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Repositioning Antiviral Drugs as a Rapid and Cost-Effective Approach to Discover Treatment against SARS-CoV-2 Infection
Published in Hajiya Mairo Inuwa, Ifeoma Maureen Ezeonu, Charles Oluwaseun Adetunji, Emmanuel Olufemi Ekundayo, Abubakar Gidado, Abdulrazak B. Ibrahim, Benjamin Ewa Ubi, Medical Biotechnology, Biopharmaceutics, Forensic Science and Bioinformatics, 2022
Omotayo Opemipo Oyedara, Folasade Muibat Adeyemi, Charles Oluwaseun Adetunji, Temidayo Oluyomi Elufisan
Oseltamivir is an anti-influenza virus that inhibits the virus neuraminidase and thus affecting the release of viral particles. It was positioned as a good drug candidate against COVID-19 based on its ability to bind stably with SARS-CoV-2 main protease in combination with lopinavir and ritonavir, as revealed by an in silico study (Muralidharan et al. 2020). Moreover, combination of antibacterial and oseltamivir therapy, and early administration of oseltamivir was reported to reduce fever in COVID-19 patients without hypoxia (Chiba, 2020). It also hastened the recovery of COVID-19 patients with illnesses similar to influenza (Coenen et al. 2020). In an in vitro study, the inability of oseltamivir to exert inhibitory effects on SARS-CoV-2 or improve patients’ signs and symptoms was reported (Tan et al. 2020). Notwithstanding, oseltamivir is undergoing several clinical studies for use in COVID-19 treatment. Umifenovir blocks the entry of virus into the cell by preventing fusion of the virus with target membrane. It is a promising drug undergoing clinical trial for the treatment of COVID-19 disease.
Pulmonary complications of bone-marrow and stem-cell transplantation
Published in Philippe Camus, Edward C Rosenow, Drug-induced and Iatrogenic Respiratory Disease, 2010
Bekele Afessa, Andrew D Badley, Steve G Peters
Since severe disease is more likely to occur near the time of transplantation, the procedure should be delayed in patients with respiratory virus infection.32 Immunization with inactivated influenza is recommended. However, response to vaccine is lost for 6 months after transplant, and chronic GVHD is associated with poor response.32 Amantidine or rimantidine prophylaxis may be used to provide partial protection when influenza A activity is detected in the community.32 Although ribavirin is active in vitro against influenza A and B viruses, clinical data are not available.32 Treatment with amantadine or rimantadine is not of benefit if initiated after the development of respiratory failure.33 Oseltamivir may play a beneficial role for therapy and for prophylaxis following confirmed exposure to influenza A and B.34 Pneumonia in patients with influenza infection is associated with 50 per cent mortality.19
Biocatalysts: The Different Classes and Applications for Synthesis of APIs
Published in Peter Grunwald, Pharmaceutical Biocatalysis, 2019
An overview of chemoenzymatic routes to oseltamivir was given by Werner et al. (2011), who rely in part on using cyclohexadiene-cis-diol, derived enzymatically from benzene derivatives, using a toluene dioxygenase (Sullivan et al., 2009; see also Semak et al., 2012). The total synthesis requires 10 steps involving apart from the toluene DO-mediated dihydroxylation, a hetero-Diels–Alder cycloaddition, and the generation of C4 acetamido functionality. Oseltamivir—sold under the brand name Tamiflu—is an antiviral neuraminidase inhibitor used to treat or to prevent (primary or secondary prophylaxis) influenza A and influenza B. The benefit of this drug, however, is controversial; due to a Cochrane review (Jefferson et al., 2014), oseltamivir in the treatment of adults reduced the time to first alleviation of symptoms from 7 days to just 6.3 days compared with the control group and there was no difference in rates of admission to hospital. Vomiting, diarrhea and headache are common side effects. Similar results have been obtained for Zanamivir (Heneghan et al., 2014). According to a meta-analysis published in The Lancet (Dobson et al., 2015) with data from 4328 patients, the time to alleviation of all symptoms for oseltamivir versus placebo recipients is reduced from 122·7 to 97.5 h, and fewer lower respiratory tract complications requiring antibiotics were noted. A recent summary of the debate concerning the use of Oseltamivir for treating seasonal and pandemic influenza has been provided by Hurt and Kelly (2016).
Preliminary results on the uptake and biochemical response to water-exposure of Tamiflu® (oseltamivir phosphate) in two marine bivalves
Published in Journal of Toxicology and Environmental Health, Part A, 2019
Sara Dallarés, Nicola Montemurro, Sandra Pérez, Neus Rodríguez-Sanchez, Montserrat Solé
Tamiflu® is the commercial brand name for the antiviral agent oseltamivir phosphate (OST), which is mostly used for the pandemic treatment of influenza (Roche 2006). Tamiflu has also been indicated by the World Health Organization as the first-line defence in case of an avian influenza pandemic (WHO 2006). In humans, the ester prodrug OST is hydrolyzed by liver esterases to oseltamivir carboxylate (OST-C), which enters the environment through wastewater discharges (Hatfield et al. 2016). During peak influenza events, almost 100 µg/L concentration levels of OST might be attained in natural water systems, as estimated by Singer et al. (2007). In the case of OST-C, due to its low retention in sediments, concentrations over 20 µg/L in water bodies of highly populated catchments were predicted during these episodes (Bartels and von Tümpling 2008; Saccà et al. 2009). However, in field studies, lower concentrations of these compounds were found. Gonçalves et al. (2011) reported up to 100 ng/L OST and 50 ng/L OST-C in Spanish river waters during flu season, while Soderstrom et al. (2009) and Ghosh et al. (2010) quantified up to 58 and 293.3 ng/L OST-C, respectively, in Japan during a flu outbreak.
Emerging technologies for diagnostics and drug delivery in the fight against COVID-19 and other pandemics
Published in Expert Review of Medical Devices, 2020
Many of the drug molecules that are currently under investigation for the COVID-19 prevention or treatment can be manufactured as solid oral dosage forms using FDM 3DP by manufacturing tablets including animal shape medications that can be used for pediatrics or geriatrics. An example of a new oral drug that is under investigation called EIDD-2801 [12]. Moreover, oral drugs that are mainly used for the treatment of malaria or inflammatory conditions, such as hydroxychloroquine (HCQ) and chloroquine (CQ), are also under investigation with or without the combination of other drug molecules, for pre- or post-exposure prophylaxis or for the treatment of COVID-19. A clinical trial started in April 2020 in New York hospitals is testing, for the first time, the effectiveness of famotidine (an antacid drug for heartburn) to COVID-19 in combination with the HCQ. Researches have also tested the CQ diphosphate in combination with azithromycin (an antibiotic used to treat chest infections) and oseltamivir (an antiviral medication used to prevent and treat influenza A & B); however, they concluded that CQ can cause to some patients with a dose-dependent increase in heart abnormality [13]. Personalized dose-dependent DDS can be quickly manufactured by 3DP in hospitals per patient's needs and avoid such complications. In June 2020, a UK clinical trial study under the codename RECOVERY shows that low doses of the steroid drug dexamethasone (DM; a common and inexpensive drug that created in 1957) in hospitalized patients with COVID-19 reduced mortality by one-third among patients in serious condition. DM filaments can be prepared by hot-melt extrusion (HME) and formulations to be printed in accurate doses by FDM 3DP. For the successful manufacturing of DDSs by 3DP, it is very important to appropriate select materials and printing parameters, by firstly understanding the physicochemical properties of the individual drug molecules that are under investigation.
2D-QSAR, 3D-QSAR, molecular docking and ADMET prediction studies of some novel 2-((1H-indol-3-yl)thio)-N-phenyl-acetamide derivatives as anti-influenza A virus
Published in Egyptian Journal of Basic and Applied Sciences, 2022
Mustapha Abdullahi, Adamu Uzairu, Gideon Adamu Shallangwa, Paul Andrew Mamza, Muhammad Tukur Ibrahim
Influenza (A) virus (IAV) infection remains one of the major causes of mortality and morbidity due to respiratory diseases in recent times even with the devastating Covid-19 pandemic [1]. The World Health Organization (WHO) reported about 2–5 million cases of severe illness caused by the ravaging seasonal influenza virus epidemic which resulted in over 500,000 deaths globally [2]. These flu epidemics cause severe respiratory infections in children, adults, the elderly, and individuals with underlying health conditions [3] [4]. Influenza virus neuraminidase (NA) is an enzyme that catalyzes the obliteration of terminal sialic acid residues (sialidase) which aids in liberating new virions formed from the infected cells and circulating to infect the neighboring cells [5]. As such, the NA inhibition can defend the host from being infected and prevent its proliferation [1]. Due to the highly preserved active site structure of neuraminidase [6], it has become an attractive molecular target for the exploration and development of novel anti-influenza inhibitors. Presently, Zanamivir (Relenza™), oseltamivir (Tamiflu™), laninamivir octanoate (Inavir™), and peramivir (Rapivab™) are the four (4) approved neuraminidase inhibitors for influenza treatment [7]. The IAV disease is usually linked to severe symptoms because of the intense genetic diversity characterized by chromosomal mutation between avian and human viruses. Presently, the only two major classes of antiviral medicines against the influenza A virus are inhibitors of M2-ion channel (rimantadine and amantadine) and neuraminidase (zanamivir and oseltamivir) targets that fight against its spreading around the globe. However, most influenza A virus strains have become resistant to these drugs in recent times. There is a lot of concern for the advent of drug resistance effects resulting from the high variability of the influenza virus or respiratory syncytial virus (RSV) [5]. This is because a patient infected with either virus can manifest similar symptoms at an early stage. The discovery of some novel compounds of 2-((1 H-indol-3-yl)thio) acetamide as dual inhibitors against IAV and RSV is a huge milestone for the rapid therapy of these respiratory co-infections. Moreover, the trial and error approach applied in the development of new drugs has been seen to be very tedious, costly, and time-consuming [8].