PMC:7417114 / 58440-59175
Annnotations
{"target":"https://pubannotation.org/docs/sourcedb/PMC/sourceid/7417114","sourcedb":"PMC","sourceid":"7417114","source_url":"https://www.ncbi.nlm.nih.gov/pmc/7417114","text":"Nintedanib (Ofev and Vargatef)\n(Boehringer Ingelheim) Fatty meal increased Cmax 15% and AUC by 20%;\nfollowing oral dosing, Tmax after 2 hours in fasted patients, 4 hours in fed patients;\nabsolute bioavailability is low (4.7%), likely due to P-gp transporters and significant first-pass metabolism (241);\nVd= 1050 L (IV administration) (suggests potentially high tissue distribution) CYP3A4 plays a minor role, accounting for 5% metabolism; esterase cleavage accounts for 25% metabolism 150 mg orally twice daily;\n100 mg orally twice daily in patients with mild hepatic impairment;\n97.8% binding (HSA) In placebo-controlled INPULSIS® trials, among adverse events leading to permanent treatment discontinuation was pneumonia (0.9%) 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