Ponesimod

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
Thumb
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

Pharmacology
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Associated Conditions
Contraindications & Blackbox Warnings
Contraindications
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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

TargetActionsOrganism
ASphingosine 1-phosphate receptor 1
agonist
modulator
regulator
Humans
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
Medicalerrors
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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.
DrugInteraction
AbametapirThe serum concentration of Ponesimod can be increased when it is combined with Abametapir.
AbataceptThe metabolism of Ponesimod can be increased when combined with Abatacept.
AcalabrutinibThe metabolism of Ponesimod can be decreased when combined with Acalabrutinib.
AcebutololThe risk or severity of bradycardia can be increased when Ponesimod is combined with Acebutolol.
AcrivastineThe risk or severity of bradycardia can be increased when Ponesimod is combined with Acrivastine.
AdalimumabThe metabolism of Ponesimod can be increased when combined with Adalimumab.
AdenineThe metabolism of Ponesimod can be decreased when combined with Adenine.
AdenosineThe risk or severity of bradycardia can be increased when Ponesimod is combined with Adenosine.
Adenovirus type 7 vaccine liveThe risk or severity of infection can be increased when Ponesimod is combined with Adenovirus type 7 vaccine live.
AjmalineThe risk or severity of bradycardia can be increased when Ponesimod is combined with Ajmaline.
Interactions
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Food Interactions
  • Take with or without food. The absorption of ponesimod is not significantly affected by food.

Products

Products
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International/Other Brands
Ponvory (Janssen)
Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
PonvoryTablet, film coated20 mg/1OralJanssen Pharmaceuticals, Inc2021-03-18Not applicableUS flag
PonvoryTablet20 mgOralJanssen PharmaceuticalsNot applicableNot applicableCanada flag
Mixture Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing EndRegionImage
PonvoryPonesimod (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)TabletOralJanssen PharmaceuticalsNot applicableNot applicableCanada flag
PonvoryPonesimod (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)TabletOralJanssen Pharmaceuticals, Inc2021-03-18Not applicableUS flag
PonvoryPonesimod (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)TabletOralJanssen PharmaceuticalsNot applicableNot applicableCanada flag
PonvoryPonesimod (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)TabletOralJanssen Pharmaceuticals, Inc2021-03-18Not applicableUS flag
PonvoryPonesimod (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)TabletOralJanssen Pharmaceuticals, Inc2021-03-18Not applicableUS flag
PonvoryPonesimod (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)TabletOralJanssen Pharmaceuticals, Inc2021-03-18Not applicableUS flag
PonvoryPonesimod (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)TabletOralJanssen PharmaceuticalsNot applicableNot applicableCanada flag
PonvoryPonesimod (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)TabletOralJanssen PharmaceuticalsNot applicableNot applicableCanada flag
PonvoryPonesimod (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)TabletOralJanssen PharmaceuticalsNot applicableNot applicableCanada flag
PonvoryPonesimod (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)TabletOralJanssen Pharmaceuticals, Inc2021-03-18Not applicableUS flag

Categories

Drug Categories
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
  1. 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]
  2. 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]
  3. FDA Approved Drug Products: Ponvory (Ponesimod) Oral Tablet [Link]
PubChem Compound
11363176
PubChem Substance
347828333
ChemSpider
9538103
BindingDB
50316768
RxNav
2532300
ChEMBL
CHEMBL1096146
ZINC
ZINC000034509627
Wikipedia
Ponesimod

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
3Active Not RecruitingTreatmentDisseminated Sclerosis1
3CompletedTreatmentDisseminated Sclerosis1
3TerminatedTreatmentDisseminated Sclerosis1
2Active Not RecruitingTreatmentDisseminated Sclerosis1
2CompletedTreatmentDisseminated Sclerosis1
2CompletedTreatmentPsoriasis1
2CompletedTreatmentPsoriasis Vulgaris (Plaque Psoriasis)1
2TerminatedTreatmentChronic Graft Versus Host Disease1
1CompletedNot AvailableHealthy Volunteers3
1CompletedNot AvailablePharmacokinetics1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage Forms
FormRouteStrength
TabletOral
TabletOral20 mg
Tablet, film coatedOral20 mg/1
Prices
Not Available
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)Region
US8273779No2005-12-172025-12-17US flag
US9062014No2012-05-062032-05-06US flag
US9000018No2004-11-162024-11-16US flag
US10220023No2015-12-102035-12-10US flag
USRE43728No2004-11-162024-11-16US flag

Properties

State
Solid
Experimental Properties
PropertyValueSource
water solubilityInsolubleFDA Label
Predicted Properties
PropertyValueSource
Water Solubility0.00626 mg/mLALOGPS
logP4.01ALOGPS
logP4.49ChemAxon
logS-4.9ALOGPS
pKa (Strongest Acidic)13.62ChemAxon
pKa (Strongest Basic)0.91ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count5ChemAxon
Hydrogen Donor Count2ChemAxon
Polar Surface Area82.36 Å2ChemAxon
Rotatable Bond Count8ChemAxon
Refractivity125.69 m3·mol-1ChemAxon
Polarizability49.67 Å3ChemAxon
Number of Rings3ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleYesChemAxon
Predicted ADMET Features
Not Available

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSNot Available

Targets

Drugtargets
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with our fully connected ADMET & drug target dataset.
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Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Agonist
Modulator
Regulator
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
  1. 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]
  2. 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]
  3. 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]
  4. 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]
  5. 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]
  6. 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]
  7. 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]
  8. 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]
  9. 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]
  10. 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]
  11. 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]
  12. 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]
  13. 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]
  14. 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]
  15. 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]
  16. 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]
  17. 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]
  18. 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]
  19. 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
  1. 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
  1. 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
  1. 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
  1. 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
  1. 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
  1. 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
  1. FDA Approved Drug Products: Ponvory (Ponesimod) Oral Tablet [Link]

Drug created on October 20, 2016 21:11 / Updated on March 26, 2021 03:55