abstract：INTRODUCTION:The introduction and exploration of novel agents has significantly improved patient outcome in the treatment of multiple myeloma (MM). One such compound, bortezomib, was the first proteasome inhibitor (PI) to be approved as a MM therapeutic. The efficacy and safety data provided by bortezomib usage has pro...

journal_title：Expert opinion on investigational drugs

authors： Bringhen S,Gay F,Donato F,Troia R,Mina R,Palumbo A

更新日期：2014-09-01 00:00:00

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 ...

journal_title：Expert opinion on investigational drugs

authors： Fleisher C,McGough J

更新日期：2014-08-01 00:00:00

abstract：INTRODUCTION:IL-6 is a key cytokine in the pathogenesis of rheumatoid arthritis (RA). The clinical efficacy of tocilizumab (TCZ), a humanized anti-IL6-receptor mAb, confirmed the value of IL-6 blockade in this disease. A number of new anti-IL-6 biologics are currently in Phase I - III of clinical development for RA. A...

journal_title：Expert opinion on investigational drugs

authors： Semerano L,Thiolat A,Minichiello E,Clavel G,Bessis N,Boissier MC

更新日期：2014-07-01 00:00:00

abstract：INTRODUCTION:Aberrant regulation of platelet-derived growth factors (PDGFs) and their receptors (PDGFR) has been shown to be involved in many solid tumors, including breast cancer. PDGFR-α and PDGFR-β expressions were documented in breast cancer and are correlated with tumor aggressiveness and metastasis. Preclinical e...

journal_title：Expert opinion on investigational drugs

authors： Criscitiello C,Gelao L,Viale G,Esposito A,Curigliano G

更新日期：2014-05-01 00:00:00

abstract：INTRODUCTION:Heat shock protein 90 (HSP90) serves as a critical facilitator for oncogene addiction. There has been augmenting enthusiasm in pursuing HSP90 as an anticancer strategy. In fact, since the initial serendipitous discovery that geldanamycin (GM) inhibits HSP90, the field has rapidly moved from proof-of-concep...

journal_title：Expert opinion on investigational drugs

authors： Jhaveri K,Ochiana SO,Dunphy MP,Gerecitano JF,Corben AD,Peter RI,Janjigian YY,Gomes-DaGama EM,Koren J 3rd,Modi S,Chiosis G

更新日期：2014-05-01 00:00:00

abstract：INTRODUCTION:The introduction of therapy with tumor necrosis factor antagonists (aTNF) was a cornerstone of treatment modalities in patients with ankylosing spondylitis (AS). After > 10 years of using aTNF, the introduction of aTNF therapy was a major step forward in the medical management of patients with spondyloarth...

journal_title：Expert opinion on investigational drugs

authors： Braun J,Baraliakos X,Heldmann F,Kiltz U

更新日期：2014-05-01 00:00:00

abstract：INTRODUCTION:Melanoma is one of the most aggressive forms of cutaneous malignancies displaying a substantial mortality rate among the various forms of skin cancers. The management of patients with advanced melanoma poses a significant challenge considering that the disease is refractory to most conventional therapies. ...

journal_title：Expert opinion on investigational drugs

authors： Bhatia S,Emdad L,Das SK,Hamed H,Dent P,Sarkar D,Fisher PB

更新日期：2014-04-01 00:00:00

abstract：INTRODUCTION:Approximately 300 million people worldwide are currently affected by asthma. Improvements in the understanding of the mechanisms involved in such inflammatory airway disorders has led to the recognition of new therapeutic approaches. Heparin, a widely used anticoagulant, has been shown to be beneficial in ...

journal_title：Expert opinion on investigational drugs

authors： Shastri MD,Peterson GM,Stewart N,Sohal SS,Patel RP

更新日期：2014-03-01 00:00:00

abstract：INTRODUCTION:The N-methyl-d-aspartate receptor-ionophore complex plays a key role in learning and memory and has efficacy in animals and humans with affective disorders. GLYX-13 is an N-methyl-d-aspartate receptor (NMDAR) glycine-site functional partial agonist and cognitive enhancer that also shows rapid antidepressan...

journal_title：Expert opinion on investigational drugs

authors： Moskal JR,Burch R,Burgdorf JS,Kroes RA,Stanton PK,Disterhoft JF,Leander JD

更新日期：2014-02-01 00:00:00

abstract：INTRODUCTION:The purpose of this article is to highlight novel therapies that are being used in scleroderma (SSc). Therapeutic interventions in SSc generally target at least one of three ongoing biological processes characteristic of the disease: vasculopathy, autoimmunity and tissue fibrosis. Treatment decisions in SS...

journal_title：Expert opinion on investigational drugs

authors： McMahan ZH,Wigley FM

更新日期：2014-02-01 00:00:00

abstract：INTRODUCTION:The ubiquitin-proteasome system (UPS) is responsible for the degradation of misfolded or damaged proteins, regulating inflammatory processes and cell cycle progression. The aim of this article is to summarize the currently available data regarding the possible utility of proteasome inhibitors (PIs) in the ...

journal_title：Expert opinion on investigational drugs

authors： Kandilis AN,Karidis NP,Kouraklis G,Patsouris E,Vasileiou I,Theocharis S

更新日期：2014-01-01 00:00:00

abstract：:Insulin-sensitizing thiazolidinediones (TZDs) correct a root cause of type 2 diabetes and potentially other diseases of metabolic dysfunction, including conditions ranging from oncologic, inflammatory, and neurodegenerative diseases. Importantly, compounds with this mode of action can modify disease progression, as op...

journal_title：Expert opinion on investigational drugs

authors： Colca JR,Tanis SP,McDonald WG,Kletzien RF

更新日期：2014-01-01 00:00:00

abstract：INTRODUCTION:Epithelial ovarian cancer (EOC) is the leading cause of gynaecologic cancer death. Although in some cases initial treatment is effective, most of the women diagnosed with EOC will probably need medical treatment for their disease. There is a critical need to develop effective new strategies for the managem...

journal_title：Expert opinion on investigational drugs

authors： Morotti M,Becker CM,Menada MV,Ferrero S

更新日期：2013-10-01 00:00:00

abstract：INTRODUCTION:The current standard treatment in persons with hemophilia (PWH) is prophylaxis, given intravenously twice or thrice weekly, which is associated with a non negligible burden on patients' quality of life. Therefore the main attempts aiming to improve the management of PWH are targeted towards the development...

journal_title：Expert opinion on investigational drugs

authors： Mannucci PM,Mancuso ME

更新日期：2013-08-01 00:00:00

abstract：INTRODUCTION:The highly divergent histological heterogeneities, aggressive invasion and extremely poor response to treatment make glioblastoma (GBM) one of the most lethal and difficult cancers in humans. Among key elements driving its behavior is epidermal growth factor receptor (EGFR), however, neither traditional th...

journal_title：Expert opinion on investigational drugs

authors： Gao Q,Lei T,Ye F

更新日期：2013-08-01 00:00:00

abstract：BACKGROUND:Age-related macular degeneration is the leading cause of blindness among elderly individuals in industrialized countries. New drugs and advanced concepts for the treatment of dry AMD (dAMD) are needed. A new approach is the application of intravenous infusions of prostaglandin E1. OBJECTIVE:The aim of this ...

journal_title：Expert opinion on investigational drugs

authors： Augustin AJ,Diehm C,Grieger F,Bentz J

更新日期：2013-07-01 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：INTRODUCTION:Because of the central role of the mammalian target of rapamycin (mTOR) pathway in the control and distribution of signals essential for mRNA translation of mitogenic genes and generation of oncogenic proteins, effective targeting of mTOR remains a major goal in medical oncology. AREAS COVERED:This articl...

journal_title：Expert opinion on investigational drugs

authors： Nelson V,Altman JK,Platanias LC

更新日期：2013-06-01 00:00:00

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：INTRODUCTION:Dysregulation of the Janus kinase-signal transducer and activator of transcription (JAK-STAT) pathway is central to the pathophysiology of myeloproliferative neoplasms (MPN). Small molecule inhibitors of JAK family members are currently under investigation for the treatment of MPN. Of these, ruxolitinib ha...

journal_title：Expert opinion on investigational drugs

authors： Tam CS,Verstovsek S

更新日期：2013-06-01 00:00:00

abstract：INTRODUCTION:AEG 35156 is an antisense oligonucleotide to X-linked inhibitor of apoptosis protein (XIAP). Overexpression of XIAP is common in acute myeloid leukemia (AML) and other cancers and is thought to cause resistance to cancer therapy. Effective treatment options for patients with relapsed or refractory AML are ...

journal_title：Expert opinion on investigational drugs

authors： Katragadda L,Carter BZ,Borthakur G

更新日期：2013-05-01 00:00:00

abstract：INTRODUCTION:Vascular-disrupting agents (VDAs) are a new class of oncology drugs, which specifically target established tumor neovasculature and have a relatively low toxicity profile. VDAs generally have non-overlapping side effects when concomitantly used with conventional cytotoxics. Several members of the VDA class...

journal_title：Expert opinion on investigational drugs

authors： Mita MM,Sargsyan L,Mita AC,Spear M

更新日期：2013-03-01 00:00:00

abstract：INTRODUCTION:Asthma is a major disease burden worldwide. Treatment with steroids and long acting β-agonists effectively manage symptoms in many patients but do not treat the underlying cause of disease and have serious side effects when used long term and in children. Therapies targeting the underlying causes of asthma...

journal_title：Expert opinion on investigational drugs

authors： Hansbro PM,Scott GV,Essilfie AT,Kim RY,Starkey MR,Nguyen DH,Allen PD,Kaiko GE,Yang M,Horvat JC,Foster PS

更新日期：2013-01-01 00:00:00

abstract：INTRODUCTION:Tetomilast is a novel thiazole phosphodiesterase-4 (PDE-4) inhibitor, which may prove useful in both the treatment of inflammatory bowel disease (IBD) and chronic obstructive pulmonary disease (COPD). Here, the authors review the pharmacology of the drug, and offer critical review of the available data for...

journal_title：Expert opinion on investigational drugs

authors： Bickston SJ,Snider KR,Kappus MR

更新日期：2012-12-01 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 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: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：:New therapies targeting critical elements of the cell cycle open novel and attractive avenues for the treatment of cancer patients. At present, the number of clinical trials that are registered with the European Organization for Research and Treatment of Cancer (EORTC) and with the US National Cancer Institute, which ...

journal_title：Expert opinion on investigational drugs

authors： Berg T,Bug G,Ottmann OG,Strebhardt K

更新日期：2012-08-01 00:00:00

abstract：INTRODUCTION:Sorafenib is an oral multikinase inhibitor with anti-angiogenic and anti-proliferative activity that is indicated for use in hepatocellular and renal cell carcinomas. Sorafenib is being developed in a number of solid tumors, including breast cancer (BC). AREAS COVERED:A series of four randomized, double-b...

journal_title：Expert opinion on investigational drugs

authors： Gradishar WJ

更新日期：2012-08-01 00:00:00

abstract：:It is now widely accepted that the renin-angiotensin system (RAS) not only contributes to pathological mechanisms involved, e.g. in hypertension or hypertensive and diabetic end-organ damage, but also harbors a "protective arm" represented mainly by two receptors, the AT2 (angiotensin type 2) receptor and the Mas rece...

journal_title：Expert opinion on investigational drugs

authors： Steckelings UM,Unger T

更新日期：2012-06-01 00:00:00

abstract：INTRODUCTION:Regorafenib (BAY 73-4506) is a novel, orally active, diphenylurea multikinase inhibitor of VEGFR1-3, c-KIT, TIE-2, PDGFR-β, FGFR-1, RET, RAF-1, BRAF and p38 MAP kinase. AREAS COVERED:This review covers the preclinical development of regorafenib as well as the pivotal Phase I studies. The safety profile of...

journal_title：Expert opinion on investigational drugs

authors： Strumberg D,Schultheis B

更新日期：2012-06-01 00:00:00

abstract：INTRODUCTION:Aurora kinases are key regulators of mitosis and inhibition of Aurora kinase activity is a rational therapeutic strategy in the treatment of solid tumors and hematological malignancies. AREAS COVERED:This paper will provide an updated summary of preclinical and clinical experience with ENMD-2076 in hemato...

journal_title：Expert opinion on investigational drugs

authors： How J,Yee K

更新日期：2012-05-01 00:00:00

abstract：INTRODUCTION:Pro-protein [corrected] convertase subtilisin kexin (PCSK)-9 is a newly discovered protein involved in intracellular and extracellular regulation of low-density lipoprotein receptor (LDLR) expression. Autosomal dominant activating mutations in PCSK-9 cause familial hypercholesterolaemia whereas inactivatin...

journal_title：Expert opinion on investigational drugs

authors： Wierzbicki AS,Hardman TC,Viljoen A

更新日期：2012-05-01 00:00:00

abstract：INTRODUCTION:Progesterone receptor (PR) agonists (progestins) and antagonists are developed for female contraceptives. However, non-contraceptive applications of newer progestins and PR modulators are being given more attention. AREAS COVERED:The newer PR agonists including drospirenone, nomegestrol, trimegestone, die...

journal_title：Expert opinion on investigational drugs

authors： Su Y,Lian QQ,Ge RS

更新日期：2012-01-01 00:00:00

abstract：INTRODUCTION:Despite recent advances, pulmonary arterial hypertension (PAH) remains a devastating disease which harbors a poor prognosis. Novel therapeutic approaches directly targeting pulmonary vascular remodeling are warranted. AREAS COVERED:This review delineates the current limitations in the management of PAH an...

journal_title：Expert opinion on investigational drugs

authors： ten Freyhaus H,Dumitrescu D,Berghausen E,Vantler M,Caglayan E,Rosenkranz S

更新日期：2012-01-01 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

authors： Garber AJ

更新日期：2012-01-01 00:00:00

abstract：BACKGROUND:Interferon-alpha (IFN-α) is the traditional therapeutic agent for chronic myeloid leukemia (CML). The molecular mechanism of IFN-α efficacy in the treatment of CML is not fully clear. OBJECTIVES:To identify the peptides and/or proteins that bind to the proteins specifically expressed on the surface of IFN-α...

journal_title：Expert opinion on investigational drugs

authors： Liu J,Chen HC,Rao ZZ,Khan MA,Wan XX,Xu AH,Zhang N,Zhang DZ

更新日期：2011-12-01 00:00:00

abstract：INTRODUCTION:The progression of the mammalian cell cycle is driven by the transient activation of complexes consisting of cyclins and cyclin-dependent kinases (CDKs). Loss of control over the cell cycle results in accelerated cell division and malignant transformation and can be caused by the upregulation of cyclins, t...

journal_title：Expert opinion on investigational drugs

authors： Węsierska-Gądek J,Kramer MP

更新日期：2011-12-01 00:00:00

abstract：INTRODUCTION:Obesity is a major health threat in the Western world because of its high incidence and prevalence, and its association with metabolic and cardiovascular disease as well as cancer. The reduction of food intake in obese patients can be achieved only transiently (generally for no longer than 6 months), in th...

journal_title：Expert opinion on investigational drugs

authors： Folli F,Guardado Mendoza R

更新日期：2011-12-01 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