圣路易斯(MD Consult)——Ista制药公司在2009年9月8日宣布：美国食品药品管理局(FDA)已经批准1.5%浓度的Bepreve(通用名：苯磺酸贝他斯汀滴眼液)用于2岁和2岁以上患者的过敏性结膜炎引起的眼部搔痒。Bepreve是一种非镇静类高选择性组胺受体拮抗剂。据生产商指出，该药物对肥大细胞有稳定作用，并可抑制嗜酸性粒细胞迁移至炎症组织。

Ista公司展开多个临床试验，用以评估Bepreve的安全性、有效性、药效开始时间及持续时间。2项双盲III期临床、安慰剂对照、结膜过敏原竞争性试验的数据显示，使用Bepreve可显著减少眼部瘙痒的发生。此外，受试者使用Bepreve后，眼部瘙痒迅速缓解。患眼每天滴Bepreve两次，1次1滴。

BEPREVE®

What BEPREVE Treats

BEPREVE is indicated for the treatment of itching associated with allergic conjunctivitis. Allergic conjunctivitis is characterized by intense ocular itching, redness, and tearing – is the most common form of ocular allergy, affecting 20% -30% of the U.S. population or 60-90 million individuals. As a result of many technological and environmental factors, the incidence of allergic conjunctivitis is believed to be increasing in industrialized countries. Allergic conjunctivitis has a significant impact on the quality of life of allergy sufferers and remains a clinical challenge for physicians.

About BEPREVE

BEPREVE (bepotastine besilate ophthalmic solution) 1.5% is a non-sedating, anti-allergy eye drop that works on multiple components of the complex physiological process that produces allergy symptoms in the eye. BEPREVE is a selective blocker of histamine (H1), a principle mediator of allergy^1,11. BEPREVE also stabilizes mast cells to prevent the release of additional pro-allergic factors .

BEPREVE has been clinically proven to produce rapid and sustained relief of ocular itching. In two well-controlled efficacy studies, BEPREVE consistently demonstrated both statistically and clinically superior reductions in ocular itching compared to placebo. These effects were observed within 3-7 minutes of a single drop and lasted for at least 8 hours^6,7. A consolidated analysis of both studies showed that BEPREVE reduced ocular itching by 82% from baseline within 3 minutes⁶. This relief was clinically significant – producing at least a 1 unit improvement in the patient’s ocular symptom score – in 95% of patients at this time point⁷. At 8 hours following a single dose, 90% of patients still reported clinically significant relief of ocular itching^7_. Sixty-eight percent of patients who had severe itching achieved complete relief within 3 minutes.

BEPREVE has demonstrated safety and comfort comparable to placebo and is indicated in patients as young as two years old^8,11. This favorable safety profile was observed in both the efficacy studies and in a separate, 6-week, randomized, placebo-controlled safety study of BEPREVE that enrolled 861 patients⁸. Furthermore, the active ingredient in BEPREVE, bepotastine besilate, has an extensive track record of systemic safety based on experience with more than 850 million doses given in Japan, where it is available in oral tablet form (Talion^®) for allergic rhinitis, urticaria and pruritus associated with allergic skin diseases such as eczema⁹.

Warnings, Precautions, Adverse Reactions

BEPREVE is for topical ophthalmic use only. To minimize risk of contamination, do not touch the dropper tip to any surface. Keep the bottle closed when not in use.  BEPREVE should not be used to treat contact lens–related irritation. Remove contact lenses prior to instillation of  BEPREVE. The most common adverse reaction occurring in approximately 25% of patients was a mild taste following instillation. Other adverse reactions occurring in 2%-5% of patients were eye irritation, headache, and nasopharyngitis.

See full prescribing information

References

1. Kato M, Nishida A, Aga Y, et al. Pharmacokinetic and pharmacodynamic evaluation of central effect of the novel antiallergicagent betotastine besilate. Arzneimittelforschung. 1997;47(10):1116-1124.
2. Yato N, Murata T, Saito N, et al. Anti-allergic activity of betotastine besilate (TAU-284), a new anti-allergic drug. Nippon Yakurigaku Zasshi. 1997;110(1):19-29.
3. Nakahara T, Urabe K, Moroi Y, Morita K, Furue M. Bepotastine besilate rapidly inhibits mite-antigen induced immediate reactions in atopic dermatitis. J Dermatol Sci. 2003;32(3):237-238.
4. Kaminuma O, Ogawa K, Kikkawa H, Kikuchi M, Naito K, Ikezawa K. A novel anti-allergic drug, betotastine besilate, suppresses interleukin-5 production by human peripheral blood mononuclear cells. Biol Pharm Bull. 1998;21(4):411-413.
5. Andoh T, Kuraishi Y. Suppression by bepotastine besilate of substance P-induced itch-associated responses through the inhibition of the leukotriene B4 action in mice. Eur J Pharmacol. 2006;547(1-3):59-64.
6. Data on fi le. NDA 22-288 (ISE). ISTA Pharmaceuticals®, Inc.
7. Data on fi le. CL-EFF-0910091-R. ISTA Pharmaceuticals®, Inc.
8. Data on fi le. CL-SAF-0405071-R. ISTA Pharmaceuticals®, Inc.
9. Data on fi le. Osaka, Japan: Tanabe Seiyaku Co; June 2009. ISTA Pharmaceuticals®, Inc.
10. Based on BEPREVE WAC (September 23, 2009) and PriceAlert (June 2009). ISTA Pharmaceuticals®, Inc.
11. BEPREVE [package insert]. Irvine, CA: ISTA Pharmaceuticals®, Inc; 2009.

包装规格:
Bepreve 1.5%  10毫升/瓶

生产厂家中文参考译名:
Ista制药公司
生产厂家英文名:
ISTA Pharmaceuticals, Inc