Abstract:
AIMS:We investigated the relative pharmacokinetics, pharmacodynamics, and safety of the proprotein convertase subtilisin/kexin type 9 (PCSK9) inhibitor alirocumab following injection at three different sites. METHODS:Sixty healthy subjects (39 male, 21 female; age 20-45 years) were randomized to receive a single subcutaneous injection of alirocumab 75 mg via 1-mL prefilled pen into the abdomen, upper arm, or thigh (NCT01785329). Subjects were followed for 85 days ± 2 days following study drug administration. Pharmacokinetic (PK) parameters for the systemic exposure of alirocumab were calculated, and levels of free PCSK9 were assessed. Percentage changes from baseline in LDL-C were compared between injection site groups using linear mixed-effects models. RESULTS:Alirocumab concentration-time profiles were similar, and free PCSK9 levels were reduced to approximately zero between Day 3 and Day 4 postinjection in all groups. LDL-C levels reached nadir on Day 15 postinjection in all groups with mean percentage reductions of 48.4% (abdomen), 39.5% (upper arm), and 45.6% (thigh) at this time point. A similar effect on LDL-C levels was seen across the entire time course of the study at all three injection sites. Treatment-emergent adverse events were experienced by 8/20 (abdomen), 11/20 (upper arm), and 13/20 (thigh) subjects. There were 2 mild/transient injection site reactions. There were no serious adverse events. DISCUSSION:A single subcutaneous administration of alirocumab 75 mg via prefilled pen was well tolerated with similar pharmacokinetics and pharmacodynamics when injected into the abdomen, upper arm, or thigh. CONCLUSION:These results suggest that alirocumab can be interchangeably injected in the abdomen, upper arm, or thigh.
journal_name
Cardiovasc Therjournal_title
Cardiovascular therapeuticsauthors
Lunven C,Paehler T,Poitiers F,Brunet A,Rey J,Hanotin C,Sasiela WJdoi
10.1111/1755-5922.12093subject
Has Abstractpub_date
2014-12-01 00:00:00pages
297-301issue
6eissn
1755-5914issn
1755-5922journal_volume
32pub_type
杂志文章,随机对照试验abstract:BACKGROUND:Intracranial hemorrhage (ICH) is the most fearful side effect of oral anticoagulant therapy. It is still unclear which risk factor is involved in ICH during vitamin K antagonists (VKAs) treatment and if commonly used bleeding risk scores are able to predict ICH. PURPOSE:Search for individual risk factors an...
journal_title:Cardiovascular therapeutics
pub_type: 杂志文章
doi:10.1111/1755-5922.12458
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journal_title:Cardiovascular therapeutics
pub_type: 杂志文章,评审
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journal_title:Cardiovascular therapeutics
pub_type: 杂志文章,多中心研究
doi:10.1111/1755-5922.12270
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journal_title:Cardiovascular therapeutics
pub_type: 杂志文章,评审
doi:10.1111/j.1755-5922.2010.00151.x
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journal_title:Cardiovascular therapeutics
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journal_title:Cardiovascular therapeutics
pub_type: 杂志文章,评审
doi:10.1111/1755-5922.12090
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journal_title:Cardiovascular therapeutics
pub_type: 杂志文章,评审
doi:10.1111/j.1755-5922.2009.00087.x
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journal_title:Cardiovascular therapeutics
pub_type: 杂志文章,评审
doi:10.1111/j.1755-5922.2010.00202.x
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journal_title:Cardiovascular therapeutics
pub_type: 杂志文章,多中心研究
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journal_title:Cardiovascular therapeutics
pub_type: 杂志文章
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journal_title:Cardiovascular therapeutics
pub_type: 杂志文章,meta分析
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journal_title:Cardiovascular therapeutics
pub_type: 杂志文章,评审
doi:10.1155/2020/1743927
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journal_title:Cardiovascular therapeutics
pub_type: 杂志文章
doi:10.1111/j.1755-5922.2011.00275.x
更新日期:2012-12-01 00:00:00
abstract:BACKGROUND AND AIM:Warfarin treatment discontinuation is significant among patients with atrial fibrillation (AF). Studies mainly focused on whether the proportion of warfarin persistence and discontinuation are clinically appropriate are absent. This study evaluates warfarin persistence with focus on predictors for, a...
journal_title:Cardiovascular therapeutics
pub_type: 杂志文章
doi:10.1111/1755-5922.12224
更新日期:2016-12-01 00:00:00
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journal_title:Cardiovascular therapeutics
pub_type: 杂志文章,评审
doi:10.1111/j.1755-5922.2010.00200.x
更新日期:2010-08-01 00:00:00
abstract:AIM:Previous studies and national assessments indicate an undertreatment of mineralocorticoid receptor antagonists (MRA) in heart failure with reduced ejection fraction (HFrEF). This study aimed to investigate why MRA is not used to full extent. METHODS:A complete community-based heart failure population was studied. ...
journal_title:Cardiovascular therapeutics
pub_type: 杂志文章
doi:10.1111/1755-5922.12459
更新日期:2018-10-01 00:00:00
abstract:AIMS:This study aimed to assess prescribers' monitoring for arrhythmic risk with QT-prolonging medications (LQT drugs). METHODS:Over a 6-month period, all inpatients under the care of Cardiologists (Cohort A) and General Physicians (Cohort B) at Aberdeen Royal Infirmary who were prescribed drugs with known risk of Tor...
journal_title:Cardiovascular therapeutics
pub_type: 杂志文章
doi:10.1111/1755-5922.12085
更新日期:2014-10-01 00:00:00
abstract::Cilnidipine is a unique Ca(2+) channel blocker with an inhibitory action on the sympathetic N-type Ca(2+) channels, which is used for patients with hypertension in Japan. Cilnidipine has been clarified to exert antisympathetic actions in various examinations from cell to human levels, in contrast to classical Ca(2+) c...
journal_title:Cardiovascular therapeutics
pub_type: 历史文章,杂志文章,评审
doi:10.1111/j.1755-5922.2009.00079.x
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abstract:INTRODUCTION:Options for a pharmacological cardioversion (CV) of short-duration atrial fibrillation (AF) in patients with a stable coronary artery disease (CAD) are limited to amiodarone or vernakalant. Antazoline has been reported to achieve high rates of AF conversion to sinus rhythm, but data on its effectiveness an...
journal_title:Cardiovascular therapeutics
pub_type: 杂志文章
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abstract::Atrial fibrillation (AF) is very common within the first 5 days of cardiac surgery. It is associated with significant morbidity including stroke, ventricular arrhythmias, myocardial infarction, heart failure, acute kidney injury, prolonged hospital stay, and also short- and long-term mortality. The underlying mechanis...
journal_title:Cardiovascular therapeutics
pub_type: 杂志文章,评审
doi:10.1111/j.1755-5922.2009.00117.x
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abstract::Atherosclerosis is one of the major macrovascular complications of diabetes mellitus (DM), and it is the main cause of death from clinical observation. Among various cell types involved in this disorder, endothelial cells, vascular smooth muscle cells (VSMCs), and macrophages play a crucial role in the occurrence and ...
journal_title:Cardiovascular therapeutics
pub_type: 杂志文章,评审
doi:10.1111/1755-5922.12436
更新日期:2018-08-01 00:00:00
abstract:BACKGROUND:Mode of death in chronic heart failure (CHF) may be of relevance to choice of therapy for this condition. Sudden death is particularly common in patients with early and/or mild/moderate CHF. β-Blockade may provide better protection against sudden death than ACE inhibition (ACEI) in this setting. METHODS:We ...
journal_title:Cardiovascular therapeutics
pub_type: 杂志文章,多中心研究,随机对照试验
doi:10.1111/j.1755-5922.2010.00185.x
更新日期:2011-04-01 00:00:00
abstract:INTRODUCTION:Statins are known to prevent heart failure (HF). However, it is unclear whether statins as class or type (lipophilic or hydrophilic) improve outcomes of established HF. AIMS:The current meta-analysis was performed to compare the treatment effects of lipophilic and hydrophilic statins on inflammation and c...
journal_title:Cardiovascular therapeutics
pub_type: 杂志文章,meta分析,评审
doi:10.1111/1755-5922.12150
更新日期:2015-12-01 00:00:00
abstract:Background:Atherosclerosis (AS) is a common severe disease around the world. The merging paper reported that long noncoding RNAs (lncRNAs) took part in diversified pathological processes of AS, although the mechanism remains unknown. This study is aimed at uncovering the profile of lncRNA taurine-upregulated gene 1 (TU...
journal_title:Cardiovascular therapeutics
pub_type: 杂志文章
doi:10.1155/2020/6758934
更新日期:2020-05-29 00:00:00
abstract:AIM:Cardiac hypertrophy and myocardial fibrosis significantly contribute to the pathogenesis of diabetic cardiomyopathy (DCM). Altered expression of several genes and their regulation by microRNAs has been reported in hypertrophied failing hearts. This study aims to examine the role of Cdc42, Pak1, and miR-30c in the p...
journal_title:Cardiovascular therapeutics
pub_type: 杂志文章
doi:10.1111/1755-5922.12113
更新日期:2015-06-01 00:00:00
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journal_title:Cardiovascular therapeutics
pub_type: 杂志文章,评审
doi:10.1111/1755-5922.12105
更新日期:2015-04-01 00:00:00
abstract::Morbidity of patients with cardiac syndrome X (typical anginal-like chest pain and normal coronary arteriogram) is high with continuing episodes of chest pain and frequent hospital readmissions. Management of this syndrome represents a major challenge for the treating physician. Conventional therapies with antianginal...
journal_title:Cardiovascular therapeutics
pub_type: 杂志文章,评审
doi:10.1111/j.1755-5922.2008.00070.x
更新日期:2009-04-01 00:00:00
abstract::Ventricular free wall rupture (FWR) is a catastrophic complication after acute myocardial infarction (AMI). However, patients with FWR die of cardiac tamponade secondary to intrapericardial hemorrhage that can be treated if properly diagnosed. Unfortunately, FWR was still not diagnosed and classified quickly and accur...
journal_title:Cardiovascular therapeutics
pub_type: 杂志文章
doi:10.1155/2021/1716546
更新日期:2021-01-02 00:00:00
abstract:BACKGROUND:Doxorubicin (DOX) is an anthracycline antitumor drug. However, its clinical use is limited by dose-dependent cardiotoxicity and even progresses to chronic heart failure (CHF). OBJECTIVE:This study aims to investigate whether the Nrf2 activator, sulforaphane (SFN), can prevent DOX-induced CHF. METHODS:Male ...
journal_title:Cardiovascular therapeutics
pub_type: 杂志文章
doi:10.1111/1755-5922.12277
更新日期:2017-10-01 00:00:00
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journal_title:Cardiovascular therapeutics
pub_type: 杂志文章,meta分析,评审
doi:10.1111/1755-5922.12062
更新日期:2014-06-01 00:00:00