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PCSK9 Inhibitors : From Nature's Lessons to Clinical Utility

Raal, Frederick J. (author)
Univ Witwatersrand, Fac Hlth Sci, Div Endocrinol & Metab, Dept Med, ZA-2193 Johannesburg, South Africa.
Chilton, Robert (author)
Univ Texas Hlth Sci Ctr, Div Cardiol & Intervent Cardiol, Fac Med, Dept Med, San Antonio, TX USA.
Ranjith, Naresh (author)
Cardiovasc Res Ctr, Dept Cardiol, Durban, South Africa.
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Rambiritch, Virendra (author)
Univ KwaZulu Natal, Discipline Pharmaceut Sci, Fac Hlth Sci, Dept Pharmacol, Durban, South Africa.
Leisegang, Rory F. (author)
Uppsala universitet,Institutionen för farmaceutisk biovetenskap
Ebrahim, Iftikhar O. (author)
Netcare Unitas Hosp, Dept Cardiol, Pretoria, South Africa.
van Tonder, Alet (author)
Sanofi, Med Affairs, Dept Diabet & Cardiovasc Med, Midrand, South Africa.
Shunmoogam, Nelusha (author)
Sanofi, Med Affairs, Dept Diabet & Cardiovasc Med, Midrand, South Africa.
Bouharati, Celia (author)
Sanofi, Clin Study Unit, Dept Clin Trials, Midrand, South Africa.
Musa, Moji G. (author)
Sanofi, Med Affairs, Dept Diabet & Cardiovasc Med, Midrand, South Africa.
Karamchand, Sumanth (author)
Stellenbosch Univ, Fac Med & Hlth Sci, Dept Med, Cape Town, South Africa.
Naidoo, Poobalan (author)
Sanofi, Med Affairs, Dept Diabet & Cardiovasc Med, Midrand, South Africa.
Blom, Dirk J. (author)
Univ Cape Town, Div Lipidol, Dept Med, Cape Town, South Africa.;Univ Cape Town, Hatter Inst Cardiovasc Res Africa, Cape Town, South Africa.
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Univ Witwatersrand, Fac Hlth Sci, Div Endocrinol & Metab, Dept Med, ZA-2193 Johannesburg, South Africa Univ Texas Hlth Sci Ctr, Div Cardiol & Intervent Cardiol, Fac Med, Dept Med, San Antonio, TX USA. (creator_code:org_t)
Bentham Science Publishers Ltd. 2020
2020
English.
In: Endocrine, Metabolic & Immune Disorders - Drug Targets. - : Bentham Science Publishers Ltd.. - 1871-5303 .- 2212-3873. ; 20:6, s. 840-854
  • Research review (peer-reviewed)
Abstract Subject headings
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  • Background: Proprotein convertase subtilisin-kexin type 9 (PCSK9) inhibitors are a novel class of non-statin lipid lowering therapy that reduce LDL-cholesterol by 50 - 6044,. PCSK9 inhibitors decrease LDL-cholesterol by preventing intracellular degradation of LDL receptors; subsequently, a greater number of LDL-receptors arc available on the cell surface to extract circulating LDL. Objective: To describe the origins of PCSK9 inhibitors and their current use in clinical practice. Methods: We performed a narrative review of the PCSK9 inhibitor class of drugs Results: Current data indicate that PCSK9 inhibitors effectively reduce LDL-cholesterol and are well tolerated and safe. PCSK9 inhibitors have also been shown to reduce cardiovascular event rates in patients with stable atherosclerotic cardiovascular disease and in patients with a recent (up to one year) acute coronary syndrome. Given the costs, chronicity of the treatment and the potential budget impact, PCSK9 inhibitors are often limited to patients with the highest absolute risk for major adverse cardiovascular events despite optimal treatment with high-intensity statin and ezetimibe. Conclusion: PCSK9 inhibitors have a favorable safety, efficacy and tolerability profile. Post marketing safety surveillance and real-world studies are needed to further support the long-term safety profile of this class of medicine.

Subject headings

MEDICIN OCH HÄLSOVETENSKAP  -- Klinisk medicin -- Kardiologi (hsv//swe)
MEDICAL AND HEALTH SCIENCES  -- Clinical Medicine -- Cardiac and Cardiovascular Systems (hsv//eng)
MEDICIN OCH HÄLSOVETENSKAP  -- Medicinska och farmaceutiska grundvetenskaper -- Farmakologi och toxikologi (hsv//swe)
MEDICAL AND HEALTH SCIENCES  -- Basic Medicine -- Pharmacology and Toxicology (hsv//eng)

Keyword

PCSK9 inhibitors
LDL-cholesterol
atherosclerotic cardiovascular disease
major adverse cardiovascular events
acute coronary syndrome
high intensity statin
ezetimibe

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