Antisense oligonucleotides targeting apolipoprotein (a) in people with raised lipoprotein (a): two randomised, double-blind, placebo-controlled, dose-ranging trials

NJ Viney, JC van Capelleveen, RS Geary, S Xia… - The Lancet, 2016 - thelancet.com
Background Elevated lipoprotein(a) (Lp[a]) is a highly prevalent (around 20% of people)
genetic risk factor for cardiovascular disease and calcific aortic valve stenosis, but no approved …

[HTML][HTML] Pharmacokinetics, biodistribution and cell uptake of antisense oligonucleotides

RS Geary, D Norris, R Yu, CF Bennett - Advanced drug delivery reviews, 2015 - Elsevier
Pharmacokinetic properties of oligonucleotides are largely driven by chemistry of the backbone
and thus are sequence independent within a chemical class. Tissue bioavailability (% of …

[HTML][HTML] Cardiovascular and Metabolic Effects of ANGPTL3 Antisense Oligonucleotides

…, A Digenio, SG Hughes, RS Geary… - … England Journal of …, 2017 - Mass Medical Soc
Background Epidemiologic and genomewide association studies have linked loss-of-function
variants in ANGPTL3, encoding angiopoietin-like 3, with low levels of plasma lipoproteins. …

[HTML][HTML] Antisense inhibition of apolipoprotein C-III in patients with hypertriglyceridemia

…, K Tremblay, W Singleton, RS Geary… - … England Journal of …, 2015 - Mass Medical Soc
rich lipoproteins. It is known to inhibit lipoprotein lipase–mediated hydrolysis of triglyceride-rich
… hepatic uptake of remnants of triglyceride-rich lipoproteins. At higher concentrations, …

[HTML][HTML] Targeting APOC3 in the familial chylomicronemia syndrome

…, W Singleton, SG Hughes, RS Geary… - … England Journal of …, 2014 - Mass Medical Soc
<p id="p001">The familial chylomicronemia syndrome is a genetic disorder characterized
by severe hypertriglyceridemia and recurrent pancreatitis due to a deficiency in lipoprotein …

Antisense therapy targeting apolipoprotein (a): a randomised, double-blind, placebo-controlled phase 1 study

…, JL Burkey, Q Yang, SM Marcovina, RS Geary… - The Lancet, 2015 - thelancet.com
Background Lipoprotein(a) (Lp[a]) is a risk factor for cardiovascular disease and calcific aortic
valve stenosis. No effective therapies to lower plasma Lp(a) concentrations exist. We have …

[HTML][HTML] Volanesorsen and triglyceride levels in familial chylomicronemia syndrome

…, Q Yang, SG Hughes, RS Geary… - … England Journal of …, 2019 - Mass Medical Soc
Background Familial chylomicronemia syndrome is a rare genetic disorder that is caused by
loss of lipoprotein lipase activity and characterized by chylomicronemia and recurrent …

Pharmacokinetic properties of 2′-O-(2-methoxyethyl)-modified oligonucleotide analogs in rats

RS Geary, TA Watanabe, LA Truong, SUE Freier… - … of Pharmacology and …, 2001 - ASPET
Plasma pharmacokinetics, biodistribution, excretion, and metabolism of four modified 20-mer
antisense oligonucleotides targeted to human intercellular adhesion molecule-1 mRNA …

Pharmacology of antisense drugs

…, N Pham, E Swayze, RS Geary - Annual review of …, 2017 - annualreviews.org
Recent studies have led to a greater appreciation of the diverse roles RNAs play in maintaining
normal cellular function and how they contribute to disease pathology, broadening the …

Vupanorsen, an N-acetyl galactosamine-conjugated antisense drug to ANGPTL3 mRNA, lowers triglycerides and atherogenic lipoproteins in patients with diabetes …

…, JL Witztum, RS Geary, S Tsimikas… - European heart …, 2020 - academic.oup.com
Aims Loss-of-function mutations in ANGPTL3 are associated with beneficial effects on lipid
and glucose metabolism and reduced risk of coronary artery disease. Vupanorsen (AKCEA-…