Macitentan: a review of its use in patients with pulmonary arterial hypertension.

Abstract:

:Macitentan (Opsumit(®)) is an orally active, dual endothelin receptor antagonist (ERA) with tissue targeting properties. Macitentan was approved recently in the EU (as monotherapy or combination therapy) for the long-term treatment of pulmonary arterial hypertension (PAH) in adults of WHO functional class II or III, and in the USA for the treatment of PAH (WHO group I) to delay disease progression and reduce hospitalization for PAH. This article reviews the pharmacological properties, efficacy and tolerability data relevant to the use of macitentan in this indication. Treatment with macitentan 10 mg once daily significantly reduced the risk for the primary composite endpoint of morbidity and mortality in patients with PAH (mostly WHO functional class II or III) in the large, randomized, placebo-controlled SERAPHIN study. Other efficacy outcomes, including exercise capacity, haemodynamic parameters and health-related quality of life also improved significantly with macitentan relative to placebo. Macitentan was generally well tolerated in this study. As with other ERAs, haemoglobin levels decreased with macitentan therapy; however, these were not progressive and stabilized following longer-term treatment. Although comparative studies are needed to definitively position macitentan with respect to other approved agents, current evidence suggests that macitentan is a useful treatment option for initial therapy in patients with WHO functional class II or III PAH, which has the potential advantage of once-daily administration.

journal_name

Drugs

journal_title

Drugs

authors

Dhillon S

doi

10.1007/s40265-014-0266-9

subject

Has Abstract

pub_date

2014-09-01 00:00:00

pages

1495-507

issue

13

eissn

0012-6667

issn

1179-1950

journal_volume

74

pub_type

杂志文章,评审

相关文献

DRUGS文献大全
  • Oxaliplatin. A review of its pharmacological properties and clinical efficacy in metastatic colorectal cancer and its potential in other malignancies.

    abstract:UNLABELLED:Oxaliplatin is a platinum compound that inhibits DNA synthesis, primarily by causing intrastrand cross-links in DNA. Oxaliplatin has a broad spectrum of antineoplastic activity and has demonstrated a lack of cross-resistance with other platinum compounds. In patients with metastatic colorectal cancer, intrav...

    journal_title:Drugs

    pub_type: 杂志文章,评审

    doi:10.2165/00003495-200060040-00005

    authors: Culy CR,Clemett D,Wiseman LR

    更新日期:2000-10-01 00:00:00

  • Eravacycline: A Review in Complicated Intra-Abdominal Infections.

    abstract::Eravacycline (Xerava™), a novel fully synthetic fluorocycline, consists of the tetracyclic core scaffold with unique modifications in the tetracyclic D ring; consequently, it exhibits potent in vitro activity against Gram-positive and -negative bacterial strains expressing certain common tetracycline-specific acquired...

    journal_title:Drugs

    pub_type: 杂志文章,评审

    doi:10.1007/s40265-019-01067-3

    authors: Scott LJ

    更新日期:2019-02-01 00:00:00

  • Value of non-drug treatment and drug treatment in hypertension.

    abstract::The benefits of the treatment of hypertension currently consist of a substantially reduced incidence of premature stroke, left ventricular failure and malignant hypertension. The benefits for the individual are most clearcut in those who have already had severe or symptomatic hypertension. Older subjects who have a hi...

    journal_title:Drugs

    pub_type: 杂志文章,评审

    doi:10.2165/00003495-198800366-00003

    authors: Beilin LJ

    更新日期:1988-01-01 00:00:00

  • Why Biologics and Biosimilars Remain So Expensive: Despite Two Wins for Biosimilars, the Supreme Court's Recent Rulings do not Solve Fundamental Barriers to Competition.

    abstract::Biologics and biosimilars are medicines made from living cells that treat common and serious diseases such as cancer, diabetes, rheumatoid arthritis, and other inflammatory diseases. They are highly targeted, efficacious, and represent an increasingly important part of physicians' armamentaria in the combat against th...

    journal_title:Drugs

    pub_type: 杂志文章

    doi:10.1007/s40265-018-1009-0

    authors: Chen BK,Yang YT,Bennett CL

    更新日期:2018-11-01 00:00:00

  • Emerging resistance to antimicrobial agents in gram-positive bacteria. Pneumococci.

    abstract::The prevalence of penicillin-resistant pneumococci is increasing worldwide. Methods for susceptibility testing, as well as in vitro susceptibility of penicillin-susceptible and -resistant strains to new and existing agents (including oral and parenteral streptogramins), are described. For all specimens except CSF, oxa...

    journal_title:Drugs

    pub_type: 杂志文章,评审

    doi:10.2165/00003495-199600511-00003

    authors: Appelbaum PC

    更新日期:1996-01-01 00:00:00

  • Current options in the treatment of non-small cell lung cancer.

    abstract::Non-small cell lung cancer (NSCLC) is a leading cause of cancer death in industrialised countries, with an overall 5-year survival rate of less than 10%. Good patient performance status is associated with a significantly improved prognosis, whereas the presence of metastases, particularly to the bone or liver, is asso...

    journal_title:Drugs

    pub_type: 杂志文章,评审

    doi:10.2165/00003495-199200444-00006

    authors: Faulds D

    更新日期:1992-01-01 00:00:00

  • Drotrecogin alfa (activated).

    abstract::Drotrecogin alfa (activated), recombinant human activated protein C, inhibits coagulation and inflammation and promotes fibrinolysis in patients with severe sepsis. 850 patients with severe sepsis treated with intravenous drotrecogin alfa (activated) 24 microg/kg/h for 96 hours had a significantly greater reduction in...

    journal_title:Drugs

    pub_type: 临床试验,杂志文章,随机对照试验

    doi:10.2165/00003495-200262040-00006

    authors: Lyseng-Williamson KA,Perry CM

    更新日期:2002-01-01 00:00:00

  • Advanced renal cell carcinoma: current and emerging management strategies.

    abstract::Management of renal cell carcinoma (RCC) has made considerable progress in recent years, and new emerging strategies are being developed. On the basis of the results of two randomised studies in the early 2000s, nephrectomy has now become the standard as cytoreductive surgery before embarking on systemic treatment wit...

    journal_title:Drugs

    pub_type: 杂志文章,评审

    doi:10.2165/00003495-200767090-00002

    authors: Escudier B

    更新日期:2007-01-01 00:00:00

  • Statins and pregnancy: between supposed risks and theoretical benefits.

    abstract::Cardiovascular diseases are the leading cause of mortality in industrialized countries. Treatment with statins is effective in primary prevention in patients at high cardiovascular risk. Statins are inhibitors of hydroxymethylglutaryl-coenzyme A (HMG-CoA) reductase and are classed as lipid-lowering drugs. In 2010, ato...

    journal_title:Drugs

    pub_type: 杂志文章,评审

    doi:10.2165/11632010-000000000-00000

    authors: Lecarpentier E,Morel O,Fournier T,Elefant E,Chavatte-Palmer P,Tsatsaris V

    更新日期:2012-04-16 00:00:00

  • Pimavanserin: First Global Approval.

    abstract::Pimavanserin (Nuplazid™) is a selective and potent serotonin 2A (5-HT2A) receptor inverse agonist and antagonist developed by ACADIA Pharmaceuticals that has been approved in the US as a treatment for patients with hallucinations and delusions associated with Parkinson's disease psychosis. Up to 60 % of patients with ...

    journal_title:Drugs

    pub_type: 杂志文章,评审

    doi:10.1007/s40265-016-0597-9

    authors: Markham A

    更新日期:2016-07-01 00:00:00

  • Optimal therapeutic strategies for resectable oesophageal or oesophagogastric junction cancer.

    abstract::Oesophageal cancer is the eighth most common cancer diagnosed worldwide, with almost half a million new cases diagnosed each year. Despite improvements in surgical and radiotherapy techniques and refinements of chemotherapeutic regimens, long-term survival, even from localized oesophageal cancer, remains poor. Surgica...

    journal_title:Drugs

    pub_type: 杂志文章,评审

    doi:10.2165/11585460-000000000-00000

    authors: Bystricky B,Okines AF,Cunningham D

    更新日期:2011-03-26 00:00:00

  • Schistosomiasis drug therapy and treatment considerations.

    abstract::Schistosomiasis, a grave and debilitating disease of socioeconomic importance, is increasing in incidence despite concerted efforts to control and contain the disease in all the endemic areas. While a multipronged method of control using health education, sanitation and snail control has been used, chemotherapy and ch...

    journal_title:Drugs

    pub_type: 杂志文章,评审

    doi:10.2165/00003495-199142030-00004

    authors: Shekhar KC

    更新日期:1991-09-01 00:00:00

  • Inhaled mometasone furoate: A review of its use in persistent asthma in adults and adolescents.

    abstract::Inhaled mometasone furoate (Asmanex) is a synthetic corticosteroid indicated for the first-line maintenance prophylactic therapy of persistent asthma in adults and adolescents. It is formulated for delivery via a breath-actuated dry powder inhaler (DPI) [Twisthaler].Inhaled mometasone furoate delivered by DPI is effec...

    journal_title:Drugs

    pub_type: 杂志文章,评审

    doi:10.2165/00003495-200666080-00011

    authors: McCormack PL,Plosker GL

    更新日期:2006-01-01 00:00:00

  • A Retrospective Cohort Study of Obstetric Outcomes in Opioid-Dependent Women Treated with Implant Naltrexone, Oral Methadone or Sublingual Buprenorphine, and Non-Dependent Controls.

    abstract:BACKGROUND:Opioid pharmacotherapies play an important role in the treatment of opioid-dependent women; however, very little is known about the safety of naltrexone in pregnant patients. OBJECTIVE:This study examined the obstetric health of opioid-dependent women who were treated with implant naltrexone during pregnanc...

    journal_title:Drugs

    pub_type: 杂志文章,meta分析

    doi:10.1007/s40265-017-0762-9

    authors: Kelty E,Hulse G

    更新日期:2017-07-01 00:00:00

  • Cefixime. A review of its therapeutic efficacy in lower respiratory tract infections.

    abstract::Cefixime is an orally active third generation cephalosporin with in vitro antibacterial activity against most important lower respiratory pathogens. The drug is active against Haemophilus influenzae, Moraxella catarrhalis and penicillin-susceptible Streptococcus pneumoniae but not Staphylococcus aureus. Cefixime has a...

    journal_title:Drugs

    pub_type: 杂志文章,评审

    doi:10.2165/00003495-199549060-00010

    authors: Markham A,Brogden RN

    更新日期:1995-06-01 00:00:00

  • Optimal pharmacological therapy for community-acquired pneumonia: the role of dual antibacterial therapy.

    abstract::The optimal pharmacological therapy of community-acquired pneumonia (CAP) is one of the most ardently debated issues in medicine. Presently, most guidelines recommend either a fluoroquinolone alone or dual therapy with a third-generation cephalosporin plus a macrolide in patients hospitalised with CAP, but few provide...

    journal_title:Drugs

    pub_type: 杂志文章,评审

    doi:10.2165/00003495-200565140-00004

    authors: Epstein BJ,Gums JG

    更新日期:2005-01-01 00:00:00

  • Pharmacokinetics of cefoperazone: a review.

    abstract::The pharmacokinetics of cefoperazone in normal subjects, and in patients with hepatic and renal dysfunction are reviewed. After intravenous administration of 2 g of cefoperazone, levels in serum ranged from 202 to 375 microgram/ml depending on the period of drug administration. After intramuscular injection of 2 g of ...

    journal_title:Drugs

    pub_type: 杂志文章,评审

    doi:10.2165/00003495-198100221-00010

    authors: Craig WA,Gerber AU

    更新日期:1981-01-01 00:00:00

  • Disease-modifying antirheumatic drugs. Using their clinical pharmacological effects as a guide to their selection.

    abstract::Rheumatoid arthritis is a disease of unknown aetiology characterised by persistent joint swelling, functional disability and increased mortality. No curative therapy exists at present but some therapeutic agents, commonly referred to as disease-modifying drugs, offer the potential for suppression of the inflammatory a...

    journal_title:Drugs

    pub_type: 杂志文章,评审

    doi:10.2165/00003495-199856030-00003

    authors: Jackson CG,Williams HJ

    更新日期:1998-09-01 00:00:00

  • Drug-induced psychiatric disorders.

    abstract::This article is a review of the principal drug-induced psychiatric symptoms that are likely to be encountered in daily clinical practice as a result of drug abuse, overdoses or side effects of drugs prescribed for treatment. Many categories of medication have the potential to produce psychiatric symptoms, but antitube...

    journal_title:Drugs

    pub_type: 杂志文章,评审

    doi:10.2165/00003495-198122010-00004

    authors: Johnson DA

    更新日期:1981-07-01 00:00:00

  • Sickle cell disease in children.

    abstract::Early identification of infants with sickle cell disease (SCD) by newborn screening, now universal in all 50 states in the US, has improved survival, mainly by preventing overwhelming sepsis with the early use of prophylactic penicillin. Routine transcranial Doppler screening with the institution of chronic transfusio...

    journal_title:Drugs

    pub_type: 杂志文章,评审

    doi:10.2165/11632890-000000000-00000

    authors: Meier ER,Miller JL

    更新日期:2012-05-07 00:00:00

  • Oxantel-pyrantel in various regimens for the treatment of soil transmitted helminthiasis in rural and urban communities.

    abstract::204 individuals from a rural community were given a single dose of oxantel-pyrantel at 15mg/kg bodyweight and if still infected, 20mg/kg bodyweight, with cure rates of 100%, 53% and 71% for ascariasis, trichuriasis and hookworm infection, respectively. From an urban community, 124 patients were given the same drug eit...

    journal_title:Drugs

    pub_type: 临床试验,杂志文章

    doi:10.2165/00003495-197800151-00016

    authors: Cabrera BD,Sy FS

    更新日期:1978-01-01 00:00:00

  • Role of the kidney in congestive heart failure. Relationship of cardiac index to kidney function.

    abstract::Because of inappropriate signals from the volume-regulation system and a reduction in renal blood flow, the kidney is not able to prevent sodium and water retention in chronic congestive heart failure (CHF). A brief summary of normal renal function and renal involvement in CHF is given and a study of renal function in...

    journal_title:Drugs

    pub_type: 杂志文章

    doi:10.2165/00003495-199000394-00004

    authors: Ljungman S,Laragh JH,Cody RJ

    更新日期:1990-01-01 00:00:00

  • Drugs affecting the inner ear. A review of their clinical efficacy, mechanisms of action, toxicity, and place in therapy.

    abstract::Many drugs have a site of action within the inner ear. The list includes therapeutic, diagnostic and ototoxic agents. Therapeutic agents are most useful in cases of infections, endolymphatic hydrops, vascular insufficiency, vertigo of peripheral origin, autoimmune disease, otosclerosis (otospongiosis), sudden hearing ...

    journal_title:Drugs

    pub_type: 杂志文章,评审

    doi:10.2165/00003495-198836060-00005

    authors: Norris CH

    更新日期:1988-12-01 00:00:00

  • Drug treatment of hypertension.

    abstract::There are several first choices for the treatment of mild and moderate hypertension. The selection of a drug may be influenced by concomitant pathology, with positive indications for particular drugs, e.g. coexistent angina, indicating use of a beta-receptor blocking drug or calcium antagonist; fluid retention indicat...

    journal_title:Drugs

    pub_type: 杂志文章,评审

    doi:10.2165/00003495-198800356-00006

    authors: Prichard BN

    更新日期:1988-01-01 00:00:00

  • Ciclesonide nasal spray: in allergic rhinitis.

    abstract::Ciclesonide nasal spray delivers the corticosteroid ciclesonide as a hypotonic spray via a metered-dose manual pump. Systemic exposure to ciclesonide and its active metabolite desisobutyryl-ciclesonide is low after intranasal administration. High protein binding (approximately 99%) and rapid first-pass clearance furth...

    journal_title:Drugs

    pub_type: 杂志文章,评审

    doi:10.2165/00003495-200868060-00009

    authors: Dhillon S,Wagstaff AJ

    更新日期:2008-01-01 00:00:00

  • Comparative efficacy of cyclandelate versus flunarizine in the prophylactic treatment of migraine.

    abstract::In a double-blind, parallel-group randomised trial of 3 months' duration, the efficacy of cyclandelate 800 mg twice daily in migraine prophylaxis was compared with that of flunarizine 5mg daily in 40 patients. In comparison with placebo and baseline values, both drugs significantly relieved symptoms of migraine as ass...

    journal_title:Drugs

    pub_type: 临床试验,杂志文章,随机对照试验

    doi:10.2165/00003495-198700332-00019

    authors: Nappi G,Sandrini G,Savoini G,Cavallini A,de Rysky C,Micieli G

    更新日期:1987-01-01 00:00:00

  • Interaction of lipoproteins with the artery wall.

    abstract::Atherosclerosis can be defined in terms of the processes involved rather than in morphological terms, and there is evidence for possible roles of the macrophage in atherogenesis. The relevance of hyperlipidaemia to the morphogenesis of the atherosclerotic plaque is important, and this has been described in animal mode...

    journal_title:Drugs

    pub_type: 杂志文章,评审

    doi:10.2165/00003495-198800363-00012

    authors: Woolf N

    更新日期:1988-01-01 00:00:00

  • Nizatidine. A preliminary review of its pharmacodynamic and pharmacokinetic properties, and its therapeutic use in peptic ulcer disease.

    abstract::Nizatidine is an H2-receptor antagonist which in animal studies was more active on a weight-for-weight basis than cimetidine in inhibiting basal and stimulated gastric acid secretion. Similarly, studies in humans have confirmed that nizatidine is a potent inhibitor of basal, nocturnal and stimulated gastric acid secre...

    journal_title:Drugs

    pub_type: 杂志文章,评审

    doi:10.2165/00003495-198836050-00002

    authors: Price AH,Brogden RN

    更新日期:1988-11-01 00:00:00

  • Tofacitinib: A Review in Rheumatoid Arthritis.

    abstract::Tofacitinib (Xeljanz®) is a potent, selective JAK inhibitor that preferentially inhibits Janus kinase (JAK) 1 and JAK3. In the EU, oral tofacitinib 5 mg twice daily is indicated for the treatment of moderate to severe active rheumatoid arthritis (RA) in adult patients who have responded inadequately to, or who are int...

    journal_title:Drugs

    pub_type: 杂志文章,评审

    doi:10.1007/s40265-017-0835-9

    authors: Dhillon S

    更新日期:2017-12-01 00:00:00

  • Pharmacological interventions for the induction of ovulation.

    abstract::Ovulation induction is the most common medical intervention for the treatment of infertility. Clomifene is generally the first treatment choice for patients with amenorrhoea, unless there is profound hypothalamic deficiency. When clomifene fails to induce ovulation, menotropins (human menopausal gonadotrophin) or gona...

    journal_title:Drugs

    pub_type: 杂志文章,评审

    doi:10.2165/00003495-199550030-00006

    authors: Collins JA,Hughes EG

    更新日期:1995-09-01 00:00:00