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Identification
NameTofacitinib
Accession NumberDB08895
TypeSmall Molecule
GroupsApproved, Investigational
DescriptionTofacitinib is an inhibitor of Janus kinases, a group of intracellular enzymes involved in signalling pathways that affect hematopoiesis and immune cell function. It is approved by the FDA for treatment of moderate to severe rheumatoid arthritis that responds inadequately to methotrexate or in those who are intolerant to methotrexate. Besides rheumatoid arthritis, tofacitinib has also been studied in clinical trials for the prevention of organ transplant rejection, and is currently under investigation for the treatment of psoriasis. Known adverse effects include nausea and headache as well as more serious immunologic and hematological adverse effects. Tofacitinib is marketed under the brand name Xeljanz by Pfizer.
Structure
Thumb
Synonyms
Tasocitinib
Tofacitinibum
External Identifiers
  • CP 690550
  • CP-690 free base
  • CP-690-550
  • CP-690,550
  • CP-690,550 free base
  • CP-690550
  • CP-690550 free base
  • CP690,550
  • CP690550
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Xeljanztablet, film coated5 mg/1oralPfizer Laboratories Div Pfizer Inc2012-11-09Not applicableUs
Xeljanztablet, film coated5 mg/1oralU.S. Pharmaceuticals2012-11-08Not applicableUs
Xeljanztablet5 mgoralPfizer Canada Inc2014-06-03Not applicableCanada
Xeljanz XRtablet, film coated, extended release11 mg/1oralPfizer Laboratories Div Pfizer Inc2016-03-07Not applicableUs
Approved Generic Prescription ProductsNot Available
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International BrandsNot Available
Brand mixturesNot Available
Salts
Name/CASStructureProperties
Tofacitinib citrate
540737-29-9
Thumb
  • InChI Key: SYIKUFDOYJFGBQ-YLAFAASESA-N
  • Monoisotopic Mass: 504.196861902
  • Average Mass: 504.4931
DBSALT000180
Categories
UNII87LA6FU830
CAS number477600-75-2
WeightAverage: 312.3696
Monoisotopic: 312.169859292
Chemical FormulaC16H20N6O
InChI KeyUJLAWZDWDVHWOW-YPMHNXCESA-N
InChI
InChI=1S/C16H20N6O/c1-11-5-8-22(14(23)3-6-17)9-13(11)21(2)16-12-4-7-18-15(12)19-10-20-16/h4,7,10-11,13H,3,5,8-9H2,1-2H3,(H,18,19,20)/t11-,13+/m1/s1
IUPAC Name
3-[(3R,4R)-4-methyl-3-[methyl({7H-pyrrolo[2,3-d]pyrimidin-4-yl})amino]piperidin-1-yl]-3-oxopropanenitrile
SMILES
[H][C@@]1(C)CCN(C[C@]1([H])N(C)C1=NC=NC2=C1C=CN2)C(=O)CC#N
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as pyrrolopyrimidines. These are compounds containing a pyrrolopyrimidine moiety, which consists of a pyrrole ring fused to a pyrimidine. Pyrrole is 5-membered ring consisting of four carbon atoms and one nitrogen atom. Pyrimidine is a 6-membered ring consisting of four carbon atoms and two nitrogen centers at the 1- and 3- ring positions.
KingdomOrganic compounds
Super ClassOrganoheterocyclic compounds
ClassPyrrolopyrimidines
Sub ClassNot Available
Direct ParentPyrrolopyrimidines
Alternative Parents
Substituents
  • Pyrrolopyrimidine
  • N-acyl-piperidine
  • Dialkylarylamine
  • Aminopyrimidine
  • 3-aminopiperidine
  • Imidolactam
  • Pyrimidine
  • Piperidine
  • Heteroaromatic compound
  • Tertiary carboxylic acid amide
  • Pyrrole
  • Tertiary amine
  • Carboxamide group
  • Azacycle
  • Nitrile
  • Carbonitrile
  • Carboxylic acid derivative
  • Hydrocarbon derivative
  • Organooxygen compound
  • Organonitrogen compound
  • Carbonyl group
  • Amine
  • Aromatic heteropolycyclic compound
Molecular FrameworkAromatic heteropolycyclic compounds
External Descriptors
Pharmacology
IndicationFor the treatment of moderate to severe rheumatoid arthritis which is resistant or intolerant to methotrexate therapy. It may also be used as an adjunct to methotrexate therapy, or other non-biologic disease-modifying antirheumatic drugs (DMARDS), when methotrexate alone is not sufficient. Tofacitinib has also been investigated as a preventative therapy for kidney transplant rejections, and as a treatment for psoriasis, ulcerative colitis, and ankylosing spondylitis. It is not to be initiated in patients with a history of chronic or recurrent infections, or in the presence of active infection, even if localized, due to reports of serious and sometimes fatal infections (commonly pneumonia, herpes zoster and urinary tract infections). Use of tofacitinib is also discouraged in those who have been, or are likely to be, exposed to TB. An increased likelihood of exposure may be encountered by traveling to certain areas. In addition, tofacitinib is not to be used in patients with severe hepatic impairment, or low hemoglobin (less than 9g/dL). Cautioned is advised when using tofacitinib in patients at risk of gastrointestinal perforation, and in the elderly who are more susceptible to infection.
PharmacodynamicsTofacitinib targets inflammation present in rheumatoid arthritis by inhibiting the janus kinases involved in the inflammatory response pathway. In placebo controlled trials of rheumatoid arthritis patients receiving 5mg or 10mg of tofacitinib twice daily, higher ACR20 responses were observed within 2 weeks in some patients (with ACR20 being defined as a minimum 20% reduction in joint pain or tenderness and 20% reduction in arthritis pain, patient disability, inflammatory markers, or global assessments of arthritis by patients or by doctors, according to the American College of Rheumatology (ACR) response criteria list), and improvements in physical functioning greater than placebo were also noted. Common known adverse effects of tofacitinib include headaches, diarrhea, nausea, nasopharyngitis and upper respiratory tract infection. More serious immunologic and hematological adverse effects have also been noted resulting in lymphopenia, neutropenia, anemia, and increased risk of cancer and infection. Before initiations of tofacitinib patients should be tested for latent infections of tuberculosis, and should be closely monitored for signs and symptoms of infection (fungal, viral, bacterial, or mycobacterial) during therapy. Therapy is not to be started in the presence of active infection, systemic or localized, and is to be interrupted if a serious infection occurs. Tofacitinib has been associated with an increased risk of lymphomas, such as Epstein-Barr virus associated lymphomas, and other malignancies (including lung, breast, gastric, and colorectal cancers). It is recommended to monitor lymphocytes, neutrophils, hemoglobin, liver enzymes, and lipids. Tofacitinib use is associated with a rapid decrease in C-reactive protein (CRP), dose dependent decreases in natural killer cells, and dose dependent increases in B cells. Depression in C-reactive protein levels continue after 2 weeks of tofacitinib discontinuation and suggest that pharmacodynamic activity last longer than pharmacokinetic half life.
Mechanism of actionRheumatoid arthritis is an autoimmune disease characterized by a dysregulation of pro-inflammatory cytokines including IL7, IL15, IL21, IL6, IFN-alpha, and IFN-beta. (3) Cytokines signalling results in tissue inflammation and joint damage by stimulating the recruitment and activation of immune cells via the janus kinase signalling pathway. Tofacitinib is a partial and reversible janus kinase (JAK) inihibitor that will prevent the body from responding to cytokine signals. By inhibiting JAKs, tofacitinib prevents the phosphorylation and activation of STATs. The JAK-STAT signalling pathway is involved in the transcription of cells involved in hematopoiesis, and immune cell function. Tofacitinib works therapeutically by inhibiting the JAK-STAT pathway to decrease the inflammatory response. However, there is evidence to suggest that it may also achieve efficacy via other pathways as well.
Related Articles
Absorption74% oral absorption (absolute bioavailability), with peak plasma concentrations (T max) achieved in 0.5-1 hour. Administration with fatty meals does not alter AUC but reduces Cmax by 32%.
Volume of distribution

Vd= 87L after intravenous administration. Distribution is equal between red blood cells and plasma.

Protein binding40%, mostly bound to albumin.
Metabolism

Metabolized in the liver by CYP3A4 and CYP2C19. Metabolites produced are inactive.

Route of elimination70% metabolized in the liver by CYP3A4 (major) and CYP2C19 (minor). Metabolites produced are inactive. 30% renally eliminated as unchanged drug.
Half life~3 hours
ClearanceNot Available
ToxicityMinimum lethal dose in rat: 500 mg/kg. Maximum asymptomatic dose in non human primate: 40 mg/kg. Lymphatic, immune system, bone marrow and erythroid cell toxicity was seen in animal studies involving rate and monkeys. Doses used in these studies ranged from 1mg/kg/day to 10mg/kg/day, over a duration of 6 weeks to 6 months. Lymphopenia, neutropenia, and anemia is seen in human subjects and may call for an interruption or discontinuation of therapy if severe. Reduced female fertility in rats was seen at exposures 17 times the maximum recommended human dose. Fertility may be impaired in human females and harm may be caused to unborn child. Carcinogenic potential is seen, however evidence for dose dependency is lacking. Because the janus kinase pathway plays a role in stimulating the production of red blood cells and is involved in immune cell function, inhibition of this pathway leads to increased risk of anemia, neutropenia, lymphopenia, cancer and infection. Lymphopenia, neutropenia, and anemia in human subjects may call for an interruption or discontinuation of therapy if severe. Role of JAK inhibition in the development of gastrointestinal perforation is not known.
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 AbsorptionNot AvailableNot Available
Blood Brain BarrierNot AvailableNot Available
Caco-2 permeableNot AvailableNot Available
P-glycoprotein substrateNot AvailableNot Available
P-glycoprotein inhibitor INot AvailableNot Available
P-glycoprotein inhibitor IINot AvailableNot Available
Renal organic cation transporterNot AvailableNot Available
CYP450 2C9 substrateNot AvailableNot Available
CYP450 2D6 substrateNot AvailableNot Available
CYP450 3A4 substrateNot AvailableNot Available
CYP450 1A2 substrateNot AvailableNot Available
CYP450 2C9 inhibitorNot AvailableNot Available
CYP450 2D6 inhibitorNot AvailableNot Available
CYP450 2C19 inhibitorNot AvailableNot Available
CYP450 3A4 inhibitorNot AvailableNot Available
CYP450 inhibitory promiscuityNot AvailableNot Available
Ames testNot AvailableNot Available
CarcinogenicityNot AvailableNot Available
BiodegradationNot AvailableNot Available
Rat acute toxicityNot AvailableNot applicable
hERG inhibition (predictor I)Not AvailableNot Available
hERG inhibition (predictor II)Not AvailableNot Available
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
ManufacturersNot Available
PackagersNot Available
Dosage forms
FormRouteStrength
Tabletoral5 mg
Tablet, film coatedoral5 mg/1
Tablet, film coated, extended releaseoral11 mg/1
PricesNot Available
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
US6956027 No2003-03-252023-03-25Us
US6956041 No2000-12-082020-12-08Us
US6965027 No2003-03-252023-03-25Us
US7091208 No2000-12-082020-12-08Us
US7265221 No2000-12-082020-12-08Us
US7301023 No2002-05-232022-05-23Us
USRE41783 No2000-12-082020-12-08Us
Properties
StateSolid
Experimental Properties
PropertyValueSource
logP1.808 MSDS, Tofacitinib Citrate
Predicted Properties
PropertyValueSource
Water Solubility0.299 mg/mLALOGPS
logP1.58ALOGPS
logP1.24ChemAxon
logS-3ALOGPS
pKa (Strongest Acidic)8.46ChemAxon
pKa (Strongest Basic)7.13ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count5ChemAxon
Hydrogen Donor Count1ChemAxon
Polar Surface Area88.91 Å2ChemAxon
Rotatable Bond Count3ChemAxon
Refractivity87.8 m3·mol-1ChemAxon
Polarizability32.65 Å3ChemAxon
Number of Rings3ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
SpectraNot Available
References
Synthesis ReferenceNot Available
General References
  1. Papp KA, Krueger JG, Feldman SR, Langley RG, Thaci D, Torii H, Tyring S, Wolk R, Gardner A, Mebus C, Tan H, Luo Y, Gupta P, Mallbris L, Tatulych S: Tofacitinib, an oral Janus kinase inhibitor, for the treatment of chronic plaque psoriasis: Long-term efficacy and safety results from 2 randomized phase-III studies and 1 open-label long-term extension study. J Am Acad Dermatol. 2016 May;74(5):841-850. doi: 10.1016/j.jaad.2016.01.013. Epub 2016 Feb 19. [PubMed:26899199 ]
  2. Link [Link]
External Links
ATC CodesL04AA29
AHFS Codes
  • 92:36
PDB Entries
FDA labelDownload (722 KB)
MSDSDownload (44.7 KB)
Interactions
Drug Interactions
Drug
2-Methoxyethanol2-Methoxyethanol may increase the immunosuppressive activities of Tofacitinib.
9-(2-phosphonylmethoxyethyl)-2,6-diaminopurine9-(2-phosphonylmethoxyethyl)-2,6-diaminopurine may increase the immunosuppressive activities of Tofacitinib.
AbataceptAbatacept may increase the immunosuppressive activities of Tofacitinib.
abetimusabetimus may increase the immunosuppressive activities of Tofacitinib.
AbirateroneThe metabolism of Tofacitinib can be decreased when combined with Abiraterone.
ABR-215757ABR-215757 may increase the immunosuppressive activities of Tofacitinib.
AcebutololTofacitinib may increase the bradycardic activities of Acebutolol.
AdalimumabThe risk or severity of adverse effects can be increased when Adalimumab is combined with Tofacitinib.
AfelimomabThe risk or severity of adverse effects can be increased when Afelimomab is combined with Tofacitinib.
AlefaceptAlefacept may increase the immunosuppressive activities of Tofacitinib.
AlemtuzumabAlemtuzumab may increase the immunosuppressive activities of Tofacitinib.
alicaforsenalicaforsen may increase the immunosuppressive activities of Tofacitinib.
AltretamineAltretamine may increase the immunosuppressive activities of Tofacitinib.
AmiodaroneTofacitinib may increase the bradycardic activities of Amiodarone.
AmiodaroneThe serum concentration of Tofacitinib can be increased when it is combined with Amiodarone.
AmsacrineAmsacrine may increase the immunosuppressive activities of Tofacitinib.
AnakinraAnakinra may increase the immunosuppressive activities of Tofacitinib.
Anti-thymocyte Globulin (Rabbit)Anti-thymocyte Globulin (Rabbit) may increase the immunosuppressive activities of Tofacitinib.
ApremilastApremilast may increase the immunosuppressive activities of Tofacitinib.
AprepitantThe serum concentration of Tofacitinib can be increased when it is combined with Aprepitant.
ArmodafinilThe metabolism of Tofacitinib can be decreased when combined with Armodafinil.
AtazanavirThe serum concentration of Tofacitinib can be increased when it is combined with Atazanavir.
AtenololTofacitinib may increase the bradycardic activities of Atenolol.
AtomoxetineThe metabolism of Tofacitinib can be decreased when combined with Atomoxetine.
AzacitidineAzacitidine may increase the immunosuppressive activities of Tofacitinib.
AzathioprineAzathioprine may increase the immunosuppressive activities of Tofacitinib.
BasiliximabBasiliximab may increase the immunosuppressive activities of Tofacitinib.
BelataceptBelatacept may increase the immunosuppressive activities of Tofacitinib.
BelimumabBelimumab may increase the immunosuppressive activities of Tofacitinib.
BendroflumethiazideTofacitinib may increase the bradycardic activities of Bendroflumethiazide.
BeractantTofacitinib may increase the bradycardic activities of Beractant.
BetamethasoneBetamethasone may increase the immunosuppressive activities of Tofacitinib.
BetaxololTofacitinib may increase the bradycardic activities of Betaxolol.
BexaroteneThe serum concentration of Tofacitinib can be decreased when it is combined with Bexarotene.
BisoprololTofacitinib may increase the bradycardic activities of Bisoprolol.
BleomycinBleomycin may increase the immunosuppressive activities of Tofacitinib.
BlinatumomabBlinatumomab may increase the immunosuppressive activities of Tofacitinib.
BoceprevirThe serum concentration of Tofacitinib can be increased when it is combined with Boceprevir.
BortezomibThe metabolism of Tofacitinib can be decreased when combined with Bortezomib.
BosentanThe serum concentration of Tofacitinib can be decreased when it is combined with Bosentan.
Brentuximab vedotinBrentuximab vedotin may increase the immunosuppressive activities of Tofacitinib.
BriakinumabBriakinumab may increase the immunosuppressive activities of Tofacitinib.
BudesonideBudesonide may increase the immunosuppressive activities of Tofacitinib.
BusulfanBusulfan may increase the immunosuppressive activities of Tofacitinib.
CabazitaxelCabazitaxel may increase the immunosuppressive activities of Tofacitinib.
CalfactantTofacitinib may increase the bradycardic activities of Calfactant.
CanakinumabCanakinumab may increase the immunosuppressive activities of Tofacitinib.
CapecitabineCapecitabine may increase the immunosuppressive activities of Tofacitinib.
CarbamazepineThe serum concentration of Tofacitinib can be decreased when it is combined with Carbamazepine.
CarboplatinCarboplatin may increase the immunosuppressive activities of Tofacitinib.
CarmustineCarmustine may increase the immunosuppressive activities of Tofacitinib.
CarteololTofacitinib may increase the bradycardic activities of Carteolol.
CarvedilolTofacitinib may increase the bradycardic activities of Carvedilol.
CastanospermineCastanospermine may increase the immunosuppressive activities of Tofacitinib.
CeritinibTofacitinib may increase the bradycardic activities of Ceritinib.
CeritinibThe serum concentration of Tofacitinib can be increased when it is combined with Ceritinib.
Certolizumab pegolThe risk or severity of adverse effects can be increased when Certolizumab pegol is combined with Tofacitinib.
ChlorambucilChlorambucil may increase the immunosuppressive activities of Tofacitinib.
ChloramphenicolThe metabolism of Tofacitinib can be decreased when combined with Chloramphenicol.
CholecalciferolThe metabolism of Tofacitinib can be decreased when combined with Cholecalciferol.
CimetidineThe metabolism of Tofacitinib can be decreased when combined with Cimetidine.
CisplatinCisplatin may increase the immunosuppressive activities of Tofacitinib.
CitalopramThe metabolism of Tofacitinib can be decreased when combined with Citalopram.
CladribineCladribine may increase the immunosuppressive activities of Tofacitinib.
ClarithromycinThe serum concentration of Tofacitinib can be increased when it is combined with Clarithromycin.
ClemastineThe metabolism of Tofacitinib can be decreased when combined with Clemastine.
ClofarabineClofarabine may increase the immunosuppressive activities of Tofacitinib.
ClonidineTofacitinib may increase the bradycardic activities of Clonidine.
ClotrimazoleThe metabolism of Tofacitinib can be decreased when combined with Clotrimazole.
ClozapineThe risk or severity of adverse effects can be increased when Tofacitinib is combined with Clozapine.
CobicistatThe serum concentration of Tofacitinib can be increased when it is combined with Cobicistat.
ConivaptanThe serum concentration of Tofacitinib can be increased when it is combined with Conivaptan.
CorticotropinCorticotropin may increase the immunosuppressive activities of Tofacitinib.
Cortisone acetateCortisone acetate may increase the immunosuppressive activities of Tofacitinib.
CrizotinibTofacitinib may increase the bradycardic activities of Crizotinib.
CrizotinibThe metabolism of Tofacitinib can be decreased when combined with Crizotinib.
CyclophosphamideCyclophosphamide may increase the immunosuppressive activities of Tofacitinib.
CyclosporineCyclosporine may increase the immunosuppressive activities of Tofacitinib.
CytarabineCytarabine may increase the immunosuppressive activities of Tofacitinib.
DabrafenibThe serum concentration of Tofacitinib can be decreased when it is combined with Dabrafenib.
DacarbazineDacarbazine may increase the immunosuppressive activities of Tofacitinib.
DaclizumabDaclizumab may increase the immunosuppressive activities of Tofacitinib.
DactinomycinDactinomycin may increase the immunosuppressive activities of Tofacitinib.
DarunavirThe serum concentration of Tofacitinib can be increased when it is combined with Darunavir.
DasatinibDasatinib may increase the immunosuppressive activities of Tofacitinib.
DaunorubicinDaunorubicin may increase the immunosuppressive activities of Tofacitinib.
DeferasiroxThe serum concentration of Tofacitinib can be decreased when it is combined with Deferasirox.
DelavirdineThe metabolism of Tofacitinib can be decreased when combined with Delavirdine.
DenosumabThe risk or severity of adverse effects can be increased when Denosumab is combined with Tofacitinib.
DexamethasoneDexamethasone may increase the immunosuppressive activities of Tofacitinib.
DexmedetomidineTofacitinib may increase the bradycardic activities of Dexmedetomidine.
DigoxinTofacitinib may increase the bradycardic activities of Digoxin.
DihydroergotamineThe metabolism of Tofacitinib can be decreased when combined with Dihydroergotamine.
DiltiazemTofacitinib may increase the bradycardic activities of Diltiazem.
DiltiazemThe metabolism of Tofacitinib can be decreased when combined with Diltiazem.
Dimethyl fumarateDimethyl fumarate may increase the immunosuppressive activities of Tofacitinib.
DinutuximabDinutuximab may increase the immunosuppressive activities of Tofacitinib.
DocetaxelDocetaxel may increase the immunosuppressive activities of Tofacitinib.
DonepezilTofacitinib may increase the bradycardic activities of Donepezil.
DoxorubicinDoxorubicin may increase the immunosuppressive activities of Tofacitinib.
DoxycyclineThe metabolism of Tofacitinib can be decreased when combined with Doxycycline.
DronedaroneTofacitinib may increase the bradycardic activities of Dronedarone.
DronedaroneThe metabolism of Tofacitinib can be decreased when combined with Dronedarone.
EculizumabEculizumab may increase the immunosuppressive activities of Tofacitinib.
EfalizumabEfalizumab may increase the immunosuppressive activities of Tofacitinib.
EfavirenzThe serum concentration of Tofacitinib can be decreased when it is combined with Efavirenz.
EnzalutamideThe serum concentration of Tofacitinib can be decreased when it is combined with Enzalutamide.
EpirubicinEpirubicin may increase the immunosuppressive activities of Tofacitinib.
ErythromycinThe metabolism of Tofacitinib can be decreased when combined with Erythromycin.
Eslicarbazepine acetateThe serum concentration of Tofacitinib can be decreased when it is combined with Eslicarbazepine acetate.
EsmololTofacitinib may increase the bradycardic activities of Esmolol.
EsomeprazoleThe metabolism of Tofacitinib can be decreased when combined with Esomeprazole.
EstramustineEstramustine may increase the immunosuppressive activities of Tofacitinib.
EtanerceptThe risk or severity of adverse effects can be increased when Etanercept is combined with Tofacitinib.
EtoposideEtoposide may increase the immunosuppressive activities of Tofacitinib.
EtravirineThe serum concentration of Tofacitinib can be decreased when it is combined with Etravirine.
EverolimusEverolimus may increase the immunosuppressive activities of Tofacitinib.
FingolimodFingolimod may increase the immunosuppressive activities of Tofacitinib.
FingolimodTofacitinib may increase the bradycardic activities of Fingolimod.
FloxuridineFloxuridine may increase the immunosuppressive activities of Tofacitinib.
FluconazoleThe metabolism of Tofacitinib can be decreased when combined with Fluconazole.
FludarabineFludarabine may increase the immunosuppressive activities of Tofacitinib.
FludrocortisoneFludrocortisone may increase the immunosuppressive activities of Tofacitinib.
FluorouracilFluorouracil may increase the immunosuppressive activities of Tofacitinib.
FluoxetineThe metabolism of Tofacitinib can be decreased when combined with Fluoxetine.
FluvoxamineThe metabolism of Tofacitinib can be decreased when combined with Fluvoxamine.
FosamprenavirThe metabolism of Tofacitinib can be decreased when combined with Fosamprenavir.
FosaprepitantThe serum concentration of Tofacitinib can be increased when it is combined with Fosaprepitant.
FosphenytoinThe serum concentration of Tofacitinib can be decreased when it is combined with Fosphenytoin.
Fusidic AcidThe serum concentration of Tofacitinib can be increased when it is combined with Fusidic Acid.
GalantamineTofacitinib may increase the bradycardic activities of Galantamine.
Gallium nitrateGallium nitrate may increase the immunosuppressive activities of Tofacitinib.
GemcitabineGemcitabine may increase the immunosuppressive activities of Tofacitinib.
GemfibrozilThe metabolism of Tofacitinib can be decreased when combined with Gemfibrozil.
Gemtuzumab ozogamicinGemtuzumab ozogamicin may increase the immunosuppressive activities of Tofacitinib.
Glatiramer AcetateGlatiramer Acetate may increase the immunosuppressive activities of Tofacitinib.
GlimepirideGlimepiride may increase the immunosuppressive activities of Tofacitinib.
GolimumabThe risk or severity of adverse effects can be increased when Golimumab is combined with Tofacitinib.
GuanfacineTofacitinib may increase the bradycardic activities of Guanfacine.
HydrocortisoneHydrocortisone may increase the immunosuppressive activities of Tofacitinib.
HydroxyureaHydroxyurea may increase the immunosuppressive activities of Tofacitinib.
Ibritumomab tiuxetanIbritumomab tiuxetan may increase the immunosuppressive activities of Tofacitinib.
IbrutinibIbrutinib may increase the immunosuppressive activities of Tofacitinib.
IcatibantIcatibant may increase the immunosuppressive activities of Tofacitinib.
IdarubicinIdarubicin may increase the immunosuppressive activities of Tofacitinib.
IdelalisibIdelalisib may increase the immunosuppressive activities of Tofacitinib.
IfosfamideIfosfamide may increase the immunosuppressive activities of Tofacitinib.
ImatinibImatinib may increase the immunosuppressive activities of Tofacitinib.
ImiquimodImiquimod may increase the immunosuppressive activities of Tofacitinib.
IndinavirThe metabolism of Tofacitinib can be decreased when combined with Indinavir.
InfliximabThe risk or severity of adverse effects can be increased when Infliximab is combined with Tofacitinib.
IrinotecanIrinotecan may increase the immunosuppressive activities of Tofacitinib.
IsavuconazoniumThe metabolism of Tofacitinib can be decreased when combined with Isavuconazonium.
IsoniazidThe metabolism of Tofacitinib can be decreased when combined with Isoniazid.
IsradipineThe metabolism of Tofacitinib can be decreased when combined with Isradipine.
ItraconazoleThe serum concentration of Tofacitinib can be increased when it is combined with Itraconazole.
IvabradineTofacitinib may increase the bradycardic activities of Ivabradine.
IvacaftorThe serum concentration of Tofacitinib can be increased when it is combined with Ivacaftor.
KetoconazoleThe metabolism of Tofacitinib can be decreased when combined with Ketoconazole.
L-PhenylalanineL-Phenylalanine may increase the immunosuppressive activities of Tofacitinib.
LabetalolTofacitinib may increase the bradycardic activities of Labetalol.
LanreotideTofacitinib may increase the bradycardic activities of Lanreotide.
LeflunomideThe risk or severity of adverse effects can be increased when Tofacitinib is combined with Leflunomide.
LeflunomideLeflunomide may increase the immunosuppressive activities of Tofacitinib.
LenalidomideLenalidomide may increase the immunosuppressive activities of Tofacitinib.
LevobunololTofacitinib may increase the bradycardic activities of Levobunolol.
LomustineLomustine may increase the immunosuppressive activities of Tofacitinib.
LopinavirThe serum concentration of Tofacitinib can be increased when it is combined with Lopinavir.
LovastatinThe metabolism of Tofacitinib can be decreased when combined with Lovastatin.
LucinactantTofacitinib may increase the bradycardic activities of Lucinactant.
LuliconazoleThe serum concentration of Tofacitinib can be increased when it is combined with Luliconazole.
LumacaftorThe serum concentration of Tofacitinib can be decreased when it is combined with Lumacaftor.
MechlorethamineMechlorethamine may increase the immunosuppressive activities of Tofacitinib.
MelphalanMelphalan may increase the immunosuppressive activities of Tofacitinib.
MepolizumabMepolizumab may increase the immunosuppressive activities of Tofacitinib.
MercaptopurineMercaptopurine may increase the immunosuppressive activities of Tofacitinib.
MetamizoleThe risk or severity of adverse effects can be increased when Metamizole is combined with Tofacitinib.
MethotrexateMethotrexate may increase the immunosuppressive activities of Tofacitinib.
MethyldopaTofacitinib may increase the bradycardic activities of Methyldopa.
MethylprednisoloneMethylprednisolone may increase the immunosuppressive activities of Tofacitinib.
MetipranololTofacitinib may increase the bradycardic activities of Metipranolol.
MetoprololTofacitinib may increase the bradycardic activities of Metoprolol.
MifepristoneThe metabolism of Tofacitinib can be decreased when combined with Mifepristone.
MitomycinMitomycin may increase the immunosuppressive activities of Tofacitinib.
MitotaneThe serum concentration of Tofacitinib can be decreased when it is combined with Mitotane.
MitoxantroneMitoxantrone may increase the immunosuppressive activities of Tofacitinib.
MoclobemideThe metabolism of Tofacitinib can be decreased when combined with Moclobemide.
ModafinilThe serum concentration of Tofacitinib can be decreased when it is combined with Modafinil.
MuromonabMuromonab may increase the immunosuppressive activities of Tofacitinib.
Mycophenolate mofetilMycophenolate mofetil may increase the immunosuppressive activities of Tofacitinib.
Mycophenolic acidMycophenolic acid may increase the immunosuppressive activities of Tofacitinib.
NadololTofacitinib may increase the bradycardic activities of Nadolol.
NafcillinThe serum concentration of Tofacitinib can be decreased when it is combined with Nafcillin.
NatalizumabThe risk or severity of adverse effects can be increased when Tofacitinib is combined with Natalizumab.
NatalizumabNatalizumab may increase the immunosuppressive activities of Tofacitinib.
NebivololTofacitinib may increase the bradycardic activities of Nebivolol.
NefazodoneThe serum concentration of Tofacitinib can be increased when it is combined with Nefazodone.
NelarabineNelarabine may increase the immunosuppressive activities of Tofacitinib.
NelfinavirThe metabolism of Tofacitinib can be decreased when combined with Nelfinavir.
NetupitantThe serum concentration of Tofacitinib can be increased when it is combined with Netupitant.
NevirapineThe serum concentration of Tofacitinib can be decreased when it is combined with Nevirapine.
NicardipineThe metabolism of Tofacitinib can be decreased when combined with Nicardipine.
NilotinibNilotinib may increase the immunosuppressive activities of Tofacitinib.
ObinutuzumabObinutuzumab may increase the immunosuppressive activities of Tofacitinib.
OctreotideTofacitinib may increase the bradycardic activities of Octreotide.
OlaparibThe metabolism of Tofacitinib can be decreased when combined with Olaparib.
OmeprazoleThe metabolism of Tofacitinib can be decreased when combined with Omeprazole.
OsimertinibThe serum concentration of Tofacitinib can be increased when it is combined with Osimertinib.
OxaliplatinOxaliplatin may increase the immunosuppressive activities of Tofacitinib.
PaclitaxelPaclitaxel may increase the immunosuppressive activities of Tofacitinib.
PalbociclibPalbociclib may increase the immunosuppressive activities of Tofacitinib.
PanobinostatPanobinostat may increase the immunosuppressive activities of Tofacitinib.
PantoprazoleThe metabolism of Tofacitinib can be decreased when combined with Pantoprazole.
PasireotideTofacitinib may increase the bradycardic activities of Pasireotide.
PazopanibPazopanib may increase the immunosuppressive activities of Tofacitinib.
PegaspargasePegaspargase may increase the immunosuppressive activities of Tofacitinib.
PemetrexedPemetrexed may increase the immunosuppressive activities of Tofacitinib.
PenbutololTofacitinib may increase the bradycardic activities of Penbutolol.
PentobarbitalThe serum concentration of Tofacitinib can be decreased when it is combined with Pentobarbital.
PentostatinPentostatin may increase the immunosuppressive activities of Tofacitinib.
PhenobarbitalThe serum concentration of Tofacitinib can be decreased when it is combined with Phenobarbital.
PhenytoinThe serum concentration of Tofacitinib can be decreased when it is combined with Phenytoin.
PimecrolimusThe risk or severity of adverse effects can be increased when Pimecrolimus is combined with Tofacitinib.
PindololTofacitinib may increase the bradycardic activities of Pindolol.
PirfenidoneThe risk or severity of adverse effects can be increased when Pirfenidone is combined with Tofacitinib.
PomalidomidePomalidomide may increase the immunosuppressive activities of Tofacitinib.
Poractant alfaTofacitinib may increase the bradycardic activities of Poractant alfa.
PosaconazoleThe serum concentration of Tofacitinib can be increased when it is combined with Posaconazole.
PralatrexatePralatrexate may increase the immunosuppressive activities of Tofacitinib.
PrednisolonePrednisolone may increase the immunosuppressive activities of Tofacitinib.
PrednisonePrednisone may increase the immunosuppressive activities of Tofacitinib.
PrimidoneThe serum concentration of Tofacitinib can be decreased when it is combined with Primidone.
ProcarbazineProcarbazine may increase the immunosuppressive activities of Tofacitinib.
PropafenoneTofacitinib may increase the bradycardic activities of Propafenone.
PropranololTofacitinib may increase the bradycardic activities of Propranolol.
Rabies vaccineThe risk or severity of adverse effects can be increased when Tofacitinib is combined with Rabies vaccine.
RanolazineThe metabolism of Tofacitinib can be decreased when combined with Ranolazine.
RifabutinThe serum concentration of Tofacitinib can be decreased when it is combined with Rifabutin.
RifampicinThe serum concentration of Tofacitinib can be decreased when it is combined with Rifampicin.
RifapentineThe serum concentration of Tofacitinib can be decreased when it is combined with Rifapentine.
RilonaceptRilonacept may increase the immunosuppressive activities of Tofacitinib.
RitonavirThe serum concentration of Tofacitinib can be increased when it is combined with Ritonavir.
RituximabRituximab may increase the immunosuppressive activities of Tofacitinib.
RivastigmineTofacitinib may increase the bradycardic activities of Rivastigmine.
RoflumilastRoflumilast may increase the immunosuppressive activities of Tofacitinib.
RuxolitinibRuxolitinib may increase the immunosuppressive activities of Tofacitinib.
SaquinavirThe serum concentration of Tofacitinib can be increased when it is combined with Saquinavir.
SecukinumabSecukinumab may increase the immunosuppressive activities of Tofacitinib.
SeocalcitolSeocalcitol may increase the immunosuppressive activities of Tofacitinib.
SertralineThe metabolism of Tofacitinib can be decreased when combined with Sertraline.
SildenafilThe metabolism of Tofacitinib can be decreased when combined with Sildenafil.
SiltuximabSiltuximab may increase the immunosuppressive activities of Tofacitinib.
SimeprevirThe serum concentration of Tofacitinib can be increased when it is combined with Simeprevir.
Sipuleucel-TThe therapeutic efficacy of Sipuleucel-T can be decreased when used in combination with Tofacitinib.
SirolimusSirolimus may increase the immunosuppressive activities of Tofacitinib.
SitaxentanThe serum concentration of Tofacitinib can be increased when it is combined with Sitaxentan.
SorafenibSorafenib may increase the immunosuppressive activities of Tofacitinib.
SotalolTofacitinib may increase the bradycardic activities of Sotalol.
St. John's WortThe serum concentration of Tofacitinib can be decreased when it is combined with St. John's Wort.
SteproninStepronin may increase the immunosuppressive activities of Tofacitinib.
StiripentolThe serum concentration of Tofacitinib can be increased when it is combined with Stiripentol.
StreptozocinStreptozocin may increase the immunosuppressive activities of Tofacitinib.
SufentanilTofacitinib may increase the bradycardic activities of Sufentanil.
SulfisoxazoleThe metabolism of Tofacitinib can be decreased when combined with Sulfisoxazole.
SunitinibSunitinib may increase the immunosuppressive activities of Tofacitinib.
TacrolimusThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Tofacitinib.
TelaprevirThe serum concentration of Tofacitinib can be increased when it is combined with Telaprevir.
TelithromycinThe serum concentration of Tofacitinib can be increased when it is combined with Telithromycin.
TemozolomideTemozolomide may increase the immunosuppressive activities of Tofacitinib.
TemsirolimusTemsirolimus may increase the immunosuppressive activities of Tofacitinib.
TeniposideTeniposide may increase the immunosuppressive activities of Tofacitinib.
TepoxalinTepoxalin may increase the immunosuppressive activities of Tofacitinib.
TeriflunomideTeriflunomide may increase the immunosuppressive activities of Tofacitinib.
ThalidomideThalidomide may increase the immunosuppressive activities of Tofacitinib.
ThiotepaThiotepa may increase the immunosuppressive activities of Tofacitinib.
TiclopidineThe metabolism of Tofacitinib can be decreased when combined with Ticlopidine.
TimololTofacitinib may increase the bradycardic activities of Timolol.
TioguanineTioguanine may increase the immunosuppressive activities of Tofacitinib.
TizanidineTofacitinib may increase the bradycardic activities of Tizanidine.
TocilizumabTocilizumab may increase the immunosuppressive activities of Tofacitinib.
TopiramateThe metabolism of Tofacitinib can be decreased when combined with Topiramate.
TopotecanTopotecan may increase the immunosuppressive activities of Tofacitinib.
TositumomabTositumomab may increase the immunosuppressive activities of Tofacitinib.
TrabectedinTrabectedin may increase the immunosuppressive activities of Tofacitinib.
TranylcypromineThe metabolism of Tofacitinib can be decreased when combined with Tranylcypromine.
TrastuzumabTrastuzumab may increase the neutropenic activities of Tofacitinib.
Trastuzumab emtansineTrastuzumab emtansine may increase the immunosuppressive activities of Tofacitinib.
TretinoinTretinoin may increase the immunosuppressive activities of Tofacitinib.
TriamcinoloneTriamcinolone may increase the immunosuppressive activities of Tofacitinib.
UstekinumabUstekinumab may increase the immunosuppressive activities of Tofacitinib.
VedolizumabVedolizumab may increase the immunosuppressive activities of Tofacitinib.
VenlafaxineThe metabolism of Tofacitinib can be decreased when combined with Venlafaxine.
VerapamilTofacitinib may increase the bradycardic activities of Verapamil.
VerapamilThe metabolism of Tofacitinib can be decreased when combined with Verapamil.
VilanterolVilanterol may increase the immunosuppressive activities of Tofacitinib.
VinblastineVinblastine may increase the immunosuppressive activities of Tofacitinib.
VincristineVincristine may increase the immunosuppressive activities of Tofacitinib.
VindesineVindesine may increase the immunosuppressive activities of Tofacitinib.
VinorelbineVinorelbine may increase the immunosuppressive activities of Tofacitinib.
VoriconazoleThe metabolism of Tofacitinib can be decreased when combined with Voriconazole.
ZiprasidoneThe metabolism of Tofacitinib can be decreased when combined with Ziprasidone.
Food InteractionsNot Available

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
antagonistinhibitor
General Function:
Sh2 domain binding
Specific Function:
Non-receptor tyrosine kinase involved in various processes such as cell growth, development, differentiation or histone modifications. Mediates essential signaling events in both innate and adaptive immunity. In the cytoplasm, plays a pivotal role in signal transduction via its association with type I receptors such as growth hormone (GHR), prolactin (PRLR), leptin (LEPR), erythropoietin (EPOR)...
Gene Name:
JAK2
Uniprot ID:
O60674
Molecular Weight:
130672.475 Da
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
inhibitor
General Function:
Ubiquitin protein ligase binding
Specific Function:
Tyrosine kinase of the non-receptor type, involved in the IFN-alpha/beta/gamma signal pathway. Kinase partner for the interleukin (IL)-2 receptor.
Gene Name:
JAK1
Uniprot ID:
P23458
Molecular Weight:
133275.995 Da
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
inhibitor
General Function:
Protein tyrosine kinase activity
Specific Function:
Non-receptor tyrosine kinase involved in various processes such as cell growth, development, or differentiation. Mediates essential signaling events in both innate and adaptive immunity and plays a crucial role in hematopoiesis during T-cells development. In the cytoplasm, plays a pivotal role in signal transduction via its association with type I receptors sharing the common subunit gamma such...
Gene Name:
JAK3
Uniprot ID:
P52333
Molecular Weight:
125097.565 Da

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
no
Actions
substrate
General Function:
Vitamin d3 25-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 performs a variety of oxidation reactions (e.g. caffeine 8-oxidation, omeprazole sulphoxidation, midazolam 1'-hydroxylation and midazolam 4-hydroxylation) of structurally unrelated compounds, including steroids, fatty acids, and xenobiot...
Gene Name:
CYP3A4
Uniprot ID:
P08684
Molecular Weight:
57342.67 Da
Kind
Protein
Organism
Human
Pharmacological action
no
Actions
substrate
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

Carriers

Kind
Protein
Organism
Human
Pharmacological action
unknown
General Function:
Toxic substance binding
Specific Function:
Serum albumin, the main protein of plasma, has a good binding capacity for water, Ca(2+), Na(+), K(+), fatty acids, hormones, bilirubin and drugs. Its main function is the regulation of the colloidal osmotic pressure of blood. Major zinc transporter in plasma, typically binds about 80% of all plasma zinc.
Gene Name:
ALB
Uniprot ID:
P02768
Molecular Weight:
69365.94 Da
Comments
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Drug created on June 03, 2013 14:44 / Updated on September 25, 2016 02:51