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https://www.readbyqxmd.com/read/28636184/pharmacokinetics-pharmacodynamics-of-bococizumab-a-monoclonal-antibody-to-pcsk9-after-single-subcutaneous-injection-at-3-sites-nct-02043301
#1
Ellen Q Wang, Anna Plotka, Joanne Salageanu, Catherine Sattler, Carla Yunis
AIM: To characterize the single-dose pharmacokinetics (PK) and pharmacodynamics (PD) of bococizumab, a monoclonal antibody inhibiting proprotein convertase subtilisin/kexin type 9 (PCSK9), administered subcutaneously (s.c.) to the abdomen, thigh, or upper arm (NCT02043301). METHODS: Seventy-five adults with low-density lipoprotein cholesterol (LDL-C) ≥130 mg/dL and not on background lipid-lowering therapy were randomized (1:1:1) to a single 150-mg s.c. dose of bococizumab administered to the abdomen, thigh, or upper arm...
June 21, 2017: Cardiovascular Therapeutics
https://www.readbyqxmd.com/read/28617192/emerging-biologic-therapies-for-hypercholesterolaemia
#2
Giacomo Pucci, Arrigo F Cicero, Claudio Borghi, Giuseppe Schillaci
LDL-cholesterol (LDL-C) is one of the most well-established risk factors for CV disease. Indeed, therapies that decrease LDL-C are proven to effectively reduce the risk of atherosclerotic CV disease. Monoclonal antibodies (mAbs) that target proprotein convertase subtilisin/kexin type 9 (PCSK9) have recently gained traction as a promising therapeutic strategy. Areas covered: In this review, the authors discuss the effectiveness of mAbs against PCSK9 in lowering low-density lipoprotein cholesterol (LDL-C) and other atherogenic lipid fractions...
June 15, 2017: Expert Opinion on Biological Therapy
https://www.readbyqxmd.com/read/28596304/pcsk9-inhibition-and-atherosclerotic-cardiovascular-disease-prevention-does-reality-match-the-hype
#3
REVIEW
Savvas Hadjiphilippou, Kausik K Ray
Within this review we look at whether the potential provided by proprotein convertase subtilisin/kexin type 9 (PCSK9) inhibition for prevention of atherosclerotic cardiovascular disease matches the excitement generated. Two fully human monoclonal antibodies to PCSK9 are currently licenced for clinical use both in the USA and the European Union: evolocumab and alirocumab. These reduce low-density lipoprotein cholesterol by over 50% across a range of populations and were generally found to have a safety profile comparable with placebo...
June 8, 2017: Heart: Official Journal of the British Cardiac Society
https://www.readbyqxmd.com/read/28552009/bococizumab-for-the-treatment-of-hypercholesterolaemia
#4
Nicola Ferri, Alberto Corsini, Cesare R Sirtori, Massimiliano Ruscica
No abstract text is available yet for this article.
July 2017: Expert Opinion on Biological Therapy
https://www.readbyqxmd.com/read/28549755/cholesterol-and-stroke-roll-of-pcsk9-inhibitors
#5
L Castilla-Guerra, M C Fernández-Moreno, M A Rico-Corral
INTRODUCTION: Proprotein convertase subtilisin/kexin type 9 (PCSK9) plays an important role in the modulation of plasma levels of low density lipoprotein cholesterol (LDLC). PCSK9 binds to the LDL receptor (LDLR), disrupts its endocytic recycling itinerary and directs it to lysosomal degradation. Activation of PCSK9 can thus decrease the expression of LDLR in the liver and inhibit LDL uptake, which leads to hypercholesterolaemia. DEVELOPMENT: Currently we now know that different polymorphisms of PCSK9 are associated with the occurrence of ischaemic stroke...
May 23, 2017: Neurología: Publicación Oficial de la Sociedad Española de Neurología
https://www.readbyqxmd.com/read/28539539/efficacy-and-safety-of-bococizumab-rn316-pf-04950615-a-monoclonal-antibody-against-proprotein-convertase-subtilisin-kexin-type-9-in-hypercholesterolemic-japanese-subjects-receiving-a-stable-dose-of-atorvastatin-or-treatment-naive%C3%A3-results-from-a-randomized
#6
Koutaro Yokote, Shigeto Kanada, Osamu Matsuoka, Hisakuni Sekino, Keiji Imai, Junichi Tabira, Nobushige Matsuoka, Sandip Chaudhuri, Tamio Teramoto
BACKGROUND: A Phase 2, dose-ranging study of bococizumab, a monoclonal anti-proprotein convertase subtilisin/kexin type 9 antibody, was conducted in Japanese subjects to assess its efficacy, safety, and tolerability in this population.Methods and Results:Two different hypercholesterolemic study populations were enrolled concurrently: Japanese subjects with uncontrolled low-density lipoprotein cholesterol (LDL-C) despite atorvastatin treatment (LDL-C ≥100 mg/dL; n=121), and Japanese subjects naive to lipid-lowering agents and with LDL-C ≥130 mg/dL (n=97)...
May 23, 2017: Circulation Journal: Official Journal of the Japanese Circulation Society
https://www.readbyqxmd.com/read/28453187/pcsk9-monoclonal-antibodies-for-the-primary-and-secondary-prevention-of-cardiovascular-disease
#7
REVIEW
Amand F Schmidt, Lucy S Pearce, John T Wilkins, John P Overington, Aroon D Hingorani, Juan P Casas
BACKGROUND: Despite the availability of effective drug therapies that reduce low-density lipoprotein (LDL)-cholesterol (LDL-C), cardiovascular disease (CVD) remains an important cause of mortality and morbidity. Therefore, additional LDL-C reduction may be warranted, especially for patients who are unresponsive to, or unable to take, existing LDL-C-reducing therapies. By inhibiting the proprotein convertase subtilisin/kexin type 9 (PCSK9) enzyme, monoclonal antibodies (PCSK9 inhibitors) may further reduce LDL-C, potentially reducing CVD risk as well...
April 28, 2017: Cochrane Database of Systematic Reviews
https://www.readbyqxmd.com/read/28304242/cardiovascular-efficacy-and-safety-of-bococizumab-in-high-risk-patients
#8
RANDOMIZED CONTROLLED TRIAL
Paul M Ridker, James Revkin, Pierre Amarenco, Robert Brunell, Madelyn Curto, Fernando Civeira, Marcus Flather, Robert J Glynn, Jean Gregoire, J Wouter Jukema, Yuri Karpov, John J P Kastelein, Wolfgang Koenig, Alberto Lorenzatti, Pravin Manga, Urszula Masiukiewicz, Michael Miller, Arend Mosterd, Jan Murin, Jose C Nicolau, Steven Nissen, Piotr Ponikowski, Raul D Santos, Pamela F Schwartz, Handrean Soran, Harvey White, R Scott Wright, Michal Vrablik, Carla Yunis, Charles L Shear, Jean-Claude Tardif
BACKGROUND: Bococizumab is a humanized monoclonal antibody that inhibits proprotein convertase subtilisin-kexin type 9 (PCSK9) and reduces levels of low-density lipoprotein (LDL) cholesterol. We sought to evaluate the efficacy of bococizumab in patients at high cardiovascular risk. METHODS: In two parallel, multinational trials with different entry criteria for LDL cholesterol levels, we randomly assigned the 27,438 patients in the combined trials to receive bococizumab (at a dose of 150 mg) subcutaneously every 2 weeks or placebo...
April 20, 2017: New England Journal of Medicine
https://www.readbyqxmd.com/read/28304227/lipid-reduction-variability-and-antidrug-antibody-formation-with-bococizumab
#9
RANDOMIZED CONTROLLED TRIAL
Paul M Ridker, Jean-Claude Tardif, Pierre Amarenco, William Duggan, Robert J Glynn, J Wouter Jukema, John J P Kastelein, Albert M Kim, Wolfgang Koenig, Steven Nissen, James Revkin, Lynda M Rose, Raul D Santos, Pamela F Schwartz, Charles L Shear, Carla Yunis
BACKGROUND: Bococizumab, a humanized monoclonal antibody targeting proprotein convertase subtilisin-kexin type 9 (PCSK9), reduces levels of low-density lipoprotein (LDL) cholesterol. However, the variability and durability of this effect are uncertain. METHODS: We conducted six parallel, multinational lipid-lowering trials enrolling 4300 patients with hyperlipidemia who were randomly assigned to receive 150 mg of bococizumab or placebo subcutaneously every 2 weeks and who were followed for up to 12 months; 96% were receiving statin therapy at the time of enrollment...
April 20, 2017: New England Journal of Medicine
https://www.readbyqxmd.com/read/28181260/a-mechanism-based-pharmacokinetic-pharmacodynamic-model-for-bococizumab-a-humanized-monoclonal-antibody-against-proprotein-convertase-subtilisin-kexin-type-9-and-its-application-in-early-clinical-development
#10
Chandrasekhar Udata, Pamela D Garzone, Barry Gumbiner, Tenshang Joh, Hong Liang, Kai-Hsin Liao, Jason H Williams, Xu Meng
Bococizumab (RN316/PF-04950615), a humanized monoclonal antibody, binds to secreted proprotein convertase subtilisin/kexin type 9 (PCSK9) and prevents its downregulation of low-density lipoprotein receptor, leading to improved clearance and reduction of low-density lipoprotein cholesterol (LDL-C) in plasma. A mechanism-based drug-target binding model was developed, accounting for bococizumab, PCSK9, and LDL-C concentrations and the effects of concomitant administration of statins. This model was utilized to better understand the pharmacokinetic/pharmacodynamic (PK/PD) data obtained from 3 phase 1 and 2 phase 2a clinical studies...
February 9, 2017: Journal of Clinical Pharmacology
https://www.readbyqxmd.com/read/28060539/bococizumab-for-the-treatment-of-hypercholesterolaemia
#11
Nicola Ferri, Alberto Corsini, Cesare R Sirtori, Massimiliano Ruscica
Low-density lipoprotein cholesterol (LDL-C) remains a well-established risk factor for cardiovascular disease (CVD). LDL-C levels are considered primary targets of therapy. A new series of systemic biomolecules, the monoclonal antibodies (mAbs) of proprotein convertase subtilisin/kexin type 9 (PCSK9), have a higher activity in reducing LDL-C. Areas covered: The authors critically review the current evidence on the efficacy and safety of bococizumab, a humanized mAb against PCSK9, which was surprisingly discontinued in November 2016...
February 2017: Expert Opinion on Biological Therapy
https://www.readbyqxmd.com/read/27888904/-anti-pcsk9-antibodies-in-type-2-diabetes-and-secondary-prevention-of-cardiovascular-diseases
#12
REVIEW
José López-Miranda, Xavier Pintó
Patients with type 2 diabetes are considered to have the same cardiovascular risk as patients with ischemia. However, the degree of lipid control in diabetic and ischemic patients remains highly deficient. The availability of new agents, such as anti-PCSK9 monoclonal antibodies, could represent a notable advance in meeting this unmet need. Alirocumab and evolucumab, followed by bococizumab, are currently under the advanced phase of research. A growing database has demonstrated a relationship between glucose metabolism, body weight and PCSK9 function, but the clinical implications of this relationship have not been well defined...
May 2016: Clínica e Investigación en Arteriosclerosis
https://www.readbyqxmd.com/read/27877050/development-of-proprotein-convertase-subtilisin-kexin-type-9-inhibitors-and-the-clinical-potential-of-monoclonal-antibodies-in-the-management-of-lipid-disorders
#13
REVIEW
Sanjiv Gupta
The aim of this manuscript is to review available data to evaluate the present status of proprotein convertase subtilisin/kexin type 9 (PCSK9) inhibitors in the treatment of hypercholesterolemia. Relevant literature since 2003 is reviewed. The effectiveness of PCSK9 inhibitors in lowering low-density lipoprotein cholesterol and other atherogenic lipid fractions was studied in various Phase 2 and Phase 3 trials of Alirocumab, Evolocumab, and Bococizumab. The results of published long-term ODYSSEY and OSLER studies are summarized...
2016: Vascular Health and Risk Management
https://www.readbyqxmd.com/read/27860267/a-phase-i-randomized-study-of-a-specifically-engineered-ph-sensitive-pcsk9-inhibitor-rn317-pf-05335810-in-hypercholesterolemic-subjects-on-statin-therapy
#14
M Levisetti, T Joh, H Wan, H Liang, P Forgues, B Gumbiner, P D Garzone
This phase I study assessed the safety, tolerability, pharmacokinetics, and pharmacodynamics of RN317 (PF-05335810), a specifically engineered, pH-sensitive, humanized proprotein convertase subtilisin kexin type 9 (PCSK9) monoclonal antibody, in hypercholesterolemic subjects (low-density lipoprotein cholesterol (LDL-C) ≥ 80 mg/dl) 18-70 years old receiving statin therapy. Subjects were randomized to: single-dose placebo, RN317 (subcutaneous (s.c.) 0.3, 1, 3, 6, or intravenous (i.v.) 1, 3, 6 mg/kg), or bococizumab (s...
January 2017: Clinical and Translational Science
https://www.readbyqxmd.com/read/27502861/evaluating-bococizumab-a-monoclonal-antibody-to-pcsk9-on-lipid-levels-and-clinical-events-in-broad-patient-groups-with-and-without-prior-cardiovascular-events-rationale-and-design-of-the-studies-of-pcsk9-inhibition-and-the-reduction-of-vascular-events-spire
#15
RANDOMIZED CONTROLLED TRIAL
Paul M Ridker, Pierre Amarenco, Robert Brunell, Robert J Glynn, J Wouter Jukema, John J P Kastelein, Wolfgang Koenig, Steven Nissen, James Revkin, Raul D Santos, Pamela F Schwartz, Carla Yunis, Jean-Claude Tardif
BACKGROUND: Although statins significantly reduce vascular event rates, residual cholesterol risk remains high in many patient groups, including those with known vascular disease as well as in the setting of high-risk primary prevention. Bococizumab is a humanized monoclonal antibody that inhibits proprotein convertase subtilisin-kexin type 9 (PCSK9), prolongs the half-life of hepatic low-density lipoprotein (LDL) receptors, and reduces circulating atherogenic cholesterol levels. DESIGN: The SPIRE program comprises 6 lipid-lowering studies and 2 cardiovascular outcomes trials, each comparing bococizumab (150 mg subcutaneously every 2 weeks) to matching placebo...
August 2016: American Heart Journal
https://www.readbyqxmd.com/read/27389630/vaccine-strategies-for-lowering-ldl-by-immunization-against-proprotein-convertase-subtilisin-kexin-type-9
#16
Bryce Chackerian, Alan Remaley
PURPOSE OF REVIEW: mAbs targeting proprotein convertase subtilisin/kexin type 9 (PCSK9) have the potential to become groundbreaking therapies for the treatment of hypercholesterolemia. However, one major drawback of mAb-based therapy for a chronic condition like dyslipidemia is its relatively high cost. This review summarizes two recent studies describing novel vaccine approaches for lowering LDL-cholesterol by active immunization against PCSK9. RECENT FINDINGS: PCSK9 is a plasma protein secreted by the liver that controls cholesterol homeostasis by enhancing endosomal and lysosomal degradation of the LDL receptor...
August 2016: Current Opinion in Lipidology
https://www.readbyqxmd.com/read/27352986/proprotein-convertase-subtilisin-kexin-type-9-pcsk9-inhibitors-present-perspectives-and-future-horizons
#17
REVIEW
K Yadav, M Sharma, K C Ferdinand
AIMS: Our comprehensive review highlights the drug development and pharmacogenomics leading to the recent approval of PCSK9 inhibitors. We also review the anticipated future advances into the uses of PCSK9 inhibition. BACKGROUND: Despite the present advances in pharmacotherapy, atherosclerotic cardiovascular disease (ASCVD) remains the leading cause of mortality worldwide. Low density lipoprotein-cholesterol (LDL-C) lowering is the primary target for ASCVD risk reduction, showing demonstrable benefits in mortality...
October 2016: Nutrition, Metabolism, and Cardiovascular Diseases: NMCD
https://www.readbyqxmd.com/read/27195910/pcsk9-inhibition-with-monoclonal-antibodies-modern-management-of-hypercholesterolemia
#18
REVIEW
Matthew K Ito, Raul D Santos
Current guidelines for hypercholesterolemia treatment emphasize lifestyle modification and lipid-modifying therapy to reduce the risk for cardiovascular disease. Statins are the primary class of agents used for the treatment of hypercholesterolemia. Although statins are effective for many patients, they fail to achieve optimal reduction in lipids for some patients, including those who have or are at high risk for cardiovascular disease. The PCSK9 gene was identified in the past decade as a potential therapeutic target for the management of patients with hypercholesterolemia...
January 2017: Journal of Clinical Pharmacology
https://www.readbyqxmd.com/read/27098076/-severe-hypercholesterolaemia-when-to-use-the-proprotein-convertase-subtilisin-kexin-type-9-protease-inhibitors-pcsk9-inhibitors-polish-society-of-cardiology-experts-group-statement
#19
Barbara Cybulska, Zbigniew Gaciong, Piotr Hoffman, Piotr Jankowski, Longina Kłosiewicz-Latoszek, Jarosław Kaźmierczak, Katarzyna Mitręga, Grzegorz Opolski, Andrzej Pająk, Piotr Ponikowski, Andrzej Rynkiewicz, Janina Stępińska, Beata Średniawa, Zbigniew Kalarus
The severe hypercholesterolaemia can be recognised when low density lipoprotein cholesterol (LDL-C) serum levels are equal to or above 5 mmol/L (≥ 190 mg/dL). The prevalence of LDL-C ≥ 5 mmol/L is 3.8% in Polish population aged 18-79 years. Among these adults there are patients with familial hypercholesterolaemia (FH). According to meta-analysis of 6 Polish population surveys prevalence of heterozygous FH (HeFH) diagnosed using Dutch Lipid Clinic criteria is 0.4% (95% Cl 0.28-0.53%) in men and women aged 20-74 years, i...
2016: Kardiologia Polska
https://www.readbyqxmd.com/read/26886466/pcsk9-inhibitors-an-innovative-approach-to-treating-hyperlipidemia
#20
REVIEW
Alexandra M Sible, James J Nawarskas, Joe R Anderson
Proprotein convertase subtilisin kexin type 9 (PCSK9) inhibitors are novel agents indicated for the treatment of hyperlipidemia. Inhibition of PCSK9 produces an increase in surface low-density lipoprotein (LDL) receptors and increases removal of LDL from the circulation. Alirocumab (Praluent; Sanofi/Regeneron, Bridgewater, NJ) and evolocumab (Repatha; Amgen, Thousand Oaks, CA) are currently available and approved for use in patients with heterozygous familial hypercholesterolemia, homozygous familial hypercholesterolemia, and clinical atherosclerotic cardiovascular disease...
May 2016: Cardiology in Review
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