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Identification
NameThalidomide
Accession NumberDB01041  (APRD01251)
TypeSmall Molecule
GroupsApproved, Investigational, Withdrawn
Description

A piperidinyl isoindole originally introduced as a non-barbiturate hypnotic, but withdrawn from the market due to teratogenic effects. It has been reintroduced and used for a number of immunological and inflammatory disorders. Thalidomide displays immunosuppresive and anti-angiogenic activity. It inhibits release of tumor necrosis factor-alpha from monocytes, and modulates other cytokine action. [PubChem]

Structure
Thumb
Synonyms
(+-)-N-(2,6-dioxo-3-Piperidyl)phthalimide
(+-)-Thalidomide
(±)-N-(2,6-dioxo-3-piperidyl)phthalimide
(±)-thalidomide
1,3-dioxo-2-(2,6-dioxopiperidin-3-yl)isoindoline
2,6-dioxo-3-phthalimidopiperidine
3-Phthalimidoglutarimide
alpha-(N-Phthalimido)glutarimide
alpha-N-Phthalylglutaramide
alpha-Phthalimidoglutarimide
Distaval
K-17
N-(2,6-dioxo-3-piperidyl)phthalimide
N-Phthaloylglutamimide
N-Phthalyl-glutaminsaeure-imid
N-Phthalylglutamic acid imide
Pro-ban M
Sedalis
Softenon
Talidomida
Talimol
Thalidomide
Thalidomidum
α-(N-phthalimido)glutarimide
α-N-phthalylglutaramide
α-phthalimidoglutarimide
External Identifiers Not Available
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Thalomidcapsule50 mg/1oralCelgene Corporation2003-06-20Not applicableUs
Thalomidcapsule150 mgoralCelgene IncNot applicableNot applicableCanada
Thalomidcapsule200 mgoralCelgene Inc2011-02-17Not applicableCanada
Thalomidcapsule100 mgoralCelgene Inc2011-02-17Not applicableCanada
Thalomidcapsule200 mg/1oralCelgene Corporation2003-06-20Not applicableUs
Thalomidcapsule150 mg/1oralCelgene Corporation2007-03-20Not applicableUs
Thalomidcapsule100 mg/1oralCelgene Corporation2003-06-20Not applicableUs
Thalomidcapsule50 mgoralCelgene Inc2010-11-01Not applicableCanada
Approved Generic Prescription ProductsNot Available
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International Brands
NameCompany
ConterganNot Available
DistavalNot Available
K-17Not Available
SedalisNot Available
SoftenonNot Available
TalimolNot Available
ThaledNot Available
Brand mixturesNot Available
SaltsNot Available
Categories
UNII4Z8R6ORS6L
CAS number50-35-1
WeightAverage: 258.2295
Monoisotopic: 258.064056818
Chemical FormulaC13H10N2O4
InChI KeyInChIKey=UEJJHQNACJXSKW-UHFFFAOYSA-N
InChI
InChI=1S/C13H10N2O4/c16-10-6-5-9(11(17)14-10)15-12(18)7-3-1-2-4-8(7)13(15)19/h1-4,9H,5-6H2,(H,14,16,17)
IUPAC Name
2-(2,6-dioxopiperidin-3-yl)-2,3-dihydro-1H-isoindole-1,3-dione
SMILES
O=C1N(C2CCC(=O)NC2=O)C(=O)C2=CC=CC=C12
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as isoindolones. These are aromatic polycyclic compounds that an isoindole bearing a ketone.
KingdomOrganic compounds
Super ClassOrganoheterocyclic compounds
ClassIsoindoles and derivatives
Sub ClassIsoindolines
Direct ParentIsoindolones
Alternative Parents
Substituents
  • Isoindolone
  • Isoindole
  • Piperidinedione
  • Piperidinone
  • Dicarboximide
  • Delta-lactam
  • 3-aminopiperidine
  • Benzenoid
  • Piperidine
  • Carboxylic acid imide, n-unsubstituted
  • Carboxylic acid imide
  • Tertiary amine
  • Lactam
  • Carboxamide group
  • Azacycle
  • Carboxylic acid derivative
  • Hydrocarbon derivative
  • Organooxygen compound
  • Organonitrogen compound
  • Carbonyl group
  • Amine
  • Aromatic heteropolycyclic compound
Molecular FrameworkAromatic heteropolycyclic compounds
External DescriptorsNot Available
Pharmacology
IndicationFor the acute treatment of the cutaneous manifestations of moderate to severe erythema nodosum leprosum (ENL). Also for use as maintenance therapy for prevention and suppression of the cutaneous manifestations of ENL recurrence.
PharmacodynamicsThalidomide is an immunomodulatory agent with a spectrum of activity that is not fully characterized. Thalidomide is racemic — it contains both left and right handed isomers in equal amounts: one enantiomer is effective against morning sickness, and the other is teratogenic. The enantiomers are converted to each other in vivo. That is, if a human is given D-thalidomide or L-thalidomide, both isomers can be found in the serum. Hence, administering only one enantiomer will not prevent the teratogenic effect in humans.
Mechanism of actionIn patients with erythema nodosum leprosum (ENL) the mechanism of action is not fully understood. Available data from in vitro studies and preliminary clinical trials suggest that the immunologic effects of this compound can vary substantially under different conditions, but may be related to suppression of excessive tumor necrosis factor-alpha (TNF-a) production and down-modulation of selected cell surface adhesion molecules involved in leukocyte migration. For example, administration of thalidomide has been reported to decrease circulating levels of TNF-a in patients with ENL, however, it has also been shown to increase plasma TNF-a levels in HIV-seropositive patients. As a cancer treatment, the drug may act as a VEGF inhibitor.
Related Articles
AbsorptionThe absolute bioavailability has not yet been characterized in human subjects due to its poor aqueous solubility. In studies of both healthy volunteers and subjects with Hansen’s disease, the mean time to peak plasma concentrations (Tmax) ranged from 2.9 to 5.7 hours indicating that thalidomide is slowly absorbed from the gastrointestinal tract.
Volume of distributionNot Available
Protein binding55% and 66% for the (+)R and (−)S enantiomers, respectively.
Metabolism

Thalidomide itself does not appear to be hepatically metabolized to any large extent, but appears to undergo non-enzymatic hydrolysis in plasma to multiple metabolites. Thalidomide may be metabolized hepatically by enzymes of the cytochrome P450 enzyme system. The end product of metabolism, phthalic acid, is excreted as a glycine conjugate.

SubstrateEnzymesProduct
Thalidomide
cis, trans-5'-HydroxythalidomideDetails
Thalidomide
5-HydroxythalidomideDetails
Thalidomide
Thalidomide arene oxideDetails
Thalidomide arene oxide
Not Available
5-HydroxythalidomideDetails
5-Hydroxythalidomide
5,6-dihydroxythalidomideDetails
Thalidomide
Not Available
4-phthalimidoglutaramic acidDetails
Thalidomide
Not Available
2-phthalimidoglutaramic acidDetails
2-phthalimidoglutaramic acid
Not Available
2-phthalimidoglutaric acidDetails
4-phthalimidoglutaramic acid
Not Available
2-phthalimidoglutaric acidDetails
Thalidomide
Not Available
alpha-(o-carboxybenzamido)glutarimideDetails
4-phthalimidoglutaramic acid
Not Available
4-(o-carboxybenzamido)glutaramic acidDetails
2-phthalimidoglutaramic acid
Not Available
2-(o-carboxybenzamido)glutaramic acidDetails
alpha-(o-carboxybenzamido)glutarimide
Not Available
2-(o-carboxybenzamido)glutaramic acidDetails
4-(o-carboxybenzamido)glutaramic acid
Not Available
2-(o-carboxybenzamido)glutaric acidDetails
4-(o-carboxybenzamido)glutaramic acid
Not Available
2-(o-carboxybenzamido)glutaric acidDetails
2-(o-carboxybenzamido)glutaramic acid
Not Available
2-(o-carboxybenzamido)glutaric acidDetails
Route of eliminationThalidomide itself has less than 0.7% of the dose excreted in the urine as unchanged drug.
Half lifeThe mean half-life of elimination ranges from approximately 5 to 7 hours following a single dose and is not altered upon multiple dosing.
ClearanceNot Available
ToxicityThe R-configuration and the S-configuration are more toxic individually than the racemic mixture. The LD50 could not be established in mice for racemic thalidomide, whereas LD50 values for the R and S configurations are reported to be 0.4 to 0.7 g/kg and 0.5 to 1.5 g/kg, respectively.
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9775
Blood Brain Barrier+0.9382
Caco-2 permeable-0.5651
P-glycoprotein substrateSubstrate0.5301
P-glycoprotein inhibitor INon-inhibitor0.5115
P-glycoprotein inhibitor IINon-inhibitor0.8951
Renal organic cation transporterNon-inhibitor0.8179
CYP450 2C9 substrateNon-substrate0.7904
CYP450 2D6 substrateNon-substrate0.9116
CYP450 3A4 substrateSubstrate0.5309
CYP450 1A2 substrateNon-inhibitor0.9045
CYP450 2C9 inhibitorNon-inhibitor0.9071
CYP450 2D6 inhibitorNon-inhibitor0.9231
CYP450 2C19 inhibitorNon-inhibitor0.9025
CYP450 3A4 inhibitorNon-inhibitor0.8309
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.8682
Ames testNon AMES toxic0.9133
CarcinogenicityNon-carcinogens0.9378
BiodegradationNot ready biodegradable0.8838
Rat acute toxicity3.3039 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9769
hERG inhibition (predictor II)Non-inhibitor0.8735
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
ManufacturersNot Available
Packagers
Dosage forms
FormRouteStrength
Capsuleoral100 mg/1
Capsuleoral100 mg
Capsuleoral150 mg
Capsuleoral150 mg/1
Capsuleoral200 mg/1
Capsuleoral200 mg
Capsuleoral50 mg/1
Capsuleoral50 mg
Prices
Unit descriptionCostUnit
Thalomid 28 50 mg capsule Disp Pack4372.47USD disp
Thalomid 200 mg capsule277.5USD capsule
Thalomid 150 mg capsule260.61USD capsule
Thalomid 100 mg capsule243.73USD capsule
Thalomid 50 mg capsule150.15USD capsule
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
CA2157288 No2005-11-082014-02-24Canada
CA2505964 No2009-07-282023-11-13Canada
US6045501 No1998-08-282018-08-28Us
US6235756 No1993-03-012013-03-01Us
US6315720 No2000-10-232020-10-23Us
US6561976 No1998-08-282018-08-28Us
US6561977 No2000-10-232020-10-23Us
US6755784 No2000-10-232020-10-23Us
US6869399 No2000-10-232020-10-23Us
US6908432 No1998-08-282018-08-28Us
US7141018 No2000-10-232020-10-23Us
US7230012 No2003-12-092023-12-09Us
US7435745 No1997-11-032017-11-03Us
US7874984 No1998-08-282018-08-28Us
US7959566 No2000-10-232020-10-23Us
US8204763 No1998-08-282018-08-28Us
US8315886 No2000-10-232020-10-23Us
US8589188 No1998-08-282018-08-28Us
US8626531 No2000-10-232020-10-23Us
Properties
StateSolid
Experimental Properties
PropertyValueSource
melting point270 °CPhysProp
water solubility545 mg/L (at 25 °C)BUDAVARI,S ET AL. (1996)
logP0.33HANSCH,C ET AL. (1995)
Predicted Properties
PropertyValueSource
Water Solubility2.55 mg/mLALOGPS
logP0.42ALOGPS
logP0.016ChemAxon
logS-2ALOGPS
pKa (Strongest Acidic)11.59ChemAxon
pKa (Strongest Basic)-6.4ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count4ChemAxon
Hydrogen Donor Count1ChemAxon
Polar Surface Area83.55 Å2ChemAxon
Rotatable Bond Count1ChemAxon
Refractivity64.32 m3·mol-1ChemAxon
Polarizability24.42 Å3ChemAxon
Number of Rings3ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
Spectra
Spectrum TypeDescriptionSplash Key
MSMass Spectrum (Electron Ionization)splash10-0wba-4900000000-77362eaf27267f59650dView in MoNA
References
Synthesis Reference

Jamshed Shah, “Synthesis and anti-tumor activity of nitrogen substituted thalidomide analogs.” U.S. Patent US20030139451, issued July 24, 2003.

US20030139451
General ReferencesNot Available
External Links
ATC CodesL04AX02
AHFS CodesNot Available
PDB EntriesNot Available
FDA labelDownload (180 KB)
MSDSDownload (58.6 KB)
Interactions
Drug Interactions
Drug
AbataceptThe risk or severity of adverse effects can be increased when Thalidomide is combined with Abatacept.
AlfentanilAlfentanil may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
AlprazolamAlprazolam may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
AmitriptylineAmitriptyline may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
AmobarbitalAmobarbital may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
AmoxapineAmoxapine may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
AnakinraThe risk or severity of adverse effects can be increased when Thalidomide is combined with Anakinra.
AripiprazoleAripiprazole may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
AsenapineAsenapine may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
AzelastineAzelastine may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
BaclofenBaclofen may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
BrexpiprazoleBrexpiprazole may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
BrimonidineBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
BromazepamBromazepam may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
BrompheniramineBrompheniramine may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
BuprenorphineBuprenorphine may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
BuspironeBuspirone may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
ButabarbitalButabarbital may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
ButorphanolButorphanol may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
CanakinumabThe risk or severity of adverse effects can be increased when Thalidomide is combined with Canakinumab.
CarbamazepineCarbamazepine may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
CarbinoxamineCarbinoxamine may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
CarisoprodolCarisoprodol may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
Certolizumab pegolThalidomide may increase the immunosuppressive activities of Certolizumab pegol.
CetirizineCetirizine may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
ChlordiazepoxideChlordiazepoxide may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
ChlorotrianiseneChlorotrianisene may increase the thrombogenic activities of Thalidomide.
ChlorphenamineChlorphenamine may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
ChlorpromazineChlorpromazine may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
ChlorzoxazoneChlorzoxazone may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
ClemastineClemastine may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
ClobazamClobazam may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
ClomipramineClomipramine may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
ClonazepamClonazepam may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
ClonidineClonidine may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
ClorazepateClorazepate may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
ClozapineClozapine may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
CyclizineCyclizine may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
CyclobenzaprineCyclobenzaprine may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
CyproheptadineCyproheptadine may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
DantroleneDantrolene may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
Darbepoetin alfaDarbepoetin alfa may increase the thrombogenic activities of Thalidomide.
DenosumabThe risk or severity of adverse effects can be increased when Denosumab is combined with Thalidomide.
DesfluraneDesflurane may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
DesipramineDesipramine may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
DesloratadineDesloratadine may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
DexamethasoneDexamethasone may increase the dermatologic adverse activities of Thalidomide.
Dexchlorpheniramine maleateDexchlorpheniramine maleate may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
DiazepamDiazepam may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
DienogestDienogest may increase the thrombogenic activities of Thalidomide.
DimenhydrinateDimenhydrinate may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
DiphenhydramineDiphenhydramine may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
DoxepinDoxepin may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
DoxylamineDoxylamine may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
DronabinolDronabinol may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
DroperidolDroperidol may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
EfavirenzEfavirenz may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
EntacaponeEntacapone may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
ErythropoietinEpoetin alfa may increase the thrombogenic activities of Thalidomide.
EstazolamEstazolam may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
EstradiolEstradiol may increase the thrombogenic activities of Thalidomide.
Estrone sulfateEstropipate may increase the thrombogenic activities of Thalidomide.
EszopicloneEszopiclone may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
EthanolThalidomide may increase the central nervous system depressant (CNS depressant) activities of Ethanol.
EthosuximideEthosuximide may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
EthotoinEthotoin may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
EtonogestrelEtonogestrel may increase the thrombogenic activities of Thalidomide.
EzogabineEzogabine may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
FelbamateFelbamate may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
FentanylFentanyl may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
FexofenadineFexofenadine may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
FlibanserinFlibanserin may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
FlunarizineFlunarizine may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
FlupentixolFlupentixol may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
FluphenazineFluphenazine may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
FlurazepamFlurazepam may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
FosphenytoinFosphenytoin may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
GabapentinGabapentin may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
gabapentin enacarbilgabapentin enacarbil may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
Gamma Hydroxybutyric AcidGamma Hydroxybutyric Acid may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
GuanfacineGuanfacine may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
HaloperidolHaloperidol may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
HydrocodoneHydrocodone may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
HydromorphoneHydromorphone may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
HydroxyzineHydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
IloperidoneIloperidone may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
ImipramineImipramine may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
IsofluraneIsoflurane may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
KetamineKetamine may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
LamotrigineLamotrigine may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
LeflunomideThe risk or severity of adverse effects can be increased when Thalidomide is combined with Leflunomide.
LevetiracetamLevetiracetam may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
LevocabastineLevocabastine may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
LevocetirizineLevocetirizine may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
LevonorgestrelLevonorgestrel may increase the thrombogenic activities of Thalidomide.
LevorphanolLevorphanol may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
LoratadineLoratadine may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
LorazepamLorazepam may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
LoxapineLoxapine may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
LurasidoneLurasidone may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
Magnesium SulfateMagnesium Sulfate may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
MaprotilineMaprotiline may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
MeclizineMeclizine may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
Medroxyprogesterone acetateMedroxyprogesterone Acetate may increase the thrombogenic activities of Thalidomide.
MeprobamateMeprobamate may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
MetamizoleThe risk or severity of adverse effects can be increased when Metamizole is combined with Thalidomide.
MetaxaloneMetaxalone may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
MethadoneMethadone may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
MethocarbamolMethocarbamol may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
MethohexitalMethohexital may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
MethotrimeprazineMethotrimeprazine may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
Methoxy polyethylene glycol-epoetin betaMethoxy polyethylene glycol-epoetin beta may increase the thrombogenic activities of Thalidomide.
MethsuximideMethsuximide may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
MetyrosineThalidomide may increase the sedative activities of Metyrosine.
MidazolamMidazolam may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
MinocyclineMinocycline may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
MirtazapineMirtazapine may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
MorphineMorphine may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
NabiloneNabilone may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
NalbuphineNalbuphine may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
NatalizumabThe risk or severity of adverse effects can be increased when Thalidomide is combined with Natalizumab.
NitrazepamNitrazepam may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
Nitrous oxideNitrous oxide may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
NorethisteroneNorethindrone may increase the thrombogenic activities of Thalidomide.
NortriptylineNortriptyline may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
OlanzapineOlanzapine may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
OlopatadineOlopatadine may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
OrphenadrineThalidomide may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
OxazepamOxazepam may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
OxycodoneOxycodone may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
OxymorphoneOxymorphone may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
PaliperidonePaliperidone may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
PamidronateThalidomide may increase the nephrotoxic activities of Pamidronate.
ParaldehydeThalidomide may increase the central nervous system depressant (CNS depressant) activities of Paraldehyde.
ParoxetineThe risk or severity of adverse effects can be increased when Thalidomide is combined with Paroxetine.
PentazocinePentazocine may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
PentobarbitalPentobarbital may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
PerampanelPerampanel may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
PerphenazinePerphenazine may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
PethidinePethidine may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
PhenobarbitalPhenobarbital may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
PhenytoinPhenytoin may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
PimecrolimusThe risk or severity of adverse effects can be increased when Pimecrolimus is combined with Thalidomide.
PimozidePimozide may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
PipotiazinePipotiazine may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
PizotifenPizotifen may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
PomalidomidePomalidomide may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
PramipexoleThalidomide may increase the sedative activities of Pramipexole.
PregabalinPregabalin may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
PrimidonePrimidone may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
ProchlorperazineProchlorperazine may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
PromazinePromazine may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
PromethazinePromethazine may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
PropofolPropofol may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
ProtriptylineProtriptyline may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
QuazepamQuazepam may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
QuetiapineQuetiapine may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
RamelteonRamelteon may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
RemifentanilRemifentanil may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
ReserpineReserpine may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
RilonaceptThe risk or severity of adverse effects can be increased when Thalidomide is combined with Rilonacept.
RisperidoneRisperidone may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
RoflumilastRoflumilast may increase the immunosuppressive activities of Thalidomide.
RopiniroleThalidomide may increase the sedative activities of Ropinirole.
RotigotineThalidomide may increase the sedative activities of Rotigotine.
RufinamideThe risk or severity of adverse effects can be increased when Rufinamide is combined with Thalidomide.
ScopolamineScopolamine may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
Scopolamine butylbromideScopolamine butylbromide may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
SecobarbitalSecobarbital may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
SevofluraneSevoflurane may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
Sipuleucel-TThe therapeutic efficacy of Sipuleucel-T can be decreased when used in combination with Thalidomide.
Sodium oxybateSodium oxybate may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
StiripentolStiripentol may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
SufentanilSufentanil may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
SuvorexantSuvorexant may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
TacrolimusThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Thalidomide.
TapentadolTapentadol may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
TasimelteonTasimelteon may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
TemazepamTemazepam may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
TetrabenazineTetrabenazine may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
ThioridazineThioridazine may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
ThiothixeneThiothixene may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
TiagabineTiagabine may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
TizanidineTizanidine may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
TocilizumabTocilizumab may increase the immunosuppressive activities of Thalidomide.
TofacitinibThe risk or severity of adverse effects can be increased when Thalidomide is combined with Tofacitinib.
TolcaponeTolcapone may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
TopiramateTopiramate may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
TramadolTramadol may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
TrastuzumabTrastuzumab may increase the neutropenic activities of Thalidomide.
TriazolamTriazolam may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
TrifluoperazineTrifluoperazine may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
TrimipramineTrimipramine may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
TriprolidineTriprolidine may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
VedolizumabThe risk or severity of adverse effects can be increased when Thalidomide is combined with Vedolizumab.
VigabatrinVigabatrin may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
ZaleplonZaleplon may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
ZiconotideZiconotide may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
ZiprasidoneZiprasidone may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
Zoledronic acidThe risk or severity of adverse effects can be increased when Thalidomide is combined with Zoledronate.
ZolpidemZolpidem may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
ZonisamideZonisamide may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
ZopicloneZopiclone may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
ZuclopenthixolZuclopenthixol may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
Food InteractionsNot Available

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. Normal degradation of key regulatory proteins is required for normal limb outgrowth and expression of the fibroblast growth factor FGF8. May play a role in memory and learning by regulating the assembly an...
Gene Name:
CRBN
Uniprot ID:
Q96SW2
Molecular Weight:
50545.375 Da
References
  1. 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 binding
Specific Function:
Cytokine that binds to TNFRSF1A/TNFR1 and TNFRSF1B/TNFBR. It is mainly secreted by macrophages and can induce cell death of certain tumor cell lines. It is potent pyrogen causing fever by direct action or by stimulation of interleukin-1 secretion and is implicated in the induction of cachexia, Under certain conditions it can stimulate cell proliferation and induce cell differentiation. Impairs ...
Gene Name:
TNF
Uniprot ID:
P01375
Molecular Weight:
25644.15 Da
References
  1. Richardson P, Hideshima T, Anderson K: Thalidomide in multiple myeloma. Biomed Pharmacother. 2002 May;56(3):115-28. [PubMed:12046682 ]
  2. Fu LM, Fu-Liu CS: Thalidomide and tuberculosis. Int J Tuberc Lung Dis. 2002 Jul;6(7):569-72. [PubMed:12102294 ]
  3. Enomoto N, Takei Y, Hirose M, Ikejima K, Miwa H, Kitamura T, Sato N: Thalidomide prevents alcoholic liver injury in rats through suppression of Kupffer cell sensitization and TNF-alpha production. Gastroenterology. 2002 Jul;123(1):291-300. [PubMed:12105857 ]
  4. Rajkumar SV: Thalidomide in the treatment of multiple myeloma. Expert Rev Anticancer Ther. 2001 Jun;1(1):20-8. [PubMed:12113124 ]
  5. Vescovo G, Ravara B, Angelini A, Sandri M, Carraro U, Ceconi C, Dalla Libera L: Effect of thalidomide on the skeletal muscle in experimental heart failure. Eur J Heart Fail. 2002 Aug;4(4):455-60. [PubMed:12167383 ]
  6. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]
  7. Turk BE, Jiang H, Liu JO: Binding of thalidomide to alpha1-acid glycoprotein may be involved in its inhibition of tumor necrosis factor alpha production. Proc Natl Acad Sci U S A. 1996 Jul 23;93(15):7552-6. [PubMed:8755512 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
antagonist
General Function:
Transcriptional repressor activity, rna polymerase ii transcription regulatory region sequence-specific binding
Specific Function:
NF-kappa-B is a pleiotropic transcription factor present in almost all cell types and is the endpoint of a series of signal transduction events that are initiated by a vast array of stimuli related to many biological processes such as inflammation, immunity, differentiation, cell growth, tumorigenesis and apoptosis. NF-kappa-B is a homo- or heterodimeric complex formed by the Rel-like domain-co...
Gene Name:
NFKB1
Uniprot ID:
P19838
Molecular Weight:
105355.175 Da
References
  1. Yasui K, Kobayashi N, Yamazaki T, Agematsu K: Thalidomide as an immunotherapeutic agent: the effects on neutrophil-mediated inflammation. Curr Pharm Des. 2005;11(3):395-401. [PubMed:15723633 ]
  2. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]
4. DNA
Kind
Nucleotide
Organism
Human
Pharmacological action
yes
Actions
intercalation
General Function:
Used for biological information storage.
Specific Function:
DNA contains the instructions needed for an organism to develop, survive and reproduce.
Molecular Weight:
2.15 x 1012 Da
References
  1. Stephens TD, Bunde CJ, Fillmore BJ: Mechanism of action in thalidomide teratogenesis. Biochem Pharmacol. 2000 Jun 15;59(12):1489-99. [PubMed:10799645 ]
  2. Shoji A, Kuwahara M, Ozaki H, Sawai H: Modified DNA aptamer that binds the (R)-isomer of a thalidomide derivative with high enantioselectivity. J Am Chem Soc. 2007 Feb 7;129(5):1456-64. [PubMed:17263432 ]
  3. Stephens TD, Fillmore BJ: Hypothesis: thalidomide embryopathy-proposed mechanism of action. Teratology. 2000 Mar;61(3):189-95. [PubMed:10661908 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
antagonist
General Function:
Protein tyrosine kinase activity
Specific Function:
Tyrosine-protein kinase that acts as cell-surface receptor for fibroblast growth factors and plays an essential role in the regulation of cell proliferation, differentiation, migration and apoptosis, and in the regulation of embryonic development. Required for normal embryonic patterning, trophoblast function, limb bud development, lung morphogenesis, osteogenesis and skin development. Plays an...
Gene Name:
FGFR2
Uniprot ID:
P21802
Molecular Weight:
92024.29 Da
References
  1. Eichholz A, Merchant S, Gaya AM: Anti-angiogenesis therapies: their potential in cancer management. Onco Targets Ther. 2010 Jun 24;3:69-82. [PubMed:20616958 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
antagonist
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 brain, and in pathological conditions, such as in cancer. PTGS2 is responsible for production of inflammatory prostaglandins. Up-regulation of PTGS2 is also associated with increased cell adhesion, p...
Gene Name:
PTGS2
Uniprot ID:
P35354
Molecular Weight:
68995.625 Da
References
  1. Horrobin DF: A low toxicity maintenance regime, using eicosapentaenoic acid and readily available drugs, for mantle cell lymphoma and other malignancies with excess cyclin D1 levels. Med Hypotheses. 2003 May;60(5):615-23. [PubMed:12710892 ]
  2. Hada M, Mizutari K: [A case report of metastatic pancreatic cancer that responded remarkably to the combination of thalidomide, celecoxib and irinotecan]. Gan To Kagaku Ryoho. 2004 Sep;31(9):1407-10. [PubMed:15446566 ]
  3. 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 ]
  4. Wiedmann MW, Caca K: Molecularly targeted therapy for gastrointestinal cancer. Curr Cancer Drug Targets. 2005 May;5(3):171-93. [PubMed:15892618 ]
  5. Du GJ, Lin HH, Xu QT, Wang MW: Thalidomide inhibits growth of tumors through COX-2 degradation independent of antiangiogenesis. Vascul Pharmacol. 2005 Aug;43(2):112-9. [PubMed:15982930 ]
  6. Kim JH, Scialli AR: Thalidomide: the tragedy of birth defects and the effective treatment of disease. Toxicol Sci. 2011 Jul;122(1):1-6. doi: 10.1093/toxsci/kfr088. Epub 2011 Apr 19. [PubMed:21507989 ]
7. Nuclear factor kappa-light-chain-enhancer of activated B cells
Kind
Protein
Organism
Human
Pharmacological action
unknown
References
  1. Kim JH, Scialli AR: Thalidomide: the tragedy of birth defects and the effective treatment of disease. Toxicol Sci. 2011 Jul;122(1):1-6. doi: 10.1093/toxsci/kfr088. Epub 2011 Apr 19. [PubMed:21507989 ]
Kind
Protein group
Organism
Human
Pharmacological action
unknown
Actions
binder
General Function:
Not Available
Specific Function:
Functions as transport protein in the blood stream. Binds various ligands in the interior of its beta-barrel domain. Also binds synthetic drugs and influences their distribution and availability in the body. Appears to function in modulating the activity of the immune system during the acute-phase reaction.
Components:
NameUniProt IDDetails
Alpha-1-acid glycoprotein 1P02763 Details
Alpha-1-acid glycoprotein 2P19652 Details
References
  1. Turk BE, Jiang H, Liu JO: Binding of thalidomide to alpha1-acid glycoprotein may be involved in its inhibition of tumor necrosis factor alpha production. Proc Natl Acad Sci U S A. 1996 Jul 23;93(15):7552-6. [PubMed:8755512 ]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrateinhibitor
General Function:
Steroid hydroxylase activity
Specific Function:
Responsible for the metabolism of a number of therapeutic agents such as the anticonvulsant drug S-mephenytoin, omeprazole, proguanil, certain barbiturates, diazepam, propranolol, citalopram and imipramine.
Gene Name:
CYP2C19
Uniprot ID:
P33261
Molecular Weight:
55930.545 Da
References
  1. Zhou SF, Zhou ZW, Yang LP, Cai JP: Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. Epub 2009 Sep 1. [PubMed:19515014 ]
  2. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygen
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics. Most active in catalyzing 2-hydroxylation. Caffeine is metabolized primarily by cytochrome CYP1A2 in the liver through an initial N...
Gene Name:
CYP1A2
Uniprot ID:
P05177
Molecular Weight:
58293.76 Da
References
  1. Wang B, Zhou SF: Synthetic and natural compounds that interact with human cytochrome P450 1A2 and implications in drug development. Curr Med Chem. 2009;16(31):4066-218. [PubMed:19754423 ]
  2. Zhou SF, Zhou ZW, Yang LP, Cai JP: Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. Epub 2009 Sep 1. [PubMed:19515014 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Vitamin d 24-hydroxylase activity
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics.
Gene Name:
CYP1A1
Uniprot ID:
P04798
Molecular Weight:
58164.815 Da
References
  1. Zhou SF, Zhou ZW, Yang LP, Cai JP: Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. Epub 2009 Sep 1. [PubMed:19515014 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Steroid hydroxylase activity
Specific Function:
Metabolizes several precarcinogens, drugs, and solvents to reactive metabolites. Inactivates a number of drugs and xenobiotics and also bioactivates many xenobiotic substrates to their hepatotoxic or carcinogenic forms.
Gene Name:
CYP2E1
Uniprot ID:
P05181
Molecular Weight:
56848.42 Da
References
  1. Zhou SF, Zhou ZW, Yang LP, Cai JP: Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. Epub 2009 Sep 1. [PubMed:19515014 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Steroid hydroxylase activity
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics. This enzyme contributes to the wide pharmacokinetics variability of the metabolism of drugs such as S-warfarin, diclofenac, phenyto...
Gene Name:
CYP2C9
Uniprot ID:
P11712
Molecular Weight:
55627.365 Da
References
  1. Zhou SF, Zhou ZW, Yang LP, Cai JP: Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. Epub 2009 Sep 1. [PubMed:19515014 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Prostaglandin-endoperoxide synthase activity
Specific Function:
Converts arachidonate to prostaglandin H2 (PGH2), a committed step in prostanoid synthesis. Involved in the constitutive production of prostanoids in particular in the stomach and platelets. In gastric epithelial cells, it is a key step in the generation of prostaglandins, such as prostaglandin E2 (PGE2), which plays an important role in cytoprotection. In platelets, it is involved in the gener...
Gene Name:
PTGS1
Uniprot ID:
P23219
Molecular Weight:
68685.82 Da
References
  1. Zhou SF, Zhou ZW, Yang LP, Cai JP: Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. Epub 2009 Sep 1. [PubMed:19515014 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
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 brain, and in pathological conditions, such as in cancer. PTGS2 is responsible for production of inflammatory prostaglandins. Up-regulation of PTGS2 is also associated with increased cell adhesion, p...
Gene Name:
PTGS2
Uniprot ID:
P35354
Molecular Weight:
68995.625 Da
References
  1. Zhou SF, Zhou ZW, Yang LP, Cai JP: Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. Epub 2009 Sep 1. [PubMed:19515014 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inducer
General Function:
Oxygen binding
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics.
Gene Name:
CYP3A5
Uniprot ID:
P20815
Molecular Weight:
57108.065 Da
References
  1. Zhou SF, Zhou ZW, Yang LP, Cai JP: Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. Epub 2009 Sep 1. [PubMed:19515014 ]
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Drug created on June 13, 2005 07:24 / Updated on July 26, 2016 01:51