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, thereby reducing the rate of decline in lung function. This therapy represents a significant advancement in the management of this chronic, progressive, and ultimately fatal lung disease, offering a targeted approach to slow its relentless progression and help preserve patients’ functional capacity.

Features

• Active Pharmaceutical Ingredient: Pirfenidone
• Available as film-coated tablets (267 mg and 801 mg)
• Oral administration
• Triple mechanism of action: antifibrotic, anti-inflammatory, antioxidant
• Dosed three times daily with food

Benefits

• Significantly reduces the rate of decline in forced vital capacity (FVC), a key measure of lung function.
• Demonstrated in clinical trials to reduce the risk of disease progression by approximately 50% over one year.
• May prolong progression-free survival in patients with mild to moderate IPF.
• Offers a well-characterized safety and tolerability profile based on extensive clinical trial data and real-world experience.
• Provides a targeted therapeutic option for a disease with historically limited treatment choices.

Common use

Esbriet is approved for the treatment of idiopathic pulmonary fibrosis (IPF). IPF is a specific, chronic, progressive, fibrosing interstitial pneumonia of unknown cause, primarily occurring in older adults. It is characterized by a progressive and irreversible decline in lung function. Diagnosis requires a combination of high-resolution computed tomography (HRCT) showing a usual interstitial pneumonia (UIP) pattern and, in certain cases, histopathological confirmation via surgical lung biopsy, following the exclusion of other known causes of interstitial lung disease (ILD). Esbriet is indicated irrespective of disease severity at the time of diagnosis, within its approved label.

Dosage and direction

The dosage of Esbriet must be titrated to the full maintenance dose to improve gastrointestinal tolerability. The recommended maintenance dosage is 801 mg (three 267 mg tablets or one 801 mg tablet) three times daily, for a total daily dose of 2403 mg.

• Weeks 1-3: 267 mg (one tablet) three times daily with food.
• Weeks 4-7: 534 mg (two 267 mg tablets) three times daily with food.
• Week 8 onward (Maintenance): 801 mg (three 267 mg tablets or one 801 mg tablet) three times daily with food.

Administration with food is crucial to minimize the potential for nausea and dizziness. Tablets should be swallowed whole and not crushed, split, or chewed. Dose modification or interruption is recommended for patients who experience significant adverse reactions. Dose reduction to 534 mg three times daily is often sufficient to manage intolerance; therapy can be re-titrated to the full dose based on clinical judgment and patient tolerance.

Precautions

• Photosensitivity and Rash: Esbriet can cause serious photosensitivity reactions and rash. Patients must be advised to avoid or minimize exposure to sunlight (including sunlamps), to use a high-factor sunblock (SPF 50 or higher), and to wear protective clothing that covers the skin when outdoors.
• Liver Enzyme Elevations: ALT, AST, and bilirubin elevations have been observed. Liver function tests (ALT, AST, and bilirubin) should be conducted prior to initiating therapy, 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 are common. These can often be managed by administering the drug with food, dose reduction, or temporary interruption, and with concomitant antiemetic or antacid therapy.
• Dizziness and Fatigue: Patients should be cautioned about engaging in activities requiring mental alertness, such as driving or operating machinery, until they understand how Esbriet affects them.
• Weight Loss: Patients should have their weight monitored regularly.

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).
• Severe renal impairment (CrCl <30 mL/min) or end-stage renal disease requiring dialysis.
• Concomitant use of fluvoxamine or other strong inhibitors of CYP1A2, due to the risk of significantly increased pirfenidone exposure.

Possible side effect

The most frequently reported adverse reactions (incidence ≥10% and more common than placebo) are:

• Nausea
• Rash
• Abdominal pain
• Upper respiratory tract infection
• Diarrhea
• Fatigue
• Headache
• Dyspepsia
• Dizziness
• Vomiting
• Anorexia
• Gastro-esophageal reflux disease
• Sinusitis
• Insomnia
• Weight decreased
• Arthralgia
• Photosensitivity reaction

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

Drug interaction

Esbriet is primarily metabolized by the hepatic enzyme CYP1A2. Concomitant medications can significantly alter its plasma concentrations.

• Strong CYP1A2 Inhibitors (e.g., fluvoxamine, enoxacin): Contraindicated. Co-administration leads to a dramatic increase in pirfenidone exposure.
• 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. Patients should be advised to stop smoking. Concomitant use of omeprazole may require monitoring.
• Other Medicinal Products: Drugs that cause dizziness, nausea, or photosensitivity as side effects may have additive effects when taken with Esbriet.

Missed dose

If a dose is missed, it should be skipped if the next dose is due within 3 hours. Patients should never take a double dose to make up for a missed one. They should resume the usual dosing schedule with the next prescribed dose.

Overdose

There is limited experience with overdose in humans. The highest known accidental ingestion was 1005 mg/kg in a patient who experienced transient nausea and vomiting. In the event of a suspected overdose, symptomatic and supportive medical therapy should be instituted. Monitoring of vital signs and close observation of the clinical status of the patient is recommended. Since pirfenidone is extensively protein-bound, dialysis is not expected to be an effective means of enhancing its elimination.

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 container to protect from light and moisture.
• Keep out of the sight and reach of children.

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

“Since initiating Esbriet 18 months ago, my patient’s FVC has remained remarkably stable. The initial GI side effects were challenging but were effectively managed with dose titration and antiemetics. This stability has had a profoundly positive impact on his quality of life and daily activities.” – Pulmonologist, Academic Medical Center

“In the real-world setting, we see that Esbriet can effectively slow disease progression in a meaningful proportion of our IPF patients. The key to success is careful patient education, particularly regarding sun protection, and proactive management of gastrointestinal symptoms during the titration phase.” – Interstitial Lung Disease Specialist

“While not a cure, Esbriet provides us with a vital tool to actively manage IPF. The clinical trial data is robust, and we now have years of post-marketing experience confirming its role in altering the natural history of this devastating disease for many patients.” – Director of Pulmonary Medicine