Article
Chemistry, Medicinal
Xun Lv, Pengfei Wang, Chenning Li, Shuihong Cheng, Yuhai Bi, Xuebing Li
Summary: The conjugation of cholesterol to ZNV shows improved antiviral efficacy and can effectively protect mice from influenza virus infection. This new treatment has the potential for sustained therapeutic effects and provides an effective strategy for improving the pharmacokinetics and efficacy of other small-molecule therapeutics.
JOURNAL OF MEDICINAL CHEMISTRY
(2021)
Article
Chemistry, Organic
Chuanqi Duan, Weiyuan Liu, Siju Bi, Liang Chen, Jing Pan, Ting Zhou, Kuaile Lin, Weicheng Zhou
Summary: The synthesis and characterization of compounds 7c and 8d, the 4(R)-epimer impurities of zanamivir and laninamivir octanoate, were reported for the first time. Their structures were confirmed by NMR and MS and distinguished from their corresponding APIs by coupling constant in H-1 NMR and HPLC spectra. This work is of great significance for the analysis of drug-related substances in zanamivir and laninamivir octanoate.
JOURNAL OF HETEROCYCLIC CHEMISTRY
(2022)
Article
Infectious Diseases
Naoki Tani, Naoki Kawai, Hideyuki Ikematsu, Takuma Bando, Norio Iwaki, Yoshio Takasaki, Shizuo Shindo, Yong Chong, Seizaburo Kashiwagi
Summary: This study investigated the clinical effectiveness of the neuraminidase inhibitor laninamivir against circulating influenza viruses. The results showed that laninamivir remains clinically effective against all types/subtypes of influenza viruses, with no safety issues.
JOURNAL OF INFECTION AND CHEMOTHERAPY
(2022)
Article
Virology
Ju Hwan Jeong, Won-Suk Choi, Khristine Joy C. Antigua, Young Ki Choi, Elena A. Govorkova, Richard J. Webby, Yun Hee Baek, Min-Suk Song
Summary: The study identified 10 NA substitutions that conferred resistance to all four NAIs tested, while the remaining 26 substitutions showed susceptibility to at least one or more NAIs. The in vitro data predicted the in vivo behavior for a small selection, highlighting the importance of screening resistance markers in NA enzyme inhibition assays and animal models of AIV infections to understand the mechanism of antiviral resistance.
JOURNAL OF VIROLOGY
(2021)
Article
Medicine, General & Internal
Chihiro Suzuki, Tsuneaki Kenzaka
Summary: We report a case of ischemic enterocolitis caused by laninamivir, a rare but similar symptom following the administration of oseltamivir.
WORLD JOURNAL OF CLINICAL CASES
(2022)
Article
Biochemistry & Molecular Biology
Kathleen D. Engelman, Alan N. Engelman
Summary: HIV-1 is the causative agent of the AIDS pandemic, but effective vaccination strategies have yet to be developed. In contrast, small molecule inhibitors of HIV-1 enzymes have been developed to effectively block virus replication. In addition to oral medications, long-acting injectable HIV-1 enzyme inhibitors are being developed to address adherence issues.
Article
Pharmacology & Pharmacy
Kelong Han, Mark Baker, Mark Lovern, Prokash Paul, Yuan Xiong, Parul Patel, Katy P. Moore, Ciara S. Seal, Amy G. Cutrell, Ronald D. D'Amico, Paul D. Benn, Raphael J. Landovitz, Mark A. Marzinke, William R. Spreen, Susan L. Ford
Summary: A population pharmacokinetic model of cabotegravir was developed using data from phase 1, 2, and 3 studies. The model provides valuable information for dosing strategies and future study design. The study found that race and age were not significant covariates, while factors such as gender, injection method, and body mass index had an impact on pharmacokinetics.
BRITISH JOURNAL OF CLINICAL PHARMACOLOGY
(2022)
Article
Biochemistry & Molecular Biology
Bettina Sehnert, Juliane Mietz, Rita Rzepka, Stefanie Buchholz, Andrea Maul-Pavicic, Sandra Schaffer, Falk Nimmerjahn, Reinhard E. Voll
Summary: The study investigates the impact of neuraminidases on rheumatoid arthritis and suggests that neuraminidase inhibitors could serve as a promising therapeutic target for RA and other antibody-mediated autoimmune diseases.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2021)
Article
Pharmacology & Pharmacy
Petra Verdino, Stacey L. Lee, Fariba N. Cooper, Steven R. Cottle, Patrick F. Grealish, Charlie C. Hu, Catalina M. Meyer, Joanne Lin, Victoria Copeland, Gina Porter, Richard L. Schroeder, Tyran D. Thompson, Leah L. Porras, Asim Dey, Hong Y. Zhang, Emily C. Beebe, Scot J. Matkovich, Tamer Coskun, Aldona M. Balciunas, Andrea Ferrante, Robert Siegel, Laurent Malherbe, Nicoletta Bivi, Chad D. Paavola, Ryan J. Hansen, Matthew M. Abernathy, Sylvia O. Nwosu, Molly C. Carr, Josef G. Heuer, Xiaojun Wang
Summary: Chronic heart failure, especially in heart failure with preserved ejection fraction, lacks effective treatment options and poses a burden on patients and society. LY3540378, a long-acting relaxin analogue, has shown promising results in preclinical studies and is progressing in clinical trials, offering a potential therapeutic approach for chronic heart failure.
BRITISH JOURNAL OF PHARMACOLOGY
(2023)
Article
Chemistry, Medicinal
Benjamin R. Taft, Fumiaki Yokokawa, Tom Kirrane, Anne-Catherine Mata, Richard Huang, Nicole Blaquiere, Grace Waldron, Bin Zou, Oliver Simon, Subramanyam Vankadara, Wai Ling Chan, Mei Ding, Sandra Sim, Judith Straimer, Armand Guiguemde, Suresh B. Lakshminarayana, Jay Prakash Jain, Christophe Bodenreider, Christopher Thompson, Christian Lanshoeft, Wei Shu, Eric Fang, Jafri Qumber, Katherine Chan, Luying Pei, Yen-Liang Chen, Hanna Schulz, Jessie Lim, Siti Nurdiana Abas, Xiaoman Ang, Yugang Liu, Inigo Angulo-Barturen, Maria Belen Jimenez-Diaz, Francisco Javier Gamo, Benigno Crespo-Fernandez, Philip J. Rosenthal, Roland A. Cooper, Patrick Tumwebaze, Anna Caroline Campos Aguiar, Brice Campo, Simon Campbell, Jurgen Wagner, Thierry T. Diagana, Christopher Sarko
Summary: A highly potent antimalarial compound, INE963 (1), with favorable pharmacological properties, has been identified through high-throughput screening and shows potential for curing uncomplicated malaria.
JOURNAL OF MEDICINAL CHEMISTRY
(2022)
Review
Pharmacology & Pharmacy
Anil B. Jindal, Atharva R. Bhide, Sagar Salave, Dhwani Rana, Derajram Benival
Summary: The use of long-acting parenteral drug delivery systems is a promising approach to improve the treatment of chronic conditions. These systems utilize various technologies to deliver different drugs and have shown potential in the treatment of chronic infections and diseases such as HIV/AIDS, tuberculosis, and malaria. Factors such as drug properties, formulation type, and administration route play a crucial role in the development of long-acting formulations. Recent advances in the field, including long-acting nanoformulations and products in clinical trials, have also been highlighted.
ADVANCED DRUG DELIVERY REVIEWS
(2023)
Article
Reproductive Biology
Juan E. Romano, Andrea Barbarossa, Giampiero Pagliuca, Graciela B. Villadoniga, Teresa Gazzotti, Beatrice Mislei, Elisa Zironi, Gaetano Mari
Summary: The study found that oxytetracycline long-acting has appropriate pharmacokinetic properties for treating bulls' genital infections when indicated.
Review
Immunology
Jean B. Nachega, Kimberly K. Scarsi, Monica Gandhi, Rachel K. Scott, Lynne M. Mofenson, Moherndran Archary, Sharon Nachman, Eric Decloedt, Elvin H. Geng, Lindsay Wilson, Angeli Rawat, John W. Mellors
Summary: Intramuscular injection of long-acting cabotegravir and rilpivirine is a new, approved antiretroviral therapy (ART) combination for people living with HIV. It reduces dosing frequency to once every month or every 2 months injections. However, more data are needed to confirm its effectiveness and cost-effectiveness in different patient groups. Advocacy efforts and policy changes are needed to ensure equitable access to long-acting ART, especially in low-income and middle-income countries.
Article
Veterinary Sciences
Salah Uddin Ahmad, Jichao Sun, Fusheng Cheng, Bing Li, Safia Arbab, Xuzheng Zhou, Jiyu Zhang
Summary: The study compared the pharmacokinetics of four long-acting enrofloxacin injectable formulations in healthy pigs, finding significant differences in C-max, T-max, and AUC(all) among the formulations compared to the reference one. However, there were no significant differences in T-1/2. The tested formulations showed somewhat better pharmacokinetic parameters compared to the reference formulation.
FRONTIERS IN VETERINARY SCIENCE
(2021)
Article
Chemistry, Multidisciplinary
Go-Wun Choi, Sangno Lee, Dong Wook Kang, Ju Hee Kim, Hea-Young Cho
Summary: Novel formulations of DNP-loaded microspheres with a one-month duration of effect were developed to reduce dosing frequency and improve patient adherence. Various factors affecting drug release were studied, and animal models were used to optimize formulations and evaluate pharmacokinetic properties. The developed PK model was extrapolated to humans to show that a formulation with PLGA 7525A and a DPR of 1/9 could maintain drug concentration for a month with controlled initial burst release.
JOURNAL OF CONTROLLED RELEASE
(2021)