VTX-1463, a novel TLR8 agonist for the treatment of allergic rhinitis.

abstract：:The Kunitz-type proteinase inhibitor, tissue factor pathway inhibitor (TFPI), is the only endogenous inhibitor of the tissue factor (TF)-mediated coagulation pathway that plays a dominant role in normal haemostasis. TFPI exerts its action by binding to factor Xa (FXa) forming a TFPI-FXa complex that then, in a second ...

journal_title：Expert opinion on investigational drugs

authors： Kaiser B,Hoppensteadt DH,Fareed J

更新日期：1998-07-01 00:00:00

abstract：IMPORTANCE OF THE FIELD:Curcumin has been investigated in preclinical and translational stroke models because of its pleiotropic 'neuroprotective' activities. Since curcumin has poor blood-brain barrier (BBB) penetration following acute administration, creative medicinal chemistry has been used to modify the parent cur...

journal_title：Expert opinion on investigational drugs

authors： Lapchak PA

更新日期：2011-01-01 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：:Many peptides are synthesised and released from the gastrointestinal tract. Although their roles in the regulation of gastrointestinal function have been known for some time, it has become increasingly evident that they also influence eating behaviour. Peptide YY (PYY) is released postprandially from gastrointestinal ...

journal_title：Expert opinion on investigational drugs

authors： Small CJ,Bloom SR

更新日期：2005-05-01 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：BACKGROUND:Age-related macular degeneration (AMD) affects > 14 million individuals worldwide. Although 90% of patients with AMD have the dry form, neovascular AMD accounts for the vast majority of patients who develop legal blindness. Until recently, few treatment options existed for treatment of neovascular AMD. The a...

journal_title：Expert opinion on investigational drugs

authors： Dixon JA,Oliver SC,Olson JL,Mandava N

更新日期：2009-10-01 00:00:00

abstract：:Celiac disease is an autoimmune condition affecting genetically susceptible individuals. It is produced by the ingestion of gluten contained in wheat, rye, barley, and related products. The only treatment currently available is strict adherence to a gluten-free diet for life. This requirement for dietary compliance is...

journal_title：Expert opinion on investigational drugs

authors： Rodrigo L

更新日期：2009-12-01 00:00:00

abstract：:Standard drug therapy of adult polymyositis, dermatomyositis and inclusion body myositis includes high-dose corticosteroids and cytotoxic drugs (methotrexate, azathioprine (AZA) and cyclophosphamide). Recent data are in favour of the early introduction of a cytotoxic or immunomodulating drug in addition to corticoster...

journal_title：Expert opinion on investigational drugs

authors： Fam AG

更新日期：2001-07-01 00:00:00

abstract：INTRODUCTION:There has been a striking increase in the emergence of multidrug-resistant pathogens in recent times. Delafloxacin is a novel, broad-spectrum fluoroquinolone with antimicrobial activity against resistant Gram-positive, Gram-negative and anaerobic organisms. It has the potential to treat a variety of infect...

journal_title：Expert opinion on investigational drugs

authors： Bassetti M,Della Siega P,Pecori D,Scarparo C,Righi E

更新日期：2015-03-01 00:00:00

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

authors： Martínez-Peinado N,Cortes-Serra N,Losada-Galvan I,Alonso-Vega C,Urbina JA,Rodríguez A,VandeBerg JL,Pinazo MJ,Gascon J,Alonso-Padilla J

更新日期：2020-09-01 00:00:00

abstract：:Diminished efficacy in terms of clinical relapses and lesion load on magnetic resonance images for patients developing neutralising antibodies (NAbs) to recombinant IFN-beta may be found in multiple sclerosis. NAbs become detectable over the first few years of therapy, disappearing during the treatment course in some ...

journal_title：Expert opinion on investigational drugs

authors： Bagnato F,Pozzilli C

更新日期：2003-07-01 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：INTRODUCTION:Frontline chemotherapy is successful against chronic lymphocytic leukemia (CLL), but results in untoward toxicity. Further, prognostic factors, cytogenetic anomalies, and compensatory cellular signaling lead to therapy resistance or disease relapse. Therefore, for the past few years, development of targete...

journal_title：Expert opinion on investigational drugs

authors： Vangapandu HV,Jain N,Gandhi V

更新日期：2017-05-01 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：:Telomerase is a holoenzyme responsible for the maintenance of telomeres, the protein-nucleic acid complexes at the ends of eukaryotic chromosomes that serve to maintain chromosomal stability and integrity. Telomerase activity is essential for the sustained proliferation of most immortal cells, including cancer cells. ...

journal_title：Expert opinion on investigational drugs

authors： Perry PJ,Arnold JR,Jenkins TC

更新日期：2001-12-01 00:00:00

abstract：INTRODUCTION:Gut-specific homing is mainly mediated by the expression of MAdCAM-1 on endothelial cells. An increase in MAdCAM-1 expression has been shown in patients with inflammatory bowel disease (IBD). Areas covered: PF-00547659 is a fully human monoclonal antibody (mAb) toward MAdCAM-1 on endothelial cells, blockin...

journal_title：Expert opinion on investigational drugs

authors： Allocca M,Gilardi D,Fiorino G,Furfaro F,Argollo M,Peyrin-Biroulet L,Danese S

更新日期：2018-07-01 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：:In spite of tremendous efforts to control cancer, the mortality associated with this disease has been increasing in developed countries in the recent decades. Inadequate efficiency of existing therapeutic regimens and the rise of multi-drug resistant cancer cells are the main factors which require a broadening of inve...

journal_title：Expert opinion on investigational drugs

authors： Pasechnik V

更新日期：2000-06-01 00:00:00

abstract：INTRODUCTION:Peripheral arterial disease (PAD) is a manifestation, and marker of severity, of a generalized atherosclerotic process. Antiplatelet therapy is recommended to prevent cardiovascular events but much of the evidence to support this is drawn from studies on older drugs. AREAS COVERED:In this review, the auth...

journal_title：Expert opinion on investigational drugs

authors： Chong AY,So DY

更新日期：2014-12-01 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：:The annual meeting of the American Diabetes Association was held in Boston, MA. There were over 6500 participants, one-third from overseas, and 1103 papers were presented. Abstracts from the meeting have been published, from which abstract numbers are given below, e.g., (A141). Considerable progress has been made in u...

journal_title：Expert opinion on investigational drugs

authors： Colca J

更新日期：1997-08-01 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：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 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：: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: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：:Tuberculosis (TB), which kills more people than any other infectious disease, was declared a global emergency by the World Health Organization in 1993. The emergence of new Mycobacterium tuberculosis strains that are resistant to some or all current antitubercular drugs seriously hampers the control of the disease. Up...

journal_title：Expert opinion on investigational drugs

authors： Kremer LS,Besra GS

更新日期：2002-08-01 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

authors： Weidle UH,König B

更新日期：1998-03-01 00:00:00

abstract：INTRODUCTION:Type 2 diabetes is a chronic metabolic disease characterized by persistent hyperglycemia resulting from progressive deficient of insulin in patients with a background of insulin resistance. Current treatment algorithms recommended by American Diabetes Association/The European Association for the Study of D...

journal_title：Expert opinion on investigational drugs

authors： Tan X,Cao X,Zhou M,Zou P,Hu J

更新日期：2017-09-01 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