Drug Research最新文献

Efficacy and Safety of Prolonged Treatment with Pemafibrate plus an HMG-CoA Reductase Inhibitor in Japanese Patients with Type 2 Diabetes Mellitus. 帕马布特联合HMG-CoA还原酶抑制剂长期治疗日本2型糖尿病患者的疗效和安全性

IF 1.7

Drug Research Pub Date : 2025-05-21 DOI: 10.1055/a-2560-9750

Masataka Kusunoki, Fumiya Hisano, Shin-Ichi Matsuda, Akiko Kusunoki, Kazuhiko Tsutsumi, Tetsuro Miyata

{"title":"Efficacy and Safety of Prolonged Treatment with Pemafibrate plus an HMG-CoA Reductase Inhibitor in Japanese Patients with Type 2 Diabetes Mellitus.","authors":"Masataka Kusunoki, Fumiya Hisano, Shin-Ichi Matsuda, Akiko Kusunoki, Kazuhiko Tsutsumi, Tetsuro Miyata","doi":"10.1055/a-2560-9750","DOIUrl":"https://doi.org/10.1055/a-2560-9750","url":null,"abstract":"It has been suggested that caution should be exercised when using HMG-CoA reductase inhibitor (statin) in combination with a drug of the fibrate family because of the potentially elevated risk of development of hepatic function impairment and myopathy. We conducted this present study to evaluate the efficacy and safety of treatment with a statin plus pemafibrate (a new fibrate) versus treatment with pemafibrate alone in Japanese patients with type 2 diabetes mellitus.In this study, a total of 23 Japanese patients with type 2 diabetes mellitus were divided into two groups: a group that received pemafibrate alone and a group that received pemafibrate+a statin for a period of 3 years, respectively. Blood levels of lipids and hepatic and renal function parameters were measured before and one and three years after the start of treatment.The pemafibrate-alone group showed reduction of the blood lipid levels, but no adverse changes of the hepatic or renal function parameters were observed. Similarly, the combined pemafibrate+statin treatment group also showed lowering of the blood lipid levels without any adverse changes of the parameters.Improvement of the blood lipid profile was observed in patients who received prolonged treatment with pemafibrate. Similarly, improvement of the blood lipid profile without any adverse changes of the hepatic or renal function parameters was also observed in patients who received prolonged combined pemafibrate+statin treatment. Thus, our findings confirm the safety and efficacy of pemafibrate administered either alone or in combination with a statin.","PeriodicalId":11451,"journal":{"name":"Drug Research","volume":" ","pages":""},"PeriodicalIF":1.7,"publicationDate":"2025-05-21","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144119242","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

A Real-world Pharmacovigilance Study Of FDA Adverse Event Reporting System (FAERS) Events For Gender Of Voriconazole Drugs. FDA不良事件报告系统（FAERS）对伏立康唑药物性别事件的现实药物警戒研究。

IF 1.7

Drug Research Pub Date : 2025-04-28 DOI: 10.1055/a-2575-1530

Qiong Xu, Hongxia Cheng, Xu Sun, Jing Zhao, Yingying Chen, Lingyu Ji, Yan Liang

引用次数: 0

Protective Effects of Niclosamide Ethanolamine Against Testosterone-Induced Benign Prostatic Hyperplasia in Rats. 氯硝胺乙醇胺对睾酮诱导的大鼠良性前列腺增生的保护作用。

IF 1.7

Drug Research Pub Date : 2025-04-28 DOI: 10.1055/a-2576-4153

Ali Hussein Jasim, Ahmed Rahmah Abu-Raghif, Zeena Ayad Hussein

{"title":"Protective Effects of Niclosamide Ethanolamine Against Testosterone-Induced Benign Prostatic Hyperplasia in Rats.","authors":"Ali Hussein Jasim, Ahmed Rahmah Abu-Raghif, Zeena Ayad Hussein","doi":"10.1055/a-2576-4153","DOIUrl":"https://doi.org/10.1055/a-2576-4153","url":null,"abstract":"Benign prostatic hyperplasia is a common urological condition in aging men. The anthelmintic agent niclosamide ethanolamide exhibits a wide range of pharmacological activities. This study aimed to evaluate the protective effect of niclosamide ethanolamide in testosterone propionate-induced benign prostatic hyperplasia in rats along with elucidating the probable mechanism of action by investigating the influence on PPAR-γ and Wnt/β-catenin. 40 male Wistar rats were divided randomly into 4 groups. The healthy (control) group, received daily oral and subcutaneous administration of the vehicle. The Induced (TP) group, received only a daily dose of testosterone propionate 3 mg/kg, SC for 28 days. The treated groups (TP+FIN) and (TP+NE), received a concomitant administration of a daily dose of testosterone propionate along with finasteride 5 mg/kg/day and niclosamide ethanolamide 50 mg/kg/day respectively through oral gavage. Animals were euthanized on day 30 of the experiment and prostate tissue samples were collected to evaluate prostate index, prostate hyperplastic markers by ELISA, and gene expression by RT-qPCR. Results revealed that niclosamide ethanolamide significantly reduced prostate index compared to the induced (TP) group (P<0.0001). The agent nearly normalized BPH markers including 5α-reductase type-2 enzyme, dihydrotestosterone, and PCNA compared to the induced (TP) group (P<0.0001). The agent reduced the tissue level of β-catenin while elevating PPAR-γ to control levels (P<0.05). The current study revealed that NE can help prevent BPH in rats by upregulating the PPAR-γ receptor and inhibiting the Wnt pathway.","PeriodicalId":11451,"journal":{"name":"Drug Research","volume":" ","pages":""},"PeriodicalIF":1.7,"publicationDate":"2025-04-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143978495","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Canagliflozin: A Comprehensive Review of Advances in Preclinical Research. 卡格列净：临床前研究进展综述。

IF 1.7

Drug Research Pub Date : 2025-04-28 DOI: 10.1055/a-2577-1899

Bushra Imran, Farogh Ahsan, Tarique Mahmood, Mohd Masih Uzzaman Khan, Shahzadi Bano, Syed Mehdi Hasan Zaidi, Jamal Akhtar Ansari, Aditya Singh

{"title":"Canagliflozin: A Comprehensive Review of Advances in Preclinical Research.","authors":"Bushra Imran, Farogh Ahsan, Tarique Mahmood, Mohd Masih Uzzaman Khan, Shahzadi Bano, Syed Mehdi Hasan Zaidi, Jamal Akhtar Ansari, Aditya Singh","doi":"10.1055/a-2577-1899","DOIUrl":"https://doi.org/10.1055/a-2577-1899","url":null,"abstract":"Canagliflozin is a synthetic sodium glucose transporter inhibitor (SGLT2i). It is the latest approved class of medicine used in the treatment of type 2 diabetes mellitus. As diabetes is emerging as the most common metabolic disorder, SGLT2i has lightened up the path of treatment with additional benefits. SGLT2 is located in the proximal convoluted tubules of the nephron and is responsible for glucose reabsorption. Thus, inhibiting the SGLT2 leads to a decline in glucose concentration in the plasma. The secondary effects of canagliflozin, such as cardiac protection, renoprotective, and decreased obesity, have made it more putative in the treatment of diabetes mellitus. There are some side effects of canagliflozin, such as volume depletion, genital and urinary tract infection, and lower limb amputation, which could be a matter of concern for patients. Being an anti-diabetic drug, canagliflozin also possesses anti-inflammatory and anti-cancer properties. Several studies have been conducted to determine the efficacy of canagliflozin as an anti-cancer agent. Its pharmacokinetics indicate rapid absorption, reaching peak plasma concentrations within 1-2 hours. With a half-life of approximately 12 hours, it undergoes minimal hepatic metabolism and is primarily excreted unchanged via urine. Common adverse drug reactions (ADRs) include urinary tract infections and dehydration. Clinical trials on canagliflozin, both alone and in combination with other diabetes complications, have been conducted, with some completed and others in various phases. This review article contains information about the pharmacokinetics, drug safety, and efficacy profile of canagliflozin, along with details regarding toxicological studies of canagliflozin.","PeriodicalId":11451,"journal":{"name":"Drug Research","volume":" ","pages":""},"PeriodicalIF":1.7,"publicationDate":"2025-04-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143967707","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Enhancing Doxorubicin Sensitivity in Osteosarcoma Cancer Cells: Unveiling the Role of Resveratrol-Induced Oxidative DNA Damage. 增强阿霉素在骨肉瘤癌细胞中的敏感性：揭示白藜芦醇诱导的DNA氧化损伤的作用。

IF 1.7

Drug Research Pub Date : 2025-04-24 DOI: 10.1055/a-2567-9916

Mohammad Reza Bazavar, Hamed Helali, Linda Mohammadzadeh Boukani, Bahman Yousefi, Amir Valizadeh

引用次数: 0

Drug Delivery Approaches for Buccal and Sublingual Administration. 口腔和舌下给药的给药途径。

IF 1.7

Drug Research Pub Date : 2025-04-22 DOI: 10.1055/a-2560-9884

Asad Ahmad, Juber Akhtar, Mohammad Ahmad, Rufaida Wasim, Mohammad Irfan Khan

{"title":"Drug Delivery Approaches for Buccal and Sublingual Administration.","authors":"Asad Ahmad, Juber Akhtar, Mohammad Ahmad, Rufaida Wasim, Mohammad Irfan Khan","doi":"10.1055/a-2560-9884","DOIUrl":"https://doi.org/10.1055/a-2560-9884","url":null,"abstract":"Both local and systemic medication delivery benefit greatly from the sublingual and buccal modes of administration. They have shown to be a successful substitute for the conventional oral route, particularly in situations requiring a quick commencement of action. Via venous drainage to the superior vena cava, drugs can enter the systemic circulation quickly and directly. They are therefore helpful for individuals who have trouble swallowing as well as for medications that are highly cleared by the liver or degraded in the gastrointestinal system. Traditionally, medications that are delivered through the buccal and sublingual channels are made in three different dose forms: liquid (such as sprays and drops), semi-solid (such as gels), and solid (such as pills, wafers, films, and patches). Physiological variables frequently influence conventional dose forms, which might decrease the formulation's interaction with the mucosa and result in unexpected medication absorption. Many formulation development advancements have been made to enhance medication absorption and retention in the buccal and sublingual areas. The physiological factors influencing buccal and sublingual drug delivery as well as developments in nanoparticulate drug delivery techniques for sublingual and buccal administration will be the main topics of this review. It also discusses about the clinical development pipeline, which includes formulations that have been authorized and are undergoing clinical studies.","PeriodicalId":11451,"journal":{"name":"Drug Research","volume":" ","pages":""},"PeriodicalIF":1.7,"publicationDate":"2025-04-22","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143964391","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Design and Optimization of Novel Pyrimidine-Morpholine Hybrids Through Computational Approaches for SRC Kinase Inhibitory Activity. 基于SRC激酶抑制活性计算方法的新型嘧啶-啉杂合体设计与优化。

IF 1.7

Drug Research Pub Date : 2025-04-17 DOI: 10.1055/a-2554-1119

Knolin K Thachil, V Soumya

{"title":"Design and Optimization of Novel Pyrimidine-Morpholine Hybrids Through Computational Approaches for SRC Kinase Inhibitory Activity.","authors":"Knolin K Thachil, V Soumya","doi":"10.1055/a-2554-1119","DOIUrl":"https://doi.org/10.1055/a-2554-1119","url":null,"abstract":"Src (non receptor tyrosine kinase) plays a role in multiple pathways leading to tumor survival, proliferation and metastasis. Inhibiting Src kinase would be a therapeutic benefit in Src dependent cancers. Most of the nitrogen containing heterocyclic moieties found to possess variety of biological activities. Combination of heterocyclic nucleus to active hybrids has proven to be a successful method of approach to augment biological activities. Hence a series of pyrimidine-morpholine hybrids were designed and its shape similarity studies calculated with the standard Dasatinib using Tanimoto coefficient. Designed molecules were docked with human tyrosine kinase (PDB ID: 2SRC) using AutoDock vina. Docked poses were ranked based on their binding affinities which are then compared with a reference. The studies revealed that docking of hybrid molecules with 2SRC showed promising interactions with affordable ADMET properties. The stability of highly docked complex was analyzed by molecular simulation studies and the results confirmed the docking outcomes thereby making it as a potential SRC kinase inhibitor. Hence these novel pyrimidine hybrids can be considered as lead molecules for developing novel druggable moieties for breast cancer research.","PeriodicalId":11451,"journal":{"name":"Drug Research","volume":" ","pages":""},"PeriodicalIF":1.7,"publicationDate":"2025-04-17","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143983873","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

A Randomized, Controlled Study Evaluating Effects of Saccharomyces boulardii in Adult Patients with Asthma. 一项评价博氏酵母菌对成年哮喘患者疗效的随机对照研究。

IF 1.7

Drug Research Pub Date : 2025-04-14 DOI: 10.1055/a-2564-2569

Kavosh Ansari Dezfouli, Mahboubeh Darban, Maral Hemmati, Mazyar Zahir, Mojtaba Soltani Kermanshahi, Anna Abdolshahi, Hani Sadr, Bahador Bagheri

{"title":"A Randomized, Controlled Study Evaluating Effects of Saccharomyces boulardii in Adult Patients with Asthma.","authors":"Kavosh Ansari Dezfouli, Mahboubeh Darban, Maral Hemmati, Mazyar Zahir, Mojtaba Soltani Kermanshahi, Anna Abdolshahi, Hani Sadr, Bahador Bagheri","doi":"10.1055/a-2564-2569","DOIUrl":"https://doi.org/10.1055/a-2564-2569","url":null,"abstract":"To determine the potential benefit of adding Saccharomyces boulardii (S. boulardii) probiotic supplementation to conventional treatments in asthmatic patients.In this randomized, double-blinded, and placebo-controlled trial 50 asthmatic patients were enrolled. The eligible subjects received either S. boulardii (N=25) or placebo (N=25) added to conventional treatments for three months. Spirometry parameters (FEV1, FVC, FEV1/FVC, and FEF 25-75%) and blood test parameters (CBC, eosinophil percentage, IgE, IL-5, ESR and CRP) were measured and compared at baseline and after treatment completion.The mean age was 39.22±12.55 years. As compared to baseline values, a significant improvement was noted in FEV1 in patients who received S. boulardii (p=0.026). Although the changes in FEV1, FVC, FEV1/FVC, and FEF 25-75% were comparable between the study groups, the differences were not statistically significant (p ˃ 0.05). In addition, patients who received probiotic showed lower levels of IL-5 and IgE in comparison with patients who received placebo.Our findings showed that the addition of S. boulardii to conventional treatments partially improved the pulmonary function and was associated with reductions in IgE and IL-5 levels.","PeriodicalId":11451,"journal":{"name":"Drug Research","volume":" ","pages":""},"PeriodicalIF":1.7,"publicationDate":"2025-04-14","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143962481","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Levocabastine ameliorates cyclophosphamide-induced nephrotoxicity in Swiss albino mice via NF-κB/cleaved caspase-3/TGF-β signaling pathways. 左旋巴丁通过NF-κB/cleaved caspase-3/TGF-β信号通路改善环磷酰胺诱导的瑞士白化小鼠肾毒性。

IF 1.7

Drug Research Pub Date : 2025-04-14 DOI: 10.1055/a-2552-2486

Wasim Akram, Abul Kalam Najmi, M Mumtaz Alam, Syed Ehtaishamul Haque

{"title":"Levocabastine ameliorates cyclophosphamide-induced nephrotoxicity in Swiss albino mice via NF-κB/cleaved caspase-3/TGF-β signaling pathways.","authors":"Wasim Akram, Abul Kalam Najmi, M Mumtaz Alam, Syed Ehtaishamul Haque","doi":"10.1055/a-2552-2486","DOIUrl":"https://doi.org/10.1055/a-2552-2486","url":null,"abstract":"Cyclophosphamide (CP) is a potent anticancer drug, but nephrotoxicity is one of the vital organ toxicities that it causes as a side effect. We tried to evaluate the nephroprotective effect of levocabastine (LEV) in CP-induced nephrotoxicity in Swiss albino mice. Mice were given CP 200 mg/kg, i.p., once on the 7th day. LEV (0.05 and 0.1 mg/kg, i.p.) and fenofibrate (FF) (80 mg/kg, p.o.) were given daily for 14 days. On the 15th day, animals were sacrificed and kidneys were removed for examination. The docking study showed significant binding of LEV and FF against TGF-β1, which is a prime target molecule involved in nephrotoxicity. CP 200 group showed nephrotoxicity in terms of oxidative stress, apoptosis, inflammation, and fibrosis as manifested by decreased levels of SOD, catalase, GSH, blood urea nitrogen/creatinine (BUN/Cr) ratio, and increased TBARS, nitrite, TNF-α, IL-6, TGF-β1, IL-1β, urea, uric acid, creatinine, and BUN. A decrease in body weight (BW) and an increase in kidney weight (KW) with an increased KW/BW ratio was also observed. Cleaved caspase-3 and NF-κB expression was also increased. Histopathological aberrations, like renal corpuscle damage, Bowman's space widening, glomerulus, mesangium cell disintegration, atrophic podocytes, vacuolation, and fibrotic changes were also seen. LEV 0.1 and FF 80 significantly reversed these changes toward normal and showed nephroprotective potential. Thus, seeing the protective effect of LEV on CP-intoxicated mice, we conclude that LEV may be used as an adjuvant with CP in cancer, however, it needs more studies with the direct cancer model to confirm the claim.","PeriodicalId":11451,"journal":{"name":"Drug Research","volume":" ","pages":""},"PeriodicalIF":1.7,"publicationDate":"2025-04-14","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143973771","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Therapeutic Potential of Sotagliflozin in Animal Models of Non-alcoholic Fatty Liver Disease with and without Diabetes. 索他列净在伴有和不伴有糖尿病的非酒精性脂肪肝动物模型中的治疗潜力

IF 1.7

Drug Research Pub Date : 2025-04-14 DOI: 10.1055/a-2557-8927

Nitin J Deshmukh, M S Kalshetti, Mohan Patil, Manohar Nandanwar, Ganesh V Sangle

{"title":"Therapeutic Potential of Sotagliflozin in Animal Models of Non-alcoholic Fatty Liver Disease with and without Diabetes.","authors":"Nitin J Deshmukh, M S Kalshetti, Mohan Patil, Manohar Nandanwar, Ganesh V Sangle","doi":"10.1055/a-2557-8927","DOIUrl":"https://doi.org/10.1055/a-2557-8927","url":null,"abstract":"Sotagliflozin, a dual SGLT1/2 inhibitor, enhances glucagon like peptide-1 (GLP-1) levels and GLP-1 receptor agonists are used to manage non-alcoholic fatty liver disease (NAFLD). Study investigates the effects of sotagliflozin on NAFLD, alone and combined with linagliptin, comparing outcomes in normoglycemic and hyperglycemic animal models.Obese fatty liver disease (FLD) model was induced by high-fat diet (HFD) feeding, while a diabetic non-alcoholic steatohepatitis (NASH) model was developed by administering a single dose of streptozotocin to neonatal mice, followed by HFD feeding post-weaning. At termination of the study, parameters including biochemical markers, inflammatory cytokines, hepatic lipid content, and histopathology were assessed.In NASH mice, sotagliflozin and linagliptin reduced hepatic triglycerides by 60% and 44%, respectively, and cholesterol by 46% and 49%. Their combination further decreased triglycerides by 68.5% and cholesterol by 83.9%. In FLD mice, sotagliflozin and linagliptin reduced triglycerides by 33% and 17%, respectively, and cholesterol by 46% and 21%. Combination treatment offered no benefit, reducing triglycerides by 38% and cholesterol by 27%. Both the treatments improved plasma fibroblast growth factor 21, hepatic interlukin-6, glucose tolerance, steatosis and mitigated fat pad weight, but their combination did not show additional benefit. However, combination treatment demonstrated added benefit in modulating NAFLD activity score, liver enzymes, glycogenated hepatic nuclei, plasma glucose and active GLP-1 levels.Study underscores sotagliflozin's potential to mitigate NAFLD and highlights the benefit of combining it with linagliptin in hyperglycemic NASH model, which showed limited efficacy in normoglycemic FLD mice.","PeriodicalId":11451,"journal":{"name":"Drug Research","volume":" ","pages":""},"PeriodicalIF":1.7,"publicationDate":"2025-04-14","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143982666","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0