Design, Synthesis, and Characterization of Prodrugs of Sulfonamide TLR4 Signaling Inhibitor TAK-242 (Resatorvid) We have previously reported two prodrug designs for the delivery of the potent TLR4 inhibitor TAK-242. Our initial design was used to covalently link TAK-242 to pancreatic islets using a linker to afford sustained delivery of the active drug after transplant. Those drug-eluting islets provided local inhibition of TLR4-linked inflammation and improved islet graft survival. Here, we describe a third family of TAK-242 prodrugs featuring two rate modulating sites, a self-immolative aniline-stabilized methylene spacer bonded directly to the sulfonamide nitrogen, an alcohol tether for bioconjugation, and a β-eliminative aryl-sulfone “trigger”. These prodrugs rapidly release TAK-242 after activation by β-elimination and a rapid subsequent 1,2-elimination, cleanly releasing the drug without detectable intermediates. This manuscript reports the preparation and characterization of a series of methylene-linked TAK-242 prodrugs, evaluating the impact of various modifications on drug release kinetics.

Design, Synthesis, and Characterization of Prodrugs of Sulfonamide TLR4 Signaling Inhibitor TAK-242 (Resatorvid) pubs.acs.org/doi/10.1021/... @pubs.acs.org

#MedicinalChemistry #DrugDesign #ProdrugStrategy #InflammationResearch #Immunology #Pharmacokinetics #Therapeutics #DrugDevelopment

www.hackedexams.com/item/112841/...
The Art And Science Of Physiologically Based Pharmacokinetics Modeling 1st Edition By Cristofoletti Rostami Hodjegan 2025 2026 Exam Success Guide
#Physiologically #Pharmacokinetics #ExamSuccessGuide #studyguide #testbank #testbankexams #hackedexams

Researcher profile Maria Kjellsson: “Our success is built on teamwork” – Department of Medicinal Chemistry – Uppsala University Researcher profile Maria Kjellsson: “Our success is built on teamwork”

Researcher #profile ➡️ Meet Maria Kjellsson, Professor of #Pharmacokinetics & Recipient of Uppsala University’s Distinguished Teaching Award for her work to include students and give them tools to navigate the challenges of academic life ✅ Read article 👉 www.uu.se/en/departmen...

Meet TC3 Member Prof. Rachel Tyndale! Her work focuses on pharmacogenomics and pharmacokinetics of substance use disorders.
#cannabis #endocannabinoid #pharmacogenomics #pharmacokinetics #cannabisusedisorder #CUD

@utoronto.ca @camhnews.bsky.social

Have you missed the terminal phases in your #pharmacokinetics study?

Check out the Pharmaceutical Journal Publications article on the #AreaUnderTheCurve parameter in pharmacokientics.

🔗 pharmaceutical-journal.com/article/opin...

#JPP Paper of the Year 2024

Assistant Professor-Pharmakinetics Job Summary: The Assistant Professor's responsibility encompasses teaching, scholarship, service, and practice. Demonstrates loyalty to the mission, policies, standards, and regulations of his/her dep...

Apply: egln.fa.us2.oraclecloud.com/hcmUI/Candid...

#AcademicPharmacy #ClinicalFaculty #PharmacyEducation #InternalMedicine #Pharmacokinetics #Mentorship #Residency

Exploration of plant alkaloids as potential inhibitors of HIV–CD4 binding: Insight into comprehensive in silico approaches

Scientists highlight magnoflurine, nitidine, and #berberine as promising #HIV–CD4 inhibitors, showing strong binding energies, stable molecular dynamics & favorable #pharmacokinetics, supporting their potential as #AntiHIV therapies.
#OpenAccess Open Chemistry: doi.org/10.1515/chem...

Pharmacokinetics of Inhibitors of Succinyl-CoA:3-Ketoacid CoA Transferase in Sprague–Dawley Rats, and the Effect of a High-Fat Diet - The AAPS Journal Pimozide and PSSI-51 are under study for their potential glucose-lowering effects in type 2 diabetes, through their abilities to inhibit succinyl-CoA:3-ketoacid CoA transferase, the rate-limiting enzy...

Happy to share a new paper we contributed to in collaboration with Dr. Dion Brocks' team @ualberta-pharm.bsky.social studying the #pharmacokinetics of #SCOT_inhibitors we've developed for the potential treatment of #T2D link.springer.com/article/10.1...

The Intact Nephron Hypothesis has guided renal drug dosing for 60+ years. The idea: as GFR drops, tubular secretion drops proportionally.
Sounds elegant, right?
But new data shows it's WRONG for many drugs in severe CKD.
Here's what you need to know 🧵👇

#Nephrology #NephSky #Pharmacokinetics

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

Exploring DMPK: How Viva Biotech Is Advancing Pharmacology Platforms in Drug Discovery Viva Biotech is innovating drug discovery with an integrated pharmacology platform that encompasses various modalities including small molecules and antibodies.

Exploring DMPK: How Viva Biotech Is Advancing Pharmacology Platforms in Drug Discovery #Shanghai #None #Pharmacokinetics #Viva_Biotech #DMPK

From structure to strategy: chemometric modeling for the prediction of terminal half-life of pharmaceuticals and its role in future therapeutics - Molecular Diversity The terminal half-life ( $$t_{1/2}$$ t 1 / 2 ) is a crucial pharmacokinetic parameter for estimating the dose regimen and duration of action of a drug. Previously, few research papers have been publis...

New study by Samanta et al. shows how q-RASAR + QSAR can predict terminal half-life (t½) for 895 drugs doi.org/10.1007/s110... using 2D descriptors from #alvaDesc.

🔗 Learn more about alvaDesc: alvascience.com/alvadesc/

#QSAR #ReadAcross #Pharmacokinetics #DrugDiscovery

Toward optimal moxifloxacin dosing in tuberculous meningitis: a translational physiologically based pharmacokinetic modeling approach
Bodilsen, J. et al.
Paper
Details
#Pharmacokinetics #TuberculousMeningitis #Moxifloxacin

This phase Ib/IIa study evaluating the safety, #Pharmacokinetics, #Pharmacodynamics, #Immunogenicity & preliminary efficacy of CM313, an anti-CD38 antibody, in SLE patients showed manageable safety & encouraging clinical efficacy. #medsky

#STTT #OpenAccess: doi.org/10.1038/s413...

U01.05.010 Types of drug interactions Match each drug combination or pharmacologic example with its correct interaction type. Focus on the relationship between the agents — whether their combined effects are additive, synergistic, permissive, antagonistic, potentiating, or lead to tachyphylaxis. Understanding these interaction types is essential for pharmacology exams and clinical applications.

Drug interactions may alter metabolism or receptor effects, impacting efficacy and safety. #DrugInteractions #Pharmacology #Pharmacokinetics #Pharmacodynamics #CytochromeP450 #DrugSafety #ClinicalPharmacology #USMLE #MedicalEducation

U01.05.006 Urine pH and drug elimination To complete this activity, carefully read the statements and identify whether the drug alters urine pH by alkalinization or acidification. Then, drag the correct words into the blanks for each sentence. Focus on the examples of drugs that are excreted more efficiently when the urine pH is altered. This exercise helps you understand renal drug excretion mechanisms and the clinical use of urine pH modifiers.

Urine pH alters drug elimination by changing ionization, aiding clearance of weak acids or bases. #UrinePH #DrugElimination #Pharmacokinetics #WeakAcids #WeakBases #RenalExcretion #OverdoseManagement #MedicalEducation #USMLE #ClinicalPharmacology

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

#Pharmacology #Pharmacokinetics #Pharmacodynamics #DrugSafety #Pharmacovigilance #Teaching #AI

🔦 Spotlight on link.springer.com/article/10.1...

🧠 Using the LeiCNS-PK3.0 PBPK model, they predicted mouse #brainECF #pharmacokinetics for 10 drugs

✅ Accurate for 7 drugs
✅ First mechanistic #CNS PBPK #model in mice
✅ Strong translational potential

#TranslationalPharmacology #DrugDevelopment

🧪 Our new paper on the #pharmacokinetics of P-glycoprotein substrates in #brainECF shows how #invitro transport data can guide #invivo 🧠🐭🚶‍♀️predictions, but that high variability still limits the robustness of these predictions.

🔗 link.springer.com/article/10.1...
👉LeiCNS-PK3.4 PBPK model #CNS #brain

AutoPK uses LLMs and hybrid metrics to extract pharmacokinetic data

AutoPK boosts PK table extraction using LLaMA 3.1‑70B, achieving 0.92 F1 for half‑life and 0.91 for clearance on 605 tables, and cuts hallucinations for smaller models. Read more: getnews.me/autopk-uses-llms-and-hyb... #pharmacokinetics #llm

Call for Papers - Special Issue

As the submission window closes in just a few hours, we encourage you to take this final opportunity to send in your manuscripts.

#CallForPapers #HimalayanHerbs #Pharmacology #Pharmacokinetics #HerbalMedicine #Research

Call for papers- Special Issue

With just a few days to go, we remind you of an opportunity to publish with us.

We hope to receive your manuscripts.

#himalayanherbs #herbalmedicine #pharmacokinetics

Call for papers - Special Issue

We are still accepting manuscripts for our special edition on the medicinal potential of Himalayan Herbs.

Check the flyer for full details.

#CallForPapers #HimalayanHerbs #Pharmacology #Pharmacokinetics #HerbalMedicine #Research

Call for Papers

Harnessing the Medicinal Potential of Himalayan Herbs: Pharmacological & Pharmacokinetic Studies

🗓 Deadline: 30 Sept 2025

Submit here: www.sciencedirect.com/special-issu...

#CallForPapers #HimalayanHerbs #Pharmacology #Pharmacokinetics #HerbalMedicine #Research

A multicenter, phase 1/2 #ClinicalTrial on the safety, #pharmacokinetics, & efficacy of HA121-28 in advanced solid tumors & advanced RET fusion-positive #NSCLC revealed the promising #AntiTumor activity of HA121-28. #medsky

#STTT #OpenAccess: doi.org/10.1038/s413...

Exploration of plant alkaloids as potential inhibitors of HIV–CD4 binding: Insight into comprehensive in silico approaches This study investigates the potential of alkaloids – nitidine, harmine, harmaline, berberine, and magnoflurine – as inhibitors of HIV –CD4 binding, focusing on their molecular interactions, binding…

In silico docking and simulations reveal #alkaloids (nitidine, berberine, magnoflurine) show strong #CD4 binding, stability and good #pharmacokinetics, highlighting their potential as novel anti-HIV inhibitors. #HIV

#OpenAccess in Open Chemistry:

Development of Pharmacokinetics (PK), Pharmacodynamics (PD) and Potency Assays With Organoids Revolutionize drug development using advanced cell-based assays with flow cytometry expertise, offering unparalleled organ mimicry and functional complexity.

Organoids in the Development of Pharmacokinetics, Pharmacodynamics, and Potency Assays
www.marinbio.com/development-...

#organoids #Pharmacokinetics, #Pharmacodynamics #potencyassays

Baked Beyond Belief How a Humble Dutch Treat Launched Itself into the Global Snackosphere

#Dutch #Amsterdam #coffeeshops #SpaceCake #baked #gebak #THC #smoke #weed #cannabinoid #pharmacokinetics #SpaceBrownie #edibles #writingcommunity #5amwritersClub #6amwritersclub #amediting #wordcount #digitaldiary #amreading #WIPwarmup #shortstories #typewriters #writerslife #Justwrite 🖖

💊 Canagliflozin is a synthetic SGLT2i, it is the latest approved class of #medicine used in the treatment of type 2 #diabetes.

💊 This #Review article contains information about the #pharmacokinetics, #drug safety, and #efficacy profile of #canagliflozin.

💻 www.thieme-connect.com/products/ejo...