One-year clinical evaluation of 0.4% ripasudil (K-115) in patients with open-angle glaucoma and ocular hypertension.
OBJECTIVE
To investigate the intra-ocular pressure (IOP)-lowering effects and safety of 0.4% ripasudil (K-115), a Rho kinase inhibitor, twice daily for 52 weeks, in patients with open-angle glaucoma or ocular hypertension (OHT).


METHODS
In this multicentre, prospective, open-label study, 388 patients with primary open-angle glaucoma, OHT or exfoliation glaucoma were enrolled and 354 of them were subdivided into four cohorts (monotherapy, 173; additive therapy to prostaglandin analogs, 62; β-blockers, 60; or fixed combination drugs, 59). The IOP reduction at trough and peak from baseline and adverse events was investigated.


RESULTS
Ripasudil showed IOP-lowering effects over 52 weeks in all the analyses of monotherapy, additive therapy and both subgroups (baseline IOP ≥21 mmHg and <21 mmHg) of monotherapy. The mean IOP reductions at trough and peak at week 52 were -2.6 and -3.7 mmHg for monotherapy, and -1.4 and -2.4, -2.2 and -3.0, and -1.7 and -1.7 mmHg, respectively, for additive therapy described above. The most frequently observed adverse events were conjunctival hyperaemia (n = 264, 74.6%), blepharitis (n = 73, 20.6%) and allergic conjunctivitis (n = 61, 17.2%). Most of the conjunctival hyperaemia findings were mild (97.0%), transient and resolved spontaneously (78.0%). Although 51 patients discontinued from the study due to blepharitis and/or allergic conjunctivitis (blepharitis, 28; allergic conjunctivitis, 17; both, 6), all the events resolved with or without treatment after the discontinuation of ripasudil administration.


CONCLUSIONS
Fifty-two week administration of 0.4% ripasudil revealed IOP-lowering effects and an acceptable safety profile when administered as monotherapy or as additive therapy, in patients with open-angle glaucoma or OHT.
Department of Ophthalmology, Faculty of Life Sciences, Kumamoto University, Kumamoto, Japan.
Hidenobu
H
Tanihara
Department of Ophthalmology, Faculty of Life Sciences, Kumamoto University, Kumamoto, Japan.
Toshihiro
T
Inoue
Department of Ophthalmology, Gifu University Graduate School of Medicine, Gifu, Japan.
Tetsuya
T
Yamamoto
Fukushima Eye Clinic, Osaka, Japan.
Yasuaki
Y
Kuwayama
Niigata University of Health and Welfare, Niigata, Japan.
Haruki
H
Abe
Department of Ophthalmology and Visual Science, Kochi Medical School, Kochi, Japan.
Atsuki
A
Fukushima
Kowa Company Ltd, Nagoya, Japan.
Hideki
H
Suganami
Kanto Central Hospital of the Mutual Aid Association of Public School Teachers, Tokyo, Japan.
Makoto
M
Araie
D000319:Adrenergic beta-Antagonists / Q000627:therapeutic use; D000368:Aged; D000959:Antihypertensive Agents / Q000009:adverse effects / Q000627:therapeutic use*; D004338:Drug Combinations; D005260:Female; D005500:Follow-Up Studies; D005902:Glaucoma, Open-Angle / Q000188:drug therapy*; D006801:Humans; D007429:Intraocular Pressure / Q000187:drug effects*; D007546:Isoquinolines / Q000009:adverse effects / Q000627:therapeutic use*; D008297:Male; D008875:Middle Aged; D009798:Ocular Hypertension / Q000188:drug therapy; D009883:Ophthalmic Solutions; D011446:Prospective Studies; D013449:Sulfonamides / Q000009:adverse effects / Q000627:therapeutic use*; D014065:Tonometry, Ocular; D054460:rho-Associated Kinases / Q000037:antagonists & inhibitors
D000319:Adrenergic beta-Antagonists; D000959:Antihypertensive Agents; D004338:Drug Combinations; D007546:Isoquinolines; C584679:K-115; D009883:Ophthalmic Solutions; D013449:Sulfonamides; D054460:rho-Associated Kinases
K-115; glaucoma; intra-ocular pressure; rho kinase inhibitor; ripasudil