In vitro–in vivo extrapolation of bexarotene metabolism in the presence of chronic kidney disease and acute kidney injury in rat using physiologically based pharmacokinetic modeling and extrapolation to human

• Published in: Biopharmaceutics & drug disposition Vol. 44; no. 3; pp. 221 - 244
• Main Authors: Alsmadi, Mo'tasem M., Alzughoul, Saja B.
• Format: Journal Article
• Language: English
• Published: England Wiley Subscription Services, Inc 01.06.2023
• Subjects: acute kidney injury; Acute Kidney Injury - metabolism; Animals; Bexarotene; bexarotene metabolism; Blood Proteins - metabolism; chronic kidney disease; Humans; Kidney diseases; Liver - metabolism; Lymphoma; Metabolism; Pharmaceutical Preparations - metabolism; Pharmacokinetics; physiologically based pharmacokinetics; Plasma; Protein turnover; Rats; Renal function; Renal Insufficiency, Chronic - metabolism; United States; uremic toxins; United States; bexarotene metabolism; chronic kidney disease; acute kidney injury; uremic toxins; physiologically based pharmacokinetics

Renal impairment can affect the elimination of hepatically metabolized drugs. Bexarotene (BXT) used for cutaneous T‐cell lymphoma is highly bound in plasma and metabolized by CYP3A4. The BXT European Medicine Agency and Food and Drug Administration packages recommended the evaluation of renal impair...