Article
Cell Biology
Tara Smith, Kaeli J. Knudsen, Shawn A. Ritchie
Summary: This study evaluated the pharmacokinetics, mass balance, and tissue distribution of PPI-1011, a synthetic plasmalogen precursor, in Sprague-Dawley rats. The results showed that oral administration of PPI-1011 resulted in high uptake across the body, including the brain. Repeated dosing increased the uptake, suggesting that it could be a viable therapeutic strategy for treating plasmalogen deficiencies.
FRONTIERS IN CELL AND DEVELOPMENTAL BIOLOGY
(2022)
Article
Pharmacology & Pharmacy
Lei He, Donglin Feng, Hui Guo, Yueyuan Zhou, Zhaozhao Li, Kuo Zhang, Wangqian Zhang, Shuning Wang, Zhaowei Wang, Qiang Hao, Cun Zhang, Yuan Gao, Jintao Gu, Yingqi Zhang, Weina Li, Meng Li
Summary: This study provides the first analysis of the pharmacokinetics of BPC157, showing linear pharmacokinetic characteristics in rats and beagle dogs. The main excretory pathways of BPC157 were found to be urine and bile. These findings are important for the clinical translation of BPC157.
FRONTIERS IN PHARMACOLOGY
(2022)
Article
Pharmacology & Pharmacy
Yvonne Fuell, Christian Wallasch, Ashley Hilton, Oliver Planz
Summary: This study reveals the absorption, distribution, metabolism, and excretion of Zapnometinib in rats. It has low absorption from the gastrointestinal tract, with most of it being excreted via feces. It is rapidly and widely distributed in circulatory and visceral tissues, but has low penetration into the brain.
FRONTIERS IN PHARMACOLOGY
(2022)
Article
Pharmacology & Pharmacy
Wei Yin, T. Eric Ballard, Sean Xiaochun Zhu, Samuel Hsiao, Hao Chen, Yuexian Li, Swapan K. Chowdhury, Annette Stevenson, Tom Hui, Allen Hunt, Mahnaz Asgharnejad, Steve Han
Summary: This study suggests that soticlestat and its metabolites are rapidly cleared and eliminated, reducing the risk of dose accumulation from repeated dosing and supporting further investigation of soticlestat.
BRITISH JOURNAL OF CLINICAL PHARMACOLOGY
(2023)
Article
Agriculture, Multidisciplinary
Lisha Wang, Zhi Wang, Tianji Xia, Fangrui Cao, Linhu Ye, Ruile Pan, Suwei Jin, Mingzhu Yan, Qi Chang
Summary: This study found that Cajaninstilbene acid (CSA) is primarily absorbed through passive transport and that metabolism is the major barrier limiting its oral bioavailability. Four new CSA metabolites were discovered in rats, mainly excreted through bile.
JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY
(2021)
Article
Pharmacology & Pharmacy
Chandrali Bhattacharya, Ann-Sofie Sandinge, Ryan A. Bragg, Maria Heijer, Jingjing Yan, Linda C. Andersson, Ulrik Jurva, Marta Pelay-Gimeno, Wouter H. J. Vaes, Rianne A. F. de Ligt, Malin Granfors, Carl Amilon, Eva-Lotte Lindstedt, Somasekhara R. Menakuru, Pavlo Garkaviy, Lars Weidolf, V. Sashi Gopaul
Summary: This study evaluated the mass balance and disposition of a novel myeloperoxidase inhibitor, AZD4831, in healthy participants using a C-14-labeled microtracer coupled with analysis by accelerator mass spectrometry. The results showed that AZD4831 was rapidly absorbed and eliminated via metabolism and renal excretion, with a long half-life of 52 hours. The study also demonstrated high absorption and good tolerability of AZD4831.
DRUG METABOLISM AND DISPOSITION
(2023)
Review
Chemistry, Medicinal
Vaclav Tvrdy, Jana Pourova, Eduard Jirkovsky, Vladimir Kren, Katerina Valentova, Premysl Mladenka
Summary: Silymarin, extracted from the seeds of Silybum marianum, contains flavonolignans and flavonoids and is used as a hepatoprotective agent. However, its low oral bioavailability and potential drug interactions have sparked debates. The main reasons for poor systemic oral bioavailability are rapid conjugation and efflux of flavonolignans, with most human studies showing no interactions with other drugs.
MEDICINAL RESEARCH REVIEWS
(2021)
Article
Chemistry, Medicinal
Srirajan Vaidyanathan, Aimee Reed
Summary: The long-lived radionuclides tritium and carbon-14 have been extensively used in pharmaceutical research and development for making key decisions regarding efficacy, toxicity, compound selection, safety evaluation, and human metabolism studies.
ACS MEDICINAL CHEMISTRY LETTERS
(2022)
Review
Environmental Sciences
Per Ola Darnerud, Ake Bergman
Summary: Even though chlorinated paraffins (CPs) have been discussed as an emerging issue recently, our understanding of their chemical fate in organisms is still incomplete. This review critically compiles existing knowledge on the ADME of CPs in biota and identifies research needs. CPs are effectively absorbed from the GI tract and possibly from the lungs, and are transported to various organs. They are metabolized in the liver and excreted mainly via bile and feces. However, the metabolic transformations of CPs are poorly studied and no complete metabolic scheme has been proposed.
ENVIRONMENT INTERNATIONAL
(2022)
Article
Agriculture, Multidisciplinary
Xiaomei Huang, Zefeng Cui, Chenhong Ding, Qiuquan Su, Xuexian Lin, Weili Wang, Qiumiao Yin, Xu Wang
Summary: Long-chain chlorinated paraffins (LCCPs) are of lesser concern in food due to lower accumulation in most organisms, but are shown to accumulate preferentially in birds. The absorption of CPs is minimally impacted by carbon chain length, with longer chain CPs accumulating preferentially in muscle and adipose tissues. The metabolic elimination rates of CPs vary depending on chain length, with C12Cl6 being the most efficiently eliminated.
JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY
(2021)
Review
Pharmacology & Pharmacy
Elka S. Waller, Ben J. Yardeny, Wan Yun Fong, Xue Yi Gan, Stephen V. Jimenez, Yijun Pan, Joshua H. Abasszade, Joseph A. Nicolazzo
Summary: Alzheimer's disease not only affects the neurological system but may also have an impact on other non-neurological systems, affecting the metabolism and excretion of drugs. Therefore, dosage adjustments may be necessary to ensure optimal pharmacotherapy for individuals with Alzheimer's disease.
ADVANCED DRUG DELIVERY REVIEWS
(2022)
Review
Chemistry, Medicinal
Simone Donati, Francesca Marini, Francesca Giusti, Gaia Palmini, Cinzia Aurilia, Irene Falsetti, Teresa Iantomasi, Maria Luisa Brandi
Summary: Vitamin D deficiency is a global health problem with negative consequences on musculoskeletal and extra-skeletal health. Increasing intake of vitamin D fortified foods and administering vitamin D supplementation, such as vitamin D3 or calcifediol, can help improve vitamin D status. This review discusses the potential medical benefits and specific clinical scenarios in which oral intake of calcifediol could be effective in restoring optimal serum levels of 25(OH)D3. Insights into calcifediol-related non-genomic responses are provided, suggesting its use as a supplement for individuals at higher risk of hypovitaminosis D.
Review
Medicine, Research & Experimental
Anuradha Ramamoorthy, Girish Bende, Edwin Chiu Yuen Chow, Hristina Dimova, Neil Hartman, Daphney Jean, Sonia Pahwa, Yunzhao Ren, Chinmay Shukla, Yuching Yang, Suresh Doddapaneni, Zhixia Yan Danielsen
Summary: Human radiolabeled mass balance studies are crucial in understanding the pharmacokinetic characteristics of drugs and informing drug development programs. A survey of FDA-approved new drug applications revealed that a significant percentage of drugs relied on findings from these studies. Most of the studies were conducted in healthy male volunteers using the final route of administration and a fit-for-purpose radiolabeled formulation.
CTS-CLINICAL AND TRANSLATIONAL SCIENCE
(2022)
Review
Medicine, Research & Experimental
Mahsa Bagheri, Cornelus F. van Nostrum, Robbert Jan Kok, Gert Storm, Wim E. Hennink, Michal Heger
Summary: This review investigates whether intravenous nanoformulations of curcumin improve its pharmacokinetics and whether improved pharmacokinetics leads to greater therapeutic efficacy. The study found that nanoencapsulation generally improved curcumin's pharmacokinetics, but the correlation between pharmacokinetics and pharmacodynamics was not significant.
MOLECULAR PHARMACEUTICS
(2022)
Article
Microbiology
Vipul K. Gupta, Gary Maier, Leanne Gasink, Amanda Ek, Mary Fudeman, Praveen Srivastava, Angela Talley
Summary: Tebipenem pivoxil hydrobromide (TBP-PI-HBr) is an oral prodrug of tebipenem (TBP), which is effective against multidrug-resistant Gram-negative pathogens. The prodrug is converted to the active moiety TBP in the gastrointestinal tract. The main clearance pathways for elimination are through urine and feces, with TBP and its ring-open metabolite LJC 11562 being the major circulating metabolites in plasma.
ANTIMICROBIAL AGENTS AND CHEMOTHERAPY
(2023)