ESBRIET

Absorption: After single oral-dose administration of 801 mg ESBRIET (three 267 mg capsules), the maximum observed plasma concentration (C max ) was achieved between 30 minutes and 4 hours (median time of 0.5 hours). Food decreased the rate and extent of absorption. Median T max increased from 0.5 hours to 3 hours with food. Maximum plasma concentrations (C max ) and AUC 0-inf decreased by approximately 49% and 16% with food, respectively. Bioequivalence was demonstrated in the fasted state when ...

The efficacy of ESBRIET was evaluated in patients with IPF in three phase 3, randomized, double-blind, placebo-controlled, multicenter trials (Studies 1, 2, and 3). Study 1 was a 52-week trial comparing ESBRIET 2403 mg/day (n=278) versus placebo (n=277) in patients with IPF. Study 2 and Study 3 were nearly identical to each other in design, with few exceptions, including an intermediate dose treatment arm in Study 2. Study 2 compared treatment with either ESBRIET 2403 mg/day (n=174) or ESBRIET 1197 mg/day (n=87) to placebo (n=174), while Study 3 compared ESBRIET 2403 mg/day (n=171) to placebo ...

The following adverse reactions are discussed in greater detail in other sections of the labeling: Liver Enzyme Elevations and Drug-Induced Liver Injury [see Warnings and Precautions (5.1) ] Photosensitivity Reaction or Rash [see Warnings and Precautions (5.2) ] Severe Cutaneous Adverse Reactions [see Warnings and Precautions (5.3) ] Gastrointestinal Disorders [see Warnings and Precautions (5.4) ] The most common adverse reactions (≥10%) are nausea, rash, abdominal pain, upper respiratory tract ...

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Elevated liver enzymes and drug-induced liver injury: ALT, AST, and bilirubin elevations have occurred with ESBRIET including cases of drug-induced liver injury. In the postmarketing setting, non-serious and serious cases of drug-induced liver injury, including severe liver injury with fatal outcomes, have been reported. Monitor ALT, AST, and bilirubin before and during treatment. Temporary dosage reductions or discontinuations may be required. ( 2.1 , 5.1 ) Photosensitivity and rash: Photosensi...

7 DRUG INTERACTIONS Moderate (e.g., ciprofloxacin) and strong inhibitors of CYP1A2 (e.g., fluvoxamine) increase systemic exposure of ESBRIET and may alter the adverse reaction profile of ESBRIET. Discontinue fluvoxamine prior to administration of ESBRIET or reduce to 267 mg three times a day . Consider dosage reduction with use of ciprofloxacin. ( 7.1 ) 7.1 CYP1A2 Inhibitors Pirfenidone is metabol...