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
Structure for Pirfenidone (DB04951)
- 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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- Contraindications & Blackbox Warnings
Avoid life-threatening adverse drug eventsImprove clinical decision support with information on contraindications & blackbox warnings, population restrictions, harmful risks, & more.Avoid life-threatening adverse drug events & improve clinical decision support.- 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
Hover over products below to view reaction partners
- 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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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.
Drug Interaction Integrate drug-drug
interactions in your softwareAbametapir The serum concentration of Pirfenidone can be increased when it is combined with Abametapir. Abatacept The metabolism of Pirfenidone can be increased when combined with Abatacept. Abiraterone The serum concentration of Pirfenidone can be increased when it is combined with Abiraterone. Abrocitinib The metabolism of Abrocitinib can be decreased when combined with Pirfenidone. Acebutolol The metabolism of Pirfenidone can be decreased when combined with Acebutolol. Acenocoumarol The metabolism of Pirfenidone can be decreased when combined with Acenocoumarol. Acetaminophen Pirfenidone may increase the hepatotoxic activities of Acetaminophen. Acetohexamide The metabolism of Pirfenidone can be decreased when combined with Acetohexamide. Acetyl sulfisoxazole The metabolism of Pirfenidone can be decreased when combined with Acetyl sulfisoxazole. Acetylsalicylic acid The metabolism of Pirfenidone can be decreased when combined with Acetylsalicylic acid. 
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- 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 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.- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Esbriet Tablet, film coated 267 mg Oral Roche Registration Gmb H 2020-12-16 Not applicable EU 
Esbriet Tablet 801 mg Oral Hoffmann La Roche 2017-07-26 Not applicable Canada 
Esbriet Tablet, coated 801 mg/1 Oral Genentech, Inc. 2017-01-11 Not applicable US 
Esbriet Tablet, film coated 267 mg Oral Roche Registration Gmb H 2020-12-16 Not applicable EU Esbriet Tablet, film coated 534 mg Oral Roche Registration Gmb H 2020-12-16 Not applicable EU Esbriet Capsule 267 mg/1 Oral Inter Mune 2014-10-16 Not applicable US Esbriet Tablet, film coated 267 mg Oral Roche Registration Gmb H 2020-12-16 2022-08-08 EU Esbriet Tablet, film coated 267 mg Oral Roche Registration Gmb H 2020-12-16 2022-08-08 EU Esbriet Tablet, film coated 267 mg Oral Roche Registration Gmb H 2020-12-16 Not applicable EU Esbriet Capsule 267 mg Oral Roche Registration Gmb H 2016-09-08 Not applicable EU - Generic Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Jamp Pirfenidone Tablet 267 mg Oral Jamp Pharma Corporation 2021-10-08 Not applicable Canada Jamp Pirfenidone Capsule 267 mg Oral Jamp Pharma Corporation 2021-06-04 Not applicable Canada Jamp Pirfenidone Tablet 801 mg Oral Jamp Pharma Corporation 2021-10-07 Not applicable Canada Pirfenidone Tablet, film coated 801 mg/1 Oral Accord Healthcare Inc. 2022-05-27 Not applicable US Pirfenidone Tablet 801 mg/1 Oral ScieGen Pharmaceuticals, Inc. 2022-08-01 Not applicable US Pirfenidone Tablet, film coated 267 mg/1 Oral Msn Laboratories Private Limited 2022-05-24 Not applicable US Pirfenidone Tablet, film coated 801 mg/1 Oral Teva Pharmaceuticals, Inc. 2022-05-11 Not applicable US Pirfenidone Capsule 267 mg/1 Oral Cipla USA Inc. 2022-08-02 Not applicable US Pirfenidone Tablet, film coated 267 mg/1 Oral Sandoz Inc 2022-05-02 Not applicable US Pirfenidone Tablet, film coated 534 mg/1 Oral Laurus Labs Limited 2022-07-19 Not applicable US
Categories
- ATC Codes
- L04AX05 — Pirfenidone
- Drug Categories
- Analgesics
- Analgesics, Non-Narcotic
- Anti-Inflammatory Agents
- Antifibrotic Agents
- Antineoplastic Agents
- Antineoplastic and Immunomodulating Agents
- Antirheumatic Agents
- Cytochrome P-450 CYP1A2 Inhibitors
- Cytochrome P-450 CYP1A2 Inhibitors (strength unknown)
- Cytochrome P-450 CYP1A2 Substrates
- Cytochrome P-450 CYP2C19 Inhibitors
- Cytochrome P-450 CYP2C19 inhibitors (strength unknown)
- Cytochrome P-450 CYP2C19 Substrates
- Cytochrome P-450 CYP2C9 Inhibitors
- Cytochrome P-450 CYP2C9 Inhibitors (strength unknown)
- Cytochrome P-450 CYP2C9 Substrates
- Cytochrome P-450 CYP2D6 Inhibitors
- Cytochrome P-450 CYP2D6 Inhibitors (strength unknown)
- Cytochrome P-450 CYP2D6 Substrates
- Cytochrome P-450 CYP2E1 Substrates
- Cytochrome P-450 CYP3A Inhibitors
- Cytochrome P-450 CYP3A4 Inhibitors
- Cytochrome P-450 CYP3A4 Inhibitors (strength unknown)
- Cytochrome P-450 Enzyme Inhibitors
- Cytochrome P-450 Substrates
- Immunosuppressive Agents
- P-glycoprotein inhibitors
- Peripheral Nervous System Agents
- Pyridines
- Pyridones
- Sensory System Agents
- Tumor Necrosis Factor Blockers
- 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
- 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]
- 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]
- 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]
- 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]
- 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]
- 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]
- 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]
- 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]
- FDA Approved Drug Products: Esbriet (pirfenidone) for oral use [Link]
- Health Canada Product Monograph: Esbriet (pirfenidone) for oral use [Link]
- CaymanChem: Pirfenidone MSDS [Link]
- EMA Approved Drug Products: Pirfenidone AET (pirfenidone) Oral Tablets [Link]
- External Links
- PubChem Compound
- 40632
- PubChem Substance
- 175426915
- ChemSpider
- 37115
- BindingDB
- 50005201
- 1592254
- ChEBI
- 32016
- ChEMBL
- CHEMBL1256391
- ZINC
- ZINC000000001958
- Wikipedia
- Pirfenidone
Clinical Trials
- Clinical Trials
Phase Status Purpose Conditions Count 4 Completed Treatment Idiopathic Pulmonary Fibrosis (IPF) 3 4 Recruiting Treatment Connective Tissue Diseases / Interstitial Lung Disease / Pirfenidone 1 4 Recruiting Treatment Coronavirus Disease 2019 (COVID‑19) / Novel Coronavirus-induced Lung Fibrosis 1 4 Recruiting Treatment Progressive Idiopathic Pulmonary Fibrosis 1 4 Unknown Status Treatment Acute Kidney Injury (AKI) / Sepsis 1 4 Unknown Status Treatment Dermatopolymyositis / Interstitial Lung Disease 1 4 Unknown Status Treatment Sarcoidosis, Pulmonary 1 3 Active Not Recruiting Treatment Albuminuria / Diabetic Nephropathy 1 3 Completed Treatment Diabetic Foot Ulcers (DFUs) 1 3 Completed Treatment Idiopathic Pulmonary Fibrosis (IPF) 5
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage Forms
Form Route Strength Capsule Oral Capsule Oral 267 mg/1 Capsule Oral 267 mg Tablet Oral 267 mg Tablet Oral 801 mg Tablet, coated Oral 267 mg/1 Tablet, coated Oral 801 mg/1 Tablet, film coated Oral 534 MG Tablet, film coated Oral 267 mg Tablet, film coated Oral 801 mg Capsule, coated Oral 267 mg Tablet, film coated Oral 267.000 mg Tablet, film coated Oral 801.000 mg Capsule Oral 267.0 mg Tablet, film coated Oral Tablet Oral 267 mg/1 Tablet Oral 801 mg/1 Tablet, film coated Oral 267 mg/1 Tablet, film coated Oral 534 mg/1 Tablet, film coated Oral 801 mg/1 - Prices
- Not Available
- Patents
Patent Number Pediatric Extension Approved Expires (estimated) Region US7988994 No 2011-08-02 2026-09-22 US US7816383 No 2010-10-19 2030-01-08 US US8013002 No 2011-09-06 2030-01-08 US US8084475 No 2011-12-27 2030-01-08 US US8778947 No 2014-07-15 2033-08-30 US US7566729 No 2009-07-28 2029-04-22 US US7767225 No 2010-08-03 2026-09-22 US US7635707 No 2009-12-22 2029-04-22 US US7767700 No 2010-08-03 2027-12-18 US US8592462 No 2013-11-26 2029-04-22 US US8383150 No 2013-02-26 2026-09-22 US US8318780 No 2012-11-27 2030-01-08 US US8420674 No 2013-04-16 2027-12-18 US US7910610 No 2011-03-22 2030-01-08 US US8648098 No 2014-02-11 2030-01-08 US US8754109 No 2014-06-17 2030-01-08 US US8609701 No 2013-12-17 2029-04-22 US US8753679 No 2014-06-17 2026-09-22 US US7696236 No 2010-04-13 2027-12-18 US US9561217 No 2017-02-07 2022-01-25 US US10188637 No 2019-01-29 2037-03-28 US
Properties
- State
- Solid
- Experimental Properties
Property Value Source melting point (°C) 109 https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/022535s012,208780s002lbl.pdf - Predicted Properties
Property Value Source Water Solubility 2.89 mg/mL ALOGPS logP 2 ALOGPS logP 2.14 ChemAxon logS -1.8 ALOGPS pKa (Strongest Basic) -1.2 ChemAxon Physiological Charge 0 ChemAxon Hydrogen Acceptor Count 1 ChemAxon Hydrogen Donor Count 0 ChemAxon Polar Surface Area 20.31 Å2 ChemAxon Rotatable Bond Count 1 ChemAxon Refractivity 57 m3·mol-1 ChemAxon Polarizability 20.28 Å3 ChemAxon Number of Rings 2 ChemAxon Bioavailability 1 ChemAxon Rule of Five Yes ChemAxon Ghose Filter Yes ChemAxon Veber's Rule Yes ChemAxon MDDR-like Rule No ChemAxon - Predicted ADMET Features
Property Value Probability Human Intestinal Absorption + 0.9932 Blood Brain Barrier + 0.996 Caco-2 permeable + 0.8614 P-glycoprotein substrate Non-substrate 0.8193 P-glycoprotein inhibitor I Non-inhibitor 0.755 P-glycoprotein inhibitor II Non-inhibitor 0.9177 Renal organic cation transporter Non-inhibitor 0.8157 CYP450 2C9 substrate Non-substrate 0.6638 CYP450 2D6 substrate Non-substrate 0.8248 CYP450 3A4 substrate Substrate 0.6111 CYP450 1A2 substrate Inhibitor 0.9108 CYP450 2C9 inhibitor Non-inhibitor 0.5982 CYP450 2D6 inhibitor Non-inhibitor 0.9231 CYP450 2C19 inhibitor Non-inhibitor 0.7166 CYP450 3A4 inhibitor Non-inhibitor 0.775 CYP450 inhibitory promiscuity High CYP Inhibitory Promiscuity 0.7633 Ames test Non AMES toxic 0.7652 Carcinogenicity Non-carcinogens 0.8992 Biodegradation Not ready biodegradable 0.9112 Rat acute toxicity 2.1330 LD50, mol/kg Not applicable hERG inhibition (predictor I) Weak inhibitor 0.9784 hERG inhibition (predictor II) Non-inhibitor 0.6301
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
Spectrum Spectrum Type Splash Key Predicted MS/MS Spectrum - 10V, Positive (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 20V, Positive (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 40V, Positive (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 10V, Negative (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 20V, Negative (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 40V, Negative (Annotated) Predicted LC-MS/MS Not Available LC-MS/MS Spectrum - LC-ESI-qTof , Positive LC-MS/MS Not Available MS/MS Spectrum - , positive LC-MS/MS splash10-000i-2900000000-b9809376eba9769e9bee
Enzymes
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- SubstrateInhibitor
- 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
- 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]
- Health Canada Product Monograph: Esbriet (pirfenidone) for oral use [Link]
- FDA Approved Drug Products: Esbriet (pirfenidone) for oral use [Link]
- Pirfenidone FDA label [File]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- SubstrateInhibitor
- 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
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- SubstrateInhibitor
- 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
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- SubstrateInhibitor
- 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
- 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
- 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
- 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
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
- FDA Approved Drug Products: Esbriet (pirfenidone) for oral use [Link]
Drug created at October 21, 2007 22:23 / Updated at August 16, 2022 17:13