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Current opinion in investigational drugs最新文献

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Novel inhibitors of mTORC1 and mTORC2. mTORC1和mTORC2的新型抑制剂。
Current opinion in investigational drugs Pub Date : 2010-06-01
Shripad V Bhagwat, Andrew P Crew
{"title":"Novel inhibitors of mTORC1 and mTORC2.","authors":"Shripad V Bhagwat,&nbsp;Andrew P Crew","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>The PI3K/Akt/mTOR pathway is frequently activated in human cancers, and mTOR is a clinically validated target for therapeutic intervention in this pathway. The discovery of the involvement of rapamycin-insensitive mTOR complex 2 (mTORC2) in the activation of Akt, combined with the limited clinical antitumor activity of mTOR complex 1 (mTORC1)-directed rapamycin analogs, have led to the discovery of ATP-competitive selective inhibitors of the mTOR kinase that inhibit the function of both mTORC1 and mTORC2. This review describes progress in the identification of selective and novel inhibitors of mTORC1/2, focusing on the profile of inhibitors that are in clinical development.</p>","PeriodicalId":10978,"journal":{"name":"Current opinion in investigational drugs","volume":" ","pages":"638-45"},"PeriodicalIF":0.0,"publicationDate":"2010-06-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"29009649","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
Recent clinical trials of vitamin D3 supplementation and serum calcium levels in humans: Implications for vitamin D-based chemoprevention. 维生素D3补充和人类血清钙水平的近期临床试验:维生素d化学预防的意义。
Current opinion in investigational drugs Pub Date : 2010-06-01
Halcyon G Skinner, Kristin Litzelman, Gary G Schwartz
{"title":"Recent clinical trials of vitamin D3 supplementation and serum calcium levels in humans: Implications for vitamin D-based chemoprevention.","authors":"Halcyon G Skinner,&nbsp;Kristin Litzelman,&nbsp;Gary G Schwartz","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>Clinical trials of vitamin D supplementation published from 2000 to 2009 are reviewed, with an emphasis on changes in serum calcium levels. In these trials, vitamin D supplementation often resulted in modest increases in serum calcium levels, but rarely caused hypercalcemia. Although hypercalcemia is considered to be the only toxicity of vitamin D, many prospective studies have demonstrated associations between high normocalcemia (serum calcium levels that are high but fall within the normal reference range) and premature mortality, predominantly from cardiovascular disease. These findings suggest that high normocalcemia may represent a more sensitive index of the long-term toxicity associated with vitamin D supplementation than hypercalcemia. Therefore, efforts to chemoprevent diseases with vitamin D must consider the potential health risks associated with high normocalcemia.</p>","PeriodicalId":10978,"journal":{"name":"Current opinion in investigational drugs","volume":" ","pages":"678-87"},"PeriodicalIF":0.0,"publicationDate":"2010-06-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"29009654","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
Emerging treatment with systemic chemotherapy and targeted agents for biliary cancers. 胆道肿瘤的系统性化疗和靶向药物的新兴治疗方法。
Current opinion in investigational drugs Pub Date : 2010-06-01
Narikazu Boku
{"title":"Emerging treatment with systemic chemotherapy and targeted agents for biliary cancers.","authors":"Narikazu Boku","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>Clinically, 5-fluorouracil (5-FU) and its derivatives, platinum-based agents and gemcitabine (GEM) are used as key treatments for unresectable or recurrent biliary cancer. A phase III clinical trial has demonstrated that treatment with GEM plus CDDP prolongs the survival of patients with biliary cancer compared with treatment with GEM alone. Moreover, promising results are also being reported against molecular targets, particularly with inhibitors of EGFR. In addition, the development of novel drugs based on biological markers might be important for the treatment of biliary cancer. In the future, a paradigm shift from disease-specific drug development to biomarker-oriented investigations may be applicable for rare diseases such as biliary cancer.</p>","PeriodicalId":10978,"journal":{"name":"Current opinion in investigational drugs","volume":" ","pages":"653-60"},"PeriodicalIF":0.0,"publicationDate":"2010-06-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"29009651","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
Intraductal therapy for the prevention of breast cancer. 导管内治疗预防乳腺癌。
Current opinion in investigational drugs Pub Date : 2010-06-01
Lisa Jacobs, Saraswati Sukumar, Vered Stearns
{"title":"Intraductal therapy for the prevention of breast cancer.","authors":"Lisa Jacobs,&nbsp;Saraswati Sukumar,&nbsp;Vered Stearns","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>Patients at high risk for developing breast cancer and those with early stage breast cancer may have treatment options in addition to systemic therapy for the prevention and treatment of this disease in the near future. Methods of intraductal diagnosis and treatment of breast cancer, including nipple aspiration, ductal lavage and ductoscopy, are discussed in this review. Advances in this field include improvements in equipment and techniques, more reliable biomarker assessment and improved targeted therapies. As a result of these advances, intraductal treatment in high-risk populations is being investigated in clinical trials.</p>","PeriodicalId":10978,"journal":{"name":"Current opinion in investigational drugs","volume":" ","pages":"646-52"},"PeriodicalIF":0.0,"publicationDate":"2010-06-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"29009650","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
Targeting the kallikrein-kinin system as a new therapeutic approach to diabetic retinopathy. 以钾化钾-激肽系统为靶点治疗糖尿病视网膜病变的新途径。
Current opinion in investigational drugs Pub Date : 2010-05-01
Didier Pruneau, Pierre Bélichard, José-Alain Sahel, Jean-Philippe Combal
{"title":"Targeting the kallikrein-kinin system as a new therapeutic approach to diabetic retinopathy.","authors":"Didier Pruneau,&nbsp;Pierre Bélichard,&nbsp;José-Alain Sahel,&nbsp;Jean-Philippe Combal","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>Diabetic retinopathy (DR) is a major microvascular complication of diabetes mellitus that can lead to visual impairment and blindness. There is no approved pharmacological treatment for DR; however, laser therapy, steroids and anti-VEGF agents appear to provide some benefit. Hyperglycemia, advanced glycation end products, growth factors, and elevated levels of circulating and vitreous cytokines and chemokines can all trigger an inflammatory response of the retinal vasculature. Features of DR can include diabetic macular edema, microhemorrhage, loss of capillaries, development of avascular areas and the vitreo-retinal proliferation of neovessels. The kallikrein-kinin system (KKS) has long been recognized as a key player of inflammatory processes in various organs. Intravitreally administered recombinant plasma kallikrein has been demonstrated to produce retinal vascular leakage and hemorrhage, while both kinin B1 and B2 receptor agonists have induced retinal edema. Furthermore, kallikrein inhibitors and peptide-based B1 receptor antagonists could reduce or block retinal vascular permeability in diabetic rats. In a diabetic rat model, FOV-2304 (Fovea Pharmaceuticals SA), a non-peptide selective B1 receptor antagonist, consistently blocked retinal vascular permeability, inhibited leukocyte adhesion and abolished the retinal mRNA expression of several inflammatory mediators. Although additional studies are required to investigate the role of the KKS in early capillary loss and late-stage neovascularization processes, the blockade of the KKS is a promising therapeutic strategy for DR.</p>","PeriodicalId":10978,"journal":{"name":"Current opinion in investigational drugs","volume":"11 5","pages":"507-14"},"PeriodicalIF":0.0,"publicationDate":"2010-05-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"28945768","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
Laquinimod, a new oral autoimmune modulator for the treatment of relapsing-remitting multiple sclerosis. Laquinimod，一种治疗复发-缓解型多发性硬化症的新型口服自身免疫调节剂。
Current opinion in investigational drugs Pub Date : 2010-05-01
Alex Tselis
{"title":"Laquinimod, a new oral autoimmune modulator for the treatment of relapsing-remitting multiple sclerosis.","authors":"Alex Tselis","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>Laquinimod, a second-generation quinoline-3-carboxamide, is being developed by Active Biotech AB and Teva Pharmaceutical Industries Ltd for the treatment for relapsing-remitting multiple sclerosis (RRMS). Laquinimod has demonstrated significant activity in suppressing experimental autoimmune encephalomyelitis, an animal model of RRMS. In phase I and II clinical trials, the drug was well tolerated, with some hints of efficacy in small numbers of patients with RRMS. While the mechanism of action of the drug is unknown, it likely involves Th1 to Th2/Th3 immune deviation, promotion of the synthesis and release of neurotrophic factors, and other possible neuroprotective effects. Two phase III clinical trials are ongoing and, if successful, will lead to the approval of the first oral immunomodulatory drug for suppressing multiple sclerosis disease activity.</p>","PeriodicalId":10978,"journal":{"name":"Current opinion in investigational drugs","volume":"11 5","pages":"577-85"},"PeriodicalIF":0.0,"publicationDate":"2010-05-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"28944112","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
Transient receptor potential channels as novel drug targets in respiratory diseases. 瞬态受体电位通道作为呼吸系统疾病的新药物靶点。
Current opinion in investigational drugs Pub Date : 2010-05-01
Romina Nassini, Serena Materazzi, Gaetano De Siena, Francesco De Cesaris, Pierangelo Geppetti
{"title":"Transient receptor potential channels as novel drug targets in respiratory diseases.","authors":"Romina Nassini,&nbsp;Serena Materazzi,&nbsp;Gaetano De Siena,&nbsp;Francesco De Cesaris,&nbsp;Pierangelo Geppetti","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>A subpopulation of nociceptive primary sensory neurons expresses six different transient receptor potential (TRP) ion channels of the vanilloid (V1, V2, V3 and V4), melastatin (M8) and ankyrin (A1) subtypes. TRPV1 mediates the tussive action of capsaicin, which is widely used in cough provocation studies. The upregulation of TRPV1 expression and function has been reported in asthma and other inflammatory conditions. TRPA1 is targeted by a series of byproducts of oxidative and nitrative stress, including acrolein, 4-hydroxy-2-nonenal and hydrogen peroxide. Proinflammatory neuropeptides are released from nociceptive nerve terminals after TRPV1/TRPA1 stimulation, thereby causing airway neurogenic inflammation. In addition, the early inflammatory response to cigarette smoke is mediated entirely by neuronal TRPA1. TRPV1 and TRPA1 antagonists may therefore represent potential antitussive and anti-inflammatory therapeutics for respiratory airway diseases.</p>","PeriodicalId":10978,"journal":{"name":"Current opinion in investigational drugs","volume":"11 5","pages":"535-42"},"PeriodicalIF":0.0,"publicationDate":"2010-05-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"28944107","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
Developing therapeutics for the treatment of pediatric asthma. 开发儿童哮喘的治疗方法。
Current opinion in investigational drugs Pub Date : 2010-05-01
Fadi Eskandar, Scott Fleming
{"title":"Developing therapeutics for the treatment of pediatric asthma.","authors":"Fadi Eskandar,&nbsp;Scott Fleming","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>The main goals for developing effective treatments for pediatric asthma are to improve the quality of life of children with asthma by reducing symptoms and the frequency of exacerbations, to allow undisturbed sleep and performance of daily activities, and to ensure a more healthy adult future. Despite advances in modern medical care and the introduction of effective therapies, such as inhaled corticosteroids, poor asthma control exists in clinical practice. This lack of control can be attributed to two primary factors: (i) poor compliance and adherence to treatment; and (ii) poor efficiency of inhalation drug delivery, resulting from the inability of young children to correctly use inhalers that were designed for adults. Both the FDA and EMEA have mandated pediatric testing regulations for drugs indicated for pediatric use and established incentives for the development of such agents; however, there are no inhalers on the market that have been specifically designed to meet the unique needs of children because most inhalers were developed for adults and then used for the treatment of children following minor modifications. Significant effort needs to be invested in the area of pediatric asthma to increase the availability of high-quality, patient-centric medication and delivery systems.</p>","PeriodicalId":10978,"journal":{"name":"Current opinion in investigational drugs","volume":"11 5","pages":"550-8"},"PeriodicalIF":0.0,"publicationDate":"2010-05-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"28944109","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
CB-01-05-MMX, a novel oral controlled-release low molecular weight heparin for the potential treatment of ulcerative colitis. CB-01-05-MMX，一种新型口服控释低分子量肝素，有望治疗溃疡性结肠炎。
Current opinion in investigational drugs Pub Date : 2010-05-01
Daniel C Baumgart
{"title":"CB-01-05-MMX, a novel oral controlled-release low molecular weight heparin for the potential treatment of ulcerative colitis.","authors":"Daniel C Baumgart","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>CB-01-05-MMX (LMW Heparin MMX), being developed by Cosmo Pharmaceuticals SpA, is a novel oral parnaparin sodium formulation for the potential treatment of ulcerative colitis. At the time of publication, clinical trial data were limited and the mechanism of action had not been elucidated. However, in one phase I and one phase IIb trial in patients with left-sided ulcerative colitis, CB-01-05-MMX had an acceptable safety profile and was not associated with bleeding complications, which is a known side effect of unfractionated heparin and low molecular weight heparin compounds previously evaluated for the treatment of ulcerative colitis. Evaluable efficacy data from the phase IIb trial revealed significant improvements in the clinical activity index values in the CB-01-05-MMX group, but this was not accompanied by mucosal healing. More research, including placebo-controlled trials in patients with left-sided ulcerative colitis and trials in patients with pancolitis, would determine the role of CB-01-05-MMX in the current spectrum of available medications for this condition.</p>","PeriodicalId":10978,"journal":{"name":"Current opinion in investigational drugs","volume":"11 5","pages":"571-6"},"PeriodicalIF":0.0,"publicationDate":"2010-05-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"28944111","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
New treatments for gout. 痛风的新疗法。
Current opinion in investigational drugs Pub Date : 2010-05-01
Janet B Mapa, Michael H Pillinger
{"title":"New treatments for gout.","authors":"Janet B Mapa,&nbsp;Michael H Pillinger","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>Gout is a commonly occurring medical condition that can lead to significant morbidity. Therapies available for the treatment of both acute and chronic gouty arthritis have not changed significantly since the 1960s. Although these treatments are well established, they are often contraindicated in the presence of various different comorbidities, including diabetes, renal insufficiency, hypertension and gastrointestinal disease, all of which can occur frequently in patients with gout. Therefore, new treatments are needed. This review describes recent advances in therapeutics for gout, including drugs designed to reduce levels of urate and to inhibit acute or chronic inflammation. While some of these strategies are currently available, others are undergoing regulatory evaluation or are at earlier stages of development.</p>","PeriodicalId":10978,"journal":{"name":"Current opinion in investigational drugs","volume":"11 5","pages":"499-506"},"PeriodicalIF":0.0,"publicationDate":"2010-05-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"28945767","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
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