Identification
- Summary
Ponesimod is a sphingosine 1-phosphate receptor modulator indicated to treat relapsing multiple sclerosis.
- Brand Names
- Ponvory
- Generic Name
- Ponesimod
- DrugBank Accession Number
- DB12016
- Background
Ponesimod is a selective sphingosine 1-phosphate receptor 1 modulator indicated in the treatment of relapsing forms of multiple sclerosis in adults.1,3 Ponesimod was developed out of a need for a more selective modulator of sphingosine 1-phosphate receptor 1 than fingolimod.1 Fingolimod's activity at sphingosine 1-phosphate receptor 3 was suspected to be responsible for a portion of it's adverse effects, and so more selective modulators were developed.1
Ponesimod was granted FDA approval on 18 March 2021.3
- Type
- Small Molecule
- Groups
- Approved, Investigational
- Structure
Structure for Ponesimod (DB12016)
- Weight
- Average: 460.97
Monoisotopic: 460.1223562 - Chemical Formula
- C23H25ClN2O4S
- Synonyms
- Ponesimod
- External IDs
- ACT 128800
- ACT-128800
- ACT128800
Pharmacology
- Indication
Ponesimod is indicated to treat adults with relapsing forms of multiple sclerosis, including clinically isolated syndrome, relapsing-remitting disease, and active secondary progressive disease.3
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 Treatment of Active secondary progressive multiple sclerosis •••••••••••• ••••• •••••• Treatment of Relapsing multiple sclerosis (rms) •••••••••••• ••••• •••••• Treatment of Relapsing multiple sclerosis (rms) •••••••••••• ••••• •••••••••• •••••••• •••••••• ••••• •••••• Treatment of Relapsing remitting multiple sclerosis (rrms) •••••••••••• ••••• •••••• - Contraindications & Blackbox Warnings
Prevent Adverse Drug Events TodayTap into our Clinical API for life-saving information on contraindications & blackbox warnings, population restrictions, harmful risks, & more.Avoid life-threatening adverse drug events with our Clinical API- Pharmacodynamics
Ponesimod is a sphingosine 1-phosphate receptor 1 modulator indicated to treat adults with relapsing forms of multiple sclerosis.3 It has a long duration of action as it is given once daily.3 Patients should be counselled about the risk of infections, bradyarrhythmia, atrioventricular conduction delays, decreased respiratory function, liver injury, increased blood pressure, cutaneous malignancies, fetal harm, and macular edema.3
- Mechanism of action
The sphingosine 1-phosphate receptor 1 (S1P1R) is expressed on the surface of lymphocytes and detects sphingosine 1-phosphate (S1P) at nanomolar concentrations.2 S1P is a metabolite of the cell membrane component, sphingomyelin.2 As sphingomyelin degrades, lymphocytes respond to agonism of S1P1R by concentration gradients of S1P.2 Lymphocytes leave the lymphoid organs in response to higher concentrations of S1P in blood and lymph.2 Ponesimod modulates this response by stimulating and internalizing S1P1R on lymphocytes, effectively blinding them to concentration gradients of S1P, reducing the number of lymphocytes in blood.2,3 Ponesimod is roughly 650 times more selective for S1P1R than S1P.2
Target Actions Organism ASphingosine 1-phosphate receptor 1 agonistmodulatorregulatorHumans - Absorption
A 10mg oral dose of ponesimod is 84% bioavailable.3 Ponesimod reaches a Cmax of 109 ng/mL, with a Tmax of 4.0 hours, and an AUC of 3872 h*ng/mL.1
- Volume of distribution
The volume of distribution of ponesimod at steady state is 160 L.3
- Protein binding
Ponesimod is >99% protein bound in plasma.3 Though the proteins it binds to have not been identified in literature.3
- Metabolism
Ponesimod can be sulfated to the M5 metabolite, oxidized to an undefined M27 metabolite, reduced to the M6 metabolite, dealkylated to the M32 metabolite, or oxidized and hydrolyzed to the M13 metabolite.1,3 Ponesimod can also be oxidized by CYP2J2, CYP3A4, CYP3A5, CYP4F3A, and CYP4F12 to the M12 metabolite.1,3 The undefined M27 metabolite can be glucuronidated by UGT1A1 and UGT 2B7 to the M38, M39, and M40 metabolites.1,3 The M12 metabolite is either dealkylated to the M32 metabolite or oxidized and hydrolyzed to M13.1 M13 is dealkylated to M32, which is reduced and oxidized to M48.1
Hover over products below to view reaction partners
- Route of elimination
57.3-79.6% of a radiolabelled oral dose is recovered in the feces, with 16-26% as the unmetabolized parent compound and 22% as the M12 metabolite.1,3 10.3-18.4% of an oral dose is eliminated in the urine.1,3 0.6-1.9% of a radiolabelled dose was recovered as expired CO2.1
- Half-life
Ponesimod has an elimination half life of 33 hours.3
- Clearance
The clearance of ponesimod is 3.8 L/h.3
- Adverse Effects
Improve decision support & research outcomesWith structured adverse effects data, including: blackbox warnings, adverse reactions, warning & precautions, & incidence rates. View sample adverse effects data in our new Data Library!Improve decision support & research outcomes with our structured adverse effects data.- Toxicity
Patients experiencing an overdose may present with bradycardia, AV conduction block, and changes in blood pressure.3 Patients should be monitored for pulse rate and blood pressure, as well as ECGs.3 Treat patients with symptomatic and supportive measures, which may include atropine for bradycardia.3 dialysis is not expected to remove a significant amount of drug from blood.3
- Pathways
- Not Available
- Pharmacogenomic Effects/ADRs
- Not Available
Interactions
- Drug Interactions
- 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 Ponesimod can be increased when it is combined with Abametapir. Abatacept The metabolism of Ponesimod can be increased when combined with Abatacept. Acalabrutinib The metabolism of Ponesimod can be decreased when combined with Acalabrutinib. Acebutolol The risk or severity of bradycardia can be increased when Ponesimod is combined with Acebutolol. Acrivastine The risk or severity of bradycardia can be increased when Ponesimod is combined with Acrivastine. - Food Interactions
- Take with or without food. The absorption of ponesimod is not significantly affected by 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.- International/Other Brands
- Ponvory (Janssen)
- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Ponvory Tablet, film coated 20 mg Oral Janssen Cilag International Nv 2022-05-04 Not applicable EU 
Ponvory Tablet 20 mg Oral Janssen Pharmaceuticals 2021-11-01 Not applicable Canada 
Ponvory Tablet, film coated 20 mg Oral Janssen Cilag International Nv 2022-05-04 Not applicable EU Ponvory Tablet, film coated 20 mg/1 Oral Janssen Pharmaceuticals, Inc 2021-03-18 Not applicable US 
- Mixture Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image Ponvory Ponesimod (10 mg) + Ponesimod (2 mg) + Ponesimod (3 mg) + Ponesimod (4 mg) + Ponesimod (5 mg) + Ponesimod (6 mg) + Ponesimod (7 mg) + Ponesimod (8 mg) + Ponesimod (9 mg) Tablet Oral Janssen Pharmaceuticals 2021-11-01 Not applicable Canada Ponvory Ponesimod (2 mg/1) + Ponesimod (3 mg/1) + Ponesimod (4 mg/1) + Ponesimod (5 mg/1) + Ponesimod (6 mg/1) + Ponesimod (7 mg/1) + Ponesimod (8 mg/1) + Ponesimod (9 mg/1) + Ponesimod (10 mg/1) Kit; Tablet, film coated Oral Janssen Pharmaceuticals, Inc 2021-03-18 Not applicable US Ponvory Ponesimod (2 mg/1) + Ponesimod (3 mg/1) + Ponesimod (4 mg/1) + Ponesimod (5 mg/1) + Ponesimod (6 mg/1) + Ponesimod (7 mg/1) + Ponesimod (8 mg/1) + Ponesimod (9 mg/1) + Ponesimod (10 mg/1) Kit; Tablet, film coated Oral Janssen Pharmaceuticals, Inc 2021-03-18 Not applicable US Ponvory Ponesimod (2 mg/1) + Ponesimod (3 mg/1) + Ponesimod (4 mg/1) + Ponesimod (5 mg/1) + Ponesimod (6 mg/1) + Ponesimod (7 mg/1) + Ponesimod (8 mg/1) + Ponesimod (9 mg/1) + Ponesimod (10 mg/1) Kit; Tablet, film coated Oral Janssen Pharmaceuticals, Inc 2021-03-18 Not applicable US Ponvory Ponesimod (10 mg) + Ponesimod (2 mg) + Ponesimod (3 mg) + Ponesimod (4 mg) + Ponesimod (5 mg) + Ponesimod (6 mg) + Ponesimod (7 mg) + Ponesimod (8 mg) + Ponesimod (9 mg) Tablet Oral Janssen Pharmaceuticals 2021-11-01 Not applicable Canada
Categories
- ATC Codes
- L04AA50 — Ponesimod
- Drug Categories
- Antineoplastic and Immunomodulating Agents
- Cytochrome P-450 CYP3A Substrates
- Cytochrome P-450 CYP3A4 Substrates
- Cytochrome P-450 CYP3A5 Substrates
- Cytochrome P-450 Substrates
- Immunologic Factors
- Immunomodulatory Agents
- Immunosuppressive Agents
- Receptors, Lysosphingolipid, antagonists & inhibitors
- Selective Immunosuppressants
- Sphingosine 1 Phosphate Receptor Modulators
- Sphingosine 1-phosphate Receptor Modulator
- Sulfur Compounds
- UGT1A1 Substrates
- UGT2B7 substrates
- Chemical TaxonomyProvided by Classyfire
- Description
- This compound belongs to the class of organic compounds known as phenol ethers. These are aromatic compounds containing an ether group substituted with a benzene ring.
- Kingdom
- Organic compounds
- Super Class
- Benzenoids
- Class
- Phenol ethers
- Sub Class
- Not Available
- Direct Parent
- Phenol ethers
- Alternative Parents
- Phenoxy compounds / Toluenes / Alkyl aryl ethers / Chlorobenzenes / Aryl chlorides / Thiazolidines / Secondary alcohols / 1,2-diols / Isothioureas / Propargyl-type 1,3-dipolar organic compounds show 8 more
- Substituents
- 1,2-diol / Alcohol / Alkyl aryl ether / Aromatic heteromonocyclic compound / Aryl chloride / Aryl halide / Azacycle / Carbonyl group / Carboxylic acid derivative / Chlorobenzene show 21 more
- Molecular Framework
- Aromatic heteromonocyclic compounds
- External Descriptors
- Not Available
- Affected organisms
- Not Available
Chemical Identifiers
- UNII
- 5G7AKV2MKP
- CAS number
- 854107-55-4
- InChI Key
- LPAUOXUZGSBGDU-STDDISTJSA-N
- InChI
- InChI=1S/C23H25ClN2O4S/c1-3-10-25-23-26(19-7-5-4-6-15(19)2)22(29)21(31-23)12-16-8-9-20(18(24)11-16)30-14-17(28)13-27/h4-9,11-12,17,27-28H,3,10,13-14H2,1-2H3/b21-12-,25-23-/t17-/m1/s1
- IUPAC Name
- (2Z,5Z)-5-({3-chloro-4-[(2R)-2,3-dihydroxypropoxy]phenyl}methylidene)-3-(2-methylphenyl)-2-(propylimino)-1,3-thiazolidin-4-one
- SMILES
- CCC\N=C1/S\C(=C/C2=CC=C(OC[C@H](O)CO)C(Cl)=C2)C(=O)N1C1=CC=CC=C1C
References
- General References
- Reyes M, Hoch M, Brossard P, Wagner-Redeker W, Miraval T, Dingemanse J: Mass balance, pharmacokinetics and metabolism of the selective S1P1 receptor modulator ponesimod in humans. Xenobiotica. 2015 Feb;45(2):139-49. doi: 10.3109/00498254.2014.955832. Epub 2014 Sep 4. [Article]
- D'Ambrosio D, Freedman MS, Prinz J: Ponesimod, a selective S1P1 receptor modulator: a potential treatment for multiple sclerosis and other immune-mediated diseases. Ther Adv Chronic Dis. 2016 Jan;7(1):18-33. doi: 10.1177/2040622315617354. [Article]
- FDA Approved Drug Products: Ponvory (Ponesimod) Oral Tablet [Link]
- External Links
- PubChem Compound
- 11363176
- PubChem Substance
- 347828333
- ChemSpider
- 9538103
- BindingDB
- 50316768
- 2532300
- ChEMBL
- CHEMBL1096146
- ZINC
- ZINC000034509627
- Wikipedia
- Ponesimod
Clinical Trials
- Clinical Trials
Phase Status Purpose Conditions Count 4 Recruiting Treatment Relapsing Remitting Multiple Sclerosis (RRMS) 1 3 Completed Treatment Coronavirus Disease 2019 (COVID‑19) / Multiple Sclerosis 1 3 Completed Treatment Multiple Sclerosis 1 3 Terminated Treatment Multiple Sclerosis 1 2 Completed Treatment Multiple Sclerosis 2
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage Forms
Form Route Strength Kit; tablet, film coated Oral Tablet Oral Tablet Oral 20 mg Tablet, film coated Oral 20 mg/1 Tablet, film coated Oral 20 mg - Prices
- Not Available
- Patents
Patent Number Pediatric Extension Approved Expires (estimated) Region US8273779 No 2012-09-25 2025-12-17 US US9062014 No 2015-06-23 2032-05-06 US US9000018 No 2015-04-07 2024-11-16 US US10220023 No 2019-03-05 2035-12-10 US USRE43728 No 2012-10-09 2024-11-16 US
Properties
- State
- Solid
- Experimental Properties
Property Value Source water solubility Insoluble FDA Label - Predicted Properties
Property Value Source Water Solubility 0.00626 mg/mL ALOGPS logP 4.01 ALOGPS logP 4.49 Chemaxon logS -4.9 ALOGPS pKa (Strongest Acidic) 13.62 Chemaxon pKa (Strongest Basic) 0.91 Chemaxon Physiological Charge 0 Chemaxon Hydrogen Acceptor Count 5 Chemaxon Hydrogen Donor Count 2 Chemaxon Polar Surface Area 82.36 Å2 Chemaxon Rotatable Bond Count 8 Chemaxon Refractivity 125.69 m3·mol-1 Chemaxon Polarizability 49.67 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 Yes Chemaxon - Predicted ADMET Features
- Not Available
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
Spectrum Spectrum Type Splash Key Predicted MS/MS Spectrum - 10V, Positive (Annotated) Predicted LC-MS/MS splash10-01tc-1000900000-db64b7f426a5ec11bff6 Predicted MS/MS Spectrum - 10V, Negative (Annotated) Predicted LC-MS/MS splash10-059f-3003900000-10bd97f5dcc6a3d8d729 Predicted MS/MS Spectrum - 20V, Positive (Annotated) Predicted LC-MS/MS splash10-004i-3004900000-d29aced208f0ef20ccb9 Predicted MS/MS Spectrum - 20V, Negative (Annotated) Predicted LC-MS/MS splash10-052o-9007300000-7cd595ec570fb5c9eebc Predicted MS/MS Spectrum - 40V, Positive (Annotated) Predicted LC-MS/MS splash10-000e-2169100000-933f5525227bb42b3a0a Predicted MS/MS Spectrum - 40V, Negative (Annotated) Predicted LC-MS/MS splash10-001m-5369000000-8caffb74b11a8a68732c 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]- 205.68571 predictedDeepCCS 1.0 (2019) [M+H]+ 208.08128 predictedDeepCCS 1.0 (2019) [M+Na]+ 214.50719 predictedDeepCCS 1.0 (2019)
Targets
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Use our structured and evidence-based datasets to unlock newinsights and accelerate drug research.
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- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- AgonistModulatorRegulator
- General Function
- Sphingosine-1-phosphate receptor activity
- Specific Function
- G-protein coupled receptor for the bioactive lysosphingolipid sphingosine 1-phosphate (S1P) that seems to be coupled to the G(i) subclass of heteromeric G proteins. Signaling leads to the activatio...
- Gene Name
- S1PR1
- Uniprot ID
- P21453
- Uniprot Name
- Sphingosine 1-phosphate receptor 1
- Molecular Weight
- 42810.195 Da
References
- Reyes M, Brossard P, Chassard D, Hoch M, Dingemanse J: Effects of ponesimod, a selective S1P1 receptor modulator, on the pharmacokinetics of a hormonal combination contraceptive. Eur J Clin Pharmacol. 2014 Mar;70(3):287-93. doi: 10.1007/s00228-013-1625-2. Epub 2013 Dec 22. [Article]
- D'Ambrosio D, Freedman MS, Prinz J: Ponesimod, a selective S1P1 receptor modulator: a potential treatment for multiple sclerosis and other immune-mediated diseases. Ther Adv Chronic Dis. 2016 Jan;7(1):18-33. doi: 10.1177/2040622315617354. [Article]
- Olsson T, Boster A, Fernandez O, Freedman MS, Pozzilli C, Bach D, Berkani O, Mueller MS, Sidorenko T, Radue EW, Melanson M: Oral ponesimod in relapsing-remitting multiple sclerosis: a randomised phase II trial. J Neurol Neurosurg Psychiatry. 2014 Nov;85(11):1198-208. doi: 10.1136/jnnp-2013-307282. Epub 2014 Mar 21. [Article]
- D'Ambrosio D, Steinmann J, Brossard P, Dingemanse J: Differential effects of ponesimod, a selective S1P1 receptor modulator, on blood-circulating human T cell subpopulations. Immunopharmacol Immunotoxicol. 2015 Feb;37(1):103-9. doi: 10.3109/08923973.2014.993084. [Article]
- Guerard N, Zwingelstein C, Hoch M, Dingemanse J: Effect of Hepatic or Renal Impairment on the Pharmacokinetics, Safety, and Tolerability of Ponesimod, a Selective S1P1 Receptor Modulator. Basic Clin Pharmacol Toxicol. 2016 May;118(5):356-68. doi: 10.1111/bcpt.12516. Epub 2015 Dec 10. [Article]
- Reyes M, Hoch M, Brossard P, Dingemanse J: Effects of ethnicity and sex on the pharmacokinetics and pharmacodynamics of the selective sphingosine-1-phosphate receptor 1 modulator ponesimod: a clinical study in Japanese and Caucasian subjects. Pharmacology. 2014;94(5-6):223-9. doi: 10.1159/000368837. Epub 2014 Nov 14. [Article]
- Lott D, Krause A, Seemayer CA, Strasser DS, Dingemanse J, Lehr T: Modeling the Effect of the Selective S1P1 Receptor Modulator Ponesimod on Subsets of Blood Lymphocytes. Pharm Res. 2017 Mar;34(3):599-609. doi: 10.1007/s11095-016-2087-x. Epub 2016 Dec 27. [Article]
- Juif PE, Hoch M, Vaclavkova A, Krause A, Bush J, Dingemanse J: Mitigation of Initial Cardiodynamic Effects of the S1P1 Receptor Modulator Ponesimod Using a Novel Up-Titration Regimen. J Clin Pharmacol. 2017 Mar;57(3):401-410. doi: 10.1002/jcph.820. Epub 2016 Sep 30. [Article]
- Fauzyah Y, Ono C, Torii S, Anzai I, Suzuki R, Izumi T, Morioka Y, Maeda Y, Okamoto T, Fukuhara T, Matsuura Y: Ponesimod suppresses hepatitis B virus infection by inhibiting endosome maturation. Antiviral Res. 2021 Feb;186:104999. doi: 10.1016/j.antiviral.2020.104999. Epub 2020 Dec 18. [Article]
- Boehler M, Juif PE, Hoch M, Dingemanse J: Absolute Bioavailability of Ponesimod, a Selective S1P1 Receptor Modulator, in Healthy Male Subjects. Eur J Drug Metab Pharmacokinet. 2017 Feb;42(1):129-134. doi: 10.1007/s13318-016-0325-6. [Article]
- Pouzol L, Piali L, Bernard CC, Martinic MM, Steiner B, Clozel M: Therapeutic Potential of Ponesimod Alone and in Combination with Dimethyl Fumarate in Experimental Models of Multiple Sclerosis. Innov Clin Neurosci. 2019 Mar 1;16(3-4):22-30. [Article]
- Hoch M, D'Ambrosio D, Wilbraham D, Brossard P, Dingemanse J: Clinical pharmacology of ponesimod, a selective S1P(1) receptor modulator, after uptitration to supratherapeutic doses in healthy subjects. Eur J Pharm Sci. 2014 Oct 15;63:147-53. doi: 10.1016/j.ejps.2014.07.005. Epub 2014 Jul 19. [Article]
- Juif PE, Hoch M, D'Ambrosio D, Dingemanse J: Biocomparison of Three Formulations of the S1P1 Receptor Modulator Ponesimod in Healthy Subjects. Drugs R D. 2015 Jun;15(2):203-10. doi: 10.1007/s40268-015-0095-7. [Article]
- Bell M, Foley D, Naylor C, Robinson C, Riley J, Epemolu O, Scullion P, Shishikura Y, Katz E, McLean WHI, Wyatt P, Read KD, Woodland A: Discovery of super soft-drug modulators of sphingosine-1-phosphate receptor 1. Bioorg Med Chem Lett. 2018 Oct 15;28(19):3255-3259. doi: 10.1016/j.bmcl.2018.07.044. Epub 2018 Jul 30. [Article]
- Janes K, Little JW, Li C, Bryant L, Chen C, Chen Z, Kamocki K, Doyle T, Snider A, Esposito E, Cuzzocrea S, Bieberich E, Obeid L, Petrache I, Nicol G, Neumann WL, Salvemini D: The development and maintenance of paclitaxel-induced neuropathic pain require activation of the sphingosine 1-phosphate receptor subtype 1. J Biol Chem. 2014 Jul 25;289(30):21082-97. doi: 10.1074/jbc.M114.569574. [Article]
- Gatfield J, Monnier L, Studer R, Bolli MH, Steiner B, Nayler O: Sphingosine-1-phosphate (S1P) displays sustained S1P1 receptor agonism and signaling through S1P lyase-dependent receptor recycling. Cell Signal. 2014 Jul;26(7):1576-88. doi: 10.1016/j.cellsig.2014.03.029. Epub 2014 Apr 2. [Article]
- Borodzicz S, Rudnicka L, Mirowska-Guzel D, Cudnoch-Jedrzejewska A: The role of epidermal sphingolipids in dermatologic diseases. Lipids Health Dis. 2016 Jan 19;15:13. doi: 10.1186/s12944-016-0178-7. [Article]
- Vaclavkova A, Chimenti S, Arenberger P, Hollo P, Sator PG, Burcklen M, Stefani M, D'Ambrosio D: Oral ponesimod in patients with chronic plaque psoriasis: a randomised, double-blind, placebo-controlled phase 2 trial. Lancet. 2014 Dec 6;384(9959):2036-45. doi: 10.1016/S0140-6736(14)60803-5. Epub 2014 Aug 10. [Article]
- FDA Approved Drug Products: Ponvory (Ponesimod) Oral Tablet [Link]
Enzymes
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Steroid hydroxylase activity
- Specific Function
- This enzyme metabolizes arachidonic acid predominantly via a NADPH-dependent olefin epoxidation to all four regioisomeric cis-epoxyeicosatrienoic acids. One of the predominant enzymes responsible f...
- Gene Name
- CYP2J2
- Uniprot ID
- P51589
- Uniprot Name
- Cytochrome P450 2J2
- Molecular Weight
- 57610.165 Da
References
- FDA Approved Drug Products: Ponvory (Ponesimod) Oral Tablet [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- 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
References
- FDA Approved Drug Products: Ponvory (Ponesimod) Oral Tablet [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- 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 un...
- Gene Name
- CYP3A5
- Uniprot ID
- P20815
- Uniprot Name
- Cytochrome P450 3A5
- Molecular Weight
- 57108.065 Da
References
- FDA Approved Drug Products: Ponvory (Ponesimod) Oral Tablet [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- A cytochrome P450 monooxygenase involved in the metabolism of various endogenous substrates, including fatty acids and their oxygenated derivatives (oxylipins) (PubMed:8486631, PubMed:9675028, PubMed:11461919, PubMed:15145985, PubMed:16547005, PubMed:16820285, PubMed:18182499, PubMed:18065749, PubMed:18577768). Mechanistically, uses molecular oxygen inserting one oxygen atom into a substrate, and reducing the second into a water molecule, with two electrons provided by NADPH via cytochrome P450 reductase (CPR; NADPH-ferrihemoprotein reductase) (PubMed:9675028). May play a role in inactivation of proinflammatory and anti-inflammatory oxylipins during the resolution of inflammation (PubMed:8486631, PubMed:9675028, PubMed:11461919, PubMed:15145985, PubMed:15364545, PubMed:16547005, PubMed:16820285, PubMed:18182499, PubMed:18065749, PubMed:18577768).
- Specific Function
- Arachidonic acid monooxygenase activity
- Gene Name
- CYP4F3
- Uniprot ID
- Q08477
- Uniprot Name
- Cytochrome P450 4F3
- Molecular Weight
- 59846.085 Da
References
- FDA Approved Drug Products: Ponvory (Ponesimod) Oral Tablet [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Leukotriene-b4 20-monooxygenase activity
- Specific Function
- Catalyzes leukotriene B4 omega-hydroxylation and arachidonic acid omega-hydroxylation but with an activity much lower than that of CYP4F2. Catalyzes the hydroxylation of the antihistamine ebastine.
- Gene Name
- CYP4F12
- Uniprot ID
- Q9HCS2
- Uniprot Name
- Cytochrome P450 4F12
- Molecular Weight
- 60269.165 Da
References
- FDA Approved Drug Products: Ponvory (Ponesimod) Oral Tablet [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Steroid binding
- Specific Function
- UDPGT is of major importance in the conjugation and subsequent elimination of potentially toxic xenobiotics and endogenous compounds. This isoform glucuronidates bilirubin IX-alpha to form both the...
- Gene Name
- UGT1A1
- Uniprot ID
- P22309
- Uniprot Name
- UDP-glucuronosyltransferase 1-1
- Molecular Weight
- 59590.91 Da
References
- FDA Approved Drug Products: Ponvory (Ponesimod) Oral Tablet [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Glucuronosyltransferase activity
- Specific Function
- UDPGT is of major importance in the conjugation and subsequent elimination of potentially toxic xenobiotics and endogenous compounds.Its unique specificity for 3,4-catechol estrogens and estriol su...
- Gene Name
- UGT2B7
- Uniprot ID
- P16662
- Uniprot Name
- UDP-glucuronosyltransferase 2B7
- Molecular Weight
- 60694.12 Da
References
- FDA Approved Drug Products: Ponvory (Ponesimod) Oral Tablet [Link]
Drug created at October 20, 2016 21:11 / Updated at April 18, 2024 09:15