PMID- 25669655 OWN - NLM STAT- MEDLINE DCOM- 20150512 LR - 20150317 IS - 1532-6535 (Electronic) IS - 0009-9236 (Linking) VI - 97 IP - 4 DP - 2015 Apr TI - The concept of fraction of drug transported (ft ) with special emphasis on BBB efflux of CNS and antiretroviral drugs. PG - 320-3 LID - 10.1002/cpt.72 [doi] AB - The fraction of drug transported (ft) into or out of a tissue is a concept useful to understand the impact of transporters on absorption, distribution, metabolism, and excretion (ADME) and tissue distribution of a drug. Here, ft is utilized to explain the impact of transporters on central nervous system (CNS) distribution of drugs, drug interactions (DDI), and to predict the unbound brain concentration (Cu,b) of the drug. The latter is important to ascertain if Cu,b is sufficient for efficacy. CI - (c) 2015 American Society for Clinical Pharmacology and Therapeutics. FAU - Prasad, B AU - Prasad B AD - Department of Pharmaceutics, University of Washington, Seattle, Washington, USA. FAU - Unadkat, J D AU - Unadkat JD LA - eng PT - Journal Article DEP - 20150213 PL - United States TA - Clin Pharmacol Ther JT - Clinical pharmacology and therapeutics JID - 0372741 RN - 0 (Antiviral Agents) RN - 0 (Carrier Proteins) RN - 0 (Membrane Transport Proteins) RN - 0 (Pharmaceutical Preparations) SB - IM MH - Animals MH - *Antiretroviral Therapy, Highly Active MH - Antiviral Agents/*pharmacokinetics MH - Biological Transport MH - Blood-Brain Barrier/*metabolism MH - Carrier Proteins/metabolism MH - Central Nervous System/*metabolism MH - Drug Interactions MH - Humans MH - Membrane Transport Proteins/metabolism MH - Pharmaceutical Preparations/*metabolism EDAT- 2015/02/12 06:00 MHDA- 2015/05/13 06:00 CRDT- 2015/02/12 06:00 PHST- 2014/11/24 00:00 [received] PHST- 2015/01/05 00:00 [revised] PHST- 2015/01/06 00:00 [accepted] PHST- 2015/02/12 06:00 [entrez] PHST- 2015/02/12 06:00 [pubmed] PHST- 2015/05/13 06:00 [medline] AID - 10.1002/cpt.72 [doi] PST - ppublish SO - Clin Pharmacol Ther. 2015 Apr;97(4):320-3. doi: 10.1002/cpt.72. Epub 2015 Feb 13.