AR-13324 mesylate

Animal models

Seven adult female cynomolgus monkeys, each weighing 3 to 5 kg with normotensive IOP

Preparation Method

50 μL (25 μL×2) of 0.04% AR-13324 was topically applied to 1 eye of each monkey. An equal volume of vehicle was applied to the contralateral control eye. IOP was measured before drug administration and 6 hours after dosing with a calibrated neumatonometer in the sit ting position. IOP reading was taken 2 times on each eye and the average of 2 values was used to perform statistical analysis.

Dosage form

50 μL (25 μL×2) of 0.04% AR-13324

Applications

Six hours after a single dose of 0.04% AR-13324 to 7 normal monkey eyes, the IOP measured by pneumatonometer in treated eyes was reduced (P< 0.005) by 25% when compared with baseline measurements and by 24% when compared with contralateral vehicle-treated eyes

Animal models

Male DB rabbits (n=11, 2.15-0.09 kg)

Preparation Method

The protocol entailed once per day—topical application of 1 drop of 0.04% AR-13324 for 2 days. Then, on the morning of the third day,the animals were anesthetized and surgically prepared, and then, measurements were obtained before dosing with AR-13324 or vehicle (baseline measurements) and for 3 h after dosing.

Dosage form

1 drop of 0.04% AR-13324 for 2 days

Applications

At 3 h postdosing, the reduction in EVP caused by AR-13324 treatment accounted for 42% of the measured reduction in IOP.

References:
[1]. Wang RF, et al. Effect of 0.04% AR-13324, a ROCK, and norepinephrine transporter inhibitor, on aqueous humor dynamics in normotensive monkey eyes. J Glaucoma. 2015 Jan;24(1):51-4.
[2]. Kiel JW, Kopczynski CC. Effect of AR-13324 on episcleral venous pressure in Dutch belted rabbits. J Ocul Pharmacol Ther. 2015 Apr;31(3):146-51.