Inhibiting signal transducer and activator of transcription 3: rationality and rationale design of inhibitors.

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：:Endothelin-1 (ET-1) is enhanced and has been demonstrated to be a prognostic marker in patients with advanced stages of heart failure, acute ischaemic syndromes, myocardial infarction and pulmonary hypertension. Activation of the endothelin (ET) system is associated with adverse haemodynamic consequences in patients w...

journal_title：Expert opinion on investigational drugs

authors： Neunteufl T,Berger R,Pacher R

更新日期：2002-03-01 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：INTRODUCTION:The Philadelphia chromosome negative myeloproliferative neoplasms (MPN) mainly comprise polycythemia vera (PV), essential thrombocythemia (ET) and myelofibrosis (MF, primary or post-PV/ET). Therapy in PV and ET focuses on minimizing thrombosis and bleeding risk, while in MF, prolongation of survival is an ...

journal_title：Expert opinion on investigational drugs

authors： Bose P,Verstovsek S

更新日期：2016-12-01 00:00:00

abstract：:Vasopressin (AVP) is a cyclic nonapeptide hormone that exhibits many physiological effects including free water reabsorption, vasoconstriction, cellular proliferation and adrenocorticotrophic hormone (ACTH) secretion. In a healthy organism, AVP plays an important role in the homeostasis of fluid osmolality and volume ...

journal_title：Expert opinion on investigational drugs

authors： Paranjape SB,Thibonnier M

更新日期：2001-05-01 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：:Type 2 diabetes and obesity are characterised by insulin and leptin resistance. Studies suggest that these may be due to defects in the insulin and leptin signalling pathways. Over the last decade, a considerable body of evidence has been amassed indicating that protein tyrosine phosphatase 1B (PTP1B) is involved in t...

journal_title：Expert opinion on investigational drugs

authors： Taylor SD,Hill B

更新日期：2004-03-01 00:00:00

abstract：INTRODUCTION:Although significant advances have been made in the treatment of advanced renal cell carcinoma (RCC), patients still develop resistance to standard therapies and require the administration of subsequent lines of treatment. New therapeutic approaches are thus imperative to improve the prognosis for patients...

journal_title：Expert opinion on investigational drugs

authors： Bilen MA,Carlisle JW,Sonpavde G

更新日期：2018-02-01 00:00:00

abstract：INTRODUCTION:Angiogenesis inhibition represents a rational therapeutic strategy in the management of solid tumors. Brivanib is a dual tyrosine kinase inhibitor with selectivity against VEFGR-2 and FGFR. AREAS COVERED:This review provides an updated summary of preclinical and clinical experience with brivanib in cancer...

journal_title：Expert opinion on investigational drugs

authors： Diaz-Padilla I,Siu LL

更新日期：2011-04-01 00:00:00

abstract：:Introduction: The conventional management of most patients with metastatic urothelial carcinoma (UC) is platinum-based chemotherapy followed by immunotherapy. Erdafitinib is an option in post-platinum patients with activating mutations in fibroblast growth factor receptor (FGFR)-3 and -2. Salvage therapy with taxanes ...

journal_title：Expert opinion on investigational drugs

authors： McGregor BA,Sonpavde G

更新日期：2019-10-01 00:00:00

abstract：:Novel classes of antibiotics that are useful against resistant bacteria are a major need in human medicine. Cationic antimicrobial peptides are utilised as nature's antibiotics, being produced constitutively or in response to infection in virtually every type of organism from plants and insects to man. Thus, these pep...

journal_title：Expert opinion on investigational drugs

authors： Hancock RE

更新日期：1998-02-01 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：:Suicide gene therapy is the approach whereby the genetic alteration of a cell renders it susceptible to an otherwise non-toxic prodrug. Suicide gene therapy for solid tumours has progressed rapidly since the concept was originally described: nearly all tumour types have been explored, with some, such as glioma, melano...

journal_title：Expert opinion on investigational drugs

authors： Perry MJ,Todryk SM,Dalgleish AG

更新日期：1999-06-01 00:00:00

abstract：:Methylphenidate (MPH) is one of the most commonly prescribed medications to treat attention deficit hyperactivity disorder (ADHD). Despite the elevated rates of ADHD in children with epilepsy, few studies have examined the use of MPH in this population. Case reports have warned about new-onset seizures in patients tre...

journal_title：Expert opinion on investigational drugs

authors： Baptista-Neto L,Dodds A,Rao S,Whitney J,Torres A,Gonzalez-Heydrich J

更新日期：2008-01-01 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: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：:Gaucher disease (GD) is an inborn error of glycosphingolipid metabolism, associated with multisystemic manifestations resulting from the lysosomal accumulation of an incompletely degraded material (glucosylceramide) within cells of monocyte/macrophage lineage. In the majority of GD patients with non-neurological invol...

journal_title：Expert opinion on investigational drugs

authors： Pastores GM,Barnett NL

更新日期：2003-02-01 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：INTRODUCTION:Minimal change disease (MCD) and Focal and segmental glomerulosclerosis (FSGS) are two of the major causes of nephrotic syndrome (NS) in children and adults. According to KDIGO (Kidney Disease: Improving Global Outcomes) guidelines, the treatment of adult primary MCD and FSGS should be based on immunosuppr...

journal_title：Expert opinion on investigational drugs

authors： Siligato R,Cernaro V,Nardi C,De Gregorio F,Gembillo G,Costantino G,Conti G,Buemi M,Santoro D

更新日期：2018-11-01 00:00:00

abstract：IMPORTANCE OF THE FIELD:Acute myeloid leukemia (AML) and myelodysplastic syndrome (MDS) incidence in the United States increases with age. Given the progressive ageing of the general population, incidence of these diseases is likely to continue to rise in the future. There is an acute need for therapeutic developments ...

journal_title：Expert opinion on investigational drugs

authors： Epling-Burnette PK,Loughran TP Jr

更新日期：2010-05-01 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: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:Noise-induced hearing loss (NIHL) due to industrial, military, and recreational noise exposure is a major, but also potentially preventable cause of acquired hearing loss. For the United States it is estimated that 26 million people (15% of the population) between the ages of 20 and 69 have a high-frequenc...

journal_title：Expert opinion on investigational drugs

authors： Sha SH,Schacht J

更新日期：2017-01-01 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:Since the discovery of the activating V617F mutation in Janus kinase 2 (JAK2), a number of pharmacologic inhibitors of JAK2 have entered clinical trials for patients with myelofibrosis. However, ruxolitinib, approved in 2011, remains the only one currently available for treatment of myelofibrosis, with man...

journal_title：Expert opinion on investigational drugs

authors： Bose P,Abou Zahr A,Verstovsek S

更新日期：2017-06-01 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：:While oral formulations of agonists at the serotonin (5-HT) receptor subdivisions 5-HT(1B/1D)--the "triptan" class of drugs--dominate the market for migraine therapy and while still more triptans are under development, recent research efforts have also explored other pharmacological avenues, which are mostly based on ...

journal_title：Expert opinion on investigational drugs

authors： Mucke H

更新日期：2002-12-01 00:00:00

abstract：:Recent advances in the treatment and management of haematological malignancies are due in large part to an improved understanding of the basic biology that drives tumour cell growth and survival. This improved understanding has led to the clinical study and approval of a number of different targeted agents across a nu...

journal_title：Expert opinion on investigational drugs

authors： Haas M,Lonial S

更新日期：2005-09-01 00:00:00

abstract：:Disruption of a vulnerable atherosclerotic plaque is well-recognised as the primary cause of stroke, non-fatal myocardial infarction and sudden cardiac death. Novel therapeutic agents are being developed to stabilise such plaques. The initial evaluation of these drugs would be facilitated by the use of non-invasive im...

journal_title：Expert opinion on investigational drugs

authors： Sosnovik DE,Muller JE,Kathiresan S,Brady TJ

更新日期：2002-05-01 00:00:00

abstract：IMPORTANCE OF THE FIELD:Antibacterial drug discovery and development has slowed considerably in recent years, with novel classes discovered decades ago and regulatory approvals tougher to get. Traditional approaches and the newer genomic mining approaches have not yielded novel classes of antibacterial compounds. Inste...

journal_title：Expert opinion on investigational drugs

authors： Devasahayam G,Scheld WM,Hoffman PS

更新日期：2010-02-01 00:00:00