Esbriet

Esbriet (pirfenidone) is an oral antifibrotic medication specifically indicated for the treatment of idiopathic pulmonary fibrosis (IPF). It is a disease-modifying agent that targets the underlying pathological processes of IPF, working to slow the decline in lung function. By reducing the rate of forced vital capacity (FVC) decline, Esbriet helps to preserve patients’ functional status and may improve long-term outcomes in this progressive and ultimately fatal condition. Treatment is initiated and monitored by pulmonologists and specialist healthcare providers.

Features

• Contains the active pharmaceutical ingredient pirfenidone.
• Available in 267 mg and 801 mg film-coated tablets for flexible dosing.
• A targeted antifibrotic and anti-inflammatory mechanism of action.
• Dosing is weight-based and follows a specific titration schedule to improve tolerability.
• Requires administration with food to maximize bioavailability and minimize adverse effects.

Benefits

• Slows Disease Progression: Clinically proven to reduce the rate of decline in lung function, as measured by forced vital capacity (FVC).
• Preserves Functional Capacity: By slowing fibrosis, it can help maintain patients’ ability to perform daily activities for a longer period.
• Improves Long-Term Outcomes: Associated with a reduction in the risk of all-cause mortality over time.
• Well-Established Efficacy: Supported by extensive clinical trial data (CAPACITY, ASCEND) and real-world evidence.
• Oral Convenience: Allows for treatment outside of a clinical setting, supporting patient independence.

Common use

Esbriet is exclusively indicated for the treatment of idiopathic pulmonary fibrosis (IPF). IPF is a chronic, progressive, and irreversible lung disease characterized by the scarring (fibrosis) of lung tissue, which leads to a gradual and unremitting loss of respiratory function. Diagnosis is typically confirmed through a multidisciplinary discussion (MDD) incorporating high-resolution computed tomography (HRCT) findings, and sometimes lung biopsy. Esbriet is prescribed for patients with mild to moderate impairment in lung function, though its use may be considered across a spectrum of disease severity at the discretion of a specialist.

Dosage and direction

Dosage must be individualized based on patient tolerability and administered under the supervision of a physician experienced in the management of IPF.

• Initial Titration: The dosage is titrated over a 14-day period to the full maintenance dose to improve gastrointestinal tolerability.
  • Days 1-7: 267 mg (one tablet) three times daily (801 mg/day total).
  • Days 8-14: 534 mg (two tablets) three times daily (1602 mg/day total).
• Maintenance Dose: From Day 15 onward, the full maintenance dose is 801 mg (three tablets) three times daily with food, for a total daily dose of 2403 mg.
• Administration: Tablets must be swallowed whole and not crushed or split. Each dose must be taken with food to reduce the likelihood of nausea and dizziness.

Precautions

• Photosensitivity: Esbriet can cause serious skin reactions to sunlight, including sunburn, rash, and blistering. Patients must be advised to use a high-SPF (50+) sunscreen, wear protective clothing, and avoid direct sun exposure, including tanning beds, during treatment and for some time after discontinuation.
• 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 may be necessary for significant elevations.
• Gastrointestinal Events: Nausea, diarrhea, dyspepsia, vomiting, and gastroesophageal reflux disease are common, particularly during the titration phase. Administration with food and antiemetic/proton-pump inhibitor therapy can help manage these effects.
• 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: Clinicians should monitor patient weight regularly, as significant, unintentional weight loss may occur.

Contraindications

Esbriet is contraindicated in patients with:

• Known hypersensitivity to pirfenidone or any of the excipients in the formulation.
• Severe hepatic impairment.
• Severe renal impairment (CrCl <30 mL/min) or end-stage renal disease requiring dialysis.
• Concomitant use with strong CYP1A2 inhibitors (e.g., fluvoxamine, enoxacin).

Possible side effect

The most common adverse reactions (incidence >5% and greater than placebo) are:

• Gastrointestinal: Nausea, diarrhea, dyspepsia, vomiting, abdominal pain, gastroesophageal reflux disease, decreased appetite.
• Dermatological: Photosensitivity reaction or rash, pruritus.
• General: Fatigue, dizziness, headache.
• Insomnia.
• Upper respiratory tract infection.
• Arthralgia. Serious side effects include drug-induced liver injury and severe photosensitivity reactions.

Drug interaction

Esbriet is primarily metabolized by the CYP1A2, and to a lesser extent, CYP2C9, CYP2C19, CYP2D6, and CYP2E1 enzyme systems. Significant interactions include:

• Strong CYP1A2 Inhibitors (e.g., fluvoxamine, enoxacin): Contraindicated. Concomitant use significantly increases pirfenidone exposure, raising the risk of adverse effects.
• Moderate CYP1A2 Inhibitors (e.g., ciprofloxacin): Use with caution. A dose reduction of Esbriet may be required.
• CYP1A2 Inducers (e.g., omeprazole, smoking): May decrease pirfenidone exposure, potentially reducing efficacy. Smokers may require a higher dose, though smoking cessation is strongly advised for IPF patients and will necessitate a dose re-evaluation.
• Other Drugs: Use caution with other medications that cause photosensitivity (e.g., tetracyclines, fluoroquinolones, thiazides) or dizziness.

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.
• Resume the normal dosing schedule with the next prescribed dose.

Overdose

• There is no known specific antidote for pirfenidone overdose.
• Reported symptoms of overdose are extensions of its known adverse effects, particularly severe nausea, vomiting, dizziness, and photosensitivity.
• Management involves immediate discontinuation of the drug, supportive and symptomatic care, including monitoring of vital signs and ECG. Gastric lavage may be considered if presented soon after ingestion.
• Hemodialysis is unlikely to be effective due to the high protein binding of pirfenidone.

Storage

• Store at room temperature between 20°C to 25°C (68°F to 77°F). Excursions are permitted between 15°C and 30°C (59°F and 86°F).
• Keep in the original bottle 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.

Reviews

“After initiating Esbriet for my IPF, my FVC decline has stabilized significantly over the past 18 months. The initial GI side effects were challenging during titration but were well-managed with dietary adjustments and supportive medications. The photosensitivity is a serious consideration, requiring diligent sun protection, but the trade-off for stabilized lung function is unequivocally worth it.” – Patient M., 68

“From a clinical perspective, Esbriet remains a cornerstone of pharmacological management for IPF. The data from long-term extension studies and real-world evidence continue to support its role in modifying the disease trajectory. Managing patient expectations regarding the side effect profile, particularly during the titration phase, is crucial for adherence and long-term success.” – Dr. A. Reynolds, Pulmonologist