Tegoprazan as a New Remedy for Gastrointestinal Diseases in Comparison with its Therapeutic Predecessors: A Mini-Review.

BACKGROUND: Potassium-competitive acid blockers (P-CABs), such as tegoprazan, are a new and diverse class of drugs that can completely block the potassium-binding site of gastric H+/K+ ATPase, potentially overcoming the limitations of proton-pump inhibitors (PPIs). A number of studies have compared the effectiveness as well as the safety profile of tegoprazan to PPIs and other P-CABs for the treatment of gastrointestinal diseases. OBJECTIVE: The current review study evaluates the published works of literature related to clinical pharmacology and clinical trials of tegoprazan for the treatment of diseases related to the gastrointestinal tract. CONCLUSION: The findings of this study revealed that tegoprazan is safe and well-tolerated and can be used to treat a group of gastrointestinal diseases, including gastroesophageal reflux disease (GERD), non-erosive reflux disease (NERD), and H. pylori infection.

A Review on Expression, Pathological Roles, and Inhibition of TMPRSS2, the Serine Protease Responsible for SARS-CoV-2 Spike Protein Activation.

SARS-CoV-2, the coronavirus responsible for the COVID-19 pandemic, uses the host cell membrane receptor angiotensin-converting enzyme 2 (ACE2) for anchoring its spike protein, and the subsequent membrane fusion process is facilitated by host membrane proteases. Recent studies have shown that transmembrane serine protease 2 (TMPRSS2), a protease known for similar role in previous coronavirus infections, severe acute respiratory syndrome (SARS), and Middle East respiratory syndrome (MERS), is responsible for the proteolytic cleavage of the SARS-CoV-2 spike protein, enabling host cell fusion of the virus. TMPRSS2 is known to be expressed in the epithelial cells of different sites including gastrointestinal, respiratory, and genitourinary system. The infection site of the SARS-CoV-2 correlates with the coexpression sites of ACE2 and TMPRSS2. Besides, age-, sex-, and comorbidity-associated variation in infection rate correlates with the expression rate of TMPRSS2 in those groups. These findings provide valid reasons for the assumption that inhibiting TMPRSS2 can have a beneficial effect in reducing the cellular entry of the virus, ultimately affecting the infection rate and case severity. Several drug development studies are going on to develop potential inhibitors of the protease, using both conventional and computational approaches. Complete understanding of the biological roles of TMPRSS2 is necessary before such therapies are applied.

Formulation Development of Nifedipine through Nanotechnology: A Comprehensive Review.

BACKGROUND: The therapeutic use of nifedipine, a dihydropyridine calcium channel blocker, is limited due to its poor solubility profile, rapid onset of its action, stability profile and short biological half-life. Many formulation techniques have been applied to improve physicochemical and pharmacological properties of the drug. OBJECTIVE: The objective of the study is to summarize the nanotechnology approaches made to improve the therapeutic and pharmacokinetic properties of nifedipine till 2020. METHODS: The searches for the related articles were done up to 28 March 2020 with the specific keywords in Pubmed and Google Scholar excluding review articles. RESULTS: The discussion showed that among the nano-carriers used to improve the pharmacological property of the drug, lipid nanoparticles, polymeric nanoparticles, crystalline nanoparticles, and nano-emulsions were prevalent. Nanotechnology has been efficient to improve the solubility profile of nifedipine, achieve sustained and controlled release by achieving targeted and local delivery and transdermal drug delivery. Exploiting nano-formulations, new windows of therapeutic applications have been achieved. Finally, micelle media, polymeric nanoparticles, and microcrystalline nanoparticles have been used to develop a photostable formulation. CONCLUSION: The technological innovations in the field of nanomedicine have paved many ways for the delivery of nifedipine and such sparingly water-soluble compounds.

COVID-19 Outbreak: Pathogenesis, Current Therapies, and Potentials for Future Management.

At the end of 2019, a novel coronavirus (CoV) was found at the seafood market of Hubei province in Wuhan, China, and this virus was officially named coronavirus diseases 2019 (COVID-19) by World Health Organization (WHO). COVID-19 is mainly characterized by severe acute respiratory syndrome coronavirus-2 (SARS-CoV2) and creates public health concerns as well as significant threats to the economy around the world. Unfortunately, the pathogenesis of COVID-19 is unclear and there is no effective treatment of this newly life-threatening and devastating virus. Therefore, it is crucial to search for alternative methods that alleviate or inhibit the spread of COVID-19. In this review, we try to find out the etiology, epidemiology, symptoms as well as transmissions of this novel virus. We also summarize therapeutic interventions and suggest antiviral treatments, immune-enhancing candidates, general supplements, and CoV specific treatments that control replication and reproduction of SARS-CoV and Middle East respiratory syndrome coronavirus (MERS-CoV).