Esbriet (Pirfenidone) – Complete Product Information

Esbriet (pirfenidone) represents a groundbreaking therapeutic approach for idiopathic pulmonary fibrosis, offering the first FDA-approved treatment specifically designed to slow the progression of this devastating lung disease. As a small molecule anti-fibrotic agent, pirfenidone addresses the fundamental pathological processes driving IPF, providing patients with a treatment option that can meaningfully impact disease trajectory and quality of life.

Idiopathic pulmonary fibrosis is a chronic, progressive, and ultimately fatal lung disease characterized by excessive accumulation of collagen and other extracellular matrix proteins in the lungs. This fibrotic process leads to progressive scarring, stiffening of lung tissue, and irreversible decline in lung function. The disease typically affects adults over 50 years of age, with a median survival of 3-5 years from diagnosis, making effective treatment critically important for patient outcomes.

Mechanism of Action and Anti-fibrotic Properties: Pirfenidone’s therapeutic effects result from its multi-faceted interference with fibrotic processes. The medication inhibits the synthesis and activity of transforming growth factor-beta (TGF-β), a key cytokine that drives fibroblast proliferation and collagen production. By blocking TGF-β pathways, pirfenidone reduces the excessive collagen deposition that characterizes IPF progression.

Additionally, pirfenidone demonstrates anti-inflammatory properties by reducing inflammatory cell infiltration and cytokine production in lung tissue. The medication also exhibits antioxidant effects, helping to reduce oxidative stress that contributes to lung tissue damage. These combined mechanisms create a comprehensive approach to slowing fibrotic progression rather than simply treating symptoms.

Clinical Evidence and Disease Modification: The efficacy of Esbriet has been demonstrated in multiple large-scale clinical trials showing significant reduction in disease progression. In the pivotal CAPACITY and ASCEND studies, pirfenidone reduced the decline in forced vital capacity (FVC) by approximately 50% compared to placebo, representing a clinically meaningful slowing of disease progression.

Importantly, Esbriet doesn’t improve existing lung function but rather slows the rate of decline, helping patients maintain their current breathing capacity longer than would occur with disease progression alone. This disease-modifying effect can translate to extended time before patients require supplemental oxygen, lung transplantation, or experience respiratory failure.

Dosing Strategy and Titration: Esbriet treatment requires careful dose titration to optimize therapeutic benefits while minimizing side effects. The medication is initiated at a low dose of 267mg three times daily for the first week, then increased gradually over 14 days to reach the target maintenance dose of 801mg three times daily (2403mg total daily dose). This titration schedule helps patients adjust to the medication and reduces the likelihood of gastrointestinal side effects.

The medication must be taken with food to improve tolerability and reduce gastrointestinal upset. The three-times-daily dosing schedule maintains consistent drug levels throughout the day, optimizing anti-fibrotic effects. Patients who experience side effects may require dose reductions or temporary treatment interruptions, but maintaining the highest tolerated dose is important for therapeutic effectiveness.

Patient Monitoring and Safety Management: Treatment with Esbriet requires comprehensive monitoring due to potential serious adverse effects. Liver function tests must be performed before starting treatment, monthly for the first six months, and every three months thereafter. Drug-induced liver injury (DILI) represents a serious risk that has resulted in severe liver damage and even fatal outcomes in rare cases.

Photosensitivity reactions occur in approximately 9% of patients, requiring strict sun protection measures including high SPF sunscreen, protective clothing, and avoidance of sun exposure. Patients must understand that even brief sun exposure can cause severe burning and skin reactions while taking Esbriet.

Drug Interactions and Contraindications: Pirfenidone undergoes extensive hepatic metabolism, primarily through CYP1A2 enzymes, creating potential for significant drug interactions. Strong CYP1A2 inhibitors like fluvoxamine can dramatically increase pirfenidone levels, requiring dose reductions or alternative treatments. Smoking, conversely, induces CYP1A2 and can reduce pirfenidone levels, potentially compromising efficacy.

Patients must discontinue smoking before starting Esbriet and avoid tobacco products throughout treatment. The interaction with smoking is clinically significant enough that continued smoking may compromise therapeutic effectiveness. Healthcare providers should provide smoking cessation support as part of comprehensive IPF management.

Quality of Life and Long-term Outcomes: While Esbriet doesn’t reverse existing lung damage, the medication can significantly impact quality of life by slowing disease progression. Patients may experience extended periods of stable breathing capacity, delayed need for supplemental oxygen, and potentially extended survival. The preservation of lung function can allow patients to maintain independence and daily activities longer than would occur with untreated disease progression.

However, patients should understand that IPF remains a progressive disease even with treatment. Esbriet represents disease modification rather than cure, and patients will likely continue to experience some decline in lung function over time, though at a slower rate than without treatment.

Treatment Adherence and Patient Education: Successful Esbriet therapy requires excellent patient adherence and understanding of treatment goals. The medication’s side effect profile, particularly gastrointestinal symptoms and photosensitivity, can challenge patient compliance. Healthcare teams must provide comprehensive education about taking the medication with food, sun protection measures, and the importance of reporting side effects promptly.

For patients with idiopathic pulmonary fibrosis, Esbriet offers significant therapeutic potential when used appropriately under pulmonologic supervision. Those exploring treatment options should work with experienced pulmonologists who can coordinate comprehensive care including pulmonary function monitoring, liver safety assessment, and management of treatment-related side effects. Patients seeking affordable IPF treatment options should understand that while Esbriet represents advanced therapy, the medication requires ongoing medical monitoring and should never be used without appropriate pulmonologic oversight and regular safety assessments, as the benefits and risks of anti-fibrotic therapy require specialized expertise for optimal patient outcomes and safety management.

Brand	Esbriet Brand
Form	267mg 90 Tablets, 801mg 90 Tablets

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Esbriet can cause significant side effects ranging from common gastrointestinal symptoms to serious liver injury and severe skin reactions. Understanding these potential effects is crucial for safe treatment, as many require immediate medical attention or dose modifications to prevent serious complications.

Most Common Side Effects (>5% of patients):

Gastrointestinal symptoms: Nausea, stomach upset, diarrhea, vomiting, loss of appetite
Heartburn (acid reflux): Gastroesophageal reflux symptoms
Weight loss: Often related to gastrointestinal side effects and reduced appetite
Fatigue: Tiredness and reduced energy levels
Dizziness: Balance problems and lightheadedness
Joint pain: Musculoskeletal discomfort affecting mobility
Skin rash: Various skin reactions, often related to sun exposure

Serious Liver Side Effects (Black Box Warning Level):

Drug-induced liver injury (DILI): Can be severe and potentially fatal
Elevated liver enzymes: ALT/AST elevations ≥3× upper normal in 3.7% vs 0.8% placebo
Severe liver injury: Elevations ≥10× upper normal in rare cases
Fatal liver damage: Rare but reported cases of death from liver injury
Yellowing of skin or eyes (jaundice): Sign of serious liver dysfunction
Dark or brown urine: Indication of liver problems
Upper right stomach pain: Liver-related abdominal discomfort
Easy bleeding or bruising: Reduced liver function affecting blood clotting
Increased fatigue: Severe tiredness from liver dysfunction

Serious Skin Reactions:

Photosensitivity reactions (9% vs 1% placebo): Severe sun sensitivity causing burns
Stevens-Johnson syndrome (SJS): Life-threatening skin and mucous membrane reactions
Toxic epidermal necrolysis (TEN): Severe skin detachment requiring emergency care
Drug reaction with eosinophilia and systemic symptoms (DRESS): Multi-organ hypersensitivity
Severe cutaneous adverse reactions (SCAR): Various serious skin complications
Severe burning with minimal sun exposure: Even brief sunlight causing significant burns
Blistering and peeling: Skin reactions requiring dermatologic evaluation

Gastrointestinal Side Effects (Very Common):

Nausea: Affecting appetite and daily activities
Diarrhea: Frequent loose stools potentially causing dehydration
Vomiting: Stomach upset affecting nutrition
Stomach upset: General gastrointestinal discomfort
Loss of appetite: Reduced food intake contributing to weight loss
Heartburn (acid reflux): Gastroesophageal reflux symptoms
Abdominal pain: Stomach discomfort of varying severity
Dyspepsia: Indigestion and upper stomach discomfort
Gastroesophageal reflux disease: Chronic acid reflux complications

Constitutional Side Effects:

Fatigue: Persistent tiredness affecting daily function
Weight loss: Often significant and requiring nutritional intervention
Weakness: Reduced strength and energy
Decreased appetite: Contributing to nutritional deficiencies
General malaise: Overall feeling of illness

Neurological Side Effects:

Dizziness: Balance problems and lightheadedness
Headache: Various types and intensities
Somnolence: Excessive sleepiness
Insomnia: Sleep disturbances

Respiratory Side Effects:

Upper respiratory tract infection: Cold-like symptoms
Cough: Persistent or worsening cough
Dyspnea: Shortness of breath (may be difficult to distinguish from IPF progression)
Chest discomfort: Non-cardiac chest symptoms

Musculoskeletal Side Effects:

Arthralgia: Joint pain affecting multiple joints
Myalgia: Muscle pain and discomfort
Back pain: Spinal discomfort
Muscle spasms: Involuntary muscle contractions

Cardiovascular Side Effects:

Peripheral edema: Swelling in extremities
Chest pain: Non-specific chest discomfort
Hypertension: Elevated blood pressure

Psychiatric Side Effects:

Depression: Mood changes and depressive symptoms
Anxiety: Increased worry and nervousness
Sleep disorders: Various sleep disturbances

Drug Interaction-Related Side Effects:

Enhanced pirfenidone toxicity: With CYP1A2 inhibitors like fluvoxamine
Increased photosensitivity: With concomitant photosensitizing medications
Reduced efficacy: With smoking or CYP1A2 inducers
Altered drug levels: Of medications metabolized by affected enzymes

Dose-Related Side Effects:

Higher GI intolerance: With faster dose escalation or higher doses
Increased liver enzyme risk: With maximum recommended doses
More frequent photosensitivity: Dose-dependent skin reaction risk

Laboratory Abnormalities:

Elevated liver enzymes: ALT, AST, bilirubin increases
Decreased white blood cell count: Mild leukopenia
Elevated BUN and creatinine: Kidney function changes

Emergency Warning Signs Requiring Immediate Medical Attention:

Signs of liver injury: Jaundice, dark urine, severe fatigue, easy bleeding
Severe skin reactions: Widespread rash, blistering, skin detachment
Severe photosensitivity: Severe burns from minimal sun exposure
Signs of DRESS syndrome: Rash with fever, lymph node swelling, organ involvement
Persistent vomiting: Inability to keep medication or fluids down
Severe dehydration: From prolonged diarrhea and vomiting

Long-term Treatment Considerations:

Chronic GI symptoms: May require ongoing management strategies
Progressive liver monitoring: Need for lifelong liver function surveillance
Skin protection requirements: Permanent lifestyle changes for sun protection
Nutritional monitoring: Regular assessment for weight loss and malnutrition

Quality of Life Impact:

Activity limitations: Due to fatigue and GI symptoms
Dietary restrictions: Food avoidance due to GI intolerance
Social isolation: Due to photosensitivity and sun avoidance requirements
Sleep disruption: From GI symptoms and medication effects
Work limitations: Due to fatigue and frequent medical monitoring

Management Strategies for Common Side Effects:

Take with food: Reduces GI side effects significantly
Gradual dose escalation: Improves tolerance during initiation
Comprehensive sun protection: SPF 50+ sunscreen, protective clothing
Temporary dose reduction: For managing severe side effects
Supportive medications: Anti-nausea drugs, acid reducers as needed

Critical Safety Warning: The most serious risks with Esbriet involve liver injury and severe skin reactions, both of which can be life-threatening. All patients require regular liver function monitoring and strict sun protection measures. Any signs of liver problems or severe skin reactions require immediate medical attention and may necessitate permanent drug discontinuation.

Esbriet (pirfenidone) has a specific FDA-approved indication for treating idiopathic pulmonary fibrosis, representing the first medication specifically designed to slow the progression of this devastating lung disease based on extensive clinical research demonstrating significant disease-modifying benefits:

Primary FDA-Approved Indication:

Idiopathic Pulmonary Fibrosis (IPF):

Disease definition: Progressive fibrotic lung disease of unknown cause
Patient population: Adults with confirmed IPF diagnosis
Treatment goal: Slowing decline in lung function and disease progression
Therapeutic approach: Anti-fibrotic therapy targeting underlying disease mechanisms
Clinical benefit: Reduced rate of forced vital capacity (FVC) decline

Diagnostic Requirements for IPF:

High-resolution CT findings: Usual interstitial pneumonia (UIP) pattern
Exclusion of other causes: Environmental exposures, connective tissue diseases, drug toxicity
Multidisciplinary diagnosis: Pulmonologist, radiologist, and pathologist evaluation
Progressive disease: Documented decline in lung function or clinical progression
Age considerations: Typically affects adults over 50 years of age

Clinical Evidence Supporting Approval:

Phase 3 Clinical Trials (CAPACITY Program):

Study design: Two identical randomized, double-blind, placebo-controlled trials
Patient population: 779 patients with mild to moderate IPF
Primary endpoint: Change in forced vital capacity (FVC) at 72 weeks
Results: Significant reduction in FVC decline in one of two studies
Secondary endpoints: Progression-free survival, dyspnea, quality of life measures

ASCEND Study (Phase 3 Confirmatory Trial):

Study design: Randomized, double-blind, placebo-controlled trial
Patient population: 555 patients with IPF
Primary endpoint: Change in percent predicted FVC at 52 weeks
Results: 47.9% reduction in FVC decline compared to placebo
Clinical significance: Meaningful preservation of lung function
Safety profile: Consistent with previous studies

Long-term Safety and Efficacy Data:

RECAP study: Open-label extension evaluating long-term safety
Real-world evidence: Post-marketing surveillance data
Patient exposure: Over 1400 subjects in clinical development
Long-term treatment: Safety in patients treated >5 years
Global experience: Extensive international use since 2011

Dosing and Administration Protocol:

Dose Titration Schedule:

Week 1: 267mg three times daily (801mg/day) with food
Week 2: 534mg three times daily (1602mg/day) with food
Week 3 and beyond: 801mg three times daily (2403mg/day) with food
Titration rationale: Gradual increase improves gastrointestinal tolerability
Food requirement: Must be taken with food to minimize side effects

Available Formulations:

Capsules: 267mg white to off-white hard gelatin capsules
Film-coated tablets: 267mg (yellow) and 801mg (brown) tablets
Dosing convenience: 801mg tablets reduce pill burden at maintenance dose
Administration: Swallow whole, do not crush or break

How long does it take for Esbriet to start working?

Esbriet doesnt improve lung function but rather slows the rate of decline characteristic of IPF. While the medication begins affecting fibrotic processes immediately, measurable benefits in slowing disease progression typically become apparent over 6-12 months of treatment. Pulmonary function tests may show slower decline compared to expected disease progression, and patients might notice they maintain their current breathing capacity longer than anticipated. The medication's effects are cumulative, so consistent long-term use is essential for maximum benefit.

Do I need to take Esbriet for life?

Most patients with IPF require long-term Esbriet treatment to maintain disease-modifying benefits. IPF is a progressive disease that continues advancing without treatment, so discontinuing Esbriet typically results in resumption of normal disease progression rates. The medication should be continued unless significant side effects develop or disease progresses despite treatment. Some patients may need treatment breaks for side effect management, but restarting is usually important for continued disease control.

Why do I need regular liver monitoring?

Esbriet can cause serious drug-induced liver injury (DILI), including severe liver damage that has been fatal in rare cases. Liver function tests are required monthly for the first 6 months, then every 3 months thereafter to detect liver problems early. Most liver enzyme elevations are reversible if caught promptly, but some patients develop severe liver injury requiring immediate drug discontinuation. Regular monitoring allows early detection and intervention to prevent serious liver complications.

How can I manage the gastrointestinal side effects?

Taking Esbriet with food significantly reduces nausea, stomach upset, and other GI symptoms. Eat a substantial meal or snack with each dose, and consider taking the medication at the end of meals. Start with small, frequent meals if appetite is poor. Your doctor may prescribe anti-nausea medications or acid reducers to help manage symptoms. If GI side effects are severe, temporary dose reduction may be necessary, but dont adjust doses without medical supervision.

What sun protection do I need while taking Esbriet?

Esbriet causes significant photosensitivity, making even brief sun exposure dangerous. Use broad-spectrum sunscreen with SPF 50 or higher, reapplying every 2 hours. Wear protective clothing including long sleeves, pants, wide-brimmed hats, and UV-blocking sunglasses. Avoid sun exposure during peak hours (10 AM to 4 PM) and seek shade whenever possible. Even on cloudy days, UV rays can cause severe burns. Avoid tanning beds completely and check that other medications dont increase photosensitivity risk.

Can I smoke while taking Esbriet?

No, smoking significantly reduces Esbriet effectiveness by decreasing blood levels of the medication. You must stop smoking before starting treatment and avoid tobacco products throughout therapy. Smoking induces liver enzymes that break down pirfenidone, potentially reducing therapeutic benefits. Since IPF is often smoking-related, quitting also supports overall lung health. Work with your healthcare team on smoking cessation programs, as this is crucial for both Esbriet effectiveness and IPF management.

What drug interactions should I be aware of?

Fluvoxamine (an antidepressant) and high-dose ciprofloxacin significantly increase Esbriet levels, requiring dose reductions or alternative medications. Many other drugs can interact by affecting liver enzymes that metabolize pirfenidone. Always inform healthcare providers about Esbriet treatment before starting new medications. Some interactions may require dose adjustments, alternative drugs, or enhanced monitoring. Herbal supplements and over-the-counter medications can also interact, so discuss all substances with your healthcare team.

How do I know if Esbriet is working?

Esbriet's benefits are measured by slowing lung function decline rather than improvement. Your doctor will monitor pulmonary function tests (especially forced vital capacity) to assess whether the rate of decline is slower than expected for untreated IPF. You might notice maintaining your current breathing capacity longer than anticipated, or slower progression of symptoms like shortness of breath. The medication's success is often measured over 6-12 months by comparing actual function decline to expected progression rates.

Can I take Esbriet if I have liver or kidney problems?

Esbriet may not be appropriate for patients with significant liver or kidney disease. The medication undergoes extensive liver metabolism, so liver impairment can increase drug levels and toxicity risk. Kidney problems may also affect drug clearance. Your doctor will assess your liver and kidney function before starting treatment and may choose alternative therapies or require enhanced monitoring if you have mild dysfunction. Severe liver or kidney disease typically precludes Esbriet use.

What should I do if I develop a severe skin reaction?

Stop Esbriet immediately and contact your doctor if you develop severe skin reactions including widespread rash, blistering, skin peeling, or signs of Stevens-Johnson syndrome. These reactions can be life-threatening and may require emergency medical care. Early recognition and prompt treatment are crucial for preventing serious complications. Your doctor may need to permanently discontinue Esbriet and provide supportive care or alternative treatments. Dont restart the medication without medical clearance.

Is Esbriet safe during pregnancy and breastfeeding?

There are no adequate human studies of Esbriet use during pregnancy or breastfeeding. Animal studies show the drug is excreted in milk, but human data are lacking. Given IPF typically affects older adults, pregnancy considerations are uncommon, but women of childbearing age should discuss contraception and pregnancy planning with their healthcare team. The risks and benefits must be carefully weighed if pregnancy occurs or is planned during treatment.

How should I store Esbriet and handle missed doses?

Store Esbriet at room temperature in its original container, protected from light and moisture. If you miss a dose, take it as soon as you remember on the same day, then return to your normal schedule. Dont take extra doses to make up for missed ones, as this increases side effect risk. If you frequently forget doses, consider setting alarms or linking doses to meals. Consistent dosing is important for maintaining therapeutic levels and disease control benefits.

Can other lung medications be used with Esbriet?

Esbriet can often be used alongside other IPF treatments and supportive care medications like bronchodilators, supplemental oxygen, or pulmonary rehabilitation. However, coordination with your pulmonologist is essential to ensure compatibility and optimize your overall treatment plan. Some patients may benefit from combination approaches including respiratory support medications or other anti-fibrotic agents, though combination anti-fibrotic therapy isnt standard practice.

What monitoring beyond liver tests do I need?

Beyond liver function tests, regular monitoring includes pulmonary function testing, blood counts, kidney function assessment, and clinical evaluation for side effects. Your doctor will track your breathing capacity, oxygen levels, exercise tolerance, and overall disease progression. Skin examinations may be needed to monitor for photosensitivity effects. Regular check-ups allow for dose adjustments, side effect management, and assessment of treatment effectiveness in slowing IPF progression.

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