Abstract:
INTRODUCTION:Psychostimulants are first-line treatments for attention-deficit/hyperactivity disorder (ADHD), but their tolerability profiles and individual response variability fuel a continuing search for alternative medications. The observation that nicotinic agents improve cognition has led pharmaceutical companies to explore the potential utility of agonists of the nicotinic acetylcholine receptor (nAChR) system for ADHD treatments. AREAS COVERED:This article reviews Phase I and Phase II trials of sofinicline (ABT-894), an agonist of the nAChR α4β2 subtype, as a potential non-stimulant treatment for ADHD. This includes one Phase II trial that compared sofinicline with atomoxetine, a noradrenergic reuptake inhibitor currently approved as a non-stimulant ADHD treatment. This article also reviews the chemistry, pharmacodynamics and pharmacokinetics of sofinicline. EXPERT OPINION:Sofinicline appears to be well tolerated and showing efficacy similar to that of atomoxetine. Although the number of patients studied to date is small, further evaluation of sofinicline in Phase II, and possibly Phase III, trials appears to be warranted. Additional studies are needed to explore the efficacy and tolerability of sofinicline with respect to: i) optimal dosing; ii) its use in combination with other medications for ADHD; and iii) its use in children and adolescents, who more commonly experience adverse effects when taking psychostimulant medications.
journal_name
Expert Opin Investig Drugsjournal_title
Expert opinion on investigational drugsauthors
Fleisher C,McGough Jdoi
10.1517/13543784.2014.934806subject
Has Abstractpub_date
2014-08-01 00:00:00pages
1157-63issue
8eissn
1354-3784issn
1744-7658journal_volume
23pub_type
杂志文章,评审abstract::Type 2 diabetes is a chronic metabolic disease that adversely affects both the quality and longevity of life. The disease is characterised by elevated blood glucose (hyperglycaemia) that is associated with microvascular complications and increased macrovascular risk. Existing oral agents, either alone or in combinatio...
journal_title:Expert opinion on investigational drugs
pub_type: 杂志文章,评审
doi:10.1517/13543784.17.2.145
更新日期:2008-02-01 00:00:00
abstract::The outcome of patients with gastrointestinal stromal tumors has been dramatically improved by therapy with imatinib mesilate (imatinib mesylate), a KIT and platelet-derived growth factor (PDGFR) tyrosine kinase inhibitor. Unfortunately, the majority of patients eventually experience disease progression due to drug re...
journal_title:Expert opinion on investigational drugs
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abstract::Increasing evidence suggests an important role for autocrine/paracrine prolactin in breast and prostate cancers and other disease states. Prolactin production in these extrapituitary sites is not governed by dopamine agonists, a finding that has spurred the production of prolactin receptor antagonists. This review foc...
journal_title:Expert opinion on investigational drugs
pub_type: 杂志文章,评审
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abstract::Introduction: Neuropathic pain is a chronic condition that significantly affects the quality of life of millions of people globally. Most of the pharmacologic treatments currently in use demonstrate modest efficacy and over half of all patients do not respond to medical management. Hence, there is a need for new, effi...
journal_title:Expert opinion on investigational drugs
pub_type: 杂志文章,评审
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abstract::Growth hormone-insensitivity syndrome (GHIS) is usually caused by mutations in the growth hormone receptor. Recombinant IGF-I has been used to treat GHIS either alone (mecasermin) or in combination with IGF-binding protein (IGFBP)-3 (mecasermin rinfabate). IGF-I increases the growth velocity of children with IGF defic...
journal_title:Expert opinion on investigational drugs
pub_type: 杂志文章,评审
doi:10.1517/13543784.15.4.409
更新日期:2006-04-01 00:00:00
abstract::Therapeutic angiogenesis is a novel approach to the treatment of ischaemic or occlusive coronary and peripheral vascular disease. The therapeutic concept is based on the restoration of distal blood flow by the enlargement of existing vessels and tissue perfusion by the induction of new capillaries. Initial studies hav...
journal_title:Expert opinion on investigational drugs
pub_type: 杂志文章,评审
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abstract::Olpadronate is a nitrogenated bisphosphonate. Although it shares the therapeutic and pharmacological properties of pamidronate and alendronate, it has a greater dosage amplitude, more predictable effects and a greater digestive tolerability than other bisphosphates. Therefore, it may be more appropriate in the treatme...
journal_title:Expert opinion on investigational drugs
pub_type: 杂志文章
doi:10.1517/13543784.7.9.1521
更新日期:1998-09-01 00:00:00
abstract::With FDA approval of monoclonal antibodies (mAb) against the B-cell-specific cell surface molecule CD20, immunotherapy in B-cell non-Hodgkin's-lymphomas (NHL) has gained momentum. Since the first description of the CD20 mAb and its use in a single patient, it has taken more than 20 years to implement this in current t...
journal_title:Expert opinion on investigational drugs
pub_type: 杂志文章
doi:10.1517/13543784.8.12.2059
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abstract:INTRODUCTION:Myocardial fibrosis is a remarkably dynamic process mediated by different molecular pathways that represent potential targets of novel therapeutic interventions. Transforming Growth Factor-beta (TGF-β), connective Tissue Growth Factor (cTGF) and Galectin-3 (Gal-3) represent the most promising targets on wh...
journal_title:Expert opinion on investigational drugs
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journal_title:Expert opinion on investigational drugs
pub_type: 杂志文章,评审
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abstract::Immunosuppressant drugs are crucial in order to protect transplanted kidney, heart or liver against the body's natural defence mechanisms. These drugs are used to prevent both acute rejection of the organ as well as chronic deterioration of the graft over longer periods of time. Currently used immunosuppressant drugs ...
journal_title:Expert opinion on investigational drugs
pub_type: 杂志文章,评审
doi:10.1517/13543784.14.3.295
更新日期:2005-03-01 00:00:00
abstract::Argatroban, a synthetic peptidomimetic antithrombin agent, is the first clinical anticoagulant solely to target thrombin. For some time, this drug has been used in Japan for the management of thromboembolic disorders. Recently, it has been approved in Japan for use in thrombotic and ischaemic stroke. Despite a large n...
journal_title:Expert opinion on investigational drugs
pub_type: 杂志文章
doi:10.1517/13543784.8.5.625
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abstract:INTRODUCTION:Chagas disease treatment relies on the lengthy administration of benznidazole and/or nifurtimox, which have frequent toxicity associated. The disease, caused by the parasite Trypanosoma cruzi, is mostly diagnosed at its chronic phase when life-threatening symptomatology manifest in approximately 30% of tho...
journal_title:Expert opinion on investigational drugs
pub_type: 杂志文章
doi:10.1080/13543784.2020.1793955
更新日期:2020-09-01 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
pub_type: 杂志文章
doi:10.1517/13543784.7.4.633
更新日期:1998-04-01 00:00:00
abstract:INTRODUCTION:GLP-1 receptor agonists have been shown to be effective in the treatment of type 2 diabetes mellitus (T2DM). Although the first GLP-1 receptor agonist, exenatide, was approved in the mid-2000s, other agents with longer durations of action (that do not require twice-daily dosing) are now being developed. In...
journal_title:Expert opinion on investigational drugs
pub_type: 杂志文章,评审
doi:10.1517/13543784.2012.638282
更新日期:2012-01-01 00:00:00
abstract::Considerable advances have been made on compounds that are active as inhibitors of HIV entry and fusion. The discovery of chemokines a few years ago focused the attention on coreceptor inhibitors in addition to fusion and attachment blockers. During the last 5 years, there has been an intense research activity from bo...
journal_title:Expert opinion on investigational drugs
pub_type: 杂志文章,评审
doi:10.1517/13543784.16.1.11
更新日期:2007-01-01 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
pub_type: 杂志文章,评审
doi:10.1517/13543784.2011.619977
更新日期:2011-11-01 00:00:00
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journal_title:Expert opinion on investigational drugs
pub_type: 杂志文章,评审
doi:10.1517/13543784.12.6.955
更新日期:2003-06-01 00:00:00
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journal_title:Expert opinion on investigational drugs
pub_type: 杂志文章
doi:10.1517/13543784.7.10.1683
更新日期:1998-10-01 00:00:00
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journal_title:Expert opinion on investigational drugs
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abstract::This review focuses on the clinical development of the prototype broad spectrum inhibitor of cyclin-dependent kinases (CDKs), flavopiridol, now undergoing Phase II single-agent trials and Phase I combination trials (with paclitaxel and cisplatin). Preclinically, flavopiridol is a potent inhibitor of CDKs 1, 2 and 4 in...
journal_title:Expert opinion on investigational drugs
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journal_title:Expert opinion on investigational drugs
pub_type: 杂志文章,评审
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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
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journal_title:Expert opinion on investigational drugs
pub_type: 杂志文章,评审
doi:10.1517/13543784.2015.1038341
更新日期:2015-01-01 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
pub_type: 评论,杂志文章
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更新日期:2012-08-01 00:00:00
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journal_title:Expert opinion on investigational drugs
pub_type: 杂志文章,评审
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更新日期:2002-11-01 00:00:00
abstract::The main cause of illness and death after the first year of heart transplantation is vasculopathy of the cardiac allograft, probably initiated by early immunological and non-immunological endothelial damage. The incidence of multiple episodes of grade 3A rejection 6 months after primary heart transplantation was lower...
journal_title:Expert opinion on investigational drugs
pub_type: 杂志文章
doi:10.1517/13543784.13.2.161
更新日期:2004-02-01 00:00:00
abstract::Therapeutic angiogenesis has yielded promising results in animal models, including the demonstration of newly created blood vessels, increased perfusion and functional benefits. On the other hand, clinical studies using similar methods of angiogenesis have so far been disappointing. The possibility that endothelial dy...
journal_title:Expert opinion on investigational drugs
pub_type: 杂志文章,评审
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更新日期:2005-01-01 00:00:00
abstract::The interaction between the urokinase receptor (uPAR) and its ligand urokinase (uPA) mediates phenomena such as tissue remodelling, chemotaxis, tumour invasion, dissemination, proliferation, and angiogenesis. The broad-spectrum of biological processes that the uPA/uPAR interaction plays a role in has led researchers t...
journal_title:Expert opinion on investigational drugs
pub_type: 杂志文章
doi:10.1517/13543784.7.3.391
更新日期:1998-03-01 00:00:00
abstract:INTRODUCTION:About 185,000,000 people worldwide are chronically infected with hepatitis C virus (HCV). Currently, the most successful HCV infection antiviral therapies reduce the chance of progression towards the advanced phases of the hepatopathy (liver cirrhosis, hepatocellular carcinoma and death). Recently, however...
journal_title:Expert opinion on investigational drugs
pub_type: 杂志文章,评审
doi:10.1517/13543784.2015.1059820
更新日期:2015-01-01 00:00:00