Discovery, Development, and Patent Trends on Molnupiravir: A Prospective Oral Treatment for COVID-19

The COVID-19 pandemic needs no introduction at present. Only a few treatments are available for this disease, including remdesivir and favipiravir. Accordingly, the pharmaceutical industry is striving to develop new treatments for COVID-19. Molnupiravir, an orally active RdRp inhibitor, is in a phase 3 clinical trial against COVID-19. The objective of this review article is to enlighten the researchers working on COVID-19 about the discovery, recent developments, and patents related to molnupiravir. Molnupiravir was originally developed for the treatment of influenza at Emory University, USA. However, this drug has also demonstrated activity against a variety of viruses, including SARS-CoV-2. Now it is being jointly developed by Emory University, Ridgeback Biotherapeutics, and Merck to treat COVID-19. The published clinical data indicate a good safety profile, tolerability, and oral bioavailability of molnupiravir in humans. The patient-compliant oral dosage form of molnupiravir may hit the market in the first or second quarter of 2022. The patent data of molnupiravir revealed its granted compound patent and process-related patent applications. We also anticipate patent filing related to oral dosage forms, inhalers, and a combination of molnupiravir with marketed drugs like remdesivir, favipiravir, and baricitinib. The current pandemic demands a patient compliant, safe, tolerable, and orally effective COVID-19 treatment. The authors believe that molnupiravir meets these requirements and is a breakthrough COVID-19 treatment.

Patentability challenges associated with emerging pharmaceutical technologies

According to the recent patent filing trends, it has been observed that certain pharmaceutical technologies are more popular than others and are commonly referred to as emerging technologies. The emerging technologies in the pharmaceutical sector include artificial intelligence, big data and certain advanced biological therapies such as personalized medicine and stem cell therapy. These trends have various applications in the medicine and healthcare industry. Since these technologies are relatively new and each of them is very unique in its own way, current patent laws are inadequate to deal with the complex challenges associated with them. A brief analysis of the challenges associated with these emerging technologies and their applications is discussed in this paper.

Current clinical trials and patent update on lung cancer: a retrospective review

Several clinical trials using different interventions are currently being sponsored to combat lung cancer at its different stages. The purpose of this study was to provide a portfolio of those trials. All active, open and recruiting clinical trials registered at ClinicalTrials.gov up to March 2018 were included. Information related to 6092 registered lung cancer trials was downloaded. Phase II trials were in the majority, comprising nearly 48.7% of total clinical trials with industry the major sponsor (41.3%) followed by NIH (12.3%). Multicenter studies were the norm accounting for 47.9% and the main study location was the USA (50.9%). Common interventions were radiation (26%), surgery (22%) and EGFR inhibitors (17%). Patent information includes major patent filing office and sponsors. The data analysis provides a comprehensive description of lung cancer trials.

Technological prospection of Diminazene Aceturate, an Angiotensin II Converting Enzyme activator, in front of diarrheic disorders

Diarrhea, which is a gastrointestinal disease, has as its main characteristic the rapid passage of gastric contents through the intestine, which leads to the loss of water and electrolytes and consequent dehydration. The most common fluid replacement is the use of oral rehydration solution (ORS) together with the use of the drug loperamide. However, the use of this medication can cause severe bacteremia followed by sepsis and even death. Currently, there is no effective pharmacological treatment for diarrhea, therefore, it is noted the importance of seeking new therapeutic targets for the treatment of this disease. Thus, the aim of the present study was to conduct a research on the biological activities already described for Diminazene Aceturate with a special focus on antidiarrheal agents. For this, a survey was carried out, through patent filing searches, in the USPTO, EPO, WIPO and INPI databases, using keywords and Boolean operators. Thus, it was found in the international patent databases the number of documents referring to the use of Diminazene Aceturate in several areas, mainly in the pharmaceutical industry, but with a relatively low number of documents regarding the description of possible antidiarrheal action of the compound under study , which reinforces the innovative character of research involving the use of Diminazene Aceturate as an antidiarrheal agent.

Technological Prospection of Oil Nanoparticles: Primary Characteristics and Profiles

Background: The search for technological applications for oils has been growing, largely due to their potential nutritional and economic applications. Encapsulation makes it possible to reduce the disadvantages of oils, such as physical instability or thermodynamics, or to improve their technological properties, enabling their use in various industrial areas. Nanoencapsulated oils have the potential to improve oil bioavailability and achieve controlled release and are able to target bioactive compounds with greater precision than microencapsulated oils. Objective: The present study aims to evaluate the primary characteristics and profiles of the technological prospection of oil nanoparticles. Results: Exponential growth in patent filing was noted with a peak in 2017, with China filing the highest numbers of patents. Regarding the area of application, the food industry was most common followed by the pharmaceutical industry. The most commonly used terms in patent documents on the subject were nanoemulsion and nanoparticle. The most commonly used oil, technique, wall materials and emulsifiers were soybean oil; emulsification; chitosan and lecithin; and Span 80, Tween 80 and Tween 40, respectively. The obtained articles were typically patent documents. The main depositor was Jiangnan University, and most inventors filed the same number of patent documents. Conclusion: Nanoencapsulation of oils has many known advantages that have been widely published in the literature and used by industry. There is a trend in the growth of patent document deposits and related scientific publications, indicating that many innovations have been made and highlighting the importance of oil nanoencapsulation.

Development Time and Patent Extension for Prescription Drugs in Canada: A Cohort Study

The Comprehensive Economic and Trade Agreement between Canada and the European Union provides for an extension of Canadian patents for prescription drugs by up to 2 years. One of the arguments advanced for longer patent time is to compensate companies for the length of the overall drug development time (the time between patent application and market approval). This study investigates overall development time in Canada for different groups of drugs approved between January 1, 2009 and December 31, 2018 and how many of these drugs are eligible for up to 2 years of patent term extension. Based on a list of patents and dates of market approval, the change in overall development time for all drugs was calculated along with whether there were differences in development time between different groups of drugs. Using Canadian patent filing dates, overall development time for all drugs went from a mean of 2240 days (95% CI: 1832, 2648) in 2009 to 4197 days (95% CI: 3728, 4665) in 2018 (analysis of variance [ANOVA], P<.0001). Using first global patent filing dates, overall development time went from a mean of 4481 days (95% CI: 3053, 5908) in 2009 to 6298 days (95% CI: 4839, 7756) in 2018 (ANOVA, P=.0118). There was a statistically significant difference in the overall development mean time between small molecule drugs (3553, 95% CI: 3361, 3746) and biologics (3903, 95% CI: 3595, 4212), (t test, P=.0487) when using Canadian patent filing dates but not when first global patent filing dates were used. There was no statistically significant change in overall development time among drugs that were substantial, moderate or little to none additional therapeutic value compared to existing drugs. Out of 238 drugs, 218 (91.6%) would have been eligible for patent term extension with 195 (80.7%) eligible for the full 2 years. Patent term extension does not appear to be justified based on changes in overall development time, except possibly in the case of biologics. There are also trade offs in terms of increased expenditures that need to be considered if patent terms are lengthened.