For the treatment of idiopathic pulmonary fibrosis (IPF).
#仿單變更2021

Nintedanib is a small molecule that inhibits multiple receptor tyrosine kinases (RTKs) and non-receptor tyrosine kinases (nRTKs). Nintedanib inhibits the following RTKs: platelet-derived growth factor receptor (PDGFR) α and β, fibroblast growth factor receptor (FGFR) 1-3, vascular endothelial growth factor receptor (VEGFR) 1-3, and Fms-like tyrosine kinase-3 (FLT3). Nintedanib binds competitively to the adenosine triphosphate (ATP) binding pocket of these receptors and blocks the intracellular signaling which is crucial for the proliferation, migration, and transformation of fibroblasts.

Absorption: bioavailability is 4.7%, Food increases exposure ~20% and delays absorption; plasma protein binding: 97.8%; Metabolism: Hydrolytic cleavage by esterases to free acid moiety BIBF 1202; Elimination Half-life: 9.5 hours.

D

Avoided

Diarrhea (most common,may lead to dehydration, renal dysfunction <2021/7/13>), Nausea, vomiting, increased liver enzyme, abdominal pain, headache<2021/7/13>

Oral: 150 mg every 12 hours (maximum: 300 mg daily). Should be taken with food and swallowed whole with liquid. OFEV capsules should not be chewed or crushed because of a bitter taste. If a dose of OFEV is missed, the next dose should be taken at the next scheduled time. Advise the patient to not make up for a missed dose. 

CrCl 30 mL/minute: No initial dosage adjustment necessary.
CrCl <30 mL/minute: There are no dosage adjustments provided in the manufacturer's labeling (has not been studied).
ESRD: There are no dosage adjustments provided in the manufacturer's labeling (has not been studied).
* Monitor kidney function especially in patients with renal dysfunction/failure risk.<2021/7/13>

• AST or ALT >3 times to <5 times ULN (without signs of severe liver damage): Interrupt treatment or reduce dosage to 100 mg Q12H. If a patient does not tolerate 100 mgQ12H, discontinue treatment.
• AST or ALT >5 times ULN or >3 times ULN with signs or symptoms of severe liver damage: Discontinue therapy.