Small-molecule EGFR tyrosine kinase inhibitors for the treatment of cancer.

abstract：:COPD is a chronic disease of the lung that is characterised by decreased air flow and associated abnormal inflammatory responses of the lungs. A total of 80% of COPD incidences are observed in patients with history of smoking tobacco. The chronic condition of COPD is characterised by airway remodelling, which leads to...

journal_title：Expert opinion on investigational drugs

authors： Srivastava PK,Dastidar SG,Ray A

更新日期：2007-07-01 00:00:00

abstract：:Toll-like receptors (TLRs) form a family of pattern recognition receptors that have emerged as key mediators of innate immunity. These receptors sense invading microbes and initiate the immune response. TLR-mediated inflammation is an important pathogenic link between innate immunity and a diverse panel of clinical di...

journal_title：Expert opinion on investigational drugs

authors： Földes G,von Haehling S,Anker SD

更新日期：2006-08-01 00:00:00

abstract：INTRODUCTION:The significant proportion of gout patients not reaching serum urate levels below 6.0 mg/dL and the debated pathogenicity of hyperuricemia (HU) itself motivate investigators to develop new drugs to decrease uricemia. AREAS COVERED:This review discusses the drugs considered to be in active development from...

journal_title：Expert opinion on investigational drugs

authors： Pascart T,Richette P

更新日期：2018-05-01 00:00:00

abstract：:The management of acute myocardial infarction (AMI) has changed dramatically over the last two decades, with the addition of fibrinolytic agents and primary coronary intervention (PCI). The more recent development of the glycoprotein (GP) IIb/IIIa antagonists, a new class of potent antiplatelet drugs, has the potentia...

journal_title：Expert opinion on investigational drugs

authors： Ferguson JJ,Vaisman D

更新日期：2001-11-01 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:Basal-like breast cancer is characterized by being triple negative and aggressive. Defects in DNA repair is a promising therapeutic target as BRCA alterations are found in 11 to 42% of these tumors, with a frequency varying according to family history and ethnicity. The oral PARP inhibitors exploit this de...

journal_title：Expert opinion on investigational drugs

authors： Robert M,Frenel JS,Gourmelon C,Patsouris A,Augereau P,Campone M

更新日期：2017-06-01 00:00:00

abstract：:The vasopressin system is complex and interacts with the central nervous, cardiovascular, renal, and hematological systems. Vasopressin plays an important role in the control of blood osmolarity and vascular tone, but is also involved in many other physiological events, which are mediated mainly via three types of vas...

journal_title：Expert opinion on investigational drugs

authors： Favory R,Salgado DR,Vincent JL

更新日期：2009-08-01 00:00:00

abstract：:IL-5 is the predominant cytokine associated with antigen-induced eosinophilic inflammation in the lung. The activation of Th-2 cells leads to the production of IL-5. The pro-eosinophilic effects of IL-5 include: (1) enhanced replication and differentiation of eosinophilic myelocytes; (2) enhanced degranulation of eosi...

journal_title：Expert opinion on investigational drugs

authors： Weltman JK,Karim AS

更新日期：2000-03-01 00:00:00

abstract：:The discovery of new antibacterial drugs can be based either upon empirical screening methods or structure-based design. Empirical methods utilise both intact bacteria and isolated biochemical targets for high throughput screening of natural product or chemical libraries to detect inhibitor leads. Structure-based meth...

journal_title：Expert opinion on investigational drugs

authors： Chopra I

更新日期：1997-08-01 00:00:00

abstract：:BCR-ABL, a constitutively active tyrosine kinase, causes chronic myeloid leukaemia (CML). Rational development of drugs targeting BCR-ABL has significantly improved the treatment of CML. Imatinib (a BCR-ABL tyrosine kinase inhibitor) produces haematological and cytogenetic remissions across all phases of CML and is th...

journal_title：Expert opinion on investigational drugs

authors： Jabbour E,Cortes J,Kantarjian H

更新日期：2007-05-01 00:00:00

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

authors： Kelland LR

更新日期：2000-12-01 00:00:00

abstract：:Introduction: Renal cell carcinoma (RCC) consists of distinct clinical and biologic entities, with an urgent need for novel therapies targeting histology-specific molecular drivers of cancer growth. The MET pathway is now being targeted by multiple novel agents in clinical development. This review highlights the upcom...

journal_title：Expert opinion on investigational drugs

authors： Nandagopal L,Sonpavde GP,Agarwal N

更新日期：2019-10-01 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：:Fatty acid synthase (FASN) is the enzyme that catalyzes the de novo synthesis of fatty acids in cells. Because of the strong expression in many cancers, FASN is an attractive and tractable target for therapeutic intervention. The discovery and development of pharmacologic agents that block FASN activity highlight the ...

journal_title：Expert opinion on investigational drugs

authors： Kridel SJ,Lowther WT,Pemble CW 4th

更新日期：2007-11-01 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：:With the current standard chemotherapy regimens only approximately 25% of acute myelogenous leukaemia (AML) patients survive > 5 years. Aurora kinases are overexpressed in many human cancers. VX-680 inhibited Aurora-A, -B, -C and the FMS-like tyrosine kinase-3 with apparent inhibitory constants of 0.6, 18, 4.6 and 30 ...

journal_title：Expert opinion on investigational drugs

authors： Doggrell SA

更新日期：2004-09-01 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

authors： Citterio P,Rusconi S

更新日期：2007-01-01 00:00:00

abstract：:Human cytomegalovirus (HCMV) is the most common viral opportunistic infection in patients suffering with acquired immunodeficiency virus (AIDS). HCMV is a systemic infection that may infect several sites in the body, including the retina, gastrointestinal tract, lungs, liver, and central nervous system. Retinitis is t...

journal_title：Expert opinion on investigational drugs

authors： Temsamani J,Pari GS,Guinot P

更新日期：1997-09-01 00:00:00

abstract：:Introduction: Osteoarthritis (OA) is the most common form of arthritis. Knee OA is associated with joint pain, activity limitation, physical disability, reduced health-related quality of life, and increased mortality. To date, all pharmacologic treatments for OA are directed toward pain management. Lorecivivint (LOR) ...

journal_title：Expert opinion on investigational drugs

authors： Sabha M,Siaton BC,Hochberg MC

更新日期：2020-12-01 00:00:00

abstract：:Obesity shortens life expectancy and is a risk factor for hypertension and Type 2 diabetes. When added to the standard chow of Sprague-Dawley or Otsuka Long-Evans Tokushima Fatty rats, alpha-lipoic acid (0.5% weight/weight) reduced body weight and food intake. Alpha-lipoic acid also increased whole-body energy expendi...

journal_title：Expert opinion on investigational drugs

authors： Doggrell SA

更新日期：2004-12-01 00:00:00

abstract：:Overactive bladder (OAB) is a chronic distressing condition characterised by urinary urgency with or without urge incontinence, usually with frequency (voiding at least eight times daily) and nocturia. It affects millions of people worldwide independent of age, sex and race. The prevalence increases with age and is re...

journal_title：Expert opinion on investigational drugs

authors： Tiwari A,Naruganahalli KS

更新日期：2006-09-01 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：: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：: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：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：:Bromocriptine, a potent dopamine D(2) receptor agonist, has been shown to reduce insulin resistance, glucose intolerance and hyperlipidaemia in both numerous animal studies and in Phase II studies. Bromocriptine has been used worldwide for over 20 years to treat Parkinson's disease, macroprolactinoma and other disorde...

journal_title：Expert opinion on investigational drugs

authors： Cincotta AH,Meier AH,Cincotta M Jr

更新日期：1999-10-01 00:00:00

abstract：IMPORTANCE OF THE FIELD:Antiangiogenic strategies are affording considerable interest and have become a major milestone in therapeutics of various adult cancers. However, progress has been slow to expand such therapies to patients with pediatric solid malignancies. AREAS COVERED IN THIS REVIEW:This review discusses th...

journal_title：Expert opinion on investigational drugs

authors： Taylor M,Rössler J,Geoerger B,Vassal G,Farace F

更新日期：2010-07-01 00:00:00

abstract：:Carvedilol is a beta-blocker with ancillary properties. Pilot clinical studies with carvedilol, added to the standard therapy of digoxin, diuretics and ACE inhibitors, showed beneficial effects in mild, moderate and severe heart failure. Patients consistently showed improvement in LV ejection fraction and NYHA functio...

journal_title：Expert opinion on investigational drugs

authors： Doggrell SA

更新日期：2001-05-01 00:00:00

abstract：IMPORTANCE OF THE FIELD:Contrasting with the broad activation of the PI3K/AKT/mammalian target of rapamycin (mTOR) survival pathway in most cancer, activity of rapalogues appears to be restricted to a few tumor types. AREAS COVERED IN THIS REVIEW:The analysis of molecular activity of the PI3K/AKT/mTOR pathway and resi...

journal_title：Expert opinion on investigational drugs

authors： Albert S,Serova M,Dreyer C,Sablin MP,Faivre S,Raymond E

更新日期：2010-08-01 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