Table 2.

Pharmacokinetic Parameters for ¹⁴C-netarsudil and ³H-AR-12286 Following a Single Topical Ocular Dose in Dutch Belted Rabbits

		14C-Netarsudil (0.02%)				3H-AR-12286 (0.5%)
Tissue	Eye	Cmax, ng·eq/g	Tmax, h	AUClast, ng·eq·h/g	T1/2,e, h	Cmax, ng·eq/g	Tmax, h	AUClast, ng·eq·h/g	T1/2,e, h
Cornea	L	3,666	0.5	63,387	14	10,309	0.25	54,433	21
	R	3,972	0.25	69,605	13	10,691	0.25	93,347	13
Conjuctiva	L	2,442	0.25	9,525	13	5,374	0.25	34,248	37
	R	3,292	0.25	12,390	17	4,071	0.5	77,672	34
Iris-ciliary body	L	955	0.25	10,845	n.d.	8,394	1	170,278	36
	R	416	8	11,555	112	6,373	1	150,748	41
Retina-choroid-plexus	L	80	0.25	1,390	204	1,074	0.25	15,117	26
	R	50	0.5	1,298	68	1,379	1	19,130	30
Aqueous humor	L	16	8	510	17	595	0.25	2,648	11
	R	23	8	613	16	734	0.5	3,205	9
Vitreous humor	L	7	0.25	51	12	35	0.5	484	10
	R	4	0.25	51	15	33	0.5	420	38
Lens	L	2	0.25	33	99	59	0.25	937	36
	R	2	0.25	37	83	55	1	1,383	19
Blood	n/a	1	0.25	15	27	40	0.5	317	27
Plasma	n/a	1	0.5	24	16	40	0.5	302	35
Liver	n/a	6	1	88	13	274	1	3,314	18
Kidney	n/a	19	1	298	16	355	0.5	2,549	15

AUC_last, area under the curve; C_max, maximum observed concentration of radioactivity; T_max, time of maximum radioactivity concentration; T_1/2,e, apparent elimination half-life of radioactivity.