NAILIN Capsules 100mg（Fosravuconazole L-LysineEthanolate）-新一代用于治疗灰指甲的口服药.

英文名：Fosravuconazole L-Lysine Ethanolate

商品名：NAILIN Capsules 100mg

中文名：磷酸咪康唑 L-赖氨酸乙醇

生产商：佐藤制药

药物分类名称

口服抗真菌剂

批准日期：

欧文商標名

NAILIN Capsules 100mg

一般名：ホスラブコナゾール　L-リシンエタノール付加物 

一般名：（欧名） Fosravuconazole L-Lysine Ethanolate 

化学名：({(2R,3R)-3-[4-(4-Cyanophenyl)thiazol-2-yl]-2-(2,4-difluorophenyl)-1-(1H-1,2,4-triazol-1-yl)butan-2-yl}oxy)methyl dihydrogen phosphate mono[(2S)-2,6-diaminohexanoic acid]monoethanolate 

分子式：C23H20F2N5O5PS・C6H14N2O2・C2H6O 

分子量：739.73 

融点：148〜156℃（分解） 

性状 

本品为白色至黄色粉末。

它易溶于可溶性水，几乎不溶于甲醇或乙醇（99.5）。

比旋光度[α] 20 D：+ 6.6°（50 mg，水，5 mL，100 mm）

处理注意事项

在室温下储存，避免潮湿。

批准条件

制定药品风险管理计划并适当实施。

药用药理学

抗真菌作用

抗真菌活性（体外）

该药物的有效成分Rabconazole对新鲜的红色毛癣菌和须癣毛癣菌的临床分离株具有很强的抗真菌活性，这是甲癣的主要致病菌。

表：针对新鲜临床分离株的抗真菌活性
 

菌種（株数）	MIC（μg/mL）
	範囲	MIC50	MIC90
T.rubrum（51）	≦0.03-0.12	≦0.03	0.06
T.mentagrophytes（20）	≦0.03-0.06	≦0.03	0.06

对豚鼠皮肤真菌病模型的作用（体内）

在豚鼠须癣毛癣菌皮肤真菌病模型中，口服ravconazole可局部改善感染区域的临床症状，并以剂量依赖的方式增加感染的局部毛发的真菌阴性率。

行动机制

该药物是ravuconazole（膦酰氧基甲基化合物：Phoslabuconazole）的前药，当给予动物和人类时，它迅速代谢为吡康唑。 Lavconazole通过抑制麦角甾醇生物合成显示出抗真菌作用，麦角甾醇生物合成是真菌细胞的膜组分。

适应症

<适应性真菌种类>

皮肤癣菌（毛癣菌种

<适应症>

甲癣

用法与用量

成人，每天一次，每次1粒胶囊（100mg），持续12周。

包装

胶囊

100毫克：84粒（PTP 14粒×6）

制造供应商

佐藤制药有限公司

Announcement of new release of oral antifungal agent "Nylin ® capsule 100 mg"

Eisai Co., Ltd. (Head office: Bunkyo-ku, Tokyo, Representative Executive Officer: Haruo Naito, hereinafter referred to as Eisai Co., Ltd.) We will inform you that we will release the fungal agent "Nylin ® capsule 100 mg" from July 27, 2018.

"Naylin ® Capsule 100 mg" contains phos- phorbuconazole L-lysine ethanol adduct with improved bioavailability of active ingredient rabconazole as the active ingredient, Eisai created and Sato Pharmaceutical orally administered onychomycosis As a therapeutic agent, we obtained manufacturing and marketing approval for about 20 years.

Tinea unguium is a fungal infection that causes symptoms such as turbidity, thickening of the nail, and hyperkeratosis around the nail, by invasion of ringworm bacteria through the skin of the limbs into the nails.
It is reported that 1 in 10 Japanese people affect about 11 million people. Although it is a disease that is easy to be left without being accompanied by pain or itching, when it progresses, it causes painful shoes from pain due to nail deformation, causing symptoms such as pain when walking, and many of patients feel deterioration in quality of life (QOL) I am bothered by. In addition Ringworm Bacillus may infect others by sharing slippers and bath mats.

"Nairin ® capsule 100 mg" is superior to placebo by orally administering 1 capsule once daily for 12 weeks in a national Phase III clinical trial conducted by Sato Pharmaceutical Co., Ltd. Effectiveness has been confirmed.

Sato Pharmaceutical will sell "Nylin ® capsule 100 mg" in the future, and Sato Pharmaceutical and Eisai will jointly provide appropriate usage information related to this drug. Both companies will expand the option of treating onychomycosis through "Nylin ® capsule 100 mg" and strive to make further contribution to the treatment of patients with tinea unguium.

Outline of Nylin ® capsule 100 mg

· Drug price criteria Listing date: May 22, 2018

Sales name:

Nylin ® capsule 100 mg

Active ingredient: Phosphabuconazole L-lysine ethanol adduct

· Indications · Effect: <Adaptive fungus species> Dermatophytes (Trichophyton species)

  <Indications> Onychomycosis

· Dosage · Dosage: Usually for adults, take 1 capsule (100 mg as lovconazole) once a day for 12 weeks.

· Packing unit: 84 capsules (PTP 14 capsules × 6)

https://www.kegg.jp/medicus-bin/japic_med?japic_code=00067275