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Ripasudil: First Global Approval

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Abstract

Ripasudil hydrochloride hydrate (Glanatec® ophthalmic solution 0.4 %; hereafter referred to as ripasudil) is a small-molecule, Rho-associated kinase inhibitor developed by Kowa Company, Ltd. for the treatment of glaucoma and ocular hypertension. This compound, which was originally discovered by D. Western Therapeutics Institute, Inc., reduces intraocular pressure (IOP) by directly acting on the trabecular meshwork, thereby increasing conventional outflow through the Schlemm’s canal. As a result of this mechanism of action, ripasudil may offer additive effects in the treatment of glaucoma and ocular hypertension when used in combination with agents such as prostaglandin analogues (which increase uveoscleral outflow) and β blockers (which reduce aqueous production). The eye drop product has been approved in Japan for the twice-daily treatment of glaucoma and ocular hypertension, when other therapeutic agents are not effective or cannot be administered. Phase II study is underway for the treatment of diabetic retinopathy. This article summarises the milestones in the development of ripasudil leading to the first approval for glaucoma and ocular hypertension.

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References

  1. Novack GD. RHO kinase inhibitors for the treatment of glaucoma. Drugs Future. 2013;38(2):107–13.

    Article  Google Scholar 

  2. Bucolo C, Salomone S, Drago F, et al. Pharmacological management of ocular hypertension: current approaches and future prospective. Curr Opin Pharmacol. 2013;13(1):50–5.

    Article  CAS  PubMed  Google Scholar 

  3. 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(8):813–22.

    Article  CAS  PubMed  Google Scholar 

  4. D. Western Therapeutics Institute. DWTI announces the acquisition of marketing approval in japan for a drug for treating glaucoma and ocular hypertension, K-115 [media release]. 26 Sept 2014. http://www.dwti.co.jp.

  5. D. Western Therapeutics Institute Inc. Notice of NDA application in Japan for a glaucoma treatment drug “K-115 (nonproprietary name: Ripasudil hydrochloride hydrate” by Kowa Company Limited [media release]. 10 Oct 2013. http://www.dwti.co.jp.

  6. D. Western Therapeutics Institute Inc. Notice of completion of late phase III clinical study of glaucoma treatment drug “K-115” in Japan [media release]. 10 Apr 2013. http://www.dwti.co.jp.

  7. Kowa Company Ltd. K-115 Clinical pharmacology study [JAPIC identifier JapicCTI-142456]. 2014. http://clinicaltrials.jp. Accessed 22 Oct 2014.

  8. D. Western Therapeutics Institute. Anti-glaucoma K-115 (Glanatec® ophthalmic solution 0.4 %). 2014. http://dwti.co.jp/english/business-outline/product-pipeline/anti-glaucoma-k-115. Accessed 23 Oct 2014.

  9. Mizuno K, Matsumoto J. United States Patent No. US 8,193,193 B2: agent for prevention or treatment of glaucoma. 2012. http://patft.uspto.gov/. Accessed 23 Oct 2014.

  10. Wato E, Omichi K, Yoneyama S, et al. Safety evaluation of morphological changes in corneal endothelial cells induced by K-115 in cynomolgus monkeys. Fundam Toxicol Sci. 2014;1(2):39–47.

    Google Scholar 

  11. Tanihara HMD, Inoue TMD, Yamamoto TMD, et al. Phase 1 clinical trials of a selective Rho kinase inhibitor, K-115. JAMA Ophthalmol. 2013;131(10):1288–95.

    Article  CAS  PubMed  Google Scholar 

  12. Nakao S, Arita R, Isobe T, et al. Therapeutic potential of topical ROCK inhibitor K-115 in retinal neovascularization [abstract no. FP-SA-51-4]. In: World Ophthalmology Congress. Tokyo; 2014.

  13. Yoshioka T, Nakabayashi S, Nagaoka T, et al. Effect of intravitreal Rho kinase inhibitors on retinal microcirculation in cats [abstract no. 6855-D1185]. In: Association for research in vision and ophthalmology annual meeting. Fort Lauderdale; 2012.

  14. Yamamoto K, Maruyama K, Himori N, et al. The novel Rho kinase (ROCK) inhibitor K-115: a new candidate drug for neuroprotective treatment in glaucoma. Invest Ophthalmol Vis Sci. 2014. doi:10.1167/iovs.13-13842.

  15. Mizuno K, Koide T, Fujieda J, et al. Ocular hypotensive and neuroprotective effects on K-115, a novel Rho-kinase inhibitor [abstract no. 4805-B998]. Invest Ophthalmol Vis Sci. 2007;48.

  16. Japanese Pharmaceuticals and Medical Devices Agency. Glanatec® (ripasudil hydrochloride hydrate ophthalmic solution 0.4 %): Japanese prescribing information. 2014. http://www.info.pmda.go.jp/. Accessed 22 Oct 2014.

  17. 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(4):731–6.

    Article  CAS  PubMed  Google Scholar 

  18. Yamamoto T, Abe H, Kuwayama Y, et al. Efficacy and safety of the Rho kinase inhibitor, K-115, over 24 h in patients with primary open-angle glaucoma and ocular hypertension [abstract no. 216/A512]. In: Association for research in vision and ophthalmology annual meeting. Orlando; 2011.

  19. Yamamoto T, Tanihara H, Kuwayama Y, et al. Phase 3 randomized clinical study of a Rho kinase inhibitor, K-115, in primary open-angle glaucoma and ocular hypertension [abstract no. FP-TH-12-6]. In: World Ophthalmology Congress. Tokyo; 2014.

  20. Tanihara H, Yamamoto T, Kuwayama Y, et al. Phase 3 randomized clinical studies of a Rho kinase inhibitor, K-115, in combination with timolol or latanoprost in primary open-angle glaucoma and ocular hypertension [abstract no. FP-TH-12-7]. In: World Ophthalmology Congress. Tokyo; 2014.

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Disclosure

The preparation of this report was not supported by any external funding. During the peer review process the manufacturer of the agent under review was offered an opportunity to comment on the article. Changes resulting from any comments received were made by the authors on the basis of scientific completeness and accuracy. K.P. Garnock-Jones is a salaried employee of Adis, Springer SBM.

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  1. Springer, Private Bag 65901, Mairangi Bay 0754, Auckland, New Zealand

    Karly P. Garnock-Jones

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  1. Karly P. Garnock-Jones
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Correspondence to Karly P. Garnock-Jones.

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This profile has been extracted and modified from the Adis R&D Insight drug pipeline database. Adis R&D Insight tracks drug development worldwide through the entire development process, from discovery, through pre-clinical and clinical studies, to market launch.

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Garnock-Jones, K.P. Ripasudil: First Global Approval. Drugs 74, 2211–2215 (2014). https://doi.org/10.1007/s40265-014-0333-2

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