Proceedings of the National Academy of Sciences of the Un... Mahoney M, Damalanka VC et. al.
Oct 13th, 2021 - The host cell serine protease TMPRSS2 is an attractive therapeutic target for COVID-19 drug discovery. This protease activates the Spike protein of severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) and of other coronaviruses and is essential for viral spread in the lung. Utilizing rational structure-based drug design (SBDD) coupled to substrate specificity screening of TMPRSS2, we ha...
Medicine Suzuki H, Tamaki T et. al.
Oct 9th, 2021 - The purpose of the present study is to investigate whether the 18F-fluorodeoxyglucose (18F-FDG) uptake parameter is related to survival outcomes for patients with clinical T3-T4a laryngeal cancer with various definitive treatments including total laryngectomy (TL). Parameters of 18F-FDG uptake in the primary tumors of 46 cases which were assessed by positron emission tomography with computed to...
The Medical Letter on Drugs and Therapeutics;
Sep 21st, 2021 - In brief: Risdiplam (Evrysdi) for spinal muscular atrophy.|2021||pharmacokinetics,therapeutic use,methods,drug therapy,epidemiology,metabolism,pharmacokinetics,therapeutic use,pharmacokinetics,therapeutic use,
The Medical Letter on Drugs and Therapeutics;
Sep 21st, 2021 - Berotralstat (Orladeyo) for prevention of hereditary angioedema.|2021||epidemiology,metabolism,prevention & control,methods,antagonists & inhibitors,metabolism,pharmacokinetics,therapeutic use,pharmacokinetics,therapeutic use,
The Medical Letter on Drugs and Therapeutics;
Sep 21st, 2021 - Voclosporin (Lupkynis) for lupus nephritis.|2021||administration & dosage,pharmacokinetics,methods,administration & dosage,pharmacokinetics,drug therapy,epidemiology,metabolism,drug therapy,epidemiology,metabolism,drug effects,metabolism,
Medicine Wang D, Li Y et. al.
Sep 4th, 2021 - The aim of this study was to retrospectively analyze 18F-FDG positron emission tomography/computed tomography (18F-FDG PET/CT) metabolic variables, programmed death-ligand 1 (PD-L1) and phosphorylated signal transducer and activator of transcription 3 (p-STAT3) tumor expression, and other factors as predictors of disease-free survival (DFS) in patients with lung adenocarcinoma (LUAD) (stage IA-...
Nature Communications; Wittwer K, Anderson DE et. al.
Sep 4th, 2021 - Measles virus (MeV) is a highly contagious pathogen that enters the human host via the respiratory route. Besides acute pathologies including fever, cough and the characteristic measles rash, the infection of lymphocytes leads to substantial immunosuppression that can exacerbate the outcome of infections with additional pathogens. Despite the availability of effective vaccine prophylaxis, measl...
The Lancet. Neurology; Reich DS, Arnold DL et. al.
Aug 22nd, 2021 - Tolebrutinib is an oral, CNS-penetrant, irreversible inhibitor of Bruton's tyrosine kinase, an enzyme expressed in B lymphocytes and myeloid cells including microglia, which are major drivers of inflammation in multiple sclerosis. We aimed to determine the dose-response relationship between tolebrutinib and the reduction in new active brain MRI lesions in patients with relapsing multiple sclero...
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International Journal of Hematology; Kawano N, Kimura S et. al.
Aug 19th, 2021 - Although tyrosine kinase inhibitors (TKIs) play a crucial role in the treatment of chronic myeloid leukemia (CML) and Philadelphia chromosome-positive acute lymphoblastic leukemia (Ph + ALL), intolerance and resistance to TKIs have been serious problems. Due to a lack of research, the importance of the pharmacokinetics (PK) of TKIs is currently unclear. We examined the PK of the third-generatio...
Undersea & Hyperbaric Medicine : Journal of the Undersea ... Lamers J, MacLaughlin K et. al.
Aug 15th, 2021 - Sudden decompression can result in bubble formation as the result of nitrogen gas (N2) dissolved in tissue during disabled submarine escape (DISSUB). This may cause dysbaric osteonecrosis (DON), a condition in long bones where bubbles in fatty marrow result in ischemia and necrosis. Previous research has shown that oxygen (O2) pre-breathe of two hours resulted in a reduction of DON; however, ef...
Drug Design, Development and Therapy; Gatti M, Andreoni M et. al.
Aug 12th, 2021 - Dalbavancin is a novel, long-acting lipoglycopeptide characterized by a long elimination half-life coupled with excellent in vitro activity against multidrug-resistant Gram-positives. Although it is currently approved only for the treatment of acute bacterial skin and skin structure infections, an ever-growing amount of evidence supports the efficacy of dalbavancin as a long-term therapy in ost...
The New England Journal of Medicine; Gaudinski MR, Berkowitz NM et. al.
Aug 12th, 2021 - Additional interventions are needed to reduce the morbidity and mortality caused by malaria. We conducted a two-part, phase 1 clinical trial to assess the safety and pharmacokinetics of CIS43LS, an antimalarial monoclonal antibody with an extended half-life, and its efficacy against infection with Plasmodium falciparum. Part A of the trial assessed the safety, initial side-effect profile, and p...
Drugs in R&D; Rajpoot S, Ohishi T et. al.
Jul 30th, 2021 - Coronavirus disease 2019 is a novel disease caused by the severe acute respiratory syndrome coronavirus (SARS-CoV)-2 virus. It was first detected in December 2019 and has since been declared a pandemic causing millions of deaths worldwide. Therefore, there is an urgent need to develop effective therapeutics against coronavirus disease 2019. A critical step in the crosstalk between the virus and...
Clinical Pharmacology and Therapeutics; Bouazza N, Treluyer JM et. al.
Jul 28th, 2021 - In preterm infants, a high risk of hemodynamically significant patent ductus arteriosus (PDA) exists and its persistence is associated with an increased risk of severe morbidity. Current pharmacological options include ibuprofen or indomethacin. However, treatment by indomethacin or ibuprofen of a large PDA was shown to reduce early pulmonary hemorrhage and later medical treatment but had no ef...
Proceedings of the National Academy of Sciences of the Un... Zhang H, Zhu W et. al.
Jul 23rd, 2021 - The global coronavirus disease 2019 (COVID-19) pandemic, caused by severe acute respiratory syndrome (SARS)-like coronavirus (SARS-CoV-2), presents an urgent health crisis. More recently, an increasing number of mutated strains of SARS-CoV-2 have been identified globally. Such mutations, especially those on the spike glycoprotein to render its higher binding affinity to human angiotensin-conver...
Expert Opinion on Drug Metabolism & Toxicology; Miao Y, Xu W et. al.
Jul 20th, 2021 - The first-in-class BTK inhibitor ibrutinib has substantially changed the therapeutic landscape of chronic lymphocytic leukemia (CLL). The next-generation BTK inhibitor acalabrutinib is more selective and may have less off-target toxicities as compared to ibrutinib. Acalabrutinib has demonstrated safety and efficacy in CLL and has been approved to treat CLL. Current clinical trials investigated ...
Toxicology Leitch AC, Ibrahim I et. al.
Jul 17th, 2021 - A methylimidizolium ionic liquid (M8OI) was recently found to be contaminating the environment and to be related to and/or potentially a component of an environmental trigger for the autoimmune liver disease primary biliary cholangitis (PBC). The aims of this study were to investigate human exposure to M8OI, hepatic metabolism and excretion. PBC patient and control sera were screened for the pr...
Antimicrobial Agents and Chemotherapy; Crass RL, Al Naimi T et. al.
Jul 13th, 2021 - The optimal polymyxin B dosage needed to achieve an efficacy target of 50 to 100 mg · h/liter when treating multidrug-resistant bacterial infections in adult cystic fibrosis (CF) patients is unclear. The pharmacokinetics of intravenous polymyxin B were evaluated to better inform dosing. This was a prospective, observational pharmacokinetic (PK) study of nine CF adults receiving intravenous poly...
European Journal of Endocrinology; Stachanow V, Neumann U et. al.
Jul 7th, 2021 - Prenatal dexamethasone therapy is used in female foetuses with congenital adrenal hyperplasia to suppress androgen excess and prevent virilisation of the external genitalia. The traditional dexamethasone dose of 20 µg/kg/day has been used since decades without examination in clinical trials and is thus still considered experimental. As the traditional dexamethasone dose potentially causes adver...
CPT: Pharmacometrics & Systems Pharmacology; Zhang X, Yang Y et. al.
Jul 5th, 2021 - A critical step to evaluate the potential in vivo antiviral activity of a drug is to connect the in vivo exposure to its in vitro antiviral activity. The Anti-SARS-CoV-2 Repurposing Drug Database is a database that includes both in vitro anti-SARS-CoV-2 activity and in vivo pharmacokinetic data to facilitate the extrapolation from in vitro antiviral activity to potential in vivo antiviral activ...