Brincidofovir Is Not a Substrate for the Human Organic Anion Transporter 1: A Mechanistic Explanation for the Lack of Nephrotoxicity Observed in Clinical Studies

• Published in: Therapeutic drug monitoring Vol. 38; no. 6; p. 777
• Main Authors: Tippin, Timothy K, Morrison, Marion E, Brundage, Thomas M, Momméja-Marin, Hervé
• Format: Journal Article
• Language: English
• Published: United States 01.12.2016
• Subjects: Adolescent; Adult; Aged; Animals; Antiviral Agents - adverse effects; Antiviral Agents - pharmacokinetics; Biological Transport - physiology; Cell Line; Child; Cytosine - adverse effects; Cytosine - analogs & derivatives; Cytosine - pharmacokinetics; Dogs; Female; Glomerular Filtration Rate - drug effects; Humans; Kidney Tubules, Proximal - drug effects; Kidney Tubules, Proximal - metabolism; Madin Darby Canine Kidney Cells; Male; Middle Aged; Organic Anion Transport Protein 1 - metabolism; Organophosphonates - adverse effects; Organophosphonates - pharmacokinetics; Young Adult

Brincidofovir (BCV) is an orally bioavailable lipid conjugate of cidofovir (CDV) with increased in vitro potency relative to CDV against all 5 families of double-stranded DNA viruses that cause human disease. After intravenous (IV) administration of CDV, the organic anion transporter 1 (OAT1) transp...