Table 1.
Summary of currently approved oligonucleotide therapeutics.
Drug Names | Market Names | Companies | FDA Approved | Indications | Drug Modality | Mechanisms | Targets |
---|---|---|---|---|---|---|---|
fomivirsen | Vitravene | Ionis Pharmaceuticals, Novartis | 1998 | Cytomegalovirus (CMV) retinitis | ASO | Translation block | CMV protein IE2 |
pegaptanib | Macugen | OSI Pharmaceuticals | 2004 | Neovascular age-related macular degeneration | Aptamer | Binding and blocking | Heparin-binding domain of VEGF-165 |
mipomersen | Kynamro | Kastle Therapeutics, Ionis Pharmaceuticals, Genzyme | 2013 | Homozygous familial hypercholesterolemia | ASO | RNase H degradation | Apolipoprotein B100 |
eteplirsen | Exondys 51 | Sarepta Therapeutics | 2016 | Duchenne muscular dystrophy | ASO | Splicing modulation | Exon 51 of DMD |
nusinersen | Spinraza | Ionis Pharmaceuticals, Biogen | 2016 | Spinal muscular atrophy | ASO | Splicing modulation | Exon 7 of SMN2 |
defibrotide | Defitelio | Jazz Pharmaceuticals | 2016 | Veno-occlusive disease in liver | Aptamer | Binding and activating | Adenosine A1/A2 receptor |
inotersen | Tegsedi | Akcea Therapeutics | 2018 | Polyneuropathy caused by hereditary transthyretin-mediated (hATTR) amyloidosis | ASO | RNase H degradation | Transthyretin |
milasen | Not applicable | Boston Children’s Hospital | 2018 | Mila Makovec’s CLN7 gene associated with Batten disease | ASO | Splicing modulation | CLN7 |
patisiran | Onpattro | Alnylam | 2018 | Polyneuropathy caused by hATTR amyloidosis | siRNA | RNAi | Transthyretin |
golodirsen | Vyondys 53 | Sarepta Therapeutics | 2019 | Duchenne muscular dystrophy | ASO | Splicing modulation | Exon 53 of DMD |
givosiran | Givlaari | Alnylam | 2019 | Acute hepatic porphyria (AHP) | siRNA | RNAi | 5-aminolevulinic acid synthase |
volanesorsen | Waylivra | Akcea Therapeutics | EMA approved in 2019 1 | Familial chylomicronemia syndrome (FCS) | ASO | RNase H degradation | Apolipoprotein C3 |
viltolarsen | Viltepso | NS Pharma | 2020 | Duchenne muscular dystrophy | ASO | Splicing modulation | Exon 53 of DMD |
casimersen | Amondys 45 | Sarepta Therapeutics | 2021 | Duchenne muscular dystrophy | ASO | Splicing modulation | Exon 45 of DMD |
1 Volanesorsen did not receive FDA approval in 2018 but was approved by European Medicines Agency (EMA) in 2019.