Search Results - "Kelem Kassahun"

Metabolism and Disposition in Humans of Raltegravir (MK-0518), an Anti-AIDS Drug Targeting the Human Immunodeficiency Virus 1 Integrase Enzyme by KASSAHUN, Kelem, MCINTOSH, Ian, DONGHUI CUI, HRENIUK, David, MERSCHMAN, Shelia, LASSETER, Kenneth, AZROLAN, Neal, IWAMOTO, Marian, WAGNER, John A, WENNING, Larissa A

“…Raltegravir is a potent human immunodeficiency virus 1 (HIV-1) integrase strand transfer inhibitor that is being developed as a novel anti-AIDS drug. The…”
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Disposition and metabolism of the cathepsin K inhibitor odanacatib in humans by Kassahun, Kelem, McIntosh, Ian, Koeplinger, Kenneth, Sun, Li, Talaty, Jennifer E, Miller, Deborah L, Dixon, Russell, Zajic, Stefan, Stoch, S Aubrey

“…Odanacatib is a selective inhibitor of the cathepsin K enzyme that is expressed in osteoclasts involved in the degradation of bone organic matrix, and is being…”
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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 by Kassahun, Kelem, Pearson, Paul G, Tang, Wei, McIntosh, Ian, Leung, Kwan, Elmore, Charles, Dean, Dennis, Wang, Regina, Doss, George, Baillie, Thomas A

“…Therapy with the oral antidiabetic agent troglitazone (Rezulin) has been associated with cases of severe hepatotoxicity and drug-induced liver failure, which…”
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Biotransformation of the Naturally Occurring Isothiocyanate Sulforaphane in the Rat:  Identification of Phase I Metabolites and Glutathione Conjugates by Kassahun, Kelem, Davis, Margaret, Hu, Pei, Martin, Bryan, Baillie, Thomas

“…Sulforaphane (SFN) is a naturally occurring isothiocyanate present in cruciferous vegetables, such as broccoli, that has been identified as a potent inducer of…”
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Disposition and Biotransformation of the Antipsychotic Agent Olanzapine in Humans by Kelem Kassahun, Edward Mattiuz, Eldon Nyhart, Jr, Boyd Obermeyer, Todd Gillespie, Anthony Murphy, R. Michael Goodwin, David Tupper, J. Thomas Callaghan, Louis Lemberger

“…Disposition and biotransformation of the new antipsychotic agent olanzapine (OLZ) were studied in six male healthy volunteers after a single oral dose of 12.5…”
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Role of Human Liver Cytochrome P4503A in the Metabolism of Etoricoxib, a Novel Cyclooxygenase-2 Selective Inhibitor by KASSAHUN, Kelem, MCINTOSH, Ian S, SHOU, Magang, WALSH, Deborah J, RODEHEFFER, Carey, SLAUGHTER, Donald E, GEER, Leslie A, HALPIN, Rita A, AGRAWAL, Nancy, RODRIGUES, A. David

“…Etoricoxib, a potent and selective cyclooxygenase-2 inhibitor, was shown to be metabolized via 6′-methylhydroxylation (M2 formation) when incubated with…”
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Determination of enzymatic kinetics of metabolism of dimethoate and omethoate in rats and humans by Nallani, Gopinath, Chandrasekaran, Appavu, Kassahun, Kelem, Shen, Li, Reiss, Rick, Whatling, Paul

“…1. Dimethoate is an organophosphate insecticide. The objective of this work was to determine the enzymatic kinetics of metabolism of dimethoate and its active…”
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In Vitro and In Vivo Metabolism of a Novel Antimitochondrial Cancer Metabolism Agent, CPI-613, in Rat and Human by Reddy, Vijay Bhasker, Boteju, Lakmal, Boteju, Asela, Shen, Li, Kassahun, Kelem, Reddy, Nageshwar, Sheldon, Adrian, Luther, Sanjeev, Hu, Ke

“…CPI-613, an inhibitor of pyruvate dehydrogenase (PDH) and -ketoglutarate dehydrogenase (KGDH) enzymes, is currently in development for the treatment of…”
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The Disposition, Metabolism, and Pharmacokinetics of a Selective Metabotropic Glutamate Receptor Agonist in Rats and Dogs by JOHNSON, Jason T, MATTIUZ, Edward L, CHAY, Sylvia H, HERMAN, Jennifer L, WHEELER, William J, KASSAHUN, Kelem, SWANSON, Steven P, PHILLIPS, Diane L

“…Compound LY354740 [(+)-2-aminobicyclo[3.1.0]hexane-2,6-dicarboxylic acid], an analog of glutamic acid, is a selective group 2 metabotropic glutamate receptor…”
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Age dependent in vitro metabolism of bifenthrin in rat and human hepatic microsomes by Nallani, Gopinath C., Chandrasekaran, Appavu, Kassahun, Kelem, Shen, Li, ElNaggar, Shaaban F., Liu, Zhiwei

“…Bifenthrin, a pyrethroid insecticide, undergoes oxidative metabolism leading to the formation of 4′-hydroxy-bifenthrin (4′-OH-BIF) and hydrolysis leading to…”
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Disposition and Metabolism of Olanzapine in Mice, Dogs, and Rhesus Monkeys by MATTIUZ, E, FRANKLIN, R, GILLESPIE, T, MURPHY, A, BERNSTEIN, J, CHIU, A, HOTTEN, T, KASSAHUN, K

“…Olanzapine (OLZ) is a novel antipsychotic agent with a high affinity for serotonin (5-HT 2 ), dopamine (D 1 /D 2 /D 4 ), muscarinic (m 1 –m 5 ), adrenergic…”
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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 by Davis, Margaret R, Kassahun, Kelem, Jochheim, Claudia M, Brandt, Kathleen M, Baillie, Thomas A

“…The antitumor agent N,N'-bis(2-chloroethyl)-N-nitrosourea (BCNU) is known to be unstable in aqueous solution, and to degrade spontaneously to reactive…”
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Pharmacokinetics and Metabolism in Rats, Dogs, and Monkeys of the Cathepsin K Inhibitor Odanacatib: Demethylation of a Methylsulfonyl Moiety as a Major Metabolic Pathway by KASSAHUN, Kelem, CAMERON BLACK, W, NICOLL-GRIFFITH, Deborah, MCINTOSH, Ian, CHAURET, Nathalie, DAY, Stephen, ROSENBERG, Elizabeth, KOEPLINGER, Kenneth

“…Odanacatib is a potent cathespin K inhibitor that is being developed as a novel therapy for osteoporosis. The disposition and metabolism of odanacatib were…”
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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 by Barrow, James C, Nantermet, Philippe G, Selnick, Harold G, Glass, Kristen L, Rittle, Kenneth E, Gilbert, Kevin F, Steele, Thomas G, Homnick, Carl F, Freidinger, Roger M, Ransom, Rick W, Kling, Paul, Reiss, Duane, Broten, Theodore P, Schorn, Terry W, Chang, Raymond S. L, O'Malley, Stacey S, Olah, Timothy V, Ellis, Joan D, Barrish, Andrea, Kassahun, Kelem, Leppert, Paula, Nagarathnam, Dhanapalan, Forray, Carlos

“…α1 Adrenergic receptors mediate both vascular and lower urinary tract tone, and α1 receptor antagonists such as terazosin (1b) are used to treat both…”
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Prednisone has no effect on the pharmacokinetics of CYP3A4 metabolized drugs - midazolam and odanacatib by Marcantonio, Eugene E., Ballard, Jeanine, Gibson, Christopher R., Kassahun, Kelem, Palamanda, Jairam, Tang, Cuyue, Evers, Raymond, Liu, Chengcheng, Zajic, Stefan, Mahon, Chantal, Mostoller, Kate, Hreniuk, David, Mehta, Anish, Morris, Denise, Wagner, John A., Stoch, S. Aubrey

“…We evaluated the effect of prednisone on midazolam and odanacatib pharmacokinetics. In this open‐label, 2‐period crossover study in healthy male subjects,…”
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Coadministration of Rifampin Significantly Reduces Odanacatib Concentrations in Healthy Subjects by Stoch, S. Aubrey, Ballard, Jeanine, Gibson, Christopher, Kesisoglou, Filippos, Witter, Rose, Kassahun, Kelem, Zajic, Stefan, Mehta, Anish, Brandquist, Christine, Dempsey, Cynthia, Stypinski, Daria, Reitman, Marc L.

“…This open‐label 2‐period study assessed the effect of multiple‐dose administration of rifampin, a strong cytochrome P450 3A (CYP3A) and P‐glycoprotein inducer,…”
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Lack of a Pharmacokinetic Effect of Raltegravir on Midazolam: In Vitro/In Vivo Correlation by Iwamoto, Marian, Kassahun, Kelem, Troyer, Matthew D., Hanley, William D., Lu, Ping, Rhoton, Alisha, Petry, Amelia S., Ghosh, Kalyan, Mangin, Eric, DeNoia, Emanuel P., Wenning, Larissa A., Stone, Julie A., Gottesdiener, Keith M., Wagner, John A.

“…Raltegravir is a novel HIV‐1 integrase inhibitor with potent in vitro activity (95% inhibitory concentration = 33 nM in 50% human serum). In vitro…”
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Approaches for minimizing metabolic activation of new drug candidates in drug discovery by Kumar, Sanjeev, Mitra, Kaushik, Kassahun, Kelem, Baillie, Thomas A

“…A large body of circumstantial evidence suggests that metabolic activation of drug candidates to chemically reactive electrophilic metabolites that are capable…”
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Lack of a Clinically Meaningful Pharmacokinetic Effect of Rifabutin on Raltegravir: In Vitro/In Vivo Correlation by Brainard, Diana M., Kassahun, Kelem, Wenning, Larissa A., Petry, Amelia S., Liu, Chengcheng, Lunceford, Jared, Hariparsad, Niresh, Eisenhandler, Roy, Norcross, Alisha, DeNoia, Emanuel P., Stone, Julie A., Wagner, John A., Iwamoto, Marian

“…Raltegravir is an HIV‐1 integrase strand transfer inhibitor with potent activity against HIV‐1. A prior investigation of raltegravir coadministered with…”
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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 by Barrow, J C, Nantermet, P G, Selnick, H G, Glass, K L, Rittle, K E, Gilbert, K F, Steele, T G, Homnick, C F, Freidinger, R M, Ransom, R W, Kling, P, Reiss, D, Broten, T P, Schorn, T W, Chang, R S, O'Malley, S S, Olah, T V, Ellis, J D, Barrish, A, Kassahun, K, Leppert, P, Nagarathnam, D, Forray, C

“…alpha(1) Adrenergic receptors mediate both vascular and lower urinary tract tone, and alpha(1) receptor antagonists such as terazosin (1b) are used to treat…”
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