Results 51 to 60 of about 1,906,831 (271)

Use of Clotrimazole in Finfish Aquaculture: Mechanistic Insights, Limitations, and Future Directions for Antifungal Therapy

Animal Research and One Health, EarlyView.
This review critically evaluates clotrimazole as a potential antifungal for finfish aquaculture, highlighting strong mechanistic and in vitro efficacy against aquatic mycoses alongside major gaps in in vivo evidence, toxicokinetics, residue safety, and environmental risk, outlining priorities for responsible therapeutic development and regulatory ...
Arya Sen, Debashri Mondal, Thangapalam Jawahar Abraham   +2 more
wiley   +1 more source

Comprehensive Characterization of Acer truncatum Leaf Extract: Identification of Systemic Metabolites and Effects on Performance, Antioxidant Status, and Intestinal Microbiota in Laying Hens

Animal Research and One Health, EarlyView.
Dietary A. truncatum leaf extract is absorbed and improves laying performance in aged hens by enhancing systemic antioxidant capacity and modulating the gut microbiota. ABSTRACT The demand for natural feed additives is considerably increasing in the antibiotic‐free feed era.
Kailong Qin, Jiantao Yang, Minglu Gao, Xiaozhao Tao, Xin Yang, Yanli Liu, Xiaojun Yang   +6 more
wiley   +1 more source

First‐in‐human, phase I, randomized, safety, pharmacokinetic, food‐effect and pharmacodynamic study of a tyrosine kinase 2/Janus kinase 1 inhibitor, SDC‐1801

British Journal of Clinical Pharmacology, EarlyView.
Aim The purpose of this study is to evaluate safety, tolerability, pharmacokinetics (PK), food‐effect (FE) and pharmacodynamics (PD) of an oral tyrosine kinase‐2 (TYK2)/Janus kinase‐1 (JAK1) inhibitor, SDC‐1801, in healthy adult participants. Methods This first‐in‐human study randomized 95 male and female participants.
Chris Brearley, Sam Francis, John Reader, Judi Proctor   +3 more
wiley   +1 more source

Monitoring pharmacodynamic and molecular drug targets in liquid biopsy: Exploratory study in liver cancer with modelling of EGFR Receptor engagement

British Journal of Clinical Pharmacology, EarlyView.
Abstract Aim Liquid biopsy is minimally invasive (compared with tissue biopsy) and has previously been used to generate systems data regarding drug elimination via hepatic enzymes and transporters. This study extends quantitative assessment of systems parameters in liquid biopsy to pharmacodynamic (PD) and disease markers relevant to cancer development
Zubida M. Al‐Majdoub, Armin Sepp, Amin Rostami‐Hodjegan, Brahim Achour   +3 more
wiley   +1 more source

In Vitro Phase I Metabolism of CRV431, a Novel Oral Drug Candidate for Chronic Hepatitis B

Pharmaceutics, 2017
The cytochrome P450-mediated Phase I in vitro metabolism of CRV431 was studied using selective chemical inhibition and recombinant human enzymes. Additionally, the metabolic profile of CRV431 in human, rat, and monkey liver microsomes was investigated ...
Daniel J. Trepanier, Daren R. Ure, Robert T. Foster   +2 more
doaj   +1 more source

Human Liver Microsomal Metabolism of (+)-Discodermolide [PDF]

Journal of Natural Products, 2009
The polyketide natural product (+)-discodermolide is a potent microtubule stabilizer that has generated considerable interest in its synthetic, medicinal, and biological chemistry. It progressed to early clinical oncology trials, where it showed some efficacy in terms of disease stabilization but also some indications of causing pneumotoxicity ...
Yun, Fan, Emanuel M, Schreiber, Billy W, Day   +2 more
openaire   +2 more sources

Repurposing Drugs for Malaria through a Human Dose Prediction: A Case Study with Berzosertib

Clinical Pharmacology &Therapeutics, EarlyView.
Repurposing drugs whose clinical safety has been established offers a valuable approach to reduce the cost and time associated with the development of new drugs for malaria. Here, we investigate the potential to repurpose the anticancer kinase inhibitor berzosertib for the treatment of malaria, by assessing whether a predicted efficacious human dose ...
Devasha Redhi, Mwila Mulubwa, Mmakwena M. Mmonwa, Mathew Njoroge, Liezl Krugmann, Kelly Chibale   +5 more
wiley   +1 more source

In Vitro Metabolism and In Vivo Pharmacokinetics Profiles of Hydroxy-α-Sanshool

Toxics
Hydroxy-α-sanshool (HAS) is the predominant active compound in Zanthoxylum bungeanum Maxim (ZBM). Our present work was aimed to explore the in vitro metabolism characteristics, and in vivo pharmacokinetic (PK) profile of HAS.
Jie Meng, Die Qian, Ruo-Lan Li, Wei Peng, Li Ai   +4 more
doaj   +1 more source

Assay for the terminal enzyme of the stearoyl coenzyme A desaturase system using chick embryo liver microsomes

Journal of Lipid Research, 1977
The NADH-dependent stearoyl CoA desaturase of hepatic microsomes (EC 1.14.99.5) is an enzyme system consisting of cytochrome b5 reductase (EC 1.6.2.2), cytochrome b5, and the terminal desaturase. We have developed a simple method for routine assay of the
V C Joshi, A C Wilson, S J Wakil
doaj   +1 more source

Characterization of Lysosomal Hydrolases and Transporters and Their Age‐Dependent Variability: Relevance to Drug Metabolism and Transport of Small Molecule and Biologic Drugs

Clinical Pharmacology &Therapeutics, EarlyView.
Lysosomes play a key role in the accumulation, catabolism, and transport of endogenous and exogenous metabolites and proteins and are involved in drug metabolism and prodrug activation. However, the protein abundance and interindividual variability of lysosomal drug‐metabolizing enzymes and transporters (DMETs) remain underexplored.
Darshak Gadara, Dilip Kumar Singh, Sandhya Subash, Guihua Yue, Deepak Ahire, Chris Bohl, Maciej Czerwinski, Stephanie Helmstetter, Scott Heyward, Robert S. Jones, Cyrus Khojasteh, Ryota Kikuchi, Priyanka Kulkarni, Bin Ma, Bernard Murray, Chris Seib, Bill Smith, David M. Stresser, Mitchell E. Taub, Ting Wang, Bhagwat Prasad   +20 more
wiley   +1 more source