K. Kassahun

发表

Design and biological activity of (S)-4-(5-([1-(3-chlorobenzyl)-2-oxopyrrolidin-3-ylamino]methyl)imidazol-1-ylmethyl)benzonitrile, a 3-aminopyrrolidinone farnesyltransferase inhibitor with excellent cell potency.

A. D. Rodrigues, E S Walsh, J B Gibbs, 2001, Journal of medicinal chemistry.

Metabolism and Disposition in Humans of Raltegravir (MK-0518), an Anti-AIDS Drug Targeting the Human Immunodeficiency Virus 1 Integrase Enzyme

I. Mcintosh, J. Wagner, K. Lasseter, 2007, Drug Metabolism and Disposition.

Lack of a Pharmacokinetic Effect of Raltegravir on Midazolam: In Vitro/In Vivo Correlation

P. Lu, J. Wagner, M. Troyer, 2008, Journal of clinical pharmacology.

Olanzapine: Interaction Study with Imipramine

G. Kondraske, B. Cerimele, J. Callaghan, 1997, Journal of clinical pharmacology.

Glutathione and N-acetylcysteine conjugates of 2-chloroethyl isocyanate. Identification as metabolites of N,N'-bis(2-chloroethyl)-N-nitrosourea in the rat and inhibitory properties toward glutathione reductase in vitro.

T. Baillie, K. Kassahun, C. Jochheim, 1993, Chemical research in toxicology.

Reversibility in glutathione-conjugate formation.

T. Baillie, K. Kassahun, 1994, Advances in pharmacology.

Effect of carbamate thioester derivatives of methyl- and 2-chloroethyl isocyanate on glutathione levels and glutathione reductase activity in isolated rat hepatocytes.

T. Baillie, K. Kassahun, C. Jochheim, 1994, Biochemical pharmacology.

Biotransformation of the naturally occurring isothiocyanate sulforaphane in the rat: identification of phase I metabolites and glutathione conjugates.

T. Baillie, K. Kassahun, M. Davis, 1997, Chemical research in toxicology.

The effect of carbamazepine on valproic acid disposition in adult volunteers.

K. Farrell, K. Kassahun, F. Abbott, 1989, British journal of clinical pharmacology.

DMD056580 818..827

K. Koeplinger, I. Mcintosh, Li Sun, 2014 .

Pharmacokinetics and Metabolism in Rats, Dogs, and Monkeys of the Cathepsin K Inhibitor Odanacatib: Demethylation of a Methylsulfonyl Moiety as a Major Metabolic Pathway

K. Koeplinger, I. Mcintosh, K. Kassahun, 2011, Drug Metabolism and Disposition.

In vitro and in vivo metabolism of a novel antimitochondrial cancer metabolism agent, CPI-613, in rats and human

K. Kassahun, V. Reddy, A. Sheldon, 2022 .

A naphthyridine carboxamide provides evidence for discordant resistance between mechanistically identical inhibitors of HIV-1 integrase.

Mark Embrey, Samson M Jolly, Wei Xu, 2004, Proceedings of the National Academy of Sciences of the United States of America.

Approaches for minimizing metabolic activation of new drug candidates in drug discovery.

T. Baillie, Sanjeev Kumar, K. Kassahun, 2010, Handbook of experimental pharmacology.

Zafirlukast Metabolism by Cytochrome P450 3A4 Produces an Electrophilic α,β-Unsaturated Iminium Species That Results in the Selective Mechanism-Based Inactivation of the Enzyme

T. Baillie, I. Mcintosh, G. Doss, 2005 .

In Vitro and in Vivo Evaluation of Dihydropyrimidinone C-5 Amides as Potent and Selective α1A Receptor Antagonists for the Treatment of Benign Prostatic Hyperplasia

J. Barrow, K. Rittle, R. Freidinger, 2000 .

Studies on the metabolism of troglitazone to reactive intermediates in vitro and in vivo. Evidence for novel biotransformation pathways involving quinone methide formation and thiazolidinedione ring scission.

T. Baillie, Wei Tang, D. Dean, 2001, Chemical research in toxicology.

De novo design of a novel oxazolidinone analogue as a potent and selective alpha1A adrenergic receptor antagonist with high oral bioavailability.

A. D. Rodrigues, R. Chang, B. Lagu, 2000, Journal of medicinal chemistry.

Mechanistic studies of valproic acid hepatotoxicity : identification and characterization of thiol conjugates

K. Kassahun, 1991 .

3-Aminopyrrolidinone farnesyltransferase inhibitors: design of macrocyclic compounds with improved pharmacokinetics and excellent cell potency.

A. D. Rodrigues, J Christopher Culberson, Ronald Robinson, 2002, Journal of medicinal chemistry.

The disposition, metabolism, and pharmacokinetics of a selective metabotropic glutamate receptor agonist in rats and dogs.

J. L. Herman, W. J. Wheeler, K. Kassahun, 2002, Drug metabolism and disposition: the biological fate of chemicals.

Metabolic profiling of valproic acid in patients using negative-ion chemical ionization gas chromatography-mass spectrometry.

K. Farrell, K. Kassahun, F. Abbott, 1990, Journal of chromatography.

Negative ion chemical ionization gas chromatography/mass spectrometry of valproic acid metabolites.

K. Kassahun, F. Abbott, R. Burton, 1989, Biomedical & environmental mass spectrometry.

Biological reactive intermediates in drug discovery and development: a perspective from the pharmaceutical industry.

T. Baillie, K. Kassahun, K Kassahun, 2001, Advances in experimental medicine and biology.

Disposition and biotransformation of the antipsychotic agent olanzapine in humans.

T. Gillespie, D. Tupper, J. Callaghan, 1997, Drug metabolism and disposition: the biological fate of chemicals.

Age dependent in vitro metabolism of bifenthrin in rat and human hepatic microsomes

K. Kassahun, Gopinath C. Nallani, Zhi-wei Liu, 2018, Toxicology and applied pharmacology.

Role of human liver cytochrome P4503A in the metabolism of etoricoxib, a novel cyclooxygenase-2 selective inhibitor.

A. D. Rodrigues, I. Mcintosh, C. Rodeheffer, 2001, Drug metabolism and disposition: the biological fate of chemicals.

Minimizing metabolic activation during pharmaceutical lead optimization: progress, knowledge gaps and future directions.

T. Baillie, Sanjeev Kumar, Thomas A Baillie, 2008, Current opinion in drug discovery & development.

Coadministration of Rifampin Significantly Reduces Odanacatib Concentrations in Healthy Subjects

M. Reitman, F. Kesisoglou, A. Mehta, 2017, Journal of clinical pharmacology.

Cytochrome P-450-mediated dehydrogenation of 2-n-propyl-2(E)-pentenoic acid, a pharmacologically-active metabolite of valproic acid, in rat liver microsomal preparations.

T. Baillie, K. Kassahun, 1993, Drug metabolism and disposition: the biological fate of chemicals.

Metabolic activation of unsaturated derivatives of valproic acid. Identification of novel glutathione adducts formed through coenzyme A-dependent and -independent processes.

T. Baillie, K. Kassahun, M. Grillo, 1994, Chemico-biological interactions.

Olanzapine 10-N-glucuronide. A tertiary N-glucuronide unique to humans.

T. Gillespie, R. Franklin, K. Kassahun, 1998, Drug metabolism and disposition: the biological fate of chemicals.

N-Glucuronidation of Xenobiotics Symposium OLANZAPINE 10N-GLUCURONIDE A Tertiary N-Glucuronide Unique to Humans

T. Gillespie, R. Franklin, K. Kassahun, 1998 .

Disposition and metabolism of olanzapine in mice, dogs, and rhesus monkeys.

T. Gillespie, R. Franklin, K. Kassahun, 1997, Drug metabolism and disposition: the biological fate of chemicals.

Simultaneous determination of urinary free cortisol and 6beta-hydroxycortisol by liquid chromatography-atmospheric pressure chemical ionization tandem mass spectrometry and its application for estimating hepatic CYP3A induction.

A. D. Rodrigues, C. Tang, I. Mcintosh, 2000, Journal of chromatography. B, Biomedical sciences and applications.

In vivo formation of the thiol conjugates of reactive metabolites of 4-ene VPA and its analog 4-pentenoic acid.

K. Kassahun, F. Abbott, 1993, Drug metabolism and disposition: the biological fate of chemicals.

Theeffect ofcarbamazepine onvalproic aciddisposition in adult volunteers

K. Farrell, K. Kassahun, F. Abbott, 1989 .

Zafirlukast metabolism by cytochrome P450 3A4 produces an electrophilic alpha,beta-unsaturated iminium species that results in the selective mechanism-based inactivation of the enzyme.

T. Baillie, I. Mcintosh, G. Doss, 2005, Chemical research in toxicology.

In vitro and in vivo evaluation of dihydropyrimidinone C-5 amides as potent and selective alpha(1A) receptor antagonists for the treatment of benign prostatic hyperplasia.

J. Barrow, K. Rittle, R. Freidinger, 2000, Journal of medicinal chemistry.

Prednisone has no effect on the pharmacokinetics of CYP3A4 metabolized drugs – midazolam and odanacatib

R. Evers, J. Wagner, A. Mehta, 2014, Journal of clinical pharmacology.

Lack of a Clinically Meaningful Pharmacokinetic Effect of Rifabutin on Raltegravir: In Vitro/In Vivo Correlation

J. Lunceford, N. Hariparsad, J. Wagner, 2011, Journal of clinical pharmacology.

Identification and characterization of the glutathione and N-acetylcysteine conjugates of (E)-2-propyl-2,4-pentadienoic acid, a toxic metabolite of valproic acid, in rats and humans.

K Farrell, K. Farrell, K. Kassahun, 1991, Drug metabolism and disposition: the biological fate of chemicals.

Metabolism and Renal Elimination of Gaboxadol in Humans: Role of UDP-Glucuronosyltransferases and Transporters

X. Chu, R. Evers, M. Braun, 2009, Pharmaceutical Research.

Lack of Effect of Olanzapine on the Pharmacokinetics of a Single Aminophylline Dose in Healthy Men

W. Macias, B. Cerimele, J. Callaghan, 1998, Pharmacotherapy.

Quantitation of geometric isomers of a phosphodiesterase inhibitor in rat and monkey plasma using liquid chromatography-tandem mass spectrometry.

Rena Zhang, Yuexia Liang, K. Kassahun, 2006, Journal of pharmaceutical and biomedical analysis.

Disposition and Metabolism of the Cathepsin K Inhibitor Odanacatib in Humans

K. Koeplinger, I. Mcintosh, S. Stoch, 2014, Drug Metabolism and Disposition.

Metabolic activation of unsaturated derivatives of valproic acid: role of microsomal versus mitochondrial enzyme systems

T. Baillie, Jasmine Lin, R. Levy, 1992 .