New antithrombotic drugs on the horizon.

abstract：:Cyclooxygenase-2 (COX-2) is constitutively expressed in the central nervous system, and is thought to have an important functional role therein. COX-2 interacts with neurotransmitters such as acetylcholine, 5-hydroxytryptamine and glutamate but is also involved in the regulation of the central nervous system immune sy...

journal_title：Expert opinion on investigational drugs

authors： Müller N,Strassnig M,Schwarz MJ,Ulmschneider M,Riedel M

更新日期：2004-08-01 00:00:00

abstract：:Asthma and chronic obstructive pulmonary disease (COPD) are diseases of the airways with an underlying inflammatory component. The prevalence and healthcare burden of asthma and COPD is still rising and is predicted to continue to rise in the current century. The beta-agonists and corticosteroids form the basis of the...

journal_title：Expert opinion on investigational drugs

authors： Hele DJ,Belvisi MG

更新日期：2003-01-01 00:00:00

abstract：INTRODUCTION:Subjects with atrial fibrillation are at risk of thromboembolic events. The vitamin K antagonists (e.g., warfarin) are useful at preventing coagulation in atrial fibrillation, but are difficult to use. One of the FXa inhibitors, oral apixaban, has been tested as an anticoagulant in atrial fibrillation. AR...

journal_title：Expert opinion on investigational drugs

authors： Doggrell SA

更新日期：2012-08-01 00:00:00

abstract：INTRODUCTION:In the last decade, concerns have been raised around the use of erythropoiesis-stimulating agents (ESAs) and intravenous iron in chronic kidney disease (CKD) patients, especially when given at high doses. Moreover, treatment with ESA is expensive. AREAS COVERED:We searched PubMed for original articles, re...

journal_title：Expert opinion on investigational drugs

authors： Del Vecchio L,Locatelli F

更新日期：2018-07-01 00:00:00

abstract：INTRODUCTION:In 2010, about 8.8 million new cases of tuberculosis were recorded and 1.1 million people died of tuberculosis worldwide. Although numbers are in decrease since 2006, tuberculosis still represents a global issue and a major public health threat, due to appearance of multidrug-resistant and extensively drug...

journal_title：Expert opinion on investigational drugs

authors： Engohang-Ndong J

更新日期：2012-12-01 00:00:00

abstract：INTRODUCTION:The unmet need and the growing prevalence of hyperuricemia and its complications worldwide have pushed investigators to identify new agents to manage hyperuricemia. AREAS COVERED:This review discusses the drugs in preclinical and early clinical trials for hyperuricemia, their mechanisms of action and avai...

journal_title：Expert opinion on investigational drugs

authors： Shahid H,Singh JA

更新日期：2015-01-01 00:00:00

abstract：INTRODUCTION:Ewing sarcoma family tumors (ESFT) are a group of aggressive diseases, characterized histologically by small, round, blue cells and genetically by translocation involving EWS and ETS partner genes. The current treatment of localized Ewing sarcoma (ES) requires a multi-disciplinary approach, including multi...

journal_title：Expert opinion on investigational drugs

authors： Vornicova O,Bar-Sela G

更新日期：2016-06-01 00:00:00

abstract：INTRODUCTION:Although the combination of an anti-CD20 monoclonal antibody and chemotherapy has widely improved survival of patients with B-cell lymphoma, the disease still relapses. A better understanding of the biology of lymphomas has highlighted the role of the cell of origin in response to treatment and outcome. Le...

journal_title：Expert opinion on investigational drugs

authors： Garciaz S,Coso D,Schiano de Colella JM,Bouabdallah R

更新日期：2016-09-01 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：:Introduction: Plasma kallikrein is a  mediator of vascular leakage and inflammation. Activation of plasma kallikrein can induce features of diabetic macular edema (DME) in preclinical models. Human vitreous shows elevated plasma kallikrein levels in patients with DME. Because of the incomplete response of some patient...

journal_title：Expert opinion on investigational drugs

authors： Bhatwadekar AD,Kansara VS,Ciulla TA

更新日期：2020-03-01 00:00:00

abstract：INTRODUCTION:Thermo transient receptor potential (thermoTRP) channels are some of the most intensely pursued therapeutic targets of the past decade. They are considered promising targets of numerous diseases including chronic pain and cancer. Modulators of these proteins, in particular TRPV1-4, TRPM8 and TRPA1, have re...

journal_title：Expert opinion on investigational drugs

authors： Fernández-Carvajal A,González-Muñiz R,Fernández-Ballester G,Ferrer-Montiel A

更新日期：2020-11-01 00:00:00

abstract：:Diabetes is a chronic, debilitating disease that afflicts millions of people worldwide and poor glycemic control in this disease leads to numerous microvascular and macrovascular complications. There is growing evidence that tight glycemic control prevents the development, and delays the progression, of microvascular ...

journal_title：Expert opinion on investigational drugs

authors： Mudaliar S

更新日期：2007-10-01 00:00:00

abstract：INTRODUCTION:The fast actions of the excitatory neurotransmitter glutamate are mediated by glutamate-gated ion channels (ionotropic Glu receptors). Metabotropic glutamate receptors (mGlus) are coupled to second messenger pathways via G proteins and modulate glutamatergic and GABAergic neurotransmission. Of the eight di...

journal_title：Expert opinion on investigational drugs

authors： Raber J,Duvoisin RM

更新日期：2015-04-01 00:00:00

abstract：INTRODUCTION:The small tyrosine kinase inhibitor Imatinib Mesylate (Gleevec) protects against diabetes, but it is not known how. AREAS COVERED:It has been suggested that islet amyloid and fibrotic deposits promote beta-cell failure and death, leading to Type-2 diabetes. As Imatinib is known to possess anti-fibrotic/am...

journal_title：Expert opinion on investigational drugs

authors： Welsh N

更新日期：2012-11-01 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：:Clinical trials showing the benefits of reducing the effects of TNF- alpha in rheumatoid arthritis have highlighted the key role of the cytokine TNF- alpha in this inflammatory condition. A new approach to reducing the effects of TNF- alpha is to decrease its synthesis by inhibiting TNF- alpha converting enzyme with G...

journal_title：Expert opinion on investigational drugs

authors： Doggrell SA

更新日期：2002-07-01 00:00:00

abstract：:Zolmitriptan is a new oral acute treatment for migraine. It is a selective and potent agonist at the serotonin (5-HT)(1B/1D) receptor and was developed to improve on the oral bioavailability, tissue selectivity and CNS penetration of earlier compounds. Animal studies confirmed that these objectives had been attained. ...

journal_title：Expert opinion on investigational drugs

authors： Rolan PE,Martin GR

更新日期：1998-04-01 00:00:00

abstract：:After thousands of years of interest the last few decades have seen a huge increase in our knowledge of the cannabinoids and their mode of action. Their potential as medical therapeutics has long been known. However, very real concerns over their safety and efficacy have lead to caution and suspicion when applying the...

journal_title：Expert opinion on investigational drugs

authors： Grundy RI

更新日期：2002-10-01 00:00:00

abstract：:Atherothrombosis, or thrombus formation, at the site of a disrupted atherosclerotic plaque is the common pathophysiology related to myocardial infarction, ischaemic stroke and peripheral arterial disease. A growing body of evidence demonstrates an important role for vascular inflammation in the pathophysiology of athe...

journal_title：Expert opinion on investigational drugs

authors： Herbert JM

更新日期：2004-05-01 00:00:00

abstract：:Sitagliptin is a once-daily, orally active, competitive and fully reversible inhibitor of dipeptidyl peptidase 4, the enzyme that is responsible for the rapid degradation of the incretin hormone glucagon-like peptide-1. It is the first in this new class of antihyperglycaemic agents to gain regulatory approval for the ...

journal_title：Expert opinion on investigational drugs

authors： Deacon CF

更新日期：2007-04-01 00:00:00

abstract：IMPORTANCE OF THE FIELD:Treatments of pulmonary arterial hypertension (PAH) that have so far proven efficacious are all based on the restoration of endothelium control of pulmonary vascular tone and structure, by administration of prostacyclins, endothelin receptor antagonists and phosphodiesterase-5 inhibitors. Howeve...

journal_title：Expert opinion on investigational drugs

authors： Dewachter L,Dewachter C,Naeije R

更新日期：2010-04-01 00:00:00

abstract：INTRODUCTION:Epithelial ovarian cancer (EOC) is the fourth commonest cause of female cancer death in the developed world. Although progress in treatment has improved survival, ∼ 80% of patients with advanced EOC will experience a recurrence and eventually will become resistant to chemotherapy. The aim of treatment for ...

journal_title：Expert opinion on investigational drugs

authors： Marchetti C,Ledermann JA,Benedetti Panici P

更新日期：2015-01-01 00:00:00

abstract：INTRODUCTION:Cardiovascular disease is the leading cause of death worldwide, accounting for 30% of all deaths, with elevated blood pressure probably the most important modifiable risk factor. Worldwide, elevated blood pressure is estimated to cause 7.5 million deaths, about 12.8% of the total of all annual deaths. New ...

journal_title：Expert opinion on investigational drugs

authors： Segura J,Salazar J,Ruilope LM

更新日期：2013-07-01 00:00:00

abstract：:There is still considerable interest in cephem antibacterial agents. In fact, there are a significant number of patents submitted for this antibacterial class. All the new cephem derivatives, independent of which group they belong to (III to V), possess a 2-amino-5-thiazolyl or a 5-amino-2-thiadiazolyl ring with an ox...

journal_title：Expert opinion on investigational drugs

authors： Bryskier A

更新日期：1997-03-01 00:00:00

abstract：:PDE3 cyclic nucleotide phosphodiesterases are important in cyclic AMP (cAMP) and possibly cyclic GMP-mediated signalling in cardiac and vascular smooth muscle myocytes. Drugs that inhibit these enzymes have inotropic and vasodilatory actions that have proven useful in the short-term treatment of contractile failure an...

journal_title：Expert opinion on investigational drugs

authors： Movsesian MA,Alharethi R

更新日期：2002-11-01 00:00:00

abstract：:Clinical trials of several platelet glycoprotein (GP) IIb/IIIa receptor inhibitors have demonstrated an unequivocal benefit of this potent antithrombotic therapy in high-risk patients with acute coronary syndromes (ACS) as well as in those undergoing percutaneous coronary intervention. In all of these major trials, ho...

journal_title：Expert opinion on investigational drugs

authors： Salam AM

更新日期：2003-09-01 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：INTRODUCTION:Glioblastoma is a primary brain tumor with a poor prognosis despite multimodal therapy including surgery, radiotherapy and alkylating chemotherapy. Novel therapeutic options are therefore urgently needed; however, there have been various drug failures in late-stage clinical development. The proteasome repr...

journal_title：Expert opinion on investigational drugs

authors： Roth P,Mason WP,Richardson PG,Weller M

更新日期：2020-10-01 00:00:00

abstract：BACKGROUND:Pompholyx is a chronic relapsing inflammatory vesicobullous skin disease of the hands and feet belonging to the spectrum of eczema. Established treatments, both topical and systemic, are limited in efficacy, risk:benefit ratio and prevention of further relapses. New treatment options are needed. OBJECTIVE:T...

journal_title：Expert opinion on investigational drugs

authors： Wollina U

更新日期：2008-06-01 00:00:00

abstract：:Restenosis, the re-narrowing of the lumen of the coronary artery, in the months following a successful percutaneous balloon angioplasty or stenting, remains the main limitation to percutaneous coronary revascularisation. Serial intravascular ultrasound studies have shown that restenosis after conventional balloon angi...

journal_title：Expert opinion on investigational drugs

authors： Gruberg L,Waksman R,Satler LF,Pichard AD,Kent KM

更新日期：2000-11-01 00:00:00