近日，美国食品和药物管理局（FDA）批准新药KERYDIN（tavaborole）外用溶液，5%，这是首个被批准用于外用治疗的氧代谢抗真菌药物。趾甲甲真菌病甲真菌病是一种真菌感染的指甲和指甲床，推荐每日一次用于感染的趾甲，疗程共48周，不需要进行趾甲清创术。
批准日期：2014年7月7日；公司：Anacor Pharmaceuticals
KERYDINTM (tavaborole)局部溶液，5%
美国初始批准：2014
作用机制
KERYDIN是一种oxaborole抗真菌药 [见临床药理学]。
适应证和用途
KERYDIN是一种oxaborole抗真菌药适用为由于红色毛癣菌[Trichophyton rubrum]或须癣毛癣菌[Trichophyton mentagrophytes]趾甲甲真菌病的局部治疗。
剂量和给药方法
⑴应用KERYDIN至受影响的趾甲每天1次共48周.
⑵KERYDIN应被应用至正在治疗的整个趾甲表面和每个趾甲的尖下。
⑶只为局部使用。
⑷不为口，眼，或阴道内使用。
剂型和规格
溶液，5%。
禁忌证
无。
不良反应
用KERYDIN治疗受试者中常见不良反应发生在≥1%包括应用部位表皮脱落，趾甲内生，应用部位红斑，和应用部位皮炎。
包装供应/贮存和处置
供应
KERYDIN (tavaborole)局部溶液，5%是一个透明，无色溶液在一个12-mL有螺旋盖的琥珀色玻璃瓶供应。在初始使用时，螺旋盖用滴组装替代。
KERYDIN (tavaborole)局部溶液，5%以下供应：
NDC 55724-111-11：一瓶含10 mL溶液有一个玻璃滴头。
贮存和处置
贮存在20–25°C (68–77°F)；外出允许至15–30°C(59–86°F)[见USP控制室温]。注意：可燃。远离热和火焰保存。插上滴头后3个月遗弃产品。紧闭保存瓶。保存在儿童拿不到的地方。
KERYDIN(tavaborole) topical solution
General Information
Kerydin(tavaborole) is an oxaborole antifungal.
Kerydin is specifically indicated for the treatment of onychomycosis of the toenails due to Trichophyton rubrum or Trichophyton mentagrophytes.
Kerydin is supplied as a topical solution, 5%. Kerydin should be applied to affected toenails once daily for 48 weeks. Kerydin should be applied to the entire toenail surface and under the tip of each toenail being treated.
Clinical Results
FDA Approval
The FDA approval of Kerydin was based on two multicenter, double-blind, randomized, vehicle-controlled trials in 1,194 subjects (795 Kerydin, 399 Vehicle) 18 to 88 years of age,. Kerydin or vehicle was applied once daily for 48 weeks in subjects with 20% to 60% clinical involvement of the target toenail, without dermatophytomas or lunula (matrix) involvement. Efficacy assessments were made at 52 weeks following a 48-week treatment period. The primary efficacy endpoint was "Complete Cure" at Week 52. "Complete Cure" is defined as "Completely Clear Nail" (0% clinical involvement of the target toenail) plus "Mycological Cure" (negative KOH wet mount and negative fungal culture). In the first trial, 6.5% of subjects treated with Kerydin reached the primary endpoint, compared to 0.5% of subjects treated with vehicle. In the second trial, 9.1% of subjects treated with Kerydin reached the primary endpoint, compared to 1.5% of subjects treated with vehicle.
Side Effects
Adverse effects associated with the use of Kerydin may include, but are not limited to, the following:
application site exfoliation
ingrown toenail
application site erythema
application site dermatitis
Mechanism of Action
Kerydin (tavaborole) is an oxaborole antifungal. The mechanism of action of tavaborole is inhibition of fungal protein synthesis. Tavaborole inhibits protein synthesis by inhibition of an aminoacyl-transfer ribonucleic acid (tRNA) synthetase (AARS).
http://www.accessdata.fda.gov/drugsatfda_docs/label/2014/204427s000lbl.pdf
https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=1ae61072-bca0-43f0-a741-07bda2d50c87