Article
Pharmacology & Pharmacy
Washim Khan, Yan-Hong Wang, Narayan D. D. Chaurasiya, N. P. Dhammika Nanayakkara, H. M. Bandara Herath, Kerri A. A. Harrison, Gray Dale, Donald A. A. Stanford, Eric P. P. Dahl, James D. D. McChesney, Waseem Gul, Mahmoud A. A. ElSohly, David Jollow, Babu L. L. Tekwani, Larry A. A. Walker
Summary: Primaquine (PQ) is an effective antimalarial drug used to treat dormant Plasmodium vivax hypnozoites and P. falciparum mature gametocytes. This study compared the tolerability and metabolism of PQ enantiomers in human volunteers and found no significant differences in safety and tolerability in G6PDn subjects.
FRONTIERS IN PHARMACOLOGY
(2023)
Article
Pharmacology & Pharmacy
Woo-Yul Lee, Dong-Woo Chae, Choon-Ok Kim, Sang-Eun Lee, Yee-Gyung Kwak, Joon-Sup Yeom, Kyung-Soo Park
Summary: The study aimed to develop a population pharmacokinetic model of primaquine and its metabolite, and found that body weight and CYP2D6 activity significantly impact primaquine pharmacokinetics. The results showed that weight and enzyme activity play crucial roles in drug metabolism and can influence drug exposure levels.
Article
Pharmacology & Pharmacy
Josefine Schulz, Antonia Thomas, Ayatallah Saleh, Gerd Mikus, Charlotte Kloft, Robin Michelet
Summary: This study quantitatively evaluated the metabolism and inhibition properties of voriconazole, a small-molecule drug with complex metabolism. The findings contribute to the understanding of voriconazole's pharmacokinetics and provide a basis for optimized treatment.
Article
Medicine, Research & Experimental
Michael Poppe, Christian Clodi, Christoph Schriefl, Matthias Mueller, Raute Sunder-Plassmann, Birgit Reiter, Maximilian Rechenmacher, Wisse van Os, J. G. Coen van Hasselt, Michael Holzer, Harald Herkner, Michael Schwameis, Bernd Jilma, Christian Schoergenhofer, Christoph Weiser
Summary: This study compared the pharmacokinetics of pantoprazole at different stages of targeted temperature management following cardiac arrest. Results showed that CYP2C19-dependent drug metabolism is downregulated during targeted temperature management, which may impact drug choice and dosing of similarly metabolized drugs.
BIOMEDICINE & PHARMACOTHERAPY
(2022)
Article
Pharmacology & Pharmacy
Lara Marques, Nuno Vale
Summary: Drug-drug interactions (DDIs) are a significant concern, especially for patients undergoing polytherapy. This study investigated the interaction between salbutamol and fluvoxamine through in silico approaches. The results showed that co-administering salbutamol with fluvoxamine increased salbutamol exposure, particularly at higher fluvoxamine dosages.
Article
Medicine, General & Internal
Sofia Cussotto, Jacinta Walsh, Anna V. Golubeva, Alexander V. Zhdanov, Conall R. Strain, Fiona Fouhy, Catherine Stanton, Timothy G. Dinan, Niall P. Hyland, Gerard Clarke, John F. Cryan, Brendan T. Grif
Summary: The study found that the oral bioavailability of olanzapine significantly increased in rats with antibiotic-induced depletion of gut microbiota, while the bioavailability of risperidone remained unchanged. Changes in the gut microbiome may influence the pharmacokinetics of olanzapine, with the relative abundance of Alistipes significantly correlated with the AUC of olanzapine.
Article
Pharmacology & Pharmacy
Daphne Vassiliou, Eliane Sardh, Pauline Harper, Amy R. Simon, Valerie A. Clausen, Nader Najafian, Gabriel J. Robbie, Sagar Agarwal
Summary: Givosiran, an RNA interference therapy for acute hepatic porphyria, has minimal impact on CYP enzymes in the liver, with study results showing little effect on heme-dependent CYP enzyme activity.
CLINICAL PHARMACOLOGY & THERAPEUTICS
(2021)
Article
Pharmacology & Pharmacy
Dhruvitkumar S. Sutaria, Grozdana Rasuo, Adam Harris, Ryan Johnson, Dale Miles, Jorge Daniel Gallo, Rucha Sane
Summary: This study evaluated the pharmacokinetics, safety, and tolerability of Ipatasertib and Daholutamide in patients with metastatic castration-resistant prostate cancer. The results showed a mild reduction in the exposure of Ipatasertib when administered in combination with Daholutamide, which was not clinically significant. Additionally, the combination therapy was well-tolerated with minimal side effects in patients.
Review
Biochemistry & Molecular Biology
Habibeh Mashayekhi-Sardoo, Adeleh Mashayekhi-Sardoo, Basil D. Roufogalis, Tannaz Jamialahmadi, Amirhossein Sahebkar
Summary: The review collects and summarizes clinical and preclinical studies of curcumin interactions, focusing on its effects on CYP450 enzymes and interactions with toxicants and drugs. Results show significant inhibition of CYP450 enzymes by curcumin and its analogs, but effects vary when combined with toxicants and drugs. Herb-drug interactions should be considered when consuming curcumin and its analogs.
CURRENT MEDICINAL CHEMISTRY
(2021)
Article
Microbiology
Pattaraporn Vanachayangkul, Darapiseth Sea, Mariusz Wojnarski, Somethy Sok, Chanikarn Kodchakorn, Winita Ta-Aksorn, Sohei Hom, Mali Ittiverakul, Worachet Kuntawunginn, Montri Arsanok, Nillawan Buathong, Thay Kheang Heng, Kong Nareth, Samon Nou, Sok Chandara, Sokna Ly, Pheaktra Oung, Brian Vesely, Jason Bennett, Gregory Reichard, Brandon Pybus, Charlotte Lanteri, David Saunders, Mark Fukuda, Philip Smith, Lek Dysoley, Huy Rekol, Norman C. Waters, Michele Spring
Summary: The active metabolites of primaquine, especially 5-hydroxyprimaquine, are produced through the hepatic CYP450 2D6 enzymatic pathway. This study found that the CYP2D6 *10 reduced activity allele was present in 57% of volunteers, and there were differences in primaquine metabolism between Normal Metabolizers and Intermediate Metabolizers. Future research may reveal the relationship between urine 5,6-orthoquinone levels and primaquine radical cure efficacy.
ANTIMICROBIAL AGENTS AND CHEMOTHERAPY
(2022)
Article
Pharmacology & Pharmacy
Li Wang, Fan Wu, Jia Xu, Yu Wang, Weidong Fei, Hui Jiang, Peiwu Geng, Quan Zhou, Shuanghu Wang, Yongquan Zheng, Huadong Deng
Summary: Drug-drug interactions (DDIs) between pyrotinib and azole antifungal drugs were studied to evaluate their effects on the pharmacokinetics of pyrotinib. The in vitro experiments showed that ketoconazole and fluconazole could significantly decrease the clearance rate of pyrotinib, while itraconazole had no impact. In vivo studies further confirmed that coadministration with ketoconazole or fluconazole resulted in increased plasma concentration and decreased clearance rate of pyrotinib.
FRONTIERS IN PHARMACOLOGY
(2022)
Review
Pharmacology & Pharmacy
Guilherme Suarez-Kurtz
Summary: Plasmodium vivax is the most widespread human malaria parasite requiring hypnozoiticide therapy for radical cure. Studies have shown the crucial role of CYP2D6 in the efficacy of primaquine and tafenoquine. Patients with decreased CYP2D6 activity may have higher relapse rates with primaquine, while tafenoquine shows less dependence on CYP2D6 activity. Additional studies with more representation of poor CYP2D6 metabolizers are needed for tafenoquine efficacy evaluation.
CLINICAL PHARMACOLOGY & THERAPEUTICS
(2021)
Article
Biology
Sarah Charnaud, Jacob E. Munro, Lucie Semenec, Ramin Mazhari, Jessica Brewster, Caitlin Bourke, Shazia Ruybal-Pesantez, Robert James, Dulcie Lautu-Gumal, Harin Karunajeewa, Ivo Mueller, Melanie Bahlo
Summary: The CYP2D6 enzyme is responsible for metabolizing 25% of commonly used pharmaceuticals and its gene typing is of great interest in pharmacogenetics due to its polymorphic nature. Accurate allele typing of the CYP2D6 gene has been challenging due to copy number variants and pseudogenes. This study presents a robust data processing pipeline called PLASTER for accurate allele typing using long-read sequencing. This pharmacogenetic method has the potential to improve drug safety and efficacy through screening prior to drug administration.
COMMUNICATIONS BIOLOGY
(2022)
Article
Chemistry, Medicinal
Atsuko Tomaru, Kota Toshimoto, Wooin Lee, Keiko Ishigame, Yuichi Sugiyama
Summary: This study proposed a method to identify oral drugs with potential nonlinear pharmacokinetics and developed a decision tree for early drug candidate screening based on experimental and data analysis.
JOURNAL OF PHARMACEUTICAL SCIENCES
(2021)
Article
Medical Laboratory Technology
Roos Achterbergh, Laureen A. Lammers, Heinz-Josef Klumpen, Ron A. A. Mathot, Johannes A. Romijn
Summary: This study found that a short-term, hypercaloric, high-fat diet increases the plasma levels of acetaminophen metabolites formed by the oxidation pathway, which may increase the risk of hepatotoxicity.
THERAPEUTIC DRUG MONITORING
(2022)
Article
Chemistry, Medicinal
Natasa Terzic, Jelena Konstantinovic, Miklos Tot, Jovana Burojevic, Olgica Djurkovic-Djakovic, Jelena Srbljanovic, Tijana Stajner, Tatjana Verbic, Mario Zlatovic, Marta Machado, Ines S. Albuquerque, Miguel Prudencio, Richard J. Sciotii, Stevan Pecic, Sarah D'Alessandro, Donatella Taramelli, Bogdan A. Solaja
JOURNAL OF MEDICINAL CHEMISTRY
(2016)
Article
Chemistry, Medicinal
Jennifer L. Woodring, Kelly A. Boehmchin, Kimberly G. Brady, Mitchell F. Gallerstein, Jessey Erath, Scott Tanghe, Susan E. Leed, Ana Rodriguez, Kojo Mensa-Wilmot, Richard J. Sciotti, Michael P. Pollastri
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2017)
Article
Biochemistry & Molecular Biology
Jelena Konstantinovic, Milica Videnovic, Jelena Srbljanovic, Olgica Djurkovic-Djakovic, Katarina Bogojevic, Richard Sciotti, Bogdan Solaja
Article
Chemistry, Medicinal
William Devine, Sarah M. Thomas, Jessey Erath, Kelly A. Bachovchin, Patricia J. Lee, Susan E. Leed, Ana Rodriguez, Richard J. Sciotti, Kojo Mensa-Wilmot, Michael P. Pollastri
ACS MEDICINAL CHEMISTRY LETTERS
(2017)
Article
Chemistry, Medicinal
Lisa Frueh, Yuexin Li, Michael W. Mather, Qigui Li, Sovitj Pou, Aaron Nilsen, Rolf W. Winter, Isaac P. Forquer, April M. Pershing, Lisa H. Xie, Martin J. Smilkstein, Diana Caridha, Dennis R. Koop, Robert F. Campbell, Richard J. Sciotti, Mara Kreishman-Deitrick, Jane X. Kelly, Brian Vesely, Akhil B. Vaidya, Michael K. Riscoe
ACS INFECTIOUS DISEASES
(2017)
Article
Chemistry, Medicinal
Naimee Mehta, Lori Ferrins, Susan E. Leed, Richard J. Sciotti, Michael P. Pollastri
ACS INFECTIOUS DISEASES
(2018)
Article
Chemistry, Medicinal
Jennifer L. Woodring, Ranjan Behera, Amrita Sharma, Justin Wiedeman, Gautam Patel, Baljinder Singh, Paul Guyett, Emanuele Amata, Jessey Erath, Norma Roncal, Erica Penn, Susan E. Leed, Ana Rodriguez, Richard J. Sciotti, Kojo Mensa-Wilmot, Michael P. Pollastri
ACS MEDICINAL CHEMISTRY LETTERS
(2018)
Article
Chemistry, Medicinal
Kelly A. Bachoychin, Amrita Sharma, Seema Bag, Dana M. Klug, Katherine M. Schneider, Baljinder Singh, Hitesh B. Jalani, Melissa J. Buskes, Naimee Mehta, Scott Tanghe, Jeremiah D. Momper, Richard J. Sciotti, Ana Rodriguez, Kojo Mensa-Wilmot, Michael P. Pollastri, Lori Ferrins
JOURNAL OF MEDICINAL CHEMISTRY
(2019)
Article
Infectious Diseases
Lori Ferrins, Amrita Sharma, Sarah M. Thomas, Naimee Mehta, Jessey Erath, Scott Tanghe, Susan E. Leed, Ana Rodriguez, Kojo Mensa-Wilmot, Richard J. Sciotti, Kirsten Gillingwater, Michael P. Pollastri
PLOS NEGLECTED TROPICAL DISEASES
(2018)
Article
Immunology
Yu-Shan Cheng, Wei Sun, Miao Xu, Min Shen, Mozna Khraiwesh, Richard J. Sciotti, Wei Zheng
FRONTIERS IN CELLULAR AND INFECTION MICROBIOLOGY
(2019)
Article
Chemistry, Medicinal
Rozalia A. Dodean, Papireddy Kancharla, Yuexin Li, Victor Melendez, Lisa Read, Charles E. Bane, Brian Vesely, Mara Kreishman-Deitrick, Chad Black, Qigui Li, Richard J. Sciotti, Raul Olmeda, Thu-Lan Luong, Heather Gaona, Brittney Potter, Jason Sousa, Sean Marcsisin, Diana Caridha, Lisa Xie, Chau Vuong, Qiang Zeng, Jing Zhang, Ping Zhang, Hsiuling Lin, Kirk Butler, Norma Roncal, Lacy Gaynor-Ohnstad, Susan E. Leed, Christina Nolan, Stephanie J. Huezo, Stephanie A. Rasmussen, Melissa T. Stephens, John C. Tan, Roland A. Cooper, Martin J. Smilkstein, Sovitj Pou, Rolf W. Winter, Michael K. Riscoe, Jane X. Kelly
JOURNAL OF MEDICINAL CHEMISTRY
(2019)
Article
Infectious Diseases
Diana Caridha, Mark Hickman, Lisa Xie, Franklyn Ngundam, Erin Milner, Amanda Schenk, Kirk Butler, Dylan Nugent, Patricia Lee, Norma Roncal, Susan Leed, Eve Hosford, Jangwoo Lee, Richard J. Sciotti, Gregory Reichard, Chad Black, Mara Kreishman-Deitrick, Qigui Li, Brian Vesely
Article
Parasitology
Katrien Van Bocxlaer, Diana Caridha, Chad Black, Brian Vesely, Susan Leed, Richard J. Sciotti, Gert-Jan Wijnant, Vanessa Yardley, Stephanie Braillard, Charles E. Mowbray, Jean-Robert Ioset, Simon L. Croft
INTERNATIONAL JOURNAL FOR PARASITOLOGY-DRUGS AND DRUG RESISTANCE
(2019)
Article
Chemistry, Medicinal
Diana Caridha, Richard J. Sciotti, Jason Sousa, Brian Vesely, Tesfaye Teshome, Gustave Bonkoungou, Chau Vuong, Susan Leed, Mozna Khraiwesh, Erica Penn, Mara Kreishman-Deitrick, Patricia Lee, Brandon Pybus, John S. Lazo, Elizabeth R. Sharlow
Summary: The study identified tretazicar as a potent inhibitor of Leishmania parasite viability and showed that it could suppress CL lesion formation in BALB/c mice completely and for an extended period. Oral administration of tretazicar also effectively healed the majority of existing L. major cutaneous lesions. In drug combination studies, a strong synergistic effect was observed when subtherapeutic doses of tretazicar and liposomal amphotericin B were administered simultaneously, resulting in faster reduction of lesion size and prolonged lesion-free period in mice.
ACS INFECTIOUS DISEASES
(2021)
Article
Microbiology
Diana Caridha, Sandi Parriot, Thomas H. Hudson, Thierry Lang, Franklyn Ngundam, Susan Leed, Jenell Sena, Michael Harris, Michael O'Neil, Richard Sciotti, Lisa Read, Herve Lecoeur, Mark Hickman, Max Grogl
ANTIMICROBIAL AGENTS AND CHEMOTHERAPY
(2017)