Drug Metabolism In Clinical Pharmacology And Therapeutic Explore the role of drug metabolism in clinical pharmacology and therapeutic design to improve safety, optimize dosing, and advance precision medicine.

Drug Metabolism in Clinical Pharmacology and Therapeutic Design

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#DrugMetabolism #ClinicalPharmacology #BIJournal #BIJournalnews #BusinessInsightsarticles #BIJournalinterview

Characterization of the Formation of the Acyl Glucuronide Metabolite of 7-Carboxy-Cannabidiol in Human Liver, Kidney, and Intestinal Microsomes and In Vivo in Mice Acyl glucuronides are common metabolites of carboxylic acids. They can be reactive and cause adverse events. The acyl glucuronide metabolite of delta-9-tetrahydrocannabinol (THC) is abundant in humans after THC consumption but acyl glucuronide formation from the cannabidiol (CBD) metabolite 7-carboxy-cannabidiol (7-COOH-CBD) has not been previously described. Here, we identified and characterized both acyl and phenolic glucuronides of 7-COOH-CBD formed in human liver, kidney, and intestinal microsomes. The 7-COOH-CBD-acyl-glucuronide was mostly formed by UGT1A1 and UGT1A3, while the 7-COOH-CBD-phenolic-glucuronide was formed by UGT1A9. 7-COOH-CBD-acyl-glucuronide formation was also detected in vivo in mice. 7-COOH-CBD-acyl-glucuronide showed extensive acyl migration while 11-COOH-THC-glucuronide did not. Human serum albumin enhanced migration, while liver fatty acid binding protein (FABP1) protected against 7-COOH-CBD-acyl-glucuronide migration. When corrected for unbound fraction, FABP1 increased 7-COOH-CBD glucuronidation efficiency. These findings suggest that 7-COOH-CBD-acyl-glucuronide is a metabolite of CBD in humans and may play a role in CBD related liver toxicity.

Characterization of the Formation of the Acyl Glucuronide Metabolite of 7-Carboxy-Cannabidiol in Human Liver, Kidney, and Intestinal Microsomes and In Vivo in Mice pubs.acs.org/doi/10.1021/... @acs.org

#KellyChibale #DrugMetabolism #LiverToxicity #Pharmacokinetics #MedicinalChemistry #DrugSafety

Hidden Players in Drug Efficacy: Using #SIRIUS6, researchers decoded the crucial role of the gut microbiome in altering the chemical structure and efficacy of GPCR drugs.
💡 Blog post: buff.ly/WtrJf2m (5 min)
📄 Publication: buff.ly/8o1ekPv

#SIRIUSDiscoveries #DrugMetabolism #PersonalizedMedicine

U01.05.004 Drug metabolism Carefully review each biochemical reaction and classify it based on its role in drug metabolism. Remember: Phase I reactions introduce or expose functional groups (increasing polarity), while Phase II reactions involve conjugation with endogenous substrates to enhance excretion. Match each reaction type accordingly to strengthen your pharmacology fundamentals.

Drug metabolism modifies drugs via Phase I and II liver reactions to aid detoxification and excretion. #DrugMetabolism #CytochromeP450 #Pharmacokinetics #PhaseI #PhaseII #Pharmacology #Liver #DrugExcretion #MedicalEducation #USMLE

At this week’s #JEMS, Michael Zimmermann (@zimmermannlab.bsky.social & @embl.org) shared insights on how gut microbiota shape #drugmetabolism and carcinogen toxicity. Fascinating findings on cancer risk, #drugresponse variability, and limits of current models. Thanks for the inspiring talk!

How soy and gut microbes alter cancer treatment results Researchers have discovered that plant-derived phytochemicals and their gut microbiome metabolites control the effectiveness of PI3K inhibitors in cancer therapy. The study reveals that dietary compon...

How soy and gut microbes alter cancer treatment results www.news-medical.net/news/2025060... #cancer #microbiome #phytochemicals #PI3Kinhibitors #drugmetabolism #soy #precisionmedicine #oncology #dieta #cancer @cellpress.bsky.social

🐻 Get ready, #P450 peeps! for guru David (aka @p450nelson.bsky.social )! #ICCP450! 🎉 He literally wrote the book (well, the website!) on P450 nomenclature 🧬 – foundational work on drug metabolism, toxicology genomics! 🗓️ #P450 #CytochromeP450 #DrugMetabolism #Pharmacology 🔬 www.iccp450bern.unibe.ch

8/ Beyond CYP3A4, grapefruit juice can affect P-glycoprotein, a transporter protein that pumps drugs out of cells. Inhibition can lead to increased drug absorption and potential toxicity.
#DrugMetabolism

📢 Get ready to hear Prof. Steve Sligar at 24th #ICCP450 meeting in #Bern, #Switzerland! 🇨🇭🗓️ 🎉
🔬✨ Don't miss the chance to learn from a true leader in #cytochromeP450 !
➡️ info: iccp450bern.unibe.ch
See you in Bern! 👋 #DrugMetabolism #Biochemistry #Science #P450 🧪🧬

Looking forward to speaking on March 13th about immigrant populations and navigating cancer care delivery at the Warmina Foundation. Please feel free to register and join.
#cancercare #patientadvocacy #2ndopinions #drugmetabolism

The role of glutathione S-transferases in human disease pathogenesis and their current inhibitors

This review discusses the role of Glutathione-S-transferase (GST) in regulating diverse functions, the association of GST isoforms with various #diseases, & the therapeutic implications of GST inhibitors. #DrugMetabolism

#OpenAccess: www.sciencedirect.co...

Drug metabolites can have unintended pharmacological or toxic effects. Profiling metabolites early prevents late-stage surprises. #DrugMetabolism #DrugSafety

Drugs with high first-pass metabolism face reduced bioavailability. Prodrugs or alternative delivery methods often mitigate this. #DrugMetabolism #PK

Case report: metoclopramide induced acute dystonic reaction in adolescent CYP2D6 poor metabolizers Metoclopramide is indicated for the management of gastroesophageal reflux, gastric stasis, nausea, and vomiting. Metoclopramide-induced acute dystonic reactions (MIADRs), along with repetitive involun...

Case report: metoclopramide induced acute dystonic reaction in adolescent CYP2D6 poor metabolizers [2023]
pmc.ncbi.nlm.nih.gov/articles/PMC...
#metoclopramide #Reglan #CYP2D6 #pharmacogenetics #pharamcogenomics #DrugMetabolism #pharmacology #gastroenterology #dopamine #AdverseReactions #SideEffects

Did you know that #microbes in your intestines can interfere with #DrugMetabolism? A new paper from @donia_lab used ex vivo ##microbial screening to learn more about these #microbiome-drug interactions. Promising step for...