Esbriet: Slowing Idiopathic Pulmonary Fibrosis Progression

Esbriet

Esbriet

Price from 100.00 $
Product dosage: 200 mg
Package (num)Per pillPriceBuy
30$3.35$100.38 (0%)🛒 Add to cart
60$3.04$200.75 $182.68 (9%)🛒 Add to cart
90$2.97$301.13 $267.00 (11%)🛒 Add to cart
120
$2.74 Best per pill
$401.50 $329.23 (18%)🛒 Add to cart

Esbriet (pirfenidone) is an oral antifibrotic agent specifically indicated for the treatment of idiopathic pulmonary fibrosis (IPF). This chronic, progressive, and ultimately fatal lung disease is characterized by scarring (fibrosis) of the pulmonary interstitium, leading to a relentless decline in lung function. Clinical trials have demonstrated that Esbriet significantly reduces the rate of decline in forced vital capacity (FVC), a key predictor of mortality in IPF. By targeting multiple pathways involved in the fibrotic process, it offers a mechanism to modify the disease course rather than merely manage symptoms. Treatment is intended for long-term management under the supervision of a pulmonologist or specialist familiar with interstitial lung diseases.

Features

  • Active Pharmaceutical Ingredient (API): Pirfenidone
  • Available Dosage Forms: Film-coated tablets (267 mg, 801 mg) and hard capsules (267 mg)
  • Mechanism of Action: Multifunctional antifibrotic; modulates key profibrotic cytokines including TGF-beta and TNF-alpha, and inhibits collagen synthesis
  • Prescription Status: Rx-only, specialty medication
  • Bioavailability: Approximately 80% following oral administration
  • Time to Peak Plasma Concentration (Tmax): Approximately 30 minutes when taken after a meal
  • Half-life: Approximately 3 hours
  • Metabolism: Primarily hepatic, via CYP1A2 and other enzymes (CYP2C9, 2C19, 2D6, 2E1)
  • Excretion: Primarily renal (≈80% as metabolites, <1% as unchanged drug)

Benefits

  • Slows Disease Progression: Clinically proven to reduce the annual rate of decline in forced vital capacity (FVC), a critical measure of lung function.
  • May Prolong Progression-Free Survival: Treatment is associated with a reduction in the risk of disease progression, as defined by categorical decline in FVC or mortality.
  • Targets Underlying Pathology: Works on multiple pathways central to the fibrotic process, addressing the core mechanism of IPF rather than just symptoms.
  • Well-Established Efficacy and Safety Profile: Supported by robust data from phase III clinical trials (CAPACITY, ASCEND) and extensive post-marketing surveillance.
  • Oral Administration: Convenient tablet or capsule formulation taken orally, facilitating outpatient treatment and patient adherence.

Common use

Esbriet is exclusively indicated for the treatment of idiopathic pulmonary fibrosis (IPF). IPF is a specific diagnosis that requires confirmation by a multidisciplinary team, typically involving a pulmonologist, radiologist, and, in some cases, a pathologist specializing in interstitial lung diseases. High-resolution computed tomography (HRCT) is essential for making a pattern-specific diagnosis (usual interstitial pneumonia - UIP pattern). It is not indicated for other interstitial lung diseases (ILDs), such as non-specific interstitial pneumonia (NSIP), hypersensitivity pneumonitis, or sarcoidosis, unless part of a carefully considered off-label use within a clinical trial or specialized practice. Its use is intended for patients with mild to moderate impairment in lung function, though treatment decisions are individualized.

Dosage and direction

Dosing requires a careful titration period to improve gastrointestinal tolerability. The medication must be taken with food to minimize nausea and dizziness.

  • Initial Titration:

    • Weeks 1-7: 267 mg (one capsule/tablet) three times daily (801 mg/day).
    • Weeks 8-14: 534 mg (two 267 mg capsules/tablets) three times daily (1602 mg/day).
    • Week 15 and Maintenance: 801 mg (three 267 mg capsules/tablets or one 801 mg tablet) three times daily (2403 mg/day).

  • Administration:

    • Take each dose with a full meal or snack.
    • Tablets should be swallowed whole; do not crush, split, or chew.
    • If a dose is missed, skip it and take the next scheduled dose. Do not double the dose.
    • Adherence to the full maintenance dose is important for achieving maximal therapeutic effect.

Dosage adjustments or discontinuation may be necessary based on tolerability and liver function tests.

Precautions

  • Liver Enzyme Elevations: ALT, AST, and bilirubin elevations have been observed. Liver function tests (ALT, AST, and bilirubin) must be conducted prior to initiating therapy, monthly for the first 6 months, and then every 3 months thereafter thereafter. Dosage modification or discontinuation is required for significant elevations.
  • Photosensitivity and Rash: Patients are at significantly increased risk of sunburn and photosensitivity reactions. Strict sun protection measures are mandatory: use sunscreen (SPF 50 or higher), wear protective clothing, and avoid direct sun exposure and sunlamps. Rash is common and may require dosage reduction or temporary interruption.
  • Gastrointestinal Disorders: Nausea, diarrhea, dyspepsia, vomiting, and abdominal pain are very common, especially during dose titration. Taking Esbriet with food is critical. Anti-emetic or anti-diarrheal agents may be used supportively.
  • Weight Loss and Anorexia: Monitor patient weight. Significant, unintentional weight loss may require nutritional support and dosage adjustment.
  • Dizziness and Fatigue: Patients should exercise caution when driving or operating machinery until they know how Esbriet affects them.
  • Smoking: Smoking induces the CYP1A2 enzyme, which metabolizes pirfenidone, potentially reducing its efficacy. Patients should be strongly advised to stop smoking.

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).
  • Severe renal impairment (end-stage renal disease requiring dialysis) or estimated glomerular filtration rate (eGFR) <30 mL/min/1.73m².
  • Concomitant use of strong CYP1A2 inhibitors (e.g., fluvoxamine, enoxacin). Use with other moderate CYP1A2 inhibitors (e.g., ciprofloxacin) requires caution and possible dose reduction.

Possible side effect

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

  • Gastrointestinal: Nausea (36%), diarrhea (26%), dyspepsia (19%), vomiting (13%), abdominal pain (15%), gastroesophageal reflux disease (11%), anorexia (11%)
  • Dermatological: Rash (30%), photosensitivity reaction (12%), pruritus (12%)
  • General: Fatigue (26%), headache (15%), dizziness (18%)
  • Insomnia (10%)

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

Drug interaction

Esbriet is primarily metabolized by CYP1A2. Concomitant medications can significantly impact its plasma levels.

  • Strong CYP1A2 Inhibitors (e.g., Fluvoxamine, Enoxacin): Contraindicated. Co-administration will markedly increase pirfenidone exposure, raising the risk of adverse effects.
  • Moderate CYP1A2 Inhibitors (e.g., Ciprofloxacin, Amiodarone, Propafenone, Zileuton, Oral Contraceptives containing desogestrel/ethinyl estradiol): Use with caution. A reduction of the Esbriet dose to 267 mg three times daily (801 mg/day) is recommended.
  • CYP1A2 Inducers (e.g., Tobacco Smoke, Omeprazole, Rifampin): May decrease pirfenidone exposure, potentially reducing its efficacy. Patients must be advised to stop smoking.
  • Other Drugs: Compounds that cause dizziness or photosensitivity (e.g., other antibiotics, antipsychotics) may have additive effects.

Missed dose

If a dose is missed, the patient should skip that dose and take the next scheduled dose at its regular time. The patient should not take a double dose to make up for the missed dose. Maintaining the regular dosing schedule is more important than catching up on a single missed dose.

Overdose

There is limited experience with overdose. Reported symptoms are consistent with the known adverse reaction profile, including severe nausea, vomiting, dizziness, fatigue, and photosensitivity. There is no known specific antidote for pirfenidone overdose. Treatment should consist of general supportive measures, including monitoring of vital signs and observation of the patient’s clinical status. Gastric lavage or administration of activated charcoal may be considered if presented soon after ingestion. Hemodialysis is unlikely to be effective due to the drug’s high protein binding and extensive metabolism.

Storage

  • Store 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 bottle tightly closed in its original container to protect from moisture and light.
  • 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 various resources but may not be exhaustive or fully updated.

Reviews

  • Clinical Consensus (Pulmonology): “Esbriet represents a cornerstone of pharmacological management for IPF. The data from the ASCEND trial was practice-changing, providing Level A evidence that we can meaningfully slow functional decline. The side effect profile is manageable with proactive patient education and dose titration. It’s not a cure, but it gives us a vital tool to fight this disease.” – Director of an ILD Program.
  • Patient Experience (Online Forum Aggregate): Many patients report a challenging initial 2-3 month adjustment period dominated by GI upset and fatigue, which often subsides for those who persist. The requirement for strict sun avoidance is frequently cited as a significant lifestyle adjustment. The common sentiment among long-term users is that managing the side effects is worth the potential benefit of stabilized lung function. Seeing a stable FVC on their pulmonary function tests is a powerful motivator for adherence.
  • Formulary & Access Perspective: “As a specialty pharmacist, navigating prior authorizations and patient assistance programs for Esbriet is a routine part of the job. While the cost is high, the clinical evidence supporting its use in IPF is solid compared to the historical lack of options.”

More info: