Results 1 to 10 of about 6,868,569 (338)

Cytochrome P450 Enzymes and Drug Metabolism in Humans

open access: yesInternational Journal of Molecular Sciences, 2021
Human cytochrome P450 (CYP) enzymes, as membrane-bound hemoproteins, play important roles in the detoxification of drugs, cellular metabolism, and homeostasis. In humans, almost 80% of oxidative metabolism and approximately 50% of the overall elimination
Mingzhe Zhao   +10 more
semanticscholar   +1 more source

Human Gut Microbiota and Drug Metabolism

open access: yesMicrobial Ecology, 2022
The efficacy of drugs widely varies in individuals, and the gut microbiota plays an important role in this variability. The commensal microbiota living in the human gut encodes several enzymes that chemically modify systemic and orally administered drugs,
Archana Pant   +3 more
semanticscholar   +1 more source

Drug metabolism and drug transport of the 100 most prescribed oral drugs

open access: yesBasic & Clinical Pharmacology & Toxicology, 2022
Safe and effective use of drugs requires an understanding of metabolism and transport. We identified the 100 most prescribed drugs in six countries and conducted a literature search on in vitro data to assess contribution of Phase I and II enzymes and ...
D. B. Iversen   +4 more
semanticscholar   +1 more source

Investigation of the human metabolism and disposition of the prolyl hydrolase inhibitor daprodustat using IV microtracer with Entero‐Test bile string

open access: yesPharmacology Research & Perspectives, 2023
Daprodustat is an oral small molecule hypoxia‐inducible factor (HIF) prolyl hydroxylase inhibitor (PHI) approved in Japan and the United States for the treatment of anemia associated with chronic kidney disease.
Guoying Tai   +8 more
doaj   +1 more source

Exploring Drug Metabolism by the Gut Microbiota: Modes of Metabolism and Experimental Approaches

open access: yesDrug Metabolism And Disposition, 2021
Increasing evidence uncovers the involvement of gut microbiota in the metabolism of numerous pharmaceutical drugs. The human gut microbiome harbors 10–100 trillion symbiotic gut microbial bacteria that use drugs as substrates for enzymatic processes to ...
Pooja Dhurjad   +3 more
semanticscholar   +1 more source

Application of a PBPK model to elucidate the changes of systemic and liver exposures for rosuvastatin, carotegrast, and bromfenac followed by OATP inhibition in monkeys

open access: yesClinical and Translational Science, 2021
The impact of organic anion‐transporting polypeptide (OATP) inhibition on systemic and liver exposures of three OATP substrates was investigated in cynomolgus monkeys.
Yaofeng Cheng   +4 more
doaj   +1 more source

Drug metabolism in the lungs: opportunities for optimising inhaled medicines

open access: yesExpert Opinion on Drug Metabolism & Toxicology, 2021
Introduction The lungs possess many xenobiotic metabolizing enzymes which influence the pharmacokinetics and safety of inhaled medicines. Anticipating metabolism in the lungs provides an opportunity to optimize new inhaled medicines and overcome ...
Zachary Enlo-Scott   +3 more
semanticscholar   +1 more source

Personalized Mapping of Drug Metabolism by the Human Gut Microbiome.

open access: yesCell, 2020
The human gut microbiome harbors hundreds of bacterial species with diverse biochemical capabilities. Dozens of drugs have been shown to be metabolized by single isolates from the gut microbiome, but the extent of this phenomenon is rarely explored in ...
Bahar Javdan   +8 more
semanticscholar   +1 more source

Applicability of free drug hypothesis to drugs with good membrane permeability that are not efflux transporter substrates: A microdialysis study in rats

open access: yesPharmacology Research & Perspectives, 2020
In clinical pharmacology, the free drug hypothesis has been widely applied in the interpretation of the relationship between pharmacokinetics and pharmacodynamics (PK/PD).
Chun Chen   +21 more
doaj   +1 more source

A novel SRSF3 inhibitor, SFI003, exerts anticancer activity against colorectal cancer by modulating the SRSF3/DHCR24/ROS axis

open access: yesCell Death Discovery, 2022
As the modulation of serine/arginine-rich splicing factor 3 (SRSF3) may be therapeutically beneficial to colorectal cancer (CRC) treatment, the identification of novel SRSF3 inhibitors is highly anticipated. However, pharmaceutical agents targeting SRSF3
Yawen Zhang   +14 more
doaj   +1 more source

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