PCSK9 Inhibitors in Development

Jul 10, 2014

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PCSK9 Inhibitors in Development. mAb = monoclonal antibody Sheridan C. Nature B iotechnology. December 12, 2013; V31:1058.

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PCSK9 Inhibitors in Development

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PCSK9 Inhibitors in Development mAb = monoclonal antibody Sheridan C. Nature Biotechnology. December 12, 2013; V31:1058.

INHIBITORS

INHIBITORS. What are some examples ? What experiments show they are SPECIFIC !!! Do they always work?. INHIBITORS Used to diminish or abolish a biological activity so that conclusions can be drawn about the properties of that activities or of a process by which the activity may play a role.

536 views • 16 slides

Protease Inhibitors

Protease Inhibitors. Protease Inhibitors. Amprenavir (APV) – GlaxoSmithKline, 1999 1,200mg 1x/day, rare side effects: Stevens-Johnsons Synd More rare side effects: diabetes, increased cholesterol levels Side effects: vomiting, perioral parethesias, diarrhea Indinavir (IDV) – Merck, 1996

820 views • 32 slides

Phosphodiesterase inhibitors

Phosphodiesterase inhibitors. By Nashwa Naeem Elfar Ass. lecturer. Phosphodiesterase enzymes (PDE).

6.35k views • 33 slides

ACE Inhibitors

ACE Inhibitors. ACE = Angiotensin I Converting Enzyme 10 ACE inhibitors available in US: benazepril, captopril, enalapril, fosinopril, lisinopril, moexipril, perindopril, quinapril, ramipril and trandolapril.

1.31k views • 22 slides

Aromatase inhibitors in pediatrics

Aromatase inhibitors in pediatrics . short stature and delayed puberty. Aromatase. Enzyme located in the endoplasmic reticulum of estrogen-producing cells Catalyzes the rate-limiting step in the conversion of androgens to estrogens in many tissues . Drugs.

755 views • 47 slides

Prevention of Inhibitors in Hemophilia

Prevention of Inhibitors in Hemophilia. Manuel Carcao MD, MSc Paediatric Hematologist Associate Professor Hospital for Sick Children University of Toronto Toronto, Canada. How to reduce inhibitors.

1.68k views • 85 slides

Allosteric Inhibitors

Allosteric Inhibitors. By Kelsey Martin and Christine Bondira. A noncompetitive inhibitor binds to the enzyme away from the active site, altering the conformation of the enzyme so that its active site no longer functions . Noncompetitive inhibitor. He took my spot!!.

338 views • 5 slides

PCSK9 relative to baseline

Mean plasma PCSK9 concentrations relative to baseline after PCSK9-siRNA treatment or placebo. PCSK9 relative to baseline. Day. Fitzgerald et al., The Lancet 2013. Mean serum LDL-c concentrations relative to baseline after PCSK9-siRNA treatment or placebo.

204 views • 2 slides

Phosphodiesterase Inhibitors

Phosphodiesterase Inhibitors. Bipyridines :( Amrinone , Milrinone ) only available in parenteral form. Half-life 3-6hrs. Excreted in urine. Mechanism of action. Inhibit phosphodiesterase isozyme 3 in cardiac & smooth muscles → : ↑ cAMP

747 views • 25 slides

Inhibitors

Inhibitors. Why they happen What are they How to control them Treatment options. Why Inhibitors H appen. Genetics Hemophilia severity More common in severe hemophilia FVIII mutations Mutations in intron 22 and 1 (regions inside a gene) Nonsense mutations Stop codon

421 views • 14 slides

Noncompetitive Inhibitors

Noncompetitive Inhibitors. John Simila Mary- Cate Welsh Brian Decorte. What are Noncompetitive Inhibitors?. A substance that interacts with the enzyme but not at the active site. They do not directly compete with the substrate to bind at the active site.

222 views • 6 slides

Acetylcholinesterase Inhibitors

PHM142 Fall 2013 Instructor: Dr. Jeffrey Henderson. Acetylcholinesterase Inhibitors. By: Rohini Bagchi , Janice Chan, John Chen, Melissa Taylor Date : December 4, 2013. Overview . Background Effects of AchE Inhibitors “Good” AChE Inhibitors “Bad” AChE Inhibitors. Background.

1.24k views • 20 slides

ACE Inhibitors

ACE Inhibitors. Charley Bruce. Plan. Indications Mechanism of action Side Effects Contraindications Metabolism Pharmacokinetics. Indications. Hypertension Heart Failure Diabetic Nephropathy Prophylaxis of Cardiovascular Events. Renin-Angiotensin-Aldosterone System. Hypertension.

731 views • 16 slides

ACE Inhibitors

ACE Inhibitors. By Jessica Davies. What are ACE Inhibitors?. Angiotensin Converting Enzyme Inhibitors Used to help control Hypertension Also they help with heart failure, preventing strokes, and preventing kidney damage in people with hypertension or diabetes.

1.13k views • 11 slides

Cholinesterase inhibitors

Cholinesterase inhibitors. R1 이영석. Cholinergic agonist. Direct acting acetylcholine, methacholine, bethanechol, carbachol Indirect acting (reversible) neostigmine, edrophonium pyridostigmine, physostigmine Indirect acting (irreversible)

1.12k views • 27 slides

Acetylcholinesterase Inhibitors

Acetylcholinesterase Inhibitors. Acetylcholinesterase Located in synapses Substrate selectivity: ACH. Plasma cholinesterase Located in plasma (non-neuronal) Substrate selectivity: ACH Succinylcholine Local anesthetics (procaine). Types of cholinesterases. Glu 327. His 440.

862 views • 37 slides

Dadu, R. T. & Ballantyne, C. M. (2014) Lipid lowering with PCSK9 inhibitors

Figure 2 Ongoing phase III clinical trials of PCSK9 inhibitors. Dadu, R. T. & Ballantyne, C. M. (2014) Lipid lowering with PCSK9 inhibitors Nat. Rev. Cardiol. doi:10.1038/nrcardio.2014.84.

429 views • 1 slides

Aromatase Inhibitors in Breast Cancer

Aromatase Inhibitors in Breast Cancer. Development of Aromatase Inhibitors: Activity Profiles. Toxicity. Specificity. Potency. First generation. Rash, etc. - Aminoglutethimide*. 1. Second generation. - Fadrozole - 4-OHA. 100. Third generation. - Anastrozole - Exemestane

1.15k views • 40 slides

PCSK9 Loss-of-function Mutations

PCSK9 Loss-of-function Mutations. PCSK9-Mediated Degradation of LDL-R. Evolution of Therapeutic Monoclonal Antibodies. Effect of PCSK9 Inhibitors on LDL-C in Heterozygous FH. DESCARTES % Change in LDL-C From Baseline at Week 52 in Patients With Hypercholesterolemia.

610 views • 19 slides

PCSK9 Mutations

PCSK9 Mutations. PCSK9 Loss-of-function Mutations. 2013 ACC/AHA Cholesterol Guidelines 4 Major Statin Benefit Groups. PCSK9 Monoclonal Antibodies. MENDEL Evolocumab Monotherapy for H ypercholesterolemia. LAPLACE-2 Study Design. LAPLACE-2 LDL-C Response at Mean of Weeks 10 and 12.

803 views • 19 slides

Cholesterol, CV Events, and PCSK9 Inhibitors Highlights From the AHA

Cholesterol, CV Events, and PCSK9 Inhibitors Highlights From the AHA. Goal. Statin Intolerance. Serial IVUS. Effect on CHD Events of Lowering LDL-C. Percent Change in LDL-C During Treatment. Primary Endpoint: PAV. Percent of Patients Showing Regression in PAV.

457 views • 34 slides

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PCSK9 Inhibitors in Development

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Presentation Transcript

INHIBITORS

Protease Inhibitors

Phosphodiesterase inhibitors

ACE Inhibitors

Aromatase inhibitors in pediatrics

Prevention of Inhibitors in Hemophilia

Allosteric Inhibitors

PCSK9 relative to baseline

Phosphodiesterase Inhibitors

Inhibitors

Noncompetitive Inhibitors

Acetylcholinesterase Inhibitors

ACE Inhibitors

ACE Inhibitors

Cholinesterase inhibitors

Acetylcholinesterase Inhibitors

Dadu, R. T. &amp; Ballantyne, C. M. (2014) Lipid lowering with PCSK9 inhibitors

Aromatase Inhibitors in Breast Cancer

PCSK9 Loss-of-function Mutations

PCSK9 Mutations

Cholesterol, CV Events, and PCSK9 Inhibitors Highlights From the AHA

Dadu, R. T. & Ballantyne, C. M. (2014) Lipid lowering with PCSK9 inhibitors