Identification

Summary

Pirfenidone is an agent used for the treatment of idiopathic pulmonary fibrosis (IPF).

Brand Names
Esbriet
Generic Name
Pirfenidone
DrugBank Accession Number
DB04951
Background

Pirfenidone is a synthetic pyridone drug.8 It is an antifibrotic agent with anti-inflammatory and antioxidant properties 8 that is used to treat idiopathic pulmonary fibrosis (IPF),9 which is a chronic, progressive form of interstitial pneumonia.8 While its mechanism of action is not yet fully understood, pirfenidone is proposed to primarily regulate tumor necrosis factor (TNF) pathways and modulate cellular oxidation.7 The FDA first approved pirfenidone alongside nintedanib as one of the first drugs to treat IPF.6

Type
Small Molecule
Groups
Approved, Investigational
Structure
Weight
Average: 185.2218
Monoisotopic: 185.084063979
Chemical Formula
C12H11NO
Synonyms
  • Pirfenidona
  • Pirfenidone
External IDs
  • AMR-69

Pharmacology

Indication

Pirfenidone is indicated for the treatment of idiopathic pulmonary fibrosis (IPF).9,10,12 In Canada and Europe, it is approved in adults only.10,12

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Associated Conditions
Contraindications & Blackbox Warnings
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Pharmacodynamics

Pirfenidone is a novel agent with anti-inflammatory, antioxidant, and antifibrotic properties. It may improve lung function and reduce the number of acute exacerbations in patients with idiopathic pulmonary fibrosis (IPF).9

Mechanism of action

The exact mechanism of action of pirfenidone is not fully understood.9 It is suggested that the antioxidant effects of pirfenidone contribute to its anti-inflammatory effects, leading to antifibrotic effects.8

Pirfenidone attenuates the production of transforming growth factor-β1 (TGF-β1), a key profibrotic and pro-inflammatory cytokine implicated in idiopathic pulmonary fibrosis (IPF). By suppressing TGF-β1, pirfenidone inhibits TGF-β1-induced differentiation of human lung fibroblasts into myofibroblasts, thereby preventing excess collagen synthesis and extracellular matrix production.1,2,3,4,7

Some evidence suggests that pirfenidone downregulates pro-inflammatory cytokines, including TNF-α, interleukin-1 (IL-1), IL-6, interferon-gamma (IFN-γ),1,3,7 and platelet-derived growth factor (PDGF).7 Animal models demonstrated that pirfenidone promotes the production of anti-inflammatory IL-10 and prevents the accumulation of various inflammatory cells, including lymphocytes, macrophages and neutrophils.7 In animal models, pirfenidone inhibited the influx of inflammatory cells and ameliorated bleomycin-induced pulmonary vascular permeability.1 Several in vitro studies show that pirfenidone mediates antioxidant actions by scavenging reactive oxygen species (ROS) and inhibiting lipid peroxidation, thereby reducing cellular injury in IPF.7

Absorption

After a single oral-dose administration of 801 mg pirfenidone (as three 267 mg capsules), the Tmax ranged from 30 minutes to four hours. Food affects the absorption and safety profile of pirfenidone: in one study, food increased Tmax; decreased Cmax and AUC by 49% and 16%, respectively; and decreased the incidence of pirfenidone-induced adverse reactions.9

Volume of distribution

Mean apparent oral volume of distribution is approximately 59 to 71 L.9 Pirfenidone is not widely distributed to tissues.7

Protein binding

At a dose range of 1 to 10 μg/mL, pirfenidone was approximately 58% bound to human plasma proteins, mainly to serum albumin.9

Metabolism

According to in vitro studies, about 70-80% of pirfenidone metabolism is mediated by CYP1A2, as well as some minor contributions from CYP2C9, 2C19, 2D6, and 2E1. Four metabolites have been detected after oral administration of pirfenidone. In vitro data suggest that metabolites are not expected to be pharmacologically active at observed metabolite concentrations. The exact metabolic pathways of pirfenidone have not been fully characterized;9 however, one of the pathways involve CYP1A2-mediated 5-hydroxylation and subsequent oxidation to form 5-carboxy pirfenidone.5 In humans, only pirfenidone and 5-carboxy pirfenidone are present in plasma in significant quantities. The mean metabolite-to-parent ratio ranged from approximately 0.6 to 0.7.9

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Route of elimination

Within 24 hours, approximately 80% of the pirfenidone dose is excreted mainly in the urine.7 About 99.6% of the recovered dose of pirfenidone was excreted as the 5-carboxy metabolite.9 About less than 1% of the dose was excreted as unchanged parent drug and less than 0.1% of the dose was excreted as other metabolites.7

Half-life

The mean terminal half-life is approximately three hours in healthy subjects.9

Clearance

Following administration of a single dose of 801 mg in healthy older adults, the mean apparent oral clearance of pirfenidone was 13.8 L/h with food and 11.8 L/h without food.7

Adverse Effects
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Toxicity

In rats, the oral and intraperitoneal LD50 are 1295 mg/kg and 430 mg/kg, respectively.11

There is limited clinical experience with overdosage of pirfenidone. A maximum tolerated pirfenidone dose of 4005 mg per day was tolerated when the drug was administered as five 267 mg capsules three times daily to healthy adult volunteers over a 12-day dose escalation. Overdosage should be managed with supportive and symptomatic care, including monitoring of vital signs and observation of the clinical status of the patient.9

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 Pirfenidone can be increased when it is combined with Abametapir.
AbataceptThe metabolism of Pirfenidone can be increased when combined with Abatacept.
AbirateroneThe serum concentration of Pirfenidone can be increased when it is combined with Abiraterone.
AbrocitinibThe metabolism of Abrocitinib can be decreased when combined with Pirfenidone.
AcebutololThe metabolism of Pirfenidone can be decreased when combined with Acebutolol.
AcenocoumarolThe metabolism of Pirfenidone can be decreased when combined with Acenocoumarol.
AcetaminophenPirfenidone may increase the hepatotoxic activities of Acetaminophen.
AcetohexamideThe metabolism of Pirfenidone can be decreased when combined with Acetohexamide.
Acetyl sulfisoxazoleThe metabolism of Pirfenidone can be decreased when combined with Acetyl sulfisoxazole.
Acetylsalicylic acidThe metabolism of Pirfenidone can be decreased when combined with Acetylsalicylic acid.
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Food Interactions
  • Take at the same time every day.
  • Take with food. Food decreased the rate and extent of absorption. Food reduces the incidence of drug-related adverse reactions.

Products

Drug product information from 10+ global regions
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dosage, form, labeller, route of administration, and marketing period.
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Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
EsbrietTablet, film coated534 mgOralRoche Registration Gmb H2020-12-16Not applicableEU flag
EsbrietTablet, film coated267 mgOralRoche Registration Gmb H2020-12-16Not applicableEU flag
EsbrietTablet, film coated267 mgOralRoche Registration Gmb H2020-12-16Not applicableEU flag
EsbrietCapsule267 mg/1OralGenentech, Inc.2014-10-15Not applicableUS flag
EsbrietTablet, film coated267 mgOralRoche Registration Gmb H2020-12-16Not applicableEU flag
EsbrietCapsule267 mgOralRoche Registration Gmb H2016-09-08Not applicableEU flag
EsbrietTablet, film coated267 mgOralRoche Registration Gmb H2020-12-16Not applicableEU flag
EsbrietTablet267 mgOralHoffmann La Roche2017-07-26Not applicableCanada flag
EsbrietTablet, film coated801 mgOralRoche Registration Gmb H2020-12-16Not applicableEU flag
EsbrietTablet, coated801 mg/1OralGenentech, Inc.2017-01-11Not applicableUS flag
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
Jamp PirfenidoneCapsule267 mgOralJamp Pharma Corporation2021-06-04Not applicableCanada flag
Jamp PirfenidoneTablet801 mgOralJamp Pharma Corporation2021-10-07Not applicableCanada flag
Jamp PirfenidoneTablet267 mgOralJamp Pharma Corporation2021-10-08Not applicableCanada flag
PirfenidoneTablet, film coated801 mg/1OralTeva Pharmaceuticals, Inc.2022-05-11Not applicableUS flag
PirfenidoneCapsule267 mg/1OralCipla USA Inc.2022-08-02Not applicableUS flag
PirfenidoneTablet, film coated267 mg/1OralSandoz Inc2022-05-02Not applicableUS flag
PirfenidoneTablet, film coated534 mg/1OralLaurus Labs Limited2022-07-19Not applicableUS flag
PirfenidoneTablet, coated801 mg/1OralAlembic Pharmaceuticals Inc.2022-06-10Not applicableUS flag
PirfenidoneCapsule267 mg/1OralAmneal Pharmaceuticals NY LLC2022-01-07Not applicableUS flag
PirfenidoneTablet, film coated267 mg/1OralAccord Healthcare Inc.2022-05-27Not applicableUS flag

Categories

ATC Codes
L04AX05 — Pirfenidone
Drug Categories
Chemical TaxonomyProvided by Classyfire
Description
This compound belongs to the class of organic compounds known as pyridinones. These are compounds containing a pyridine ring, which bears a ketone.
Kingdom
Organic compounds
Super Class
Organoheterocyclic compounds
Class
Pyridines and derivatives
Sub Class
Hydropyridines
Direct Parent
Pyridinones
Alternative Parents
Methylpyridines / Dihydropyridines / Benzene and substituted derivatives / Heteroaromatic compounds / Lactams / Azacyclic compounds / Organopnictogen compounds / Organooxygen compounds / Organonitrogen compounds / Organic oxides
show 1 more
Substituents
Aromatic heteromonocyclic compound / Azacycle / Benzenoid / Dihydropyridine / Heteroaromatic compound / Hydrocarbon derivative / Lactam / Methylpyridine / Monocyclic benzene moiety / Organic nitrogen compound
show 6 more
Molecular Framework
Aromatic heteromonocyclic compounds
External Descriptors
ring assembly, pyridone (CHEBI:32016)
Affected organisms
  • Humans and other mammals

Chemical Identifiers

UNII
D7NLD2JX7U
CAS number
53179-13-8
InChI Key
ISWRGOKTTBVCFA-UHFFFAOYSA-N
InChI
InChI=1S/C12H11NO/c1-10-7-8-12(14)13(9-10)11-5-3-2-4-6-11/h2-9H,1H3
IUPAC Name
5-methyl-1-phenyl-1,2-dihydropyridin-2-one
SMILES
CC1=CN(C(=O)C=C1)C1=CC=CC=C1

References

General References
  1. Cho ME, Kopp JB: Pirfenidone: an anti-fibrotic therapy for progressive kidney disease. Expert Opin Investig Drugs. 2010 Feb;19(2):275-83. doi: 10.1517/13543780903501539. [Article]
  2. Biernacka A, Dobaczewski M, Frangogiannis NG: TGF-beta signaling in fibrosis. Growth Factors. 2011 Oct;29(5):196-202. doi: 10.3109/08977194.2011.595714. Epub 2011 Jul 11. [Article]
  3. Ruwanpura SM, Thomas BJ, Bardin PG: Pirfenidone: Molecular Mechanisms and Potential Clinical Applications in Lung Disease. Am J Respir Cell Mol Biol. 2020 Apr;62(4):413-422. doi: 10.1165/rcmb.2019-0328TR. [Article]
  4. Ballester B, Milara J, Cortijo J: Pirfenidone anti-fibrotic effects are partially mediated by the inhibition of MUC1 bioactivation. Oncotarget. 2020 Apr 14;11(15):1306-1320. doi: 10.18632/oncotarget.27526. eCollection 2020 Apr 14. [Article]
  5. Zhang Y, Sato R, Fukami T, Nakano M, Nakajima M: Pirfenidone 5-hydroxylation is mainly catalysed by CYP1A2 and partly catalysed by CYP2C19 and CYP2D6 in the human liver. Xenobiotica. 2021 Dec;51(12):1352-1359. doi: 10.1080/00498254.2021.2007553. Epub 2021 Nov 30. [Article]
  6. Dempsey TM, Payne S, Sangaralingham L, Yao X, Shah ND, Limper AH: Adoption of the Antifibrotic Medications Pirfenidone and Nintedanib for Patients with Idiopathic Pulmonary Fibrosis. Ann Am Thorac Soc. 2021 Jul;18(7):1121-1128. doi: 10.1513/AnnalsATS.202007-901OC. [Article]
  7. Aravena C, Labarca G, Venegas C, Arenas A, Rada G: Pirfenidone for Idiopathic Pulmonary Fibrosis: A Systematic Review and Meta-Analysis. PLoS One. 2015 Aug 26;10(8):e0136160. doi: 10.1371/journal.pone.0136160. eCollection 2015. [Article]
  8. Kim ES, Keating GM: Pirfenidone: a review of its use in idiopathic pulmonary fibrosis. Drugs. 2015 Feb;75(2):219-30. doi: 10.1007/s40265-015-0350-9. [Article]
  9. FDA Approved Drug Products: Esbriet (pirfenidone) for oral use [Link]
  10. Health Canada Product Monograph: Esbriet (pirfenidone) for oral use [Link]
  11. CaymanChem: Pirfenidone MSDS [Link]
  12. EMA Approved Drug Products: Pirfenidone AET (pirfenidone) Oral Tablets [Link]
PubChem Compound
40632
PubChem Substance
175426915
ChemSpider
37115
BindingDB
50005201
RxNav
1592254
ChEBI
32016
ChEMBL
CHEMBL1256391
ZINC
ZINC000000001958
Wikipedia
Pirfenidone

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
4CompletedTreatmentIdiopathic Pulmonary Fibrosis (IPF)3
4RecruitingTreatmentConnective Tissue Diseases / Interstitial Lung Disease / Pirfenidone1
4RecruitingTreatmentCoronavirus Disease 2019 (COVID‑19) / Novel Coronavirus-induced Lung Fibrosis1
4RecruitingTreatmentProgressive Idiopathic Pulmonary Fibrosis1
4Unknown StatusTreatmentAcute Kidney Injury (AKI) / Sepsis1
4Unknown StatusTreatmentDermatopolymyositis / Interstitial Lung Disease1
4Unknown StatusTreatmentSarcoidosis, Pulmonary1
3Active Not RecruitingTreatmentAlbuminuria / Diabetic Nephropathy1
3CompletedTreatmentDiabetic Foot Ulcers (DFUs)1
3CompletedTreatmentIdiopathic Pulmonary Fibrosis (IPF)5

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage Forms
FormRouteStrength
CapsuleOral
CapsuleOral267 mg
CapsuleOral267 mg/1
TabletOral267 mg
TabletOral801 mg
Tablet, coatedOral267 mg/1
Tablet, coatedOral801 mg/1
Tablet, film coatedOral534 MG
Tablet, film coatedOral267 mg
Tablet, film coatedOral801 mg
Capsule, coatedOral267 mg
Tablet, film coatedOral267.000 mg
Tablet, film coatedOral801.000 mg
CapsuleOral267.0 mg
Tablet, film coatedOral
TabletOral267 mg/1
TabletOral801 mg/1
Tablet, film coatedOral267 mg/1
Tablet, film coatedOral534 mg/1
Tablet, film coatedOral801 mg/1
Prices
Not Available
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)Region
US7988994No2011-08-022026-09-22US flag
US7816383No2010-10-192030-01-08US flag
US8013002No2011-09-062030-01-08US flag
US8084475No2011-12-272030-01-08US flag
US8778947No2014-07-152033-08-30US flag
US7566729No2009-07-282029-04-22US flag
US7767225No2010-08-032026-09-22US flag
US7635707No2009-12-222029-04-22US flag
US7767700No2010-08-032027-12-18US flag
US8592462No2013-11-262029-04-22US flag
US8383150No2013-02-262026-09-22US flag
US8318780No2012-11-272030-01-08US flag
US8420674No2013-04-162027-12-18US flag
US7910610No2011-03-222030-01-08US flag
US8648098No2014-02-112030-01-08US flag
US8754109No2014-06-172030-01-08US flag
US8609701No2013-12-172029-04-22US flag
US8753679No2014-06-172026-09-22US flag
US7696236No2010-04-132027-12-18US flag
US9561217No2017-02-072022-01-25US flag
US10188637No2019-01-292037-03-28US flag

Properties

State
Solid
Experimental Properties
PropertyValueSource
melting point (°C)109https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/022535s012,208780s002lbl.pdf
Predicted Properties
PropertyValueSource
Water Solubility2.89 mg/mLALOGPS
logP2ALOGPS
logP2.14ChemAxon
logS-1.8ALOGPS
pKa (Strongest Basic)-1.2ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count1ChemAxon
Hydrogen Donor Count0ChemAxon
Polar Surface Area20.31 Å2ChemAxon
Rotatable Bond Count1ChemAxon
Refractivity57 m3·mol-1ChemAxon
Polarizability20.28 Å3ChemAxon
Number of Rings2ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleNoChemAxon
Predicted ADMET Features
PropertyValueProbability
Human Intestinal Absorption+0.9932
Blood Brain Barrier+0.996
Caco-2 permeable+0.8614
P-glycoprotein substrateNon-substrate0.8193
P-glycoprotein inhibitor INon-inhibitor0.755
P-glycoprotein inhibitor IINon-inhibitor0.9177
Renal organic cation transporterNon-inhibitor0.8157
CYP450 2C9 substrateNon-substrate0.6638
CYP450 2D6 substrateNon-substrate0.8248
CYP450 3A4 substrateSubstrate0.6111
CYP450 1A2 substrateInhibitor0.9108
CYP450 2C9 inhibitorNon-inhibitor0.5982
CYP450 2D6 inhibitorNon-inhibitor0.9231
CYP450 2C19 inhibitorNon-inhibitor0.7166
CYP450 3A4 inhibitorNon-inhibitor0.775
CYP450 inhibitory promiscuityHigh CYP Inhibitory Promiscuity0.7633
Ames testNon AMES toxic0.7652
CarcinogenicityNon-carcinogens0.8992
BiodegradationNot ready biodegradable0.9112
Rat acute toxicity2.1330 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9784
hERG inhibition (predictor II)Non-inhibitor0.6301
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397)

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
LC-MS/MS Spectrum - LC-ESI-qTof , PositiveLC-MS/MSNot Available
MS/MS Spectrum - , positiveLC-MS/MSsplash10-000i-2900000000-b9809376eba9769e9bee

Enzymes

Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
Inhibitor
Curator comments
Pirfenidone showed a concentration-dependent inhibition on CYP1A2. At 1000 µM, pirfenidone inhibits the activity of this enzyme by 34.1%.
General Function
Oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygen
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
Gene Name
CYP1A2
Uniprot ID
P05177
Uniprot Name
Cytochrome P450 1A2
Molecular Weight
58293.76 Da
References
  1. Arai T, Inoue Y, Sasaki Y, Tachibana K, Nakao K, Sugimoto C, Okuma T, Akira M, Kitaichi M, Hayashi S: Predictors of the clinical effects of pirfenidone on idiopathic pulmonary fibrosis. Respir Investig. 2014 Mar;52(2):136-43. doi: 10.1016/j.resinv.2013.09.002. Epub 2013 Oct 24. [Article]
  2. Health Canada Product Monograph: Esbriet (pirfenidone) for oral use [Link]
  3. FDA Approved Drug Products: Esbriet (pirfenidone) for oral use [Link]
  4. Pirfenidone FDA label [File]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
Inhibitor
Curator comments
Pirfenidone showed a concentration-dependent inhibition on CYP2C9. At 1000 µM, pirfenidone inhibits the activity of this enzyme by 30.4%.
General Function
Steroid hydroxylase activity
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
Gene Name
CYP2C9
Uniprot ID
P11712
Uniprot Name
Cytochrome P450 2C9
Molecular Weight
55627.365 Da
References
  1. Health Canada Product Monograph: Esbriet (pirfenidone) for oral use [Link]
  2. FDA Approved Drug Products: Esbriet (pirfenidone) for oral use [Link]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
Inhibitor
Curator comments
Pirfenidone showed a concentration-dependent inhibition on CYP2C19. At 1000 µM, pirfenidone inhibits the activity of this enzyme by 27.5%.
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
References
  1. Health Canada Product Monograph: Esbriet (pirfenidone) for oral use [Link]
  2. FDA Approved Drug Products: Esbriet (pirfenidone) for oral use [Link]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
Inhibitor
Curator comments
Pirfenidone showed a concentration-dependent inhibition on CYP2D6. At 1000 µM, pirfenidone inhibits the activity of this enzyme by 21%.
General Function
Steroid hydroxylase activity
Specific Function
Responsible for the metabolism of many drugs and environmental chemicals that it oxidizes. It is involved in the metabolism of drugs such as antiarrhythmics, adrenoceptor antagonists, and tricyclic...
Gene Name
CYP2D6
Uniprot ID
P10635
Uniprot Name
Cytochrome P450 2D6
Molecular Weight
55768.94 Da
References
  1. Health Canada Product Monograph: Esbriet (pirfenidone) for oral use [Link]
  2. FDA Approved Drug Products: Esbriet (pirfenidone) for oral use [Link]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Steroid hydroxylase activity
Specific Function
Metabolizes several precarcinogens, drugs, and solvents to reactive metabolites. Inactivates a number of drugs and xenobiotics and also bioactivates many xenobiotic substrates to their hepatotoxic ...
Gene Name
CYP2E1
Uniprot ID
P05181
Uniprot Name
Cytochrome P450 2E1
Molecular Weight
56848.42 Da
References
  1. Health Canada Product Monograph: Esbriet (pirfenidone) for oral use [Link]
  2. FDA Approved Drug Products: Esbriet (pirfenidone) for oral use [Link]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inhibitor
Curator comments
Pirfenidone showed a concentration-dependent inhibition on CYP3A4. At 1000 µM, pirfenidone inhibits the activity of this enzyme by 9.6%.
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: Esbriet (pirfenidone) for oral use [Link]

Carriers

Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Binder
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
References
  1. Health Canada Product Monograph: Esbriet (pirfenidone) for oral use [Link]
  2. FDA Approved Drug Products: Esbriet (pirfenidone) for oral use [Link]

Transporters

Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Xenobiotic-transporting atpase activity
Specific Function
Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells.
Gene Name
ABCB1
Uniprot ID
P08183
Uniprot Name
Multidrug resistance protein 1
Molecular Weight
141477.255 Da
References
  1. FDA Approved Drug Products: Esbriet (pirfenidone) for oral use [Link]

Drug created at October 21, 2007 22:23 / Updated at August 09, 2022 10:05