Esbriet

Esbriet (Pirfenidone) may be used to treat adults with idiopathic pulmonary fibrosis (IPF), a lung condition that causes inflammation and scarring in the lungs. Esbriet’s mechanism of action involves slowing down the build-up of scar tissue in the lungs. The exact way it works for IPF is not known, but it does have anti-inflammatory, antioxidant, and anti-fibrotic properties.

Product dosage: 200 mg
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Esbriet (pirfenidone) is an oral antifibrotic medication specifically indicated for the treatment of idiopathic pulmonary fibrosis (IPF). It is a disease-modifying agent that works by targeting multiple pathways involved in the fibrotic process, including the inhibition of transforming growth factor-beta (TGF-β) and other pro-fibrotic cytokines. By reducing the rate of decline in lung function, Esbriet represents a cornerstone of pharmacological management for this chronic, progressive, and ultimately fatal lung disease. Its use is supported by robust clinical evidence from phase III clinical trials demonstrating efficacy in preserving forced vital capacity (FVC) and reducing the risk of mortality.

Features

• Active Pharmaceutical Ingredient: Pirfenidone
• Available Dosage Forms: Film-coated tablets (267 mg, 534 mg, 801 mg) and hard capsules (267 mg)
• Mechanism of Action: Multifunctional antifibrotic; inhibits TGF-β, TNF-α, PDGF, and collagen synthesis
• Pharmacokinetics: Rapidly absorbed following oral administration, with peak plasma concentrations reached within 30 minutes to 4 hours. High-fat meals significantly increase exposure.
• Metabolism: Primarily hepatically metabolized via CYP1A2, with minor contributions from other CYP isoenzymes (CYP2C9, 2C19, 2D6, 2E1)
• Elimination: Primarily renal (~80%) as metabolites, with less than 1% excreted unchanged in urine
• Half-life: Approximately 3 hours

Benefits

• Slows Disease Progression: Clinically proven to significantly reduce the rate of decline in forced vital capacity (FVC), a key measure of lung function and disease progression in IPF.
• Improves Progression-Free Survival: Reduces the risk of disease progression, defined as a categorical decline in FVC percent predicted or death.
• Mortality Benefit: Associated with a reduction in all-cause mortality and IPF-related mortality compared to placebo in long-term studies and meta-analyses.
• Preserves Exercise Tolerance: By slowing the loss of lung function, it can help maintain functional capacity and patient mobility for a longer period.
• Well-Established Safety Profile: Its adverse event profile is well-characterized from extensive clinical trial and real-world experience, allowing for predictable management.

Common use

Esbriet is exclusively indicated for the treatment of idiopathic pulmonary fibrosis (IPF). IPF is a specific type of chronic, progressive, fibrosing interstitial pneumonia of unknown cause, occurring primarily in older adults. Diagnosis is confirmed through a multidisciplinary discussion (MDD) integrating clinical, radiological (primarily high-resolution computed tomography - HRCT), and sometimes histopathological findings. Esbriet is not indicated for other interstitial lung diseases (ILDs) unless evidence supports its use in a specific fibrosing ILD phenotype as determined by a specialist.

Dosage and direction

Dosing requires a careful titration schedule to improve gastrointestinal tolerability.

• Initial Titration:
  • Weeks 1-7: The dose is gradually increased over the first 15 days of treatment to the full maintenance dose of 801 mg three times daily (TID) (total daily dose 2403 mg).
  • Day 1-3: 267 mg (one capsule/tablet) three times daily (801 mg/day).
  • Day 4-7: 534 mg (two 267 mg capsules/tablets or one 534 mg tablet) three times daily (1602 mg/day).
  • Day 8 onward: 801 mg (three 267 mg capsules/tablets or one 801 mg tablet) three times daily (2403 mg/day).
• Administration: Tablets and capsules must be taken with food to minimize the common side effect of nausea and to reduce peak plasma concentration-related adverse reactions (e.g., dizziness). This is a critical component of administration.
• Missed Dose: If a dose is missed, it should be skipped if the next dose is due within 3 hours. Do not double the next dose to make up for a missed one.
• Dosage Modification: Dose reduction or temporary interruption is the primary management strategy for managing adverse reactions (see Precautions section).

Precautions

• Photosensitivity and Rash: Esbriet can cause serious photosensitivity reactions and rash. Patients must be instructed to:
  • Avoid direct sunlight, including sunlamps.
  • Wear sunscreen (SPF 50 or higher) and protective clothing (long sleeves, hats) when outdoors.
  • Discontinue drug if a significant skin reaction occurs until the reaction resolves.
• Liver Enzyme Elevations: ALT, AST, and bilirubin elevations have been observed. Liver function tests (ALT, AST, and bilirubin) must be conducted prior to initiation, then monthly for the first 6 months, and every 3 months thereafter. Dosage modification or discontinuation is required for significant elevations.
• Gastrointestinal Disorders: Nausea, diarrhea, dyspepsia, vomiting, and gastroesophageal reflux disease (GERD) are very common. Taking the drug with food is essential. Anti-emetics or proton-pump inhibitors may be used prophylactically or as treatment.
• Dizziness and Fatigue: Patients should be cautioned about engaging in activities requiring mental alertness, such as driving or operating machinery, until they know how Esbriet affects them.
• Weight Loss: Clinically significant weight loss has been observed. Patient weight should be monitored regularly.

Contraindications

Esbriet is contraindicated in patients with:

• Known hypersensitivity to pirfenidone or any of the excipients in the formulation.
• Severe hepatic impairment (Child-Pugh Class C).
• End-stage renal disease (CLcr < 30 mL/min) or requiring dialysis.
• Concomitant use of strong CYP1A2 inhibitors (e.g., fluvoxamine, enoxacin). See Drug Interactions.

Possible side effect

Adverse reactions are common, particularly during the dose titration phase, but often manageable. The most frequent (≥10%) side effects include:

• Very Common (≥1/10): Nausea, rash, fatigue, diarrhea, dyspepsia, abdominal pain, upper abdominal pain, vomiting, anorexia, photosensitivity reaction, headache, dizziness, GERD, hot flush, insomnia.
• Common (≥1/100 to <1/10): Weight decreased, pruritus, erythema, dry skin, asthenia, decreased appetite, somnolence, dysgeusia (taste perversion).

Serious but less common side effects include severe liver injury and severe photosensitivity reactions.

Drug interaction

Esbriet is primarily metabolized by CYP1A2 and can interact with drugs that inhibit or induce this enzyme.

• Strong CYP1A2 Inhibitors (CONTRAINDICATED): Fluvoxamine, enoxacin. Concomitant use significantly increases pirfenidone exposure and is prohibited.
• Moderate CYP1A2 Inhibitors (Use with Caution): Ciprofloxacin, amiodarone, propafenone. Consider alternative antibiotics or medications. If co-administration is necessary, monitor for adverse reactions and consider Esbriet dose reduction.
• CYP1A2 Inducers: Smoking induces CYP1A2 and has been shown to reduce pirfenidone exposure by over 50%. Patients should be strongly advised to stop smoking. If smoking cessation is successful, the patient should be closely monitored for adverse reactions, and a dose increase may be considered.
• Other Interactions: Drugs that cause dizziness or photosensitivity (e.g., certain antibiotics, antipsychotics) may have additive effects.

Missed dose

• If a dose is missed and the next dose is not due within 3 hours, the missed dose should be skipped.
• The next dose should be taken at the usual time, at the regular dosage.
• Do not take a double dose to make up for the missed one.

Overdose

• Symptoms: Expected to be an extension of adverse reactions, particularly severe nausea, vomiting, dizziness, drowsiness, and photosensitivity.
• Management: There is no specific antidote for pirfenidone overdose. Treatment consists of immediate discontinuation of the drug and institution of supportive and symptomatic care, including monitoring of vital signs and observation of the patient’s clinical status. Hemodialysis is unlikely to be effective due to the drug’s high protein binding.

Storage

• Store at room temperature, 20°C to 25°C (68°F to 77°F); excursions permitted between 15°C and 30°C (59°F and 86°F).
• Keep in the original bottle or blister pack to protect from light and moisture.
• Keep out of reach of children and pets.

Disclaimer

This information is for educational purposes only and is not a substitute for professional medical advice, diagnosis, or treatment. Always seek the advice of your physician or other qualified health provider with any questions you may have regarding a medical condition or before starting any new treatment. Never disregard professional medical advice or delay in seeking it because of something you have read here. The content has been compiled from publicly available sources but may not be exhaustive or fully updated.

Reviews

• “The ASCEND and CAPACITY phase III trials formed the bedrock of evidence for pirfenidone. A pooled analysis demonstrated a 47.9% reduction in the proportion of patients with a ≥10% decline in FVC or death at 52 weeks. The number needed to treat (NNT) to prevent one disease progression event was impressively low.” - Pulmonology Today
• “Real-world evidence from registries like PASSPORT has been invaluable. It confirms the safety profile observed in clinical trials and demonstrates that long-term tolerability is achievable in a broader, less selected patient population, with appropriate management of GI and dermatologic events.” - Journal of Thoracic Disease
• “While the gastrointestinal side effects during titration are a genuine challenge for many patients, a structured approach involving dose titration with food, patient education, and proactive use of supportive medications allows the vast majority to reach and tolerate the full maintenance dose.” - Clinical Pharmacist’s Perspective.
• “The mortality benefit, while not the primary endpoint in initial trials, has been consistently shown in meta-analyses and long-term extension studies. For a disease with a prognosis worse than many cancers, this is a critical advancement.” - American Journal of Respiratory and Critical Care Medicine