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Keith A Hoffmaster

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Recent Articles
1.
Giacomini K, Huang S, Tweedie D, Benet L, Brouwer K, Chu X, et al.
Nat Rev Drug Discov . 2010 Mar; 9(3):215-36. PMID: 20190787
Membrane transporters can be major determinants of the pharmacokinetic, safety and efficacy profiles of drugs. This presents several key questions for drug development, including which transporters are clinically important in...
2.
Zamek-Gliszczynski M, Hoffmaster K, Nezasa K, Brouwer K
Drug Metab Dispos . 2008 Aug; 36(11):2156-8. PMID: 18719241
Previous experiments demonstrated that the biliary excretion of harmol sulfate (HS) was mediated by breast cancer resistance protein (Bcrp) and not by multidrug resistance-associated protein (Mrp)2 or P-glycoprotein in mice....
3.
Zamek-Gliszczynski M, Hoffmaster K, Humphreys J, Tian X, Nezasa K, Brouwer K
J Pharmacol Exp Ther . 2006 Jul; 319(1):459-67. PMID: 16857726
The hepatic excretion of hydrophilic conjugates, end products of phase II metabolism, is not completely understood. In the present studies, transport mechanism(s) responsible for the biliary excretion of 4-methylumbelliferyl glucuronide...
4.
Turncliff R, Hoffmaster K, Kalvass J, Pollack G, Brouwer K
J Pharmacol Exp Ther . 2006 May; 318(2):881-9. PMID: 16690724
The hepatobiliary disposition of xenobiotics may involve passive and/or active uptake, metabolism by cytochromes P450, and excretion of the parent compound and/or metabolite(s) into bile. Although in vitro systems have...
5.
Zamek-Gliszczynski M, Hoffmaster K, Nezasa K, Tallman M, Brouwer K
Eur J Pharm Sci . 2006 Feb; 27(5):447-86. PMID: 16472997
The liver is the primary site of drug metabolism in the body. Typically, metabolic conversion of a drug results in inactivation, detoxification, and enhanced likelihood for excretion in urine or...
6.
Zamek-Gliszczynski M, Hoffmaster K, Tian X, Zhao R, Polli J, Humphreys J, et al.
Drug Metab Dispos . 2005 Apr; 33(8):1158-65. PMID: 15860656
Previous reports have demonstrated that sulfate metabolites may be excreted into bile by the multidrug resistance-associated protein 2 (Mrp2, Abcc2). Although recombinant human breast cancer resistance protein (BCRP, ABCG2) has...
7.
Hoffmaster K, Zamek-Gliszczynski M, Pollack G, Brouwer K
Drug Metab Dispos . 2004 Nov; 33(2):287-93. PMID: 15528320
Rapid and extensive biliary excretion of [D-penicillamine2,5]enkephalin (DPDPE) in rats as the unchanged peptide suggests that multiple transport proteins may be involved in the hepatobiliary disposition of this zwitterionic peptide....
8.
Hoffmaster K, Zamek-Gliszczynski M, Pollack G, Brouwer K
J Pharmacol Exp Ther . 2004 Aug; 311(3):1203-10. PMID: 15302892
[D-Pen2,D-Pen5]-Enkephalin (DPDPE) is excreted extensively into the bile. Although DPDPE is transported by P-glycoprotein (P-gp), multidrug resistance-associated protein 2 (Mrp2) has been identified as an important mechanism for DPDPE transport...
9.
Hoffmaster K, Turncliff R, LeCluyse E, Kim R, Meier P, Brouwer K
Pharm Res . 2004 Aug; 21(7):1294-302. PMID: 15290872
Purpose: The isolation of hepatocytes from intact liver involves collagenase digestion of the tissue, resulting in loss of cell polarization and functional vectorial excretion. These studies examined repolarization, localization of...
10.
Paine M, Wagner D, Hoffmaster K, Watkins P
Clin Pharmacol Ther . 2002 Nov; 72(5):524-35. PMID: 12426516
Background: The intravenous (14)C-erythromycin breath test (ERMBT(IV)) does not measure aggregate liver and intestinal cytochrome P450 (CYP) 3A4 activity. Accordingly, we evaluated an oral stable-labeled ((13)C) formulation of the test...