Idiopathic pulmonary fibrosis, progressive pulmonary fibrosis, systemic sclerosis-associated interstitial lung disease

Tyrosine Kinase Inhibitor

Absorption: Food increases exposure ~20% and delays absorptionDistribution: Vss: 1050 LProtein binding: ~98%Metabolism: Hydrolytic cleavage by esterases to free acid moiety BIBF 1202; which is then glucuronidated by UGT 1A1, UGT 1A7, UGT 1A8, and UGT 1A10 to BIBF 1202 glucuronide; CYP 3A4 (minor).Bioavailability: ~5%Half-life elimination: 9.5 hoursTime to peak, plasma: 2 hours (4 hours with food)Excretion: Feces (~93%); urine (<1%)

Hypersensitivity to nintedanib, peanut, or soya or any component of the formulation; pregnancy

May cause fetal harm

Infant risk cannot be ruled out. Women that breastfeeding is not recommended during therapy with nintedanib

>10%:Dermatologic: Dermal ulcer Endocrine & metabolic: Weight lossGastrointestinal: Abdominal pain, decreased appetite, diarrhea, nausea, vomitingHepatic: Increased liver enzymesNervous system: FatigueRespiratory: Nasopharyngitis1% to 10%:Cardiovascular: Acute myocardial infarction, arterial thrombosis, hypertension Endocrine & metabolic: Hypothyroidism Genitourinary: Urinary tract infectionHematologic & oncologic: Hemorrhage (10%; can be major hemorrhage)Nervous system: Dizziness, headacheNeuromuscular & skeletal: Back pain Respiratory: Bronchitis, pneumonia, upper respiratory tract infectionMiscellaneous: Fever<1%: Gastrointestinal: Gastrointestinal perforationPostmarketing:Dermatologic: Pruritus, skin rashGastrointestinal: PancreatitisGenitourinary: ProteinuriaHematologic & oncologic: ThrombocytopeniaHepatic: HepatoxicityNervous system: Posterior reversible encephalopathy syndrome

Idiopathic pulmonary fibrosis: 150 mg Q12h; maximum daily dose: 300 mg/day. Consider a lower starting dose of 100 mg BID in patients with concern for tolerability.Progressive pulmonary fibrosis: 150 mg Q12h; maximum daily dose: 300 mg/day.Systemic sclerosis–associated interstitial lung disease: 150 mg Q12h; maximum daily dose: 300 mg/day.

Safety and effectiveness in pediatric patients have not been established.【文字內容由仿單翻譯而來】

no dosage adjustments provided in the manufacturer's labeling

Child-Pugh class A:100 mg Q12h. If a patient does not tolerate 100 mg Q12h, consider treatment interruption or discontinue treatment to manage adverse reactions.Child-Pugh class B or C: Use is not recommended.Hepatotoxicity during treatment:AST or ALT >3 times to <5 times ULN (without signs of liver damage): Interrupt treatment or reduce dosage to 100 mg Q12h. Once liver enzymes have returned to baseline values after treatment interruption, reintroduce therapy at 100 mg Q12h; may be subsequently increased to 150 mg Q12h.AST or ALT >5 times ULN or >3 times ULN with signs or symptoms of liver damage: Discontinue therapy.

Store at temperatures below 25°C.