Mandell Kenneth J, Kudelka Matthew R, Wirostko Barbara
Massachusetts Institute of Technology, Cambridge, MA 02139, USA.
Emory University, Atlanta, GA 30303-3031, USA.
Expert Rev Ophthalmol. 2011;6(6):611-622. doi: 10.1586/eop.11.65. Epub 2014 Jan 9.
Affecting 60 million patients, glaucoma is the second leading cause of blindness worldwide. Despite the availability of multiple medical and surgical treatments with effective intraocular pressure lowering, many patients still progress to become visually handicapped from glaucoma due to therapeutic failure. There is therefore a great need for novel therapies to improve the standard of care, and Rho kinase (ROCK) inhibitors represent a promising new class of drugs for treatment of glaucoma. ROCK inhibitors act by increasing facility of fluid outflow from the eye, thereby reducing intraocular pressure. ROCK inhibitors also have a vasodilatory effect on conjunctival vessels, which can lead to eye redness, a less than desirable cosmetic side effect for patients that would use this medication. Although there is promising data to support the clinical potential of this class of drug, the occurrence of conjunctival hyperemia remains a potential deterrent for use by patients. Studies are underway to assess alternative dosing strategies, delivery methods and prodrug formulations that may circumvent this unwanted side effect. This review provides an up-to-date account of the basic scientific data, as well as nonclinical and clinical studies to support use of ROCK inhibitors for treatment of glaucoma.
青光眼影响着6000万患者,是全球第二大致盲原因。尽管有多种降低眼压的药物和手术治疗方法,但由于治疗失败,许多青光眼患者仍会发展为视力障碍。因此,迫切需要新的疗法来提高治疗水平,而Rho激酶(ROCK)抑制剂是一类有前景的治疗青光眼的新型药物。ROCK抑制剂通过增加眼内液体流出的通畅性来发挥作用,从而降低眼压。ROCK抑制剂对结膜血管也有血管舒张作用,这可能导致眼睛发红,对于使用这种药物的患者来说,这是一种不太理想的美容副作用。尽管有支持这类药物临床潜力的有前景的数据,但结膜充血的发生仍然是患者使用该药物的潜在阻碍。目前正在进行研究,以评估可能避免这种不良副作用的替代给药策略、给药方法和前药制剂。本综述提供了最新的基础科学数据以及非临床和临床研究,以支持使用ROCK抑制剂治疗青光眼。