Identification
- Summary
Tofacitinib is a Janus kinase (JAK) inhibitor used to treat rheumatic conditions, such as rheumatoid arthritis and ankylosing spondylitis, and ulcerative colitis.
- Brand Names
- Xeljanz
- Generic Name
- Tofacitinib
- DrugBank Accession Number
- DB08895
- Background
Tofacitinib 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.
- Type
- Small Molecule
- Groups
- Approved, Investigational
- Structure
Structure for Tofacitinib (DB08895)
- Weight
- Average: 312.3696
Monoisotopic: 312.169859292 - Chemical Formula
- C16H20N6O
- Synonyms
- Tasocitinib
- Tofacitinib
- Tofacitinibum
- External IDs
- CP 690550
- CP- 690 550
- CP-690 free base
- CP-690-550
- CP-690,550
- CP-690,550 free base
- CP-690550
- CP-690550 free base
- CP690,550
- CP690550
Pharmacology
- Indication
Tofacitinib is indicated for the treatment of adult patients with moderately-to-severely active rheumatoid arthritis (RA), active psoriatic arthritis, active ankylosing spondylitis, or moderately-to-severely active ulcerative colitis who have had an inadequate response or intolerance to one or more TNF blockers.5 It is also indicated as an oral solution in patients ≥2 years of age for the treatment of polyarticular course juvenile idiopathic arthritis who have had an inadequate response or intolerance to one or more TNF blockers.5
Tofacitinib is not recommended to be used in combination with other biologic disease-modifying anti-rheumatic drugs (DMARDs) or potent immunosuppressive agents such as azathioprine or cyclosporine.5
Reduce drug development failure ratesBuild, train, & validate machine-learning modelswith evidence-based and structured datasets.Build, train, & validate predictive machine-learning models with structured datasets.- Associated Conditions
Indication Type Indication Combined Product Details Approval Level Age Group Patient Characteristics Dose Form Management of Moderate to severe ulcerative colitis •••••••••••• ••••• •••••••••• •••••••• •• ••••••••••• •• ••• •••••••• ••••••••• ••••••• ••••••• •••••••• ••••••• Treatment of Polyarticular-course juvenile idiopathic arthritis (jia) •••••••••••• ••••••••• •••••• Management of Psoriatic arthritis •••••••••••• ••••• •••••••••• •••••••• •• ••••••••••• •• •••••• ••••••••• ••••••• ••••••• •••••••• ••••••• Management of Active ankylosing spondylitis •••••••••••• ••••• •••••••••• •••••••• •• •••••••••••• ••••••• ••••••••• ••••••• ••••••• •••••••• ••••••• Management of Moderate rheumatoid arthritis •••••••••••• ••••• •••••••••• •• ••••••••••••• •••••••••••• •••••••• •• •••••••••••• ••••••••• ••••••• ••••••• •••••••• ••••••• - Contraindications & Blackbox Warnings
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Tofacitinib 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 action
Rheumatoid 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.
Target Actions Organism ATyrosine-protein kinase JAK1 inhibitorHumans ATyrosine-protein kinase JAK2 antagonistinhibitorHumans ATyrosine-protein kinase JAK3 inhibitorHumans UNon-receptor tyrosine-protein kinase TYK2 Not Available Humans - Absorption
74% 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 binding
40%, mostly bound to albumin.
- Metabolism
Metabolized in the liver by CYP3A4 and CYP2C19. Metabolites produced are inactive.
- Route of elimination
70% metabolized in the liver by CYP3A4 (major) and CYP2C19 (minor). Metabolites produced are inactive. 30% renally eliminated as unchanged drug.
- Half-life
~3 hours
- Clearance
Not Available
- Adverse Effects
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Minimum 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.
- Pathways
- Not Available
- Pharmacogenomic Effects/ADRs Browse all" title="About SNP Mediated Effects/ADRs" id="snp-actions-info" class="drug-info-popup" href="javascript:void(0);">
- Not Available
Interactions
- Drug Interactions Learn More" title="About Drug Interactions" id="structured-interactions-info" class="drug-info-popup" href="javascript:void(0);">
- This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
Drug Interaction Integrate drug-drug
interactions in your softwareAbametapir The serum concentration of Tofacitinib can be increased when it is combined with Abametapir. Abatacept The risk or severity of adverse effects can be increased when Abatacept is combined with Tofacitinib. Abciximab The risk or severity of bleeding can be increased when Abciximab is combined with Tofacitinib. Acalabrutinib The metabolism of Tofacitinib can be decreased when combined with Acalabrutinib. Acebutolol Acebutolol may increase the bradycardic activities of Tofacitinib. - Food Interactions
- Avoid grapefruit products. Dose adjustments are required when administering CYP3A4 inhibitors (grapefruit) and CYP2C19 inhibitors with tofacitinib.
- Avoid St. John's Wort. This herb induces the CYP3A4 metabolism of tofacitinib and may reduce its serum concentration.
- Take with or without food.
Products
Drug product information from 10+ global regionsOur datasets provide approved product information including:dosage, form, labeller, route of administration, and marketing period.Access drug product information from over 10 global regions.- Product Ingredients
Ingredient UNII CAS InChI Key Tofacitinib citrate O1FF4DIV0D 540737-29-9 SYIKUFDOYJFGBQ-YLAFAASESA-N - Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Xeljanz Tablet, film coated 5 mg Oral Pfizer Europe Ma Eeig 2021-01-27 Not applicable EU 
Xeljanz Tablet, extended release 11 mg Oral Pfizer Europe Ma Eeig 2021-01-27 Not applicable EU Xeljanz Tablet 5 mg Oral Pfizer Canada Ulc 2014-06-03 Not applicable Canada 
Xeljanz Tablet, film coated 10 mg Oral Pfizer Europe Ma Eeig 2021-01-27 Not applicable EU Xeljanz Tablet, film coated 10 mg/1 Oral Pfizer Laboratories Div Pfizer Inc 2018-07-02 Not applicable US 
- Generic Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Apo-tofacitinib Tablet 5 mg Oral Apotex Corporation Not applicable Not applicable Canada Apo-tofacitinib Tablet 10 mg Oral Apotex Corporation Not applicable Not applicable Canada Auro-tofacitinib Tablet 10 mg Oral Auro Pharma Inc 2022-11-28 Not applicable Canada Auro-tofacitinib Tablet 5 mg Oral Auro Pharma Inc 2022-11-28 Not applicable Canada Jamp Tofacitinib Tablet 5 mg Oral Jamp Pharma Corporation 2023-10-20 Not applicable Canada
Categories
- ATC Codes
- L04AA29 — Tofacitinib
- Drug Categories
- Antineoplastic and Immunomodulating Agents
- Antirheumatic Agents
- Biologics for Rheumatoid Arthritis Treatment
- Bradycardia-Causing Agents
- Cytochrome P-450 CYP2C19 Substrates
- Cytochrome P-450 CYP3A Substrates
- Cytochrome P-450 CYP3A4 Substrates
- Cytochrome P-450 Substrates
- Disease-modifying Antirheumatic Agents
- Enzyme Inhibitors
- Immunosuppressive Agents
- Janus Kinase 3, antagonists & inhibitors
- Janus Kinase Inhibitor
- Janus Kinase Inhibitors
- Janus Kinases, antagonists & inhibitors
- Myelosuppressive Agents
- Protein Kinase Inhibitors
- Selective Immunosuppressants
- Chemical TaxonomyProvided by Classyfire
- Description
- This compound belongs to the class of organic compounds known as n-acylpiperidines. These are compounds containing an N-acyethanolamine moiety, which is characterized by an acyl group is linked to the nitrogen atom of a piperidine.
- Kingdom
- Organic compounds
- Super Class
- Organoheterocyclic compounds
- Class
- Piperidines
- Sub Class
- N-acylpiperidines
- Direct Parent
- N-acylpiperidines
- Alternative Parents
- Pyrrolo[2,3-d]pyrimidines / Dialkylarylamines / Aminopyrimidines and derivatives / Aminopiperidines / Imidolactams / Tertiary carboxylic acid amides / Pyrroles / Heteroaromatic compounds / Nitriles / Azacyclic compounds show 4 more
- Substituents
- 3-aminopiperidine / Aminopyrimidine / Aromatic heteropolycyclic compound / Azacycle / Carbonitrile / Carbonyl group / Carboxamide group / Carboxylic acid derivative / Dialkylarylamine / Heteroaromatic compound show 15 more
- Molecular Framework
- Aromatic heteropolycyclic compounds
- External Descriptors
- tertiary amino compound, N-acylpiperidine, nitrile, pyrrolopyrimidine (CHEBI:71200)
- Affected organisms
- Humans and other mammals
Chemical Identifiers
- UNII
- 87LA6FU830
- CAS number
- 477600-75-2
- InChI Key
- UJLAWZDWDVHWOW-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
- C[C@@H]1CCN(C[C@@H]1N(C)C1=NC=NC2=C1C=CN2)C(=O)CC#N
References
- General References
- 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. [Article]
- Link [Link]
- BusinessWire: U.S. FDA Approves Pfizer’s XELJANZ® (tofacitinib) for the Treatment of Active Polyarticular Course Juvenile Idiopathic Arthritis [Link]
- BioSpace: XELJANZ for the treatment of Ankylosing Spondylitis [Link]
- FDA Approved Drug Products: Xeljanz (Tofacitinib) Oral Solution, Tablets, and Extended Release Tablets [Link]
- External Links
- KEGG Drug
- D09970
- PubChem Compound
- 9926791
- PubChem Substance
- 347827811
- ChemSpider
- 8102425
- BindingDB
- 50193995
- 1357536
- ChEBI
- 71200
- ChEMBL
- CHEMBL221959
- ZINC
- ZINC000003818808
- PDBe Ligand
- MI1
- RxList
- RxList Drug Page
- Drugs.com
- Drugs.com Drug Page
- PDRhealth
- PDRhealth Drug Page
- Wikipedia
- Tofacitinib
- PDB Entries
- 3eyg / 3fup / 3lxn / 4oti
- FDA label
- Download (722 KB)
- MSDS
- Download (44.7 KB)
Clinical Trials
- Clinical Trials Learn More" title="About Clinical Trials" id="clinical-trials-info" class="drug-info-popup" href="javascript:void(0);">
Phase Status Purpose Conditions Count 4 Completed Treatment Alopecia Areata (AA) 1 4 Completed Treatment Rheumatoid Arthritis 5 4 Not Yet Recruiting Treatment Axial Spondyloarthritis (AxSpA) 1 4 Not Yet Recruiting Treatment Rheumatoid Arthritis 1 4 Not Yet Recruiting Treatment Ulcerative Colitis 1
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage Forms
Form Route Strength Solution Oral 1 mg/1mL Solution Oral 1 MG/ML Tablet Oral 10 mg Tablet Oral 11 MG Tablet Oral 5 mg Tablet Oral 8.078 mg Tablet, film coated Oral 10 mg/1 Tablet, film coated Oral 10 MG Tablet, film coated Oral 5 MG Tablet, film coated Oral 5 mg/1 Tablet, film coated Oral Tablet, film coated Oral 8.078 mg Tablet, extended release Oral 11 mg Tablet, extended release Oral 11 mg/1 Tablet, extended release Oral 22 mg/1 Tablet, film coated, extended release Oral 11 mg/1 Tablet, film coated, extended release Oral 22 mg/1 Tablet, film coated, extended release Oral 11 mg Tablet, delayed release Oral 11 mg Tablet, delayed release Oral 1100000 mg Tablet, coated Oral 5 mg - Prices
- Not Available
- Patents
Patent Number Pediatric Extension Approved Expires (estimated) Region US7091208 No 2006-08-15 2020-12-08 US US6965027 No 2005-11-15 2023-03-25 US USRE41783 No 2010-09-28 2020-12-08 US US7265221 No 2007-09-04 2020-12-08 US US6956041 No 2005-10-18 2020-12-08 US US7301023 No 2007-11-27 2022-05-23 US US6956027 No 2005-10-18 2023-03-25 US US9937181 No 2018-04-10 2034-03-14 US US7842699 No 2010-11-30 2020-12-08 US US10639309 No 2020-05-05 2034-03-14 US US11253523 No 2014-03-14 2034-03-14 US
Properties
- State
- Solid
- Experimental Properties
Property Value Source logP 1.808 MSDS, Tofacitinib Citrate - Predicted Properties
Property Value Source Water Solubility 0.299 mg/mL ALOGPS logP 1.58 ALOGPS logP 1.24 Chemaxon logS -3 ALOGPS pKa (Strongest Acidic) 9.15 Chemaxon pKa (Strongest Basic) 6.44 Chemaxon Physiological Charge 1 Chemaxon Hydrogen Acceptor Count 5 Chemaxon Hydrogen Donor Count 1 Chemaxon Polar Surface Area 88.91 Å2 Chemaxon Rotatable Bond Count 3 Chemaxon Refractivity 87.8 m3·mol-1 Chemaxon Polarizability 32.38 Å3 Chemaxon Number of Rings 3 Chemaxon Bioavailability 1 Chemaxon Rule of Five Yes Chemaxon Ghose Filter Yes Chemaxon Veber's Rule No Chemaxon MDDR-like Rule No Chemaxon - Predicted ADMET Features
Property Value Probability Human Intestinal Absorption + 0.9897 Blood Brain Barrier + 0.9568 Caco-2 permeable + 0.5154 P-glycoprotein substrate Substrate 0.6524 P-glycoprotein inhibitor I Inhibitor 0.7609 P-glycoprotein inhibitor II Inhibitor 0.8898 Renal organic cation transporter Inhibitor 0.6368 CYP450 2C9 substrate Non-substrate 0.8246 CYP450 2D6 substrate Non-substrate 0.723 CYP450 3A4 substrate Substrate 0.7649 CYP450 1A2 substrate Non-inhibitor 0.734 CYP450 2C9 inhibitor Non-inhibitor 0.8014 CYP450 2D6 inhibitor Non-inhibitor 0.9537 CYP450 2C19 inhibitor Non-inhibitor 0.8036 CYP450 3A4 inhibitor Non-inhibitor 0.9307 CYP450 inhibitory promiscuity Low CYP Inhibitory Promiscuity 0.7937 Ames test Non AMES toxic 0.5492 Carcinogenicity Non-carcinogens 0.9032 Biodegradation Not ready biodegradable 0.9956 Rat acute toxicity 2.7249 LD50, mol/kg Not applicable hERG inhibition (predictor I) Weak inhibitor 0.5995 hERG inhibition (predictor II) Inhibitor 0.7324
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
Spectrum Spectrum Type Splash Key Predicted MS/MS Spectrum - 10V, Positive (Annotated) Predicted LC-MS/MS splash10-0002-0093000000-b23dc070d9ff1a022034 Predicted MS/MS Spectrum - 10V, Negative (Annotated) Predicted LC-MS/MS splash10-01ox-1196000000-e377644cabf3b2c6f277 Predicted MS/MS Spectrum - 20V, Positive (Annotated) Predicted LC-MS/MS splash10-0002-2492000000-83cd627c567ff5d53a6e Predicted MS/MS Spectrum - 20V, Negative (Annotated) Predicted LC-MS/MS splash10-002g-0791000000-b81308a30b541ad3612e Predicted MS/MS Spectrum - 40V, Positive (Annotated) Predicted LC-MS/MS splash10-0002-9581000000-d392c6e5e4523f88366a Predicted MS/MS Spectrum - 40V, Negative (Annotated) Predicted LC-MS/MS splash10-00ls-4930000000-eeb3707934d886835da1 Predicted 1H NMR Spectrum 1D NMR Not Applicable Predicted 13C NMR Spectrum 1D NMR Not Applicable - Chromatographic Properties
Collision Cross Sections (CCS)
Adduct CCS Value (Å2) Source type Source [M-H]- 167.35583 predictedDeepCCS 1.0 (2019) [M+H]+ 169.71384 predictedDeepCCS 1.0 (2019) [M+Na]+ 175.95518 predictedDeepCCS 1.0 (2019)
Targets
- Kind
- Protein
- Organism
- Humans
- 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
- Uniprot Name
- Tyrosine-protein kinase JAK1
- Molecular Weight
- 133275.995 Da
References
- Berman HM, Westbrook J, Feng Z, Gilliland G, Bhat TN, Weissig H, Shindyalov IN, Bourne PE: The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42. [Article]
- Kind
- Protein
- Organism
- Humans
- 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 adaptiv...
- Gene Name
- JAK2
- Uniprot ID
- O60674
- Uniprot Name
- Tyrosine-protein kinase JAK2
- Molecular Weight
- 130672.475 Da
References
- Berman HM, Westbrook J, Feng Z, Gilliland G, Bhat TN, Weissig H, Shindyalov IN, Bourne PE: The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42. [Article]
- Kind
- Protein
- Organism
- Humans
- 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...
- Gene Name
- JAK3
- Uniprot ID
- P52333
- Uniprot Name
- Tyrosine-protein kinase JAK3
- Molecular Weight
- 125097.565 Da
References
- Berman HM, Westbrook J, Feng Z, Gilliland G, Bhat TN, Weissig H, Shindyalov IN, Bourne PE: The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- General Function
- Protein tyrosine kinase activity
- Specific Function
- Probably involved in intracellular signal transduction by being involved in the initiation of type I IFN signaling. Phosphorylates the interferon-alpha/beta receptor alpha chain.
- Gene Name
- TYK2
- Uniprot ID
- P29597
- Uniprot Name
- Non-receptor tyrosine-protein kinase TYK2
- Molecular Weight
- 133648.77 Da
References
- Berman HM, Westbrook J, Feng Z, Gilliland G, Bhat TN, Weissig H, Shindyalov IN, Bourne PE: The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42. [Article]
Enzymes
- Kind
- Protein
- Organism
- Humans
- 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 react...
- Gene Name
- CYP3A4
- Uniprot ID
- P08684
- Uniprot Name
- Cytochrome P450 3A4
- Molecular Weight
- 57342.67 Da
- Kind
- Protein
- Organism
- Humans
- 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 im...
- Gene Name
- CYP2C19
- Uniprot ID
- P33261
- Uniprot Name
- Cytochrome P450 2C19
- Molecular Weight
- 55930.545 Da
Carriers
- Kind
- Protein
- Organism
- Humans
- 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 colloid...
- Gene Name
- ALB
- Uniprot ID
- P02768
- Uniprot Name
- Serum albumin
- Molecular Weight
- 69365.94 Da
Drug created at June 03, 2013 20:44 / Updated at February 20, 2024 23:55