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 hematological malignancies. The MEDLINE (OVID) (1980 through 31 January 2012) was searched with the term combinations including Aurora, multiple myeloma, leukemia, lymphoma, myelodysplastic syndrome and myeloproliferative neoplasms. In addition, the American Society of Clinical Oncology (ASCO) (1997 - 2011) and the American Society of Hematology (ASH) (1997 - 2011) conference proceedings were searched for reports of new or ongoing trials. EXPERT OPINION:ENMD-2076 is a multi-kinase inhibitor, with activity against Aurora A kinase, FLT3, c-KIT, c-FMS and VEGFR-2 and -3. It appears to be tolerable, exhibits favorable pharmacokinetic profiles and has activity in patients with acute myeloid leukemia and multiple myeloma. Further evaluation with cytotoxic chemotherapy and targeted agents, which affect different pathways and have non-overlapping toxicities, in patients with hematological malignancies are warranted.
journal_name
Expert Opin Investig Drugsjournal_title
Expert opinion on investigational drugsauthors
How J,Yee Kdoi
10.1517/13543784.2012.668882subject
Has Abstractpub_date
2012-05-01 00:00:00pages
717-32issue
5eissn
1354-3784issn
1744-7658journal_volume
21pub_type
杂志文章,评审abstract::PTI-821 is a long-acting formulation of oxycodone that is intended to deter abuse through its gel-cap technology. Produced by Pain Therapeutics in alliance with King Pharmaceuticals, PTI-821 is designed to provide strong pain relief with the intent of offering greater safety than is presently available from convention...
journal_title:Expert opinion on investigational drugs
pub_type: 杂志文章,评审
doi:10.1517/13543784.16.3.359
更新日期:2007-03-01 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
pub_type: 杂志文章,评审
doi:10.1517/13543784.14.5.647
更新日期:2005-05-01 00:00:00
abstract::A major session at this annual gathering of the cancer researchers from around the globe dealt with the current state of immunotherapy for cancer. Immunotherapy is a form of cancer treatment that enhances its scientific promise and legitimacy with each passing year. As a result, this topic has become one of the most h...
journal_title:Expert opinion on investigational drugs
pub_type:
doi:10.1517/13543784.9.6.1413
更新日期:2000-06-01 00:00:00
abstract::Recent landmark studies using hydroxy-methyl-glutaryl-Co-enzyme A reductase inhibitors (HMG-CoA reductase inhibitors or statins), specifically, pravastatin and simvastatin, have led to dramatic changes in medical practice. These clinical trials have demonstrated that clinicians can impact coronary morbidity and mortal...
journal_title:Expert opinion on investigational drugs
pub_type: 杂志文章
doi:10.1517/13543784.6.1.31
更新日期:1997-01-01 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
pub_type: 杂志文章,评审
doi:10.1517/13543784.16.10.1549
更新日期:2007-10-01 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
pub_type: 杂志文章,评审
doi:10.1080/13543784.2016.1208170
更新日期:2016-09-01 00:00:00
abstract:INTRODUCTION:Circadian rhythm is a natural endogenous process occurring roughly every 24 hours. Circadian rhythm dysfunction is involved in diabetic retinopathy (DR) pathogenesis. Interestingly, there are investigational drugs that exhibit potential in the treatment of DR by targeting circadian rhythm dysfunction. ARE...
journal_title:Expert opinion on investigational drugs
pub_type: 杂志文章
doi:10.1080/13543784.2020.1842872
更新日期:2020-12-01 00:00:00
abstract::IBC's 5(th) Annual Conference on Blood Substitutes was held on November 20-21, 1997. Approximately 100 medical researchers, academic scientists, blood substitute company speakers and representatives from major pharmaceutical companies with an interest or partner in the field attended. The papers presented focused on t...
journal_title:Expert opinion on investigational drugs
pub_type: 杂志文章
doi:10.1517/13543784.7.2.283
更新日期:1998-02-01 00:00:00
abstract::Targeting cellular proliferation persists as a mainstay of cancer therapeutic strategy. Although microtubule-targeting drugs (such as taxanes and vinca alkaloids) have been used successfully in the clinic to treat a variety of cancers, they carry substantial liabilities that have spurred drug companies to aggressively...
journal_title:Expert opinion on investigational drugs
pub_type: 杂志文章,评审
doi:10.1517/13543784.15.11.1411
更新日期:2006-11-01 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
pub_type: 杂志文章,评审
doi:10.1080/13543784.2016.1250882
更新日期:2016-12-01 00:00:00
abstract::Phytoestrogens, such as the soya isoflavones genistein and daidzein, are currently being extensively investigated through both molecular, preclinical and clinical studies to determine their potential health benefits. Phytoestrogens may protect against chronic diseases such as hormone-dependent cancer (e.g., breast and...
journal_title:Expert opinion on investigational drugs
pub_type: 杂志文章,评审
doi:10.1517/13543784.9.8.1829
更新日期:2000-08-01 00:00:00
abstract:BACKGROUND:Hematopoietic stem cell (HSC) transplantation is a treatment option for hematological malignancies. Current mobilization regimes frequently result in inadequate numbers of HSC for transplant therefore alternative methods of mobilization are required. OBJECTIVE:The chemokine receptor CXCR4 and ligand SDF-1 a...
journal_title:Expert opinion on investigational drugs
pub_type: 杂志文章,评审
doi:10.1517/13543784.17.11.1749
更新日期:2008-11-01 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
pub_type: 杂志文章,评审
doi:10.1080/13543784.2018.1471133
更新日期:2018-05-01 00:00:00
abstract::Introduction: Therapeutic oligonucleotides have emerged as a promising new class of drug that could silence undruggable targets; they can potentially treat metabolic liver diseases such as nonalcoholic fatty liver disease (NAFLD), hereditary hemochromatosis and alpha 1 antitrypsin deficiency. Areas covered: This artic...
journal_title:Expert opinion on investigational drugs
pub_type: 杂志文章
doi:10.1080/13543784.2021.1879792
更新日期:2021-01-29 00:00:00
abstract::Inhibiting the tyrosine kinase activity of the epidermal growth factor receptor (EGFR) has an established role in the treatment of advanced non-small cell lung cancer. The first-generation EGFR inhibitors erlotinib and gefitinib have been approved for treatment in the second- and third-line setting. Second-generation ...
journal_title:Expert opinion on investigational drugs
pub_type: 杂志文章,评审
doi:10.1517/13543780902762843
更新日期:2009-03-01 00:00:00
abstract::Numerous studies over the last few years have suggested that modulating the glutamatergic system may be an efficient method to achieve an antidepressant effect. Data suggest that metabotropic glutamate receptors (mGlu receptors), related to long-term, modulatory effects on glutamatergic neurotransmission, may be a goo...
journal_title:Expert opinion on investigational drugs
pub_type: 杂志文章,评审
doi:10.1517/13543784.15.12.1545
更新日期:2006-12-01 00:00:00
abstract:INTRODUCTION:Despite the substantial reduction in cardiovascular morbidity and mortality after the management of dyslipidemia with statins, residual risk remains even after achieving low-density lipoprotein cholesterol targets. This residual risk appears to be partly attributed to low levels of high-density lipoprotein...
journal_title:Expert opinion on investigational drugs
pub_type: 杂志文章,评审
doi:10.1080/13543784.2019.1582028
更新日期:2019-04-01 00:00:00
abstract::Age-related macular degeneration (AMD) is the leading cause of blindness in the Western world for those patients aged 50 years or older. Neovascular AMD, a subtype characterized by the growth of new, pathologic blood vessels, results in most of the cases of severe and rapid vision loss associated with AMD. A critical ...
journal_title:Expert opinion on investigational drugs
pub_type: 杂志文章,评审
doi:10.1517/13543780902855316
更新日期:2009-05-01 00:00:00
abstract:INTRODUCTION:Posttraumatic stress disorder (PTSD) is a prevalent, chronic and disabling anxiety disorder that may develop following exposure to a traumatic event. There is currently no effective pharmacotherapy for PTSD and therefore the discovery of novel, evidence-based treatments is particularly important. This revi...
journal_title:Expert opinion on investigational drugs
pub_type: 杂志文章,评审
doi:10.1517/13543784.2015.1020109
更新日期:2015-05-01 00:00:00
abstract::Gene transfer technology is under exploration to find therapies for the treatment of Parkinson's disease (PD) and other neurodegenerative disorders. The technology of genetic transfer can also be used as a neurobiological tool to understand the role of various genes in animal models of neurodegeneration. We describe t...
journal_title:Expert opinion on investigational drugs
pub_type: 杂志文章
doi:10.1517/13543784.8.10.1551
更新日期:1999-10-01 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
pub_type: 杂志文章
doi:10.1517/13543784.8.10.1683
更新日期:1999-10-01 00:00:00
abstract:INTRODUCTION:Ewing sarcoma family tumors (ESFT) are a group of aggressive diseases, characterized histologically by small, round, blue cells and genetically by translocation involving EWS and ETS partner genes. The current treatment of localized Ewing sarcoma (ES) requires a multi-disciplinary approach, including multi...
journal_title:Expert opinion on investigational drugs
pub_type: 杂志文章,评审
doi:10.1517/13543784.2016.1168398
更新日期:2016-06-01 00:00:00
abstract::The epidermal growth factor receptor is a cell membrane growth factor receptor that plays a key role in cancer development and progression. Epidermal growth factor receptor-activated signalling pathways control cell proliferation, apoptosis, angiogenesis and metastatic spread in the majority of human epithelial cancer...
journal_title:Expert opinion on investigational drugs
pub_type: 杂志文章,评审
doi:10.1517/13543784.11.6.755
更新日期:2002-06-01 00:00:00
abstract::Atopic dermatitis (AD) is a common inflammatory disease involving the skin and often other organs and systems, mainly respiratory. A definitive general consensus on the AD pathogenesis has not yet been established, however several lines of evidence suggest that T-cells play a crucial role in priming AD early-stage les...
journal_title:Expert opinion on investigational drugs
pub_type: 杂志文章,评审
doi:10.1517/13543784.10.1.49
更新日期:2001-01-01 00:00:00
abstract::Advances in molecular medicine have revealed a key role for altered gene expression in the aetiology of many inflammatory diseases, including asthma, rheumatoid arthritis, inflammatory bowel disease and sepsis. Until recently, however, modulation of gene transcription has not been the subject of directed pharmaceutica...
journal_title:Expert opinion on investigational drugs
pub_type: 杂志文章
doi:10.1517/13543784.6.5.555
更新日期:1997-05-01 00:00:00
abstract::At present, the nucleoside reverse transcriptase (RT) inhibitors and protease inhibitors (PI) have dominated the therapeutic options for the treatment of human immunodeficiency virus (HIV) infection. From the initial monotherapeutic strategies, to the widely accepted multi-drug cocktails of today, the use of these two...
journal_title:Expert opinion on investigational drugs
pub_type: 杂志文章,评审
doi:10.1517/13543784.10.8.1423
更新日期:2001-08-01 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
pub_type: 杂志文章,评审
doi:10.1517/13543784.16.10.1673
更新日期:2007-10-01 00:00:00
abstract:INTRODUCTION:Dyslipidemia is one of the most important risk factors for cardiovascular disease. Insufficient reduction in LDL-C from existing therapies in patients at high risk of atherogenic cardiovascular disease is an unmet clinical need. Circulating PCSK9 causes hypercholesterolemia by reducing LDL receptors in hep...
journal_title:Expert opinion on investigational drugs
pub_type: 杂志文章,评审
doi:10.1080/13543784.2018.1442435
更新日期:2018-03-01 00:00:00
abstract::Restenosis, the re-narrowing of the lumen of the coronary artery, in the months following a successful percutaneous balloon angioplasty or stenting, remains the main limitation to percutaneous coronary revascularisation. Serial intravascular ultrasound studies have shown that restenosis after conventional balloon angi...
journal_title:Expert opinion on investigational drugs
pub_type: 杂志文章,评审
doi:10.1517/13543784.9.11.2555
更新日期:2000-11-01 00:00:00
abstract::The focus of this meeting was the interface between eating disorders and obesity. A symposium at this meeting dealt with advances in treatment for bulimia nervosa (BN) and binge eating disorder. There were two presentations in this symposium that addressed pharmacological treatments. One reviewed drug treatments for B...
journal_title:Expert opinion on investigational drugs
pub_type:
doi:10.1517/13543784.12.8.1441
更新日期:2003-08-01 00:00:00