TABLE 2.

Biodistribution of the FDA-approved ASO drugs

The data are extracted from the FDA drug labels of each ASO drug.

	Biodistribution
Drug	Protein Binding	Bioavailability	AUC	Volume of Distribution
Fomivirsen	40% (from analysis of vitreous samples from treated rabbits and monkey)	N/A	N/A	N/A
Pegaptanib	N/A	N/A	25 μg/h per ml (at 3 mg monocular dose)	N/A
Nusinersen	CSF: <25%; plasma: >94%	100% (intrathecal)	N/A	CSF: 0.4 L; plasma: 29 L
Mipomersen	≥90% at clinically relevant concentrations (1–8 μg/ml)	54% to 78%	N/A	N/A
Inotersen	>94% (independent of dosage)	N/A	90 mcg/h per ml	293 L
Defibrotide	Average of 93%	100% (i.v.)	26.9–48.1 μg/ml × h	8.1–9.1 L
Eteplirsen	6% to 17%	100% (i.v.)	N/A	600 ml/kg
Golodirsen	33% to 39% (independent of dosage)	100% (i.v.)	34% to 44%a	668 ml/kg (at dose of 30 mg/kg)
Viltolarsen	∼40%	100% (i.v.)	16% to 27%a	300 ml/kg
Casimersen	8% to 32%	100% (i.v.)	16% to 34%a	367 ml/kg

N/A, no specific information available.

^aIntersubject variability