The efficacy and safety of telaprevir - a new protease inhibitor against hepatitis C virus.

Abstract:

IMPORTANCE OF THE FIELD:Hepatitis C virus (HCV) is the main agent of chronic hepatitis, liver cirrhosis and hepatocellular carcinoma in the western world. It affects more than 170 million people worldwide. HCV treatment, based on the combination of Peg-interferon and ribavirin, is effective in about 50% of treated patients. Therefore, there is a need to develop new drugs active against HCV. AREAS COVERED IN THIS REVIEW:Data were obtained by searching for all full articles on Medline and abstracts presented at major international congresses on viral hepatitis. WHAT THE READER WILL GAIN:A review of clinical data about the efficacy and safety of telaprevir (VX-950), the HCV protease inhibitor that is in the most advanced phase of clinical development. TAKE HOME MESSAGE:Telaprevir has an acceptable pharmacokinetic profile and seems to be a potent antiviral drug against HCV, although, owing to a low genetic barrier, resistant variants emerge within a few days when used in monotherapy, thereby decreasing its efficacy. Consequently, telaprevir has been combined with pegylated-interferon and ribavirin in clinical trials. This triple combination is more effective but has a higher rate of adverse events (notably rash) than the standard of care, despite the shorter duration of therapy.

authors

Gentile I,Carleo MA,Borgia F,Castaldo G,Borgia G

doi

10.1517/13543780903501505

subject

Has Abstract

pub_date

2010-01-01 00:00:00

pages

151-9

issue

1

eissn

1354-3784

issn

1744-7658

journal_volume

19

pub_type

杂志文章,评审
  • Dawn of Aurora kinase inhibitors as anticancer drugs.

    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

    pub_type: 杂志文章,评审

    doi:10.1517/13543784.13.9.1199

    authors: Doggrell SA

    更新日期:2004-09-01 00:00:00

  • Strategies for blocking angiogenesis in diabetic retinopathy: from basic science to clinical practice.

    abstract::Proliferative diabetic retinopathy (PDR) demands both more effective and less expensive biologically based treatments. Our understanding of the pathophysiology of the disease is increasing as new biochemical pathways are identified. Most reports emphasize proangiogenic stimuli, with the natural inhibitory elements rec...

    journal_title:Expert opinion on investigational drugs

    pub_type: 杂志文章,评审

    doi:10.1517/13543784.16.8.1209

    authors: Hernández C,Simó R

    更新日期:2007-08-01 00:00:00

  • TACE inhibition: a new approach to treating inflammation.

    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

    pub_type: 杂志文章

    doi:10.1517/13543784.11.7.1003

    authors: Doggrell SA

    更新日期:2002-07-01 00:00:00

  • Novel antiarrhythmic drugs in atrial fibrillation: focus on tedisamil.

    abstract:BACKGROUND:Even established and effective antiarrhythmic drugs (AADs) in atrial fibrillation (AF) are limited by their pro-arrhythmic and non-target organ side effects. Therefore the search continues for safer and effective new AADs. OBJECTIVE:This review will examine a novel AAD, tedisamil--a multichannel potassium c...

    journal_title:Expert opinion on investigational drugs

    pub_type: 杂志文章,评审

    doi:10.1517/13543780903114150

    authors: Krishnamoorthy S,Lip GY

    更新日期:2009-08-01 00:00:00

  • Investigational PPAR-gamma agonists for the treatment of Type 2 diabetes.

    abstract::The tremendous increase in the global prevalence of Type 2 diabetes (T2D) and its conglomeration of metabolic disorders has dramatically intensified the search for innovative therapies to fight this emerging epidemic. Over the last decade, the family of nuclear receptors, especially the peroxisome proliferator-activat...

    journal_title:Expert opinion on investigational drugs

    pub_type: 杂志文章,评审

    doi:10.1517/13543784.15.7.763

    authors: Savkur RS,Miller AR

    更新日期:2006-07-01 00:00:00

  • Early clinical development of epidermal growth factor receptor targeted therapy in breast cancer.

    abstract:INTRODUCTION:Epidermal growth factor receptor (EGFR) targeted treatment has been evaluated but has not shown a clear clinical benefit for breast cancer. This review article aims to consider the knowledge of the biological background of EGFR pathways in dissecting clinical studies of EGFR targeted treatment in breast ca...

    journal_title:Expert opinion on investigational drugs

    pub_type: 杂志文章,评审

    doi:10.1080/13543784.2017.1299707

    authors: Matsuda N,Lim B,Wang X,Ueno NT

    更新日期:2017-04-01 00:00:00

  • Targeting IL-6 for the treatment of rheumatoid arthritis: Phase II investigational drugs.

    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

    pub_type: 杂志文章,评审

    doi:10.1517/13543784.2014.912276

    authors: Semerano L,Thiolat A,Minichiello E,Clavel G,Bessis N,Boissier MC

    更新日期:2014-07-01 00:00:00

  • IBC's 5th Annual Conference on Blood Substitutes.

    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

    authors: Shorr RG

    更新日期:1998-02-01 00:00:00

  • Antimicrobial peptides: therapeutic potential for the treatment of Candida infections.

    abstract::The increasing frequency of fungal infections in immunocompromised patients together with the emergence of strains resistant to currently used antifungal drugs point to an increased need for a new class of antimycotics. Antimicrobial peptides are promising candidates for the treatment of fungal infections since they h...

    journal_title:Expert opinion on investigational drugs

    pub_type: 杂志文章,评审

    doi:10.1517/13543784.11.2.309

    authors: Lupetti A,Danesi R,van 't Wout JW,van Dissel JT,Senesi S,Nibbering PH

    更新日期:2002-02-01 00:00:00

  • The prospects of hepatic drug delivery and gene therapy.

    abstract::Liver targeted therapy is designed to deliver a substance preferentially to the organ in order to increase the accumulation, improve the therapeutic effect and reduce toxicity to other organs. The aim of selective targeting is to deliver a substance to a specific cell type in the liver. A variety of vehicles have been...

    journal_title:Expert opinion on investigational drugs

    pub_type: 杂志文章

    doi:10.1517/13543784.7.11.1795

    authors: Wu J,Wu GY,Zern MA

    更新日期:1998-11-01 00:00:00

  • Osteoarthritic pain: a review of current, theoretical and emerging therapeutics.

    abstract:BACKGROUND:Despite exciting progress and growth in the understanding of molecular and cellular mechanisms of chronic pain, osteoarthritis (OA) pain remains a challenging clinical entity to treat. There is an emerging diversity of algogenic mechanisms suggesting heterogeneity in pain aetiology in the OA patient populati...

    journal_title:Expert opinion on investigational drugs

    pub_type: 杂志文章,评审

    doi:10.1517/13543784.17.5.619

    authors: Read SJ,Dray A

    更新日期:2008-05-01 00:00:00

  • Custirsen (OGX-011): a second-generation antisense inhibitor of clusterin for the treatment of cancer.

    abstract:BACKGROUND:Clusterin is a stress-induced cytoprotective chaperone protein, regulated by HSF1, and functions similarly to a small heat-shock protein. Clusterin is expressed in a variety of cancers and associated with broad-spectrum treatment resistance. Custirsen (OGX-011) is a 2'-methoxyethyl modified phosphorothioate ...

    journal_title:Expert opinion on investigational drugs

    pub_type: 杂志文章,评审

    doi:10.1517/13543780802528609

    authors: Chi KN,Zoubeidi A,Gleave ME

    更新日期:2008-12-01 00:00:00

  • Pharmacology and clinical trial results of lanoteplase in acute myocardial infarction.

    abstract::New bolus fibrinolytic agents derived from the recombinant human tissue plasminogen activator (t-PA) have emerged as a new means of dissolution of the occlusive thrombosis associated with acute myocardial infarction. Lanoteplase is a fibrinolytic drug derived from t-PA by deleting its fibronectin finger-like and epide...

    journal_title:Expert opinion on investigational drugs

    pub_type: 杂志文章,评审

    doi:10.1517/13543784.9.11.2689

    authors: Llevadot J,Guigliano RP

    更新日期:2000-11-01 00:00:00

  • Urokinase receptor antagonists: novel agents for the treatment of cancer.

    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

    pub_type: 杂志文章

    doi:10.1517/13543784.7.3.391

    authors: Weidle UH,König B

    更新日期:1998-03-01 00:00:00

  • The therapeutic potential of the cannabinoids in neuroprotection.

    abstract::After thousands of years of interest the last few decades have seen a huge increase in our knowledge of the cannabinoids and their mode of action. Their potential as medical therapeutics has long been known. However, very real concerns over their safety and efficacy have lead to caution and suspicion when applying the...

    journal_title:Expert opinion on investigational drugs

    pub_type: 杂志文章,评审

    doi:10.1517/13543784.11.10.1365

    authors: Grundy RI

    更新日期:2002-10-01 00:00:00

  • Therapeutic potential of S179D prolactin--from prostate cancer to angioproliferative disorders: the first selective prolactin receptor modulator.

    abstract::Increasing evidence suggests an important role for autocrine/paracrine prolactin in breast and prostate cancers and other disease states. Prolactin production in these extrapituitary sites is not governed by dopamine agonists, a finding that has spurred the production of prolactin receptor antagonists. This review foc...

    journal_title:Expert opinion on investigational drugs

    pub_type: 杂志文章,评审

    doi:10.1517/13543784.15.10.1257

    authors: Walker AM

    更新日期:2006-10-01 00:00:00

  • The role of mineralocorticoid receptor antagonists in the treatment of cardiac failure.

    abstract::In most countries the last two decades have seen a very substantial rise in the prevalence of heart failure, and in a majority of patients hypertension is both an antecedent condition and a contributing cause. Heart failure is also a major cause of hospital admissions; its amelioration and, as far as possible, prevent...

    journal_title:Expert opinion on investigational drugs

    pub_type: 杂志文章,评审

    doi:10.1517/13543784.12.12.1963

    authors: Funder JW

    更新日期:2003-12-01 00:00:00

  • The prospects for combination therapy with capecitabine in the rapidly evolving treatment landscape of renal cell carcinoma.

    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

    pub_type: 杂志文章,评审

    doi:10.1080/13543784.2018.1427731

    authors: Bilen MA,Carlisle JW,Sonpavde G

    更新日期:2018-02-01 00:00:00

  • Biological versatility of crotamine--a cationic peptide from the venom of a South American rattlesnake.

    abstract:IMPORTANCE OF THE FIELD:Molecules isolated from animals, insects, plants or microorganisms can provide prototypes for design of biopharmaceutical products. Some venom toxins and their derivatives are used in medicine, while others provide templates for development of new drugs. AREAS COVERED IN THIS REVIEW:The mild to...

    journal_title:Expert opinion on investigational drugs

    pub_type: 杂志文章,评审

    doi:10.1517/13543784.2010.534457

    authors: Kerkis I,Silva Fde S,Pereira A,Kerkis A,Rádis-Baptista G

    更新日期:2010-12-01 00:00:00

  • Inhibiting PAR-1 in the prevention and treatment of atherothrombotic events.

    abstract:IMPORTANCE OF THE FIELD:Aspirin, an irreversible inhibitor of thromboxane A(2) production, in combination with clopidogrel, an inhibitor of PY(12) ADP platelet receptors, represents the current standard-of-care of antiplatelet therapy for patients with acute coronary syndrome and those undergoing percutaneous coronary ...

    journal_title:Expert opinion on investigational drugs

    pub_type: 杂志文章,评审

    doi:10.1517/13543784.2010.521741

    authors: Tomasello SD,Angiolillo DJ,Goto S

    更新日期:2010-12-01 00:00:00

  • Investigational therapies for Ewing sarcoma: a search without a clear finding.

    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

    authors: Vornicova O,Bar-Sela G

    更新日期:2016-06-01 00:00:00

  • Future options for imatinib mesilate-resistant tumors.

    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

    authors: Sankhala KK,Papadopoulos KP

    更新日期:2007-10-01 00:00:00

  • Vascular-disrupting agents in oncology.

    abstract:INTRODUCTION:Vascular-disrupting agents (VDAs) are a new class of oncology drugs, which specifically target established tumor neovasculature and have a relatively low toxicity profile. VDAs generally have non-overlapping side effects when concomitantly used with conventional cytotoxics. Several members of the VDA class...

    journal_title:Expert opinion on investigational drugs

    pub_type: 杂志文章,评审

    doi:10.1517/13543784.2013.759557

    authors: Mita MM,Sargsyan L,Mita AC,Spear M

    更新日期:2013-03-01 00:00:00

  • Tetomilast: new promise for phosphodiesterase-4 inhibitors?

    abstract:INTRODUCTION:Tetomilast is a novel thiazole phosphodiesterase-4 (PDE-4) inhibitor, which may prove useful in both the treatment of inflammatory bowel disease (IBD) and chronic obstructive pulmonary disease (COPD). Here, the authors review the pharmacology of the drug, and offer critical review of the available data for...

    journal_title:Expert opinion on investigational drugs

    pub_type: 杂志文章,评审

    doi:10.1517/13543784.2012.732065

    authors: Bickston SJ,Snider KR,Kappus MR

    更新日期:2012-12-01 00:00:00

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

    abstract:INTRODUCTION:Signal transducer and activator of transcription 3 (STAT3) controls a key signaling pathway in the development of many malignant diseases. Several genetic studies have proven its central role in the regulation of apoptosis, proliferation, angiogenesis and immune responses making it an attractive target for...

    journal_title:Expert opinion on investigational drugs

    pub_type: 杂志文章,评审

    doi:10.1517/13543784.2011.601739

    authors: Mankan AK,Greten FR

    更新日期:2011-09-01 00:00:00

  • Cannabinoids against pain. Efficacy and strategies to reduce psychoactivity: a clinical perspective.

    abstract::The clinical use of cannabinoids is currently a topic of interest not exclusively, but most importantly, concerning different areas of pain therapy. One of the major obstacles in developing clinically acceptable compounds is the cannabimimetic side-effect profile of delta-9-tetrahydrocannabinol (THC) and other cannabi...

    journal_title:Expert opinion on investigational drugs

    pub_type: 杂志文章,评审

    doi:10.1517/13543780802691951

    authors: Karst M,Wippermann S

    更新日期:2009-02-01 00:00:00

  • Promising antitumor activity with MGCD0103, a novel isotype-selective histone deacetylase inhibitor.

    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

    pub_type: 杂志文章,评审

    doi:10.1517/13543784.17.8.1247

    authors: Le Tourneau C,Siu LL

    更新日期:2008-08-01 00:00:00

  • Non-invasive imaging of plaque vulnerability: an important tool for the assessment of agents to stabilise atherosclerotic plaques.

    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

    pub_type: 杂志文章,评审

    doi:10.1517/13543784.11.5.693

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

    更新日期:2002-05-01 00:00:00

  • Targeting tyrosine-kinases in ovarian cancer.

    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

    pub_type: 杂志文章,评审

    doi:10.1517/13543784.2013.816282

    authors: Morotti M,Becker CM,Menada MV,Ferrero S

    更新日期:2013-10-01 00:00:00

  • Recent advances in natriuretic peptides in congestive heart failure.

    abstract::Atrial natriuretic peptide (ANP) and B-type natriuretic peptide (BNP) are secreted by the heart and play important roles in the compensation of congestive heart failure with their vasodilating, natriuretic, antiproliferative, lusitropic and neurohumoral-modulating properties. Based on these beneficial properties, exog...

    journal_title:Expert opinion on investigational drugs

    pub_type: 杂志文章,评审

    doi:10.1517/13543784.13.6.643

    authors: Boerrigter G,Burnett JC Jr

    更新日期:2004-06-01 00:00:00