Zobrazeno 1 - 10
of 27
pro vyhledávání: '"Mithat Gunduz"'
Autor:
David, Pearson, Yi, Jin, Andrea, Romeo, Bertrand-Luc, Birlinger, Hilmar, Schiller, Yan, Ji, Mithat, Gunduz, Daniela, Baldoni, Markus, Walles
Publikováno v:
Xenobiotica. 52:26-37
LSZ102 is an orally bioavailable selective oestrogen receptor degrader in clinical development for the treatment of breast cancer. Preclinical studies showed efficacy in xenograft models on oral dosing. However, oral bioavailability was relatively lo
Publikováno v:
Drug Metabolism Letters
Background: Acyl glucuronides of xenobiotics have been a subject of wide interest from the pharmaceutical industry with respect to biochemical reactivity, hepatic disposition, and enterohepatic cir-culation. The reactivity and lack of stability of an
Autor:
James E. Chastain, Upendra A. Argikar, Nagendra V. Chemuturi, Markus Walles, Gian Camenisch, Vito G. Sasseville, Jennifer L. Dumouchel, Mark Milton, Ganesh R. Iyer, Mithat Gunduz
Publikováno v:
Drug Metabolism and Disposition. 46:1670-1683
The eye is a complex organ with a series of anatomic barriers that provide protection from physical and chemical injury while maintaining homeostasis and function. The physiology of the eye is multifaceted, with dynamic flows and clearance mechanisms
Autor:
Valerie M. Kramlinger, Christine E. Dunne, Amanda L. Cirello, Jennifer L. Dumouchel, Upendra A. Argikar, Bindi Sohal, Mithat Gunduz
Publikováno v:
Journal of Pharmaceutical Sciences. 106:2276-2281
The liver is known to be the principal site of drug metabolism. Depending on the route of administration, especially in cases of topical and local delivery, evaluation of local drug metabolism in extrahepatic tissues is vital to assess fraction of th
Autor:
Mithat Gunduz, Christine E. Dunne, Upendra A. Argikar, Amanda L. Cirello, Jennifer L. Dumouchel
Publikováno v:
Drug Metabolism and Pharmacokinetics. 32:121-126
Oral ketoconazole is clinically administered for treatment of severe cases for fungal keratitis. Pharmacodynamics and efficacy of oral and topical (ocular) ketoconazole have been explored in rabbit. However, metabolism of ketoconazole in the eye in a
Autor:
Christine E. Dunne, Jennifer L. Dumouchel, Mithat Gunduz, Chitra Saran, Amanda L. Cirello, Upendra A. Argikar
Publikováno v:
Drug Metabolism and Disposition. 44:1304-1312
Although ocular transport and delivery have been well studied, metabolism in the eye is not well documented, even for clinically available medications such as levobunolol, a potent and nonselective β-adrenergic receptor antagonist. Recently, we repo
Autor:
Amin Kamel, Elizabeth George, Xiaolin Gao, Antonin V. Tutter, Diksha Bhatia, Vic E. Myer, Mark Labow, Irina Alimov, Panagiotis Hatsis, Alan Buckler, Louis Wang, Mithat Gunduz, Christine D. Wilson, Earl Mcdonald, Gregory A. Michaud, Yucheng Ni, Kavitha Venkatesan, Jeffrey A. Porter, Yan Feng, Shaowen Wang, Deborah Rothman, Timothy Rasmusson, Mary Ellen Digan, David Farley, John A. Tallarico, Fred Harbinski
Publikováno v:
Chemistry & Biology. 22:1228-1237
SummaryIn an attempt to identify novel therapeutics and mechanisms to differentially kill tumor cells using phenotypic screening, we identified N-benzyl indole carbinols (N-BICs), synthetic analogs of the natural product indole-3-carbinol (I3C). To u
Publikováno v:
Drug Metabolism Letters. 11
Background 4-(piperazin-1-yl)-8-(trifluoromethyl)pyrido[2,3-e][1,2,4]triazolo[4,3-a]pyrazine (1) is a small-molecule which demonstrated a sub-nM inhibitory potency toward the histamine H4 receptor (H4R). However, it was found to be mutagenic in an in
Autor:
Mithat Gunduz, Amanda L. Cirello, Upendra A. Argikar, Ann Brown, Christine E. Dunne, Jennifer L. Dumouchel, Jaimie Spear, Valerie M. Kramlinger
Publikováno v:
Drug Metabolism Letters. 11
BACKGROUND Timolol is clinically administered topically (ocular) to reduce intraocular pressure and treat open-angle glaucoma. Ocular administration of timolol in low doses (0.5% w/v in the form of eye drops) has led to challenges for in vivo metabol
Autor:
Michelle K. Dennehy, Mithat Gunduz, Shawn Harriman, Ivana Liric Rajlic, Nigel J. Waters, R. Scott Obach, Upendra A. Argikar, Jenny Zhan, Franco Lombardo, Giuliano Berellini
Publikováno v:
The Journal of Clinical Pharmacology. 53:167-177
The authors present a comprehensive analysis on the estimation of volume of distribution at steady state (VD(ss) ) in human based on rat, dog, and monkey data on nearly 400 compounds for which there are also associated human data. This data set, to t