Aromatic diamidines as antiparasitic agents.

abstract：INTRODUCTION:Dasatinib is a novel tyrosine kinase inhibitor with activity against the Src family kinases. The Src pathway is active in breast cancer and has been shown to promote cell proliferation, invasiveness, and metastases. Preclinical data support the use of dasatinib to inhibit breast cancer cell growth, modulat...

journal_title：Expert opinion on investigational drugs

authors： Scher KS,Somlo G

更新日期：2013-06-01 00:00:00

abstract：:Plasma concentrations of the peptide endothelin (ET) are elevated in several cardiovascular diseases. Animal studies suggest that activation of ET receptors may contribute to the increase in vascular resistance and remodelling of cardiovascular tissues that are characteristic of these pathologies. Antagonists of these...

journal_title：Expert opinion on investigational drugs

authors： Maguire JJ,Davenport AP

更新日期：1999-01-01 00:00:00

abstract：:'Male factor' problems contribute to subfertility in a significant proportion of couples. In some instances, defective sperm production has qualitative and/or quantitative effects on the semen profile; in others, no obvious defects can be detected, yet spermatozoa are non-fertilising. Recent studies have revealed that...

journal_title：Expert opinion on investigational drugs

authors： Fraser LR

更新日期：1997-12-01 00:00:00

abstract：:At present, the nucleoside reverse transcriptase (RT) inhibitors and protease inhibitors (PI) have dominated the therapeutic options for the treatment of human immunodeficiency virus (HIV) infection. From the initial monotherapeutic strategies, to the widely accepted multi-drug cocktails of today, the use of these two...

journal_title：Expert opinion on investigational drugs

authors： Buckheit RW

更新日期：2001-08-01 00:00:00

abstract：:Advances in molecular medicine have revealed a key role for altered gene expression in the aetiology of many inflammatory diseases, including asthma, rheumatoid arthritis, inflammatory bowel disease and sepsis. Until recently, however, modulation of gene transcription has not been the subject of directed pharmaceutica...

journal_title：Expert opinion on investigational drugs

authors： Manning AM,Mercurio F

更新日期：1997-05-01 00:00:00

abstract：:Neuroimmunophilin ligands are a class of compounds that hold great promise for the treatment of nerve injuries and neurological disease. In contrast to neurotrophins (e.g., nerve growth factor), these compounds readily cross the blood-brain barrier, being orally effective in a variety of animal models of ischaemia, tr...

journal_title：Expert opinion on investigational drugs

authors： Gold BG

更新日期：2000-10-01 00:00:00

abstract：INTRODUCTION:Inhaled corticosteroids are the only drugs that effectively suppress the airway inflammation, but they can induce considerable systemic and adverse effects when they are administered chronically at high doses. Consequently, the pharmaceutical industry is still searching for newer entities with an improved ...

journal_title：Expert opinion on investigational drugs

authors： Cazzola M,Coppola A,Rogliani P,Matera MG

更新日期：2015-01-01 00:00:00

abstract：:This review highlights some important advances that have taken place in cannabinoid research over the last four years. It focuses on novel ligands that are of interest either as experimental tools or as lead compounds for therapeutic agents and possible clinical applications for some of these ligands. The molecular ta...

journal_title：Expert opinion on investigational drugs

authors： Pertwee RG

更新日期：2000-07-01 00:00:00

abstract：:The epidermal growth factor receptor is a cell membrane growth factor receptor that plays a key role in cancer development and progression. Epidermal growth factor receptor-activated signalling pathways control cell proliferation, apoptosis, angiogenesis and metastatic spread in the majority of human epithelial cancer...

journal_title：Expert opinion on investigational drugs

authors： Ciardiello F,Tortora G

更新日期：2002-06-01 00:00:00

abstract：:IL-5 is the predominant cytokine associated with antigen-induced eosinophilic inflammation in the lung. The activation of Th-2 cells leads to the production of IL-5. The pro-eosinophilic effects of IL-5 include: (1) enhanced replication and differentiation of eosinophilic myelocytes; (2) enhanced degranulation of eosi...

journal_title：Expert opinion on investigational drugs

authors： Weltman JK,Karim AS

更新日期：2000-03-01 00:00:00

abstract：:Introduction: Respiratory syncytial virus (RSV) causes lower respiratory tract infections and can lead to morbidity and mortality in the infant, elderly and immunocompromised. There is no vaccine and therapeutic interventions are limited. RSV disease research has yielded the development of several prophylactic and the...

journal_title：Expert opinion on investigational drugs

authors： Bergeron HC,Tripp RA

更新日期：2020-03-01 00:00:00

abstract：:Marfan syndrome is the most common genetic disorder of the connective tissue with an estimated prevalence of 1:10,000. The disease is characterised by manifestations in the cardiovascular, skeletal and ocular systems. The most severe manifestations are those of the cardiovascular system: mitral valve prolapse and dila...

journal_title：Expert opinion on investigational drugs

authors： Phylactou LA,Kilpatrick MW

更新日期：1999-07-01 00:00:00

abstract：:PTI-821 is a long-acting formulation of oxycodone that is intended to deter abuse through its gel-cap technology. Produced by Pain Therapeutics in alliance with King Pharmaceuticals, PTI-821 is designed to provide strong pain relief with the intent of offering greater safety than is presently available from convention...

journal_title：Expert opinion on investigational drugs

authors： Webster LR

更新日期：2007-03-01 00:00:00

abstract：INTRODUCTION:Duchenne muscular dystrophy (DMD) is an X-linked recessive disorder caused by mutations in the dystrophin (DMD) gene. Most patients die from respiratory failure or cardiomyopathy. There are significant unmet needs for treatments for DMD as the standard of care is principally limited to symptom relief throu...

journal_title：Expert opinion on investigational drugs

authors： Sheikh O,Yokota T

更新日期：2021-01-06 00:00:00

abstract：INTRODUCTION:Obinutuzumab is a novel humanized type II glycoengineered anti-CD20 antibody approved for first-line treatment of chronic lymphocytic leukemia (CLL) in combination with chlorambucil and for treatment of rituximab-refractory follicular lymphoma (FL). Areas covered: We describe current preclinical and clinic...

journal_title：Expert opinion on investigational drugs

authors： Klein C,Bacac M,Umana P,Fingerle-Rowson G

更新日期：2017-10-01 00:00:00

abstract：:BCR-ABL, a constitutively active tyrosine kinase, causes chronic myeloid leukaemia (CML). Rational development of drugs targeting BCR-ABL has significantly improved the treatment of CML. Imatinib (a BCR-ABL tyrosine kinase inhibitor) produces haematological and cytogenetic remissions across all phases of CML and is th...

journal_title：Expert opinion on investigational drugs

authors： Jabbour E,Cortes J,Kantarjian H

更新日期：2007-05-01 00:00:00

abstract：:Introduction: Advanced melanoma historically had a very poor outcome but targeted therapies and immune checkpoint inhibitors (IC) have changed the course of the disease and made durable responses possible. However, most patients will develop progressive disease, so further strategies to overcome treatment resistance a...

journal_title：Expert opinion on investigational drugs

authors： Boos LA,Leslie I,Larkin J

更新日期：2020-07-01 00:00:00

abstract：IMPORTANCE OF THE FIELD:The use of traditional medicines of natural origin is being encouraged for the treatment of chronic disorders, as synthetic drugs in such cases may cause unpredictable adverse effects. Berberine, a traditional plant alkaloid, is used in Ayurvedic and Chinese medicine for its antimicrobial and an...

journal_title：Expert opinion on investigational drugs

authors： Vuddanda PR,Chakraborty S,Singh S

更新日期：2010-10-01 00:00:00

abstract：BACKGROUND:Peritoneal carcinomatosis (PC) is a challenging consequence of certain malignancies, associated with a poor prognosis and limited treatment options. Generally, PC has been treated similarly to metastatic cancers of the primary tumor, but associated with worse outcomes when compared to other sites of metastat...

journal_title：Expert opinion on investigational drugs

authors： Davies JM,O'Neil B

更新日期：2009-07-01 00:00:00

abstract：:Leukotriene B(4) (LTB(4)) is a lipid inflammatory mediator derived from membrane phospholipids by the sequential actions of cytosolic phospholipase A2 (PLA2), 5-lipoxygenase (5-LO) and leukotriene A(4) (LTA(4)) hydrolase. Several inflammatory diseases, including asthma, chronic obstructive pulmonary disease, arthritis...

journal_title：Expert opinion on investigational drugs

authors： Hicks A,Monkarsh SP,Hoffman AF,Goodnow R Jr

更新日期：2007-12-01 00:00:00

abstract：INTRODUCTION:We carried out a screen for small molecule selective inhibitors of eukaryotic DNA polymerases (pols). Dehydroaltenusin, isolated from a fungus (Alternaria tenuis), was found to be a specific inhibitor of pol α. AREAS COVERED:We succeeded in chemically synthesizing dehydroaltenusin along with five analogs....

journal_title：Expert opinion on investigational drugs

authors： Mizushina Y,Maeda N,Kuriyama I,Yoshida H

更新日期：2011-11-01 00:00:00

abstract：:Improving the tumour selectivity of cytotoxic drugs through conjugation to tumour-reactive monoclonal antibodies may lead to novel, more potent agents for cancer therapy. The maytansinoid drugs are 100- to 1000-fold more cytotoxic in vitro than current clinical anticancer drugs. We recently demonstrated that conjugati...

journal_title：Expert opinion on investigational drugs

authors： Liu C,Chari RV

更新日期：1997-02-01 00:00:00

abstract：INTRODUCTION:Stroke is the second leading cause of death worldwide and the leading cause of adult neurological disability. Despite advances in stroke unit care, and increasing use of thrombolysis, there remains an urgent need for safe and effective treatments for acute ischaemic stroke. However, this is against a backd...

journal_title：Expert opinion on investigational drugs

authors： Smith CJ,Denes A,Tyrrell PJ,Di Napoli M

更新日期：2015-05-01 00:00:00

abstract：INTRODUCTION:In the treatment of advanced/metastatic head and neck cancer (HNC), resistance to chemotherapy and to anti-EGFR agents remains a major issue, and new molecular drugs are eagerly awaited. Over the last decade, knowledge of the genetic landscape of HNC has rapidly grown. However, no tailored therapeutic inte...

journal_title：Expert opinion on investigational drugs

authors： Bossi P,Alfieri S

更新日期：2016-07-01 00:00:00

abstract：BACKGROUND:Today, propofol or 2,6-diisopropylphenol is the anesthetic mainly used for monitored anesthetic care sedation and during intravenous anesthesia. The formulation, a lipid macroemulsion, shows several disadvantages. Therefore, during the past years considerable scientific effort has been undertaken to find eit...

journal_title：Expert opinion on investigational drugs

authors： Fechner J,Ihmsen H,Jeleazcov C,Schüttler J

更新日期：2009-10-01 00:00:00

abstract：BACKGROUND:Histone deacetylases (HDACs), which target histones as well as non-histone proteins as substrates, have the potential to regulate aberrant gene expression and restore normal growth control in malignancies. OBJECTIVE:This review provides an updated summary of preclinical and clinical experience with the oral...

journal_title：Expert opinion on investigational drugs

authors： Le Tourneau C,Siu LL

更新日期：2008-08-01 00:00:00

abstract：:Innate immune mechanisms respond rapidly to bacterial infection. A key cellular component of the innate immune response is the neutrophil, whose cytoplasmic granules contain a variety of antimicrobial proteins and peptides. Among these is the bactericidal/permeability-increasing protein (BPI), a cationic 55 kDa protei...

journal_title：Expert opinion on investigational drugs

authors： Levy O

更新日期：2002-02-01 00:00:00

abstract：:Major depressive disorder (MDD) is a serious illness with far reaching societal and economic ramifications. The monoamine-deficiency hypothesis that depressive symptoms are associated with reductions in monoamine neurotransmission, particularly serotonin and noradrenaline, is supported by both neurochemical findings a...

journal_title：Expert opinion on investigational drugs

authors： Bymaster FP,McNamara RK,Tran PV

更新日期：2003-04-01 00:00:00

abstract：BACKGROUND:In the past years the bone seeking radiopharmaceutical samarium lexidronam ((153)Sm-EDTMP) has been increasingly used alone or in conjunction with chemotherapy and/or bisphosphonates for the treatment of painful bone metastasis. OBJECTIVE:Its use has been explored in different solid tumours. In this report ...

journal_title：Expert opinion on investigational drugs

authors： Abruzzese E,Iuliano F,Trawinska MM,Di Maio M

更新日期：2008-09-01 00:00:00

abstract：:Obesity shortens life expectancy and is a risk factor for hypertension and Type 2 diabetes. When added to the standard chow of Sprague-Dawley or Otsuka Long-Evans Tokushima Fatty rats, alpha-lipoic acid (0.5% weight/weight) reduced body weight and food intake. Alpha-lipoic acid also increased whole-body energy expendi...

journal_title：Expert opinion on investigational drugs

authors： Doggrell SA

更新日期：2004-12-01 00:00:00