Michael B Fisher
Affiliation: Boehringer Ingelheim
- In vivo use of the P450 inactivator 1-aminobenzotriazole in the rat: varied dosing route to elucidate gut and liver contributions to first-pass and systemic clearanceTimothy J Strelevitz
Pfizer Inc, PGRD, Pharmacokinetics, Dynamics, and Metabolism, Eastern Point Road, Groton, CT 06340, USA
J Pharm Sci 95:1334-41. 2006..This method should have utility in drug discovery for the identification of factors limiting oral bioavailability...
- Prevention of organ allograft rejection by a specific Janus kinase 3 inhibitorPaul S Changelian
Immunology Group, Department of Antibacterials and Immunology, Pfizer Global Researchand Development, Groton, CT 06340, USA
Science 302:875-8. 2003..On the basis of these preclinical results, we believe JAK3 blockade by CP-690,550 has potential for therapeutically desirable immunosuppression in human organ transplantation and in other clinical settings...
- Altered AZT (3'-azido-3'-deoxythymidine) glucuronidation kinetics in liver microsomes as an explanation for underprediction of in vivo clearance: comparison to hepatocytes and effect of incubation environmentJuntyma J Engtrakul
Pharmacokinetics, Dynamics, and Metabolism, Pfizer Global Research and Development, Groton, CT 06340, USA
Drug Metab Dispos 33:1621-7. 2005....
- A streamlined method to predict hepatic clearance using human liver microsomes in the presence of human plasmaSara M Skaggs
Pfizer Global Research and Development, Pharmacokinetics, Dynamics, and Metabolism Pfizer, Inc Groton, CT 06340, USA
J Pharmacol Toxicol Methods 53:284-90. 2006..This can be time consuming for multiple compounds since it requires separate experiments to determine in vitro lability, and free fraction...
- The complexities inherent in attempts to decrease drug clearance by blocking sites of CYP-mediated metabolismMichael B Fisher
Boehringer Ingelheim Pharmaceuticals Inc, 900 Ridgebury Road, Ridgefield, CT 06877, USA
Curr Opin Drug Discov Devel 9:101-9. 2006..The concepts and evidence behind this phenomenon as it relates to complexities in blocking metabolic clearance are presented herein...
- Time-dependent inhibition and estimation of CYP3A clinical pharmacokinetic drug-drug interactions using plated human cell systemsDaniel R Albaugh
Boehringer Ingelheim Pharmaceuticals Inc, Medicinal Chemistry Drug Metabolism and Pharmacokinetics, 175 Briar Ridge Road, R and D 10574, Ridgefield, CT 06877, USA
Drug Metab Dispos 40:1336-44. 2012..Overall, results from these studies suggest that in vitro inactivation parameters generated from plated cell systems may be a practical approach for identifying time-dependent inhibitors and for estimating the magnitude of clinical DDIs...
- Characterization of aldehyde oxidase enzyme activity in cryopreserved human hepatocytesJ Matthew Hutzler
Boehringer Ingelheim Pharmaceuticals Inc, Translational Research Drug Metabolism and Pharmacokinetics, 175 Briar Ridge Road, R and D 10578, Ridgefield, CT 06877, USA
Drug Metab Dispos 40:267-75. 2012..These data taken together suggest that the use of cryopreserved hepatocytes may be a practical approach for assessing AO-mediated metabolism in discovery and potentially useful for predicting hepatic clearance of AO substrates...
- The role of the intestine in drug metabolism and pharmacokinetics: an industry perspectiveMichael B Fisher
Cara Therapeutics, Tarrytown, NY 10591, USA
Curr Drug Metab 8:694-9. 2007..The opportunity exists to increase the examination of intestinal metabolism of drugs and drug candidates in industry...
- Recent advances in high throughput screening for ADME propertiesTimothy J Carlson
Amgen Inc, 1120 Veterans Boulevard, South San Francisco, CA 94080, USA
Comb Chem High Throughput Screen 11:258-64. 2008..Future advances will further improve the ability to make decisions on molecules earlier in drug discovery...