Esbriet: Slows Idiopathic Pulmonary Fibrosis Progression
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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, as well as reducing collagen synthesis. Clinical trials have consistently demonstrated its efficacy in significantly slowing the decline of forced vital capacity (FVC), a key measure of lung function, and reducing the risk of all-cause mortality. This medication represents a cornerstone of pharmacological management for IPF, offering a proactive approach to disease management for appropriate patients under specialist supervision.
Features
- Active Pharmaceutical Ingredient: Pirfenidone
- Available Dosage Forms: Film-coated tablets (267 mg, 801 mg) and hard capsules (267 mg)
- Mechanism of Action: Multifunctional antifibrotic with anti-inflammatory and antioxidant properties
- Regulatory Status: FDA-approved, EMA-approved
- Recommended Titration: Requires a structured dose-escalation regimen over 14 days
- Bioavailability: High, with peak plasma concentrations reached within ~3 hours post-dose
- Metabolism: Primarily hepatic, via CYP1A2 and other enzymes
- Elimination Half-life: Approximately 3 hours
Benefits
- Slows Disease Progression: Clinically proven to significantly reduce the rate of decline in forced vital capacity (FVC), a primary predictor of mortality in IPF.
- Improves Long-Term Outcomes: Associated with a reduction in the risk of all-cause mortality and disease progression over time.
- Preserves Functional Capacity: By slowing the loss of lung function, it can help maintain patients’ ability to perform daily activities and exercise tolerance for longer.
- Well-Established Efficacy and Safety Profile: Supported by extensive clinical trial data and years of real-world post-marketing experience, providing confidence in its use.
- Oral Administration: Convenient oral dosing allows for treatment in an outpatient setting, supporting patient independence.
Common use
Esbriet is exclusively indicated for the treatment of idiopathic pulmonary fibrosis (IPF). IPF is a chronic, progressive, and ultimately fatal lung disease characterized by the scarring (fibrosis) of lung tissue, leading to a progressive and irreversible loss of lung function. Diagnosis must be confirmed by a specialist, typically through a multidisciplinary discussion (MDD) that integrates high-resolution computed tomography (HRCT) findings and, in some cases, histopathology. Esbriet is not indicated for other interstitial lung diseases (ILDs) unless evidence supports its use in specific non-IPF progressive fibrosing ILDs, as per local guidelines.
Dosage and direction
The dosage of Esbriet must be carefully titrated to improve gastrointestinal tolerability. The recommended maintenance dosage is 801 mg (three 267 mg tablets or one 801 mg tablet) taken three times daily with food, for a total daily dose of 2403 mg.
- Weeks 1 and 2 (Titration):
- Days 1-7: 267 mg (one tablet/capsule) three times daily (total 801 mg/day).
- Days 8-14: 534 mg (two 267 mg tablets/capsules) three times daily (total 1602 mg/day).
- Day 15 onward (Maintenance): 801 mg three times daily (total 2403 mg/day). Doses should be taken at the same times each day, approximately 8 hours apart, with a meal or snack to minimize nausea and dizziness.
Dosage adjustments, interruptions, or discontinuation may be necessary based on tolerability, particularly for management of photosensitivity reactions or liver enzyme elevations.
Precautions
- Photosensitivity and Phototoxicity: Esbriet can cause serious skin reactions to sunlight (including sunburn, rash, and blistering). Patients must adopt stringent sun-protective measures: wear sunscreen (SPF 50+), sun-protective clothing, and avoid direct sun exposure, including through glass. This precaution should continue for at least two weeks after the last dose.
- Liver Enzyme Elevations: ALT, AST, and bilirubin levels should be monitored prior to initiation, monthly for the first 6 months, and then every 3 months thereafter. Dosage modification or discontinuation is required for significant elevations.
- Gastrointestinal Events: Nausea, diarrhea, dyspepsia, vomiting, and gastroesophageal reflux disease (GERD) are common. Taking the medication with food and using antiemetic or antacid therapy prophylactically is advised.
- 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: Monitor patient weight regularly. Significant, unintentional weight loss may require nutritional support and dose modification.
Contraindications
Esbriet is contraindicated in patients with:
- A 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) requiring dialysis.
- Concomitant use of strong inhibitors of both CYP1A2 and other CYP enzymes involved in pirfenidone’s metabolism (e.g., fluvoxamine, enoxacin).
- Concomitant use of strong CYP1A2 inducers (e.g., tobacco smoking, rifampin).
Possible side effect
The most frequently observed adverse reactions are largely gastrointestinal and dermatological. Their incidence can often be mitigated by dose titration and concomitant administration with food.
- Very Common (≥1/10): Nausea, rash, fatigue, diarrhea, dyspepsia, abdominal discomfort, anorexia, photosensitivity reaction, vomiting, GERD, dizziness.
- Common (≥1/100 to <1/10): Insomnia, headache, dysgeusia (taste perversion), hot flush, decreased appetite, weight decrease, pruritus, eczema, sunburn, elevated gamma-glutamyltransferase (GGT).
- Uncommon (≥1/1,000 to <1/100): Angioedema, drug-induced liver injury.
Drug interaction
Esbriet has a significant and complex drug interaction profile due to its metabolism primarily by CYP1A2.
- CYP1A2 Inhibitors (Strong/Moderate): Concomitant use with strong inhibitors (e.g., fluvoxamine, enoxacin) is contraindicated. Use with moderate inhibitors (e.g., ciprofloxacin, amiodarone, oral contraceptives) should be avoided. If unavoidable, reduce the Esbriet dose to 267 mg three times daily (801 mg/day).
- CYP1A2 Inducers: Concomitant use with strong inducers (e.g., tobacco smoking, rifampin, carbamazepine, omeprazole) is contraindicated, as they can significantly decrease pirfenidone exposure, rendering it therapeutically ineffective.
- Other Medicinal Products: Caution is advised with other drugs known to cause photosensitivity (e.g., tetracyclines, fluoroquinolones, thiazides) due to the additive risk of phototoxic reactions.
- Other CYP Substrates: Pirfenidone may potentially influence the metabolism of other drugs metabolized by CYP1A2, CYP2C9, CYP2C19, CYP2D6, and CYP3A4.
Missed dose
If a dose is missed, it should be skipped if the next dose is due within 3 hours. The patient should then resume the normal dosing schedule with the next planned dose. Do not double the next dose to make up for the missed one. Maintaining a consistent dosing schedule is important for stable plasma levels.
Overdose
There is limited experience with pirfenidone overdose. Single doses up to 4005 mg and repeated doses up to 3600 mg/day for up to 10 days have been reported with adverse events similar to those seen at recommended doses (e.g., GI events, photosensitivity, dizziness). There is no known specific antidote. In the event of a suspected overdose, general supportive measures should be initiated, 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 in the original package at 20°C to 25°C (68°F to 77°F); excursions permitted between 15°C and 30°C (59°F and 86°F).
- Keep the blister strips in the outer carton to protect from light and moisture.
- Keep out of the sight and reach of children.
- Do not use after the expiration date printed on the packaging.
Disclaimer
This information is intended for educational and informational purposes only for healthcare professionals and does not constitute medical advice. It is a summary based on the approved product labeling and may not encompass all available data. The ultimate authority regarding a patient’s treatment plan resides with the qualified treating physician, who must make decisions based on the individual patient’s clinical status, official prescribing information, and current clinical guidelines. Patients must be directed to consult their healthcare provider for any questions about their medical condition or treatment.
Reviews
- Clinical Trial Data (ASCEND and CAPACITY): “Pirfenidone demonstrated a statistically significant reduction in the decline of FVC percent predicted at week 52 compared to placebo. The relative reduction in the proportion of patients with a ≥10% decline in FVC or death was also significant. The safety profile was manageable with proactive monitoring and dose adjustment.” - New England Journal of Medicine
- Real-World Evidence (RECAP): “This long-term open-label extension study supported the sustained efficacy and acceptable long-term tolerability profile of pirfenidone in patients with IPF, with a safety profile consistent with that observed in the pivotal phase 3 trials.” - Lancet Respiratory Medicine
- Expert Consensus (ATS/ERS/JRS/ALAT Guidelines): “Pirfenidone is conditionally recommended for the treatment of IPF based on high-quality evidence showing a reduction in disease progression.” - American Journal of Respiratory and Critical Care Medicine