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Drug Evaluation

Ripasudil hydrochloride hydrate: targeting Rho kinase in the treatment of glaucoma

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Pages 1669-1673 | Received 13 Apr 2017, Accepted 06 Sep 2017, Published online: 14 Sep 2017

References

  • AGIS Investigators. The advanced glaucoma intervention study (AGIS), 7: the relationship between control of intraocular pressure and visual field deterioration. Am J Ophthalmol. 2000;130:429–440.
  • Kass MA, Heuer DK, Higginbotham EJ, et al. The ocular hypertension treatment study: a randomized trial determines that topical ocular hypotensive medication delays or prevents the onset of primary open-angle glaucoma. Arch Ophthalmol. 2002;120:701–713.
  • Garway-Heath DF, Crabb DP, Bunce C, et al. Latanoprost for open-angle glaucoma (UKGTS): a randomised, multicentre, placebo-controlled trial. Lancet. 2015;385:1295–1304.
  • Honjo M, Tanihara H, Inatani M, et al. Effects of Rho-associated protein kinase inhibitor Y-27632 on intraocular pressure and outflow facility. Invest Ophthalmol Vis Sci. 2001;42:137–144.
  • Kameda T, Inoue T, Inatani M, et al. The effect of Rho-associated protein kinase inhibitor on monkey Schlemm’s canal endothelial cells. Invest Ophthalmol Vis Sci. 2012;53:3092–3103.
  • Kaneko Y, Ohta M, Inoue T, et al. Effects of K-115 (Ripasudil), a novel ROCK inhibitor, on trabecular meshwork and Schlemm’s canal endothelial cells. Sci Rep. 2016;6:19640.
  • Fujimoto T, Inoue T, Kameda T, et al. Involvement of RhoA/Rho-associated kinase signal transduction pathway in dexamethasone-induced alterations in aqueous outflow. Invest Ophthalmol Vis Sci. 2012;53:7097–7108.
  • Inoue-Mochita M, Inoue T, Fujimoto T, et al. p38 MAP kinase inhibitor suppresses transforming growth factor-β2-induced type 1 collagen production in trabecular meshwork cells. PLoS One. 2015;10:e0120774.
  • Li T, Lindsley K, Rouse B, et al. Comparative effectiveness of first-line medications for primary open-angle glaucoma: a systematic review and network meta-analysis. Ophthalmology. 2016;123:129–140.
  • Zhang K, Zhang L, Weinreb RN. Ophthalmic drug discovery: novel targets and mechanisms for retinal diseases and glaucoma. Nat Rev Drug Discov. 2012;11:541–559.
  • Tanihara H, Inatani M, Honjo M, et al. Intraocular pressure-lowering effects and safety of topical administration of a selective ROCK inhibitor, SNJ-1656, in healthy volunteers. Arch Ophthalmol. 2008;126:309–315.
  • Hidaka H, Inagaki M, Kawamoto S, et al. Isoquinolinesulfonamides, novel and potent inhibitors of cyclic nucleotide dependent protein kinase and protein kinase C. Biochemistry. 1984;23:5036–5041.
  • Asano T, Suzuki T, Tsuchiya M, et al. Vasodilator actions of HA1077 in vitro and in vivo putatively mediated by the inhibition of protein kinase. Br J Pharmacol. 1989;98:1091–1100.
  • Sasaki Y, Suzuki M, Hidaka H. The novel and specific Rho-kinase inhibitor (S)-(+)-2-methyl-1-[(4-methyl-5-isoquinoline)sulfonyl]-homopiperazine as a probing molecule for Rho-kinase-involved pathway. Pharmacol Ther. 2002;93:225–232.
  • Tamura M, Nakao H, Yoshizaki H, et al. Development of specific Rho-kinase inhibitors and their clinical application. Biochim Biophys Acta. 2005;1754:245–252.
  • Isobe T, Mizuno K, Kaneko Y, et al. Effects of K-115, a Rho-kinase inhibitor, on aqueous humor dynamics in rabbits. Curr Eye Res. 2014;39:813–822.
  • Garnock-Jones KP. Ripasudil: first global approval. Drugs. 2014;74:2211–2215.
  • Gomi N, Ohgiya T, Shibuya K, et al. A practical synthesis of novel Rho-kinase inhibitor, (S)-4-fluoro-5-(2-methyl-1,4-diazepan-1-ylsulfonyl)isoquinoline. Heterocycles. 2011;83:1771–1781.
  • Gomi N, Kouketsu A, Ohgiya T, et al. A practical synthesis of (S)-tert-butyl 3-methyl-1,4-diazepane-1-carboxylate for the key intermediate of Rho kinase inhibitor, K-115. Synthesis. 2012;44:3171–3178.
  • Isobe T, Ohta M, Kaneko Y, et al. Species differences in metabolism of ripasudil (K-115) are attributed to aldehyde oxidase. Xenobiotica. 2016;46:579–590.
  • Isobe T, Kasai T, Kawai H. Ocular penetration and pharmacokinetics of ripasudil following topical administration to rabbits. J Ocul Pharmacol Ther. 2016;32:405–414.
  • Tanihara H, Inoue T, Yamamoto T, et al. Phase 1 clinical trials of a selective Rho kinase inhibitor K-115. JAMA Ophthalmol. 2013;131:1288–1295.
  • Tanihara H, Inoue T, Yamamoto T, et al. Intra-ocular pressure-lowering effects of a Rho kinase inhibitor, ripasudil (K-115), over 24 hours in primary open-angle glaucoma and ocular hypertension: a randomized, open-label, crossover study. Acta Ophthalmol. 2015;93:e254–e260.
  • Tanihara H, Inoue T, Yamamoto T, et al. Phase 2 randomized clinical study of a Rho kinase inhibitor, K-115, in primary open-angle glaucoma and ocular hypertension. Am J Ophthalmol. 2013;156:731–736.
  • Tanihara H, Inoue T, Yamamoto T, et al. Additive intraocular pressure-lowering effects of the Rho kinase inhibitor ripasudil (K-115) combined with timolol or latanoprost: a report of 2 randomized clinical trials. JAMA Ophthalmol. 2015;133:755–761.
  • Tanihara H, Inoue T, Yamamoto T, et al. One-year clinical evaluation of 0.4% ripasudil (K-115) in patients with open-angle glaucoma and ocular hypertension. Acta Ophthalmol. 2016;94:e26–e34.
  • Sato S, Hirooka K, Nitta E, et al. Additive intraocular pressure lowering effects of the Rho kinase inhibitor, ripasudil in glaucoma patients not able to obtain adequate control after other maximal tolerated medical therapy. Adv Ther. 2016;33:1628–1634.
  • Inazaki H, Kobayashi S, Anzai Y, et al. Efficacy of the additional use of ripasudil, a Rho-kinase inhibitor, in patients with glaucoma inadequately controlled under maximum medical therapy. J Glaucoma. 2016;26:96–100.
  • Omichi K, Wato F, Kaneko Y, et al. Nonclinical safety assessment for the sensitizing potential of K-115. Fundam Toxicological Sci. 2014;1:19–27.
  • Inoue K, Okayama R, Shiokawa M, et al. Efficacy and safety of adding ripasudil to existing treatment regimens for reducing intraocular pressure. Int Ophthalmol. Forth coming 2017. DOI:10.1007/s10792-016-0427-9
  • Terao E, Nakakura S, Fujisawa Y, et al. Time course of conjunctival hyperemia induced by a Rho-kinase inhibitor anti-glaucoma eye drop: ripasudil 0.4. Curr Eye Res. 2016;42:738–742.
  • Ashpole NE, Overby DR, Ethier CR, et al. Shear stress-triggered nitric oxide release from Schlemm’s canal cells. Invest Ophthalmol Vis Sci. 2014;55:8067–8076.
  • Pattabiraman PP, Rinkoski T, Poeschla E, et al. RhoA GTPase-induced ocular hypertension in a rodent model is associated with increased fibrogenic activity in the trabecular meshwork. Am J Pathol. 2015;185:496–512.

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