Non-BRAF targeted therapies for melanoma: protein kinase inhibitors in Phase II clinical trials.

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:Inhibitors against the PD-1/PD-L1 pathway are revolutionizing the treatment and management of malignancies. AREAS COVERED:We summarize our current understanding of the function of PD-1, its role in immune evasion, the clinical data available that support the use of PD-1 antagonist in Hodgkin and non-Hodgk...

journal_title：Expert opinion on investigational drugs

authors： Chang A,Schlafer D,Flowers CR,Allen PB

更新日期：2018-01-01 00:00:00

abstract：INTRODUCTION:Medical treatment of brain metastases (BM) is still a controversial issue in cancer therapy being mainly limited by the existence of the BBB. Temozolomide (TMZ) can cross BBB and several clinical trials have been performed attempting to demonstrate the activity of TMZ in combination with whole brain radiot...

journal_title：Expert opinion on investigational drugs

authors： Addeo R,Caraglia M

更新日期：2011-07-01 00:00:00

abstract：IMPORTANCE OF THE FIELD:Treatments of pulmonary arterial hypertension (PAH) that have so far proven efficacious are all based on the restoration of endothelium control of pulmonary vascular tone and structure, by administration of prostacyclins, endothelin receptor antagonists and phosphodiesterase-5 inhibitors. Howeve...

journal_title：Expert opinion on investigational drugs

authors： Dewachter L,Dewachter C,Naeije R

更新日期：2010-04-01 00:00:00

abstract：:The role of nerve growth factor in stimulating cholinergic function, loss of which is a cardinal feature in Alzheimer's disease, has been documented for many years from preclinical animal model studies. This anabolic growth factor has been delivered into the forebrain of patients with mild Alzheimer's disease using tr...

journal_title：Expert opinion on investigational drugs

authors： Braddock M

更新日期：2005-07-01 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：BACKGROUND:Histone deacetylases (HDACs), which target histones as well as non-histone proteins as substrates, have the potential to regulate aberrant gene expression and restore normal growth control in malignancies. OBJECTIVE:This review provides an updated summary of preclinical and clinical experience with the oral...

journal_title：Expert opinion on investigational drugs

authors： Le Tourneau C,Siu LL

更新日期：2008-08-01 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：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：INTRODUCTION:The addition of monoclonal antibody (mAb) epidermal growth factor receptor (EGFR) inhibitors to classic chemotherapy doublet backbones has improved survival of metastatic colorectal cancer (mCRC). However, the role of triple-drug chemotherapy regimens in combination with an anti-EGFR mAb inhibitor is not y...

journal_title：Expert opinion on investigational drugs

authors： Matos I,Noguerido A,Ros J,Mulet N,Argilés G,Elez É,Tabernero J

更新日期：2019-05-01 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: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:Metastases to the central nervous system are the most common cause of malignant intracranial tumors in adults. Current standard of care includes surgery and radiation, but overall survival remains poor. A range of systemic therapies are emerging as promising treatment options for these patients. AREAS COV...

journal_title：Expert opinion on investigational drugs

authors： McMahon JT,Faraj RR,Adamson DC

更新日期：2020-12-01 00:00:00

abstract：INTRODUCTION:Axial spondyloarthritis (AxS pA) is a chronic inflammatory disease for which, until recently, there were no valid therapeutic alternatives to TNF-α blocking agents. This unmet clinical need led to explore several therapeutic targets, from proinflammatory cytokines to intracellular signaling systems. The re...

journal_title：Expert opinion on investigational drugs

authors： Clavel G,Boissier MC,Sigaux J,Semerano L

更新日期：2017-07-01 00:00:00

abstract：:There are several reasons to believe that agents that augment cAMP-mediated signalling in cardiac myocytes should have beneficial effects in patients with heart failure. However, clinical trials of first-generation cyclic nucleotide phosphodiesterase (PDE3) inhibitors, which raise cAMP content by blocking its hydrolys...

journal_title：Expert opinion on investigational drugs

authors： Movsesian MA

更新日期：2000-05-01 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：:Argatroban, a synthetic peptidomimetic antithrombin agent, is the first clinical anticoagulant solely to target thrombin. For some time, this drug has been used in Japan for the management of thromboembolic disorders. Recently, it has been approved in Japan for use in thrombotic and ischaemic stroke. Despite a large n...

journal_title：Expert opinion on investigational drugs

authors： Jeske W,Walenga JM,Lewis BE,Fareed J

更新日期：1999-05-01 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：:This paper gives an overview of the available pharmacological and clinical data of a new class of anticancer drugs which act by binding DNA in the minor groove, comprising cyclopropylpyrrolo-indole (CC-1065) derivatives and Distamycin derivatives. The emphasis of this review is placed on the distinctive mode of action...

journal_title：Expert opinion on investigational drugs

authors： D'Incalci M,Sessa C

更新日期：1997-07-01 00:00:00

abstract：INTRODUCTION:Crizotinib is a first-in-class ALK tyrosine kinase inhibitor (TKI), which has proven its superiority over standard platinum-based chemotherapy for the first-line therapy of ALK-rearranged non-small cell lung cancer (NSCLC) patients. The development of acquired resistance to crizotinib represents an ongoing...

journal_title：Expert opinion on investigational drugs

authors： Karachaliou N,Santarpia M,Gonzalez Cao M,Teixido C,Sosa AE,Berenguer J,Rodriguez Capote A,Altavilla G,Rosell R

更新日期：2017-06-01 00:00:00

abstract：:There is a growing understanding of the central role that platelets play in coronary artery disease. The glycoprotein IIb/IIIa receptor has recently been identified as the final common pathway for platelet aggregation and hence has been the focus of many clinical trials to influence various aspects of coronary artery ...

journal_title：Expert opinion on investigational drugs

authors： Salam AM,Suwaidi JA

更新日期：2002-11-01 00:00:00

abstract：:Cholesterol can promote inflammation by its ability to stimulate the production of reactive oxygen species that result in the formation of pro-inflammatory oxidised phospholipids. High-density lipoproteins (HDLs) are part of the innate immune response and can be either pro- or anti-inflammatory independently of plasma...

journal_title：Expert opinion on investigational drugs

authors： Reddy ST,Anantharamaiah GM,Navab M,Hama S,Hough G,Grijalva V,Garber DW,Datta G,Fogelman AM

更新日期：2006-01-01 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: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：:Currently available antifungal drugs for serious infections are either fungistatic and vulnerable to resistance (azoles) or fungicidal but toxic to the host (polyenes). Cell wall-acting antifungals are inherently selective and fungicidal, features that make them particularly attractive for clinical development. Three ...

journal_title：Expert opinion on investigational drugs

authors： Georgopapadakou NH

更新日期：2001-02-01 00:00:00

abstract：:This paper reviews the clinical pharmacology, efficacy and safety of the novel antipsychotic drug aripiprazole. All published citations regarding aripiprazole were reviewed using a Medline((R)) search (completed for citations through mid-year, 2002). In addition, abstracts from recent scientific meetings presenting da...

journal_title：Expert opinion on investigational drugs

authors： Keck PE Jr,McElroy SL

更新日期：2003-04-01 00:00:00

abstract：INTRODUCTION:Stroke is the second leading cause of death worldwide and the leading cause of adult neurological disability. Despite advances in stroke unit care, and increasing use of thrombolysis, there remains an urgent need for safe and effective treatments for acute ischaemic stroke. However, this is against a backd...

journal_title：Expert opinion on investigational drugs

authors： Smith CJ,Denes A,Tyrrell PJ,Di Napoli M

更新日期：2015-05-01 00:00:00

abstract：:With FDA approval of monoclonal antibodies (mAb) against the B-cell-specific cell surface molecule CD20, immunotherapy in B-cell non-Hodgkin's-lymphomas (NHL) has gained momentum. Since the first description of the CD20 mAb and its use in a single patient, it has taken more than 20 years to implement this in current t...

journal_title：Expert opinion on investigational drugs

authors： Schultze JL

更新日期：1999-12-01 00:00:00

abstract：:Prinomastat (formerly AG3340, Agouron Pharmaceuticals, Inc.) is a potent, selective oral inhibitor of matrix metalloproteinase-2, -9, -13 and -14. This peculiar selectivity should represent an advantage for prinomastat in terms of efficacy/tolerability. The drug has been shown to inhibit tumour growth and angiogenesis...

journal_title：Expert opinion on investigational drugs

authors： Scatena R

更新日期：2000-09-01 00:00:00