Results 71 to 80 of about 27,101 (273)

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

Payload‐Based Clinical Pharmacology Review of Approved Antibody–Drug Conjugates: Commonalities and Considerations for Streamlined Development

Clinical Pharmacology &Therapeutics, EarlyView.
Antibody–drug conjugates (ADCs) combine the specificity of an antibody with the potency of a cytotoxic drug. Thirteen ADCs, utilizing seven unique cytotoxic payloads and targeting 11 distinct antigens, are currently approved by the US Food and Drug Administration as of June 2025, representing a rapidly growing and highly promising class of anticancer ...
Sijie Lu, Qingqing Xiao, Lixuan Qian, Siyuan Sun, Zhu Zhou, Michael Z. Liao, Chunze Li   +6 more
wiley   +1 more source

Metabolism and Metabolic Inhibition of Xanthotoxol in Human Liver Microsomes [PDF]

Evidence-Based Complementary and Alternative Medicine, 2016
Cytochrome p450 (CYP450) enzymes are predominantly involved in Phase I metabolism of xenobiotics. In this study, the CYP450 isoforms involved in xanthotoxol metabolism were identified using recombinant CYP450s. In addition, the inhibitory effects of xanthotoxol on eight CYP450 isoforms and its pharmacokinetic parameters were determined using human ...
Zhongnv Ma, Xianbao Shi, Gang Zhang, Feng Guo, Lina Shan, Jiqun Cai   +5 more
openaire   +3 more sources

Metabolic Difference of CZ48 in Human and Mouse Liver Microsomes

, 2012
CZ48, chemically camptothecin-20-O-propionate hydrate, is currently under clinical investigation. The kinetics of the metabolite camptothecin (CPT) formation and of CZ48 depletion in mouse and human liver microsomes in the presence or absence of NADPH ...
Xing Liu, Albert DeJesus, Zhisong Cao, Dana Vardeman, Beppino Giovanella   +4 more
core   +1 more source

A Novel Workflow for Fast Elucidation of Drug Metabolites for Screening—Combining In Silico Metabolite Prediction With Trapped Ion Mobility QTOF‐MS

Drug Testing and Analysis, EarlyView.
UHPLC‐timsTOF‐MS with in silico prediction and automated annotation enabled rapid identification of quetiapine metabolites from pHLMs, facilitating their inclusion in targeted LC‐QTOF‐MS urine screening and improving biomarker detection for toxicological applications.
Annette Zschiesche, Birgit Schneider, Ilona Nordhorn, Carsten Baessmann, Laura M. Huppertz, Jürgen Kempf   +5 more
wiley   +1 more source

Metabolism of (+)-Fenchone by CYP2A6 and CYP2B6 in Human Liver Microsomes

Biological and Pharmaceutical Bulletin, 2006
The in vitro metabolism of (+)-fenchone was examined in human liver microsomes and recombinant enzymes. Biotransformation of (+)-fenchone was investigated by gas chromatography-mass spectrometry. (+)-Fenchone was found to be oxidized to 6-exo-hydroxyfenchone, 6-endo-hydroxyfenchone and 10-hydroxyfenchone by human liver microsomal P450 enzymes.
Miyazawa, Mitsuo, Gyoubu, Kunihiko
openaire   +4 more sources

Scheme for metabolites of 2a observed with human liver microsomes.

, 2018
Scheme for metabolites of 2a observed with human liver microsomes.
Alfin D. N. Vaz (172262), Joseph S. Warmus (1997752), Suvi T. M. Orr (1485076), Kentaro Futatsugi (1399639), David W. Piotrowski (1944802), Angela C. Wolford (2004778), Yinsheng Zhang (321530), Hao Sun (14095), Steven B. Coffey (1463167)   +8 more
core   +1 more source

Analysis and Characterization of Kisspeptin and Its Analogues in Serum and Urine Samples by Liquid Chromatography–High‐Resolution Mass Spectrometry for Doping Control Purposes

Drug Testing and Analysis, EarlyView.
Sensitive LC‐HRMS methods were established for the detection of kisspeptin and its analogues in serum and urine, alongside their analytical and metabolic characterization. Stability studies were conducted in serum, plasma, and urine, highlighting the importance of appropriate sample handling for reliable anti‐doping analysis.
Sophia Krombholz, Linus Korsmeier, Andreas Thomas, Mario Thevis   +3 more
wiley   +1 more source

Scheme for metabolites of 1a observed with human liver microsomes.

, 2018
Scheme for metabolites of 1a observed with human liver microsomes.
Alfin D. N. Vaz (172262), Joseph S. Warmus (1997752), Suvi T. M. Orr (1485076), Kentaro Futatsugi (1399639), David W. Piotrowski (1944802), Angela C. Wolford (2004778), Yinsheng Zhang (321530), Hao Sun (14095), Steven B. Coffey (1463167)   +8 more
core   +1 more source

Investigation of the In Vitro and In Vivo Metabolism and μ‐Opioid Receptor Affinity of the Nitazene N‐Pyrrolidino Fluetonitazene

Drug Testing and Analysis, EarlyView.
Eight metabolites for N‐pyrrolidino fluetonitazene were identified in vitro, three of which (M2, M6 and M8) were present in an authentic urine sample. M2 was the most abundant in vivo metabolite and is a common marker metabolite of nitazepyne‐type substances.
Severin Zemp, Gaia Alluisetti, Wolfgang Weinmann, Bettina Schrag, Frank Sporkert, Maurine Leclerc, Katharina Elisabeth Grafinger   +6 more
wiley   +1 more source