amine, piperidones, isoindoles (CHEBI:63791)
Targets
- Kind
- Protein
- Organism
- Human
- Pharmacological action
- Yes
- Actions
- Inhibitor
- General Function
- Metal ion binding
- Specific Function
- Substrate recognition component of a DCX (DDB1-CUL4-X-box) E3 protein ligase complex that mediates the ubiquitination and subsequent proteasomal degradation of target proteins, such as MEIS2. Norma...
- Gene Name
- CRBN
- Uniprot ID
- Q96SW2
- Uniprot Name
- Protein cereblon
- Molecular Weight
- 50545.375 Da
References
- Zhu YX, Kortuem KM, Stewart AK: Molecular mechanism of action of immune-modulatory drugs thalidomide, lenalidomide and pomalidomide in multiple myeloma. Leuk Lymphoma. 2013 Apr;54(4):683-7. doi: 10.3109/10428194.2012.728597. Epub 2012 Sep 28. [PubMed:22966948]
- Kind
- Protein
- Organism
- Human
- Pharmacological action
- Yes
- Actions
- Inhibitor
- General Function
- Tumor necrosis factor receptor superfamily binding
- Specific Function
- Cytokine that binds to TNFRSF11B/OPG and to TNFRSF11A/RANK. Osteoclast differentiation and activation factor. Augments the ability of dendritic cells to stimulate naive T-cell proliferation. May be...
- Gene Name
- TNFSF11
- Uniprot ID
- O14788
- Uniprot Name
- Tumor necrosis factor ligand superfamily member 11
- Molecular Weight
- 35477.81 Da
References
- Akobeng AK, Stokkers PC: Thalidomide and thalidomide analogues for maintenance of remission in Crohn's disease. Cochrane Database Syst Rev. 2009 Apr 15;(2):CD007351. doi: 10.1002/14651858.CD007351.pub2. [PubMed:19370685]
- Melchert M, List A: The thalidomide saga. Int J Biochem Cell Biol. 2007;39(7-8):1489-99. Epub 2007 Jan 30. [PubMed:17369076]
- Kind
- Protein
- Organism
- Human
- Pharmacological action
- Unknown
- Actions
- Antagonist
- General Function
- Receptor binding
- Specific Function
- Cadherins are calcium-dependent cell adhesion proteins. They preferentially interact with themselves in a homophilic manner in connecting cells; cadherins may thus contribute to the sorting of hete...
- Gene Name
- CDH5
- Uniprot ID
- P33151
- Uniprot Name
- Cadherin-5
- Molecular Weight
- 87527.715 Da
References
- Lu L, Payvandi F, Wu L, Zhang LH, Hariri RJ, Man HW, Chen RS, Muller GW, Hughes CC, Stirling DI, Schafer PH, Bartlett JB: The anti-cancer drug lenalidomide inhibits angiogenesis and metastasis via multiple inhibitory effects on endothelial cell function in normoxic and hypoxic conditions. Microvasc Res. 2009 Mar;77(2):78-86. doi: 10.1016/j.mvr.2008.08.003. Epub 2008 Sep 4. [PubMed:18805433]
- Kind
- Protein
- Organism
- Human
- Pharmacological action
- Unknown
- Actions
- Negative modulator
- General Function
- Prostaglandin-endoperoxide synthase activity
- Specific Function
- Converts arachidonate to prostaglandin H2 (PGH2), a committed step in prostanoid synthesis. Constitutively expressed in some tissues in physiological conditions, such as the endothelium, kidney and...
- Gene Name
- PTGS2
- Uniprot ID
- P35354
- Uniprot Name
- Prostaglandin G/H synthase 2
- Molecular Weight
- 68995.625 Da
References
- Payvandi F, Wu L, Haley M, Schafer PH, Zhang LH, Chen RS, Muller GW, Stirling DI: Immunomodulatory drugs inhibit expression of cyclooxygenase-2 from TNF-alpha, IL-1beta, and LPS-stimulated human PBMC in a partially IL-10-dependent manner. Cell Immunol. 2004 Aug;230(2):81-8. [PubMed:15598423]
- Zeldis JB, Schafer PH, Bennett BL, Mercurio F, Stirling DI: Potential new therapeutics for Waldenstrom's macroglobulinemia. Semin Oncol. 2003 Apr;30(2):275-81. [PubMed:12720152]
Transporters
- Kind
- Protein
- Organism
- Human
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Xenobiotic-transporting atpase activity
- Specific Function
- Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells.
- Gene Name
- ABCB1
- Uniprot ID
- P08183
- Uniprot Name
- Multidrug resistance protein 1
- Molecular Weight
- 141477.255 Da
Drug created on June 13, 2005 07:24 / Updated on October 21, 2017 19:23