Esbriet (pirfenidone)
Last reviewed · Source: First Databank (FDB) drug data
Overview
Pirfenidone, a synthetic pyridone, is an antifibrotic agent.
Pirfenidone, a synthetic pyridone, is an antifibrotic agent. Although the precise mechanism of action of pirfenidone in the treatment of idiopathic pulmonary fibrosis (IPF) has not been fully elucidated, it is thought to be related to the drug's antifibrotic, anti-inflammatory, and antioxidant properties.
Pirfenidone has been shown to inhibit the activation of transforming growth factor-beta (TGF-beta), a profibrotic, proinflammatory cytokine. In vitro, pirfenidone suppressed TGF-beta-mediated proliferation of human lung fibroblasts and differentiation into myofibroblasts, a process that may lead to excessive collagen deposition and fibrosis in the lungs. Pirfenidone also inhibited the release of proinflammatory cytokines (e.g., IL-1beta, IL-6, tumor necrosis factor (TNF)-alpha, platelet derived growth factor (PDGF)) in animal models and in vitro.
In addition, pirfenidone demonstrated antioxidant activity in vitro through its ability to scavenge reactive oxygen species (ROS), including hydroxyl radicals and superoxide anions.
Following oral administration, peak plasma concentrations of pirfenidone are achieved at a median of 0.5 hours (range 0.5-4 hours). Administration with food decreases the systemic exposure of pirfenidone by 16%, delays median time to peak plasma concentrations by 2.5 hours, and reduces the incidence of adverse effects compared with administration in the fasting state. Pirfenidone is 58% bound to plasma proteins (mainly albumin) at therapeutic concentrations.
Pirfenidone is metabolized principally (70-80%) by cytochrome P-450 (CYP) isoenzyme 1A2; CYP2C9, 2C19, 2D6, and 2E1 also play a role in the drug's overall metabolism. Approximately 80% of a dose is excreted in urine within 24 hours, mainly as its major metabolite, 5-carboxy-pirfenidone, which is expected to be pharmacologically inactive. The mean terminal half-life of pirfenidone in healthy individuals is approximately 3 hours.
Bioequivalence was demonstrated during the fasting state between the 801 mg tablet and three 267 mg capsules; the effects of food on pirfenidone exposure was also consistent between the two formulations. Data from a population pharmacokinetic analysis indicate that age, gender, body mass index (BMI), and race do not have clinically important effects on the pharmacokinetics of pirfenidone.
USES: Pirfenidone is used to treat a certain lung disease called idiopathic pulmonary fibrosis (IPF). This disease causes the lungs to get scarred and become stiff, making it hard to breathe. Pirfenidone may help slow down the worsening of your IPF.
Generic name: pirfenidone
Pronunciation: (pir-FEN-i-done)
Reference product & biosimilars
No reference, biosimilar or interchangeable associated with this drug.
Today’s intelligence on Esbriet
Indications
The following indications are listed for Esbriet:
- Idiopathic Pulmonary Fibrosis
Also known as: Cryptogenic Fibrosing Alveolitis, Idiopathic Fibrosing Alveolitis.
Dosing
No dosing information is available for this tab.
Pirfenidone is administered orally 3 times daily with food, at the same time every day.
If a dose of pirfenidone is missed, the next dose should be administered as soon as it is remembered; a double dose should not be administered to make up for a missed dose. No more than 3 doses should be taken per day.
Store capsules and tablets at 25degreesC; excursions permitted between 15-30degreesC.
No dosing information is available for this tab.
No dosing information is available for this tab.
Drug interactions
Pirfenidone is metabolized principally by cytochrome P-450 (CYP) isoenzyme 1A2, and, to a lesser extent, by CYP isoenzymes 2C9, 2C19, 2D6, and 2E1.
In vitro studies indicate that pirfenidone has a weak inhibitory potential on P-glycoprotein (P-gp); effects of pirfenidone on P-gp substrates have not been studied to date.
Pirfenidone also demonstrated concentration-dependent inhibition of CYP2C9, 2C19, 1A2, 2D6, and 3A4 in vitro; effects of pirfenidone on drugs metabolized by these isoenzymes have not been studied to date.
There are no contraindication interactions for this drug.
There are no severe interactions for this drug.
There are no moderate interactions for this drug.
Contraindications
*None.
There are no contraindication contraindications for this drug.
There are no severe contraindications for this drug.
There are no moderate contraindications for this drug.
Adverse reactions
Adverse effects reported in >=10% of patients receiving pirfenidone include nausea, rash, abdominal pain, upper respiratory tract infection, diarrhea, fatigue, headache, dyspepsia, dizziness, vomiting, decreased appetite, GERD, sinusitis, insomnia, decreased weight, and arthralgia.
There are no severe adverse reactions for this drug.
There are no less severe adverse reactions for this drug.
Precautions
No enhanced messaging available.
Safety and efficacy of pirfenidone have not been established in pediatric patients.
Data on the use of pirfenidone in pregnant females are insufficient to determine the drug-associated risks of birth defects and miscarriage. In animal reproductive studies, pirfenidone was not teratogenic when administered at oral doses up to 2 and 3 times the maximum recommended adult dosage.
No data is available on the presence of pirfenidone or its metabolites in human milk, the effects of the drug on the breastfed child, or the effects of the drug on milk production. The known benefits of breastfeeding should be considered along with the mother's clinical need for pirfenidone and any potential adverse effects on the breast-fed infant from either the drug or the underlying maternal condition.
Pirfenidone or its metabolites are distributed into milk in rats; it is not known whether the drug is distributed into human milk.
No dosage adjustment is required for geriatric patients.
In clinical studies of pirfenidone, 67% of patients were >=65 years of age and 22% were >=75 years of age. No overall differences in safety and efficacy were observed between geriatric patients and younger adults.
ICD codes
No ICD codes are available for this drug.
Formulary status
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Last reviewed · Source: First Databank (FDB) drug data
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