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美国FDA批准治疗痛风新药-FEBUXOSTAT（中文：非布索坦）

2010-10-05 21:43:50 作者：新特药房来源：中国新特药网天津分站浏览次数：4394 文字大小：【大】【中】【小】

简介： 美国FDA批准了近40年来的首个个用于治疗痛风药物FEBUXOSTAT（商品名ULORIC） 2009年2月16日，美国FDA批准了近40年来的第1个用于治疗高尿酸症的痛风药物。其为武田制药北美公司（Takeda Pharmaceutical ...

关键字：非布索坦（FEBUXOSTAT ULORIC）痛风

美国FDA批准了近40年来的首个个用于治疗痛风药物FEBUXOSTAT（商品名ULORIC）

2009年2月16日，美国FDA批准了近40年来的第1个用于治疗高尿酸症的痛风药物。其为武田制药北美公司（Takeda Pharmaceuticals North America）的非布索坦（febuxostat，ULORIC）。本品通过降低患者血液中的尿酸水平改善痛风患者的症状。此外，武田制药北美公司作为本品在美国市场中的独立开发商与销售商。

根据武田公司的一项声明：本品的结构与40年前开发的黄嘌呤氧化酶抑制剂药物完全不同，它是一种全新的高效的非嘌呤类黄嘌呤氧化酶选择性抑制剂。黄嘌呤氧化酶是促进尿酸生成的关键酶。本品可以降低高尿酸血症痛风患者血液中的尿酸水平，在临床研究中已经证明了本品的安全性和有效性，而且在中-重度肝肾功能不全的患者中也不需要进行剂量调整。

本品的服用剂量为每日1次，一次40 毫克或者80毫克，但是本品不推荐用于无高尿酸血症的痛风患者。

本品的原研厂家为日本的另一家公司－－日本帝人制药（Teijin Pharma）。在帝人制药公司总裁最近的一份声明中，我们可以了解公司对本品采取的全球战略。他称，在本品获得FDA的许可之前，Ipsen公司的产品也获得了欧盟的上市许可。Ipsen 公司是帝人制药关于本品在欧盟的许可公司，而武田北美制药是本品在美国的许可公司。所以公司在全球已经取得的了里程碑式的战略意义。同时他还指出，在亚洲市场，帝人制药将采取自主开发或联合开发的形式。

痛风是一组异质性疾病，遗传性和（或）获得性引起的尿酸排泄减少和（或）嘌呤代谢障碍。临床特点：高尿酸血症，以及尿酸盐结晶，沉积所致的特征性急性关节炎、痛风石、间质性肾炎、严重者呈关节畸形及功能脏爱。常伴尿酸性尿路结石。假性痛风常常与痛风混淆，因为其症状非常的相似，然后，假性痛风是由于磷酸钙的代谢障碍引起，而不是尿酸代谢障碍引起。

根据美国国家关节肌肉骨骼疾病与皮肤病研究所（NIAMS）的研究数据表明，在美国有600万20岁及其以上的人群生平中有患痛风的经历。通常40-50 岁的男性患者较为常见，而绝经前的女性患者少见。经历过器官移植的患者也容易患痛风。

NIAMS指出下列药物会增加患痛风的风险
（1）利尿剂：呋塞米（furosemide）；氢氯噻嗪（hydrochlorothiazide）；美托拉宗（metolazone）
（2）水杨酸类：如阿司匹林（aspirin）
（3）烟酸
（4）环孢菌素 (Cyclosporine Neoral),
（5）左旋多巴 (Levodopa)。

The FDA has approved Uloric (febuxostat, from Takeda) a once-daily tablet for the chronic management of hyperuricemia in patients with gout. This approval is based on a phase 3 clinical trial demonstrating that Uloric 80mg was superior to Uloric 40mg and allopurinol 300/200mg (67%, 45%, and 42%, respectively) at achieving the primary end point of a serum uric acid level <6.0 mg/L at the final visit.

Uloric will be available in 40mg and 80mg dosage strengths.

ULORIC

Indication(s):

Chronic management of hyperuricemia in patients with gout.

Pharmacology:

Gout is a chronic condition characterized by attacks, or “flares,” that are marked by intense pain, redness, swelling and heat in the affected joint. These symptoms are caused by the buildup of uric acid which crystallizes and deposits under the skin and in joints. Gout is the most common inflammatory arthritis presented in men over 40 years of age.

Febuxostat exerts its therapeutic effect by blocking the enzyme xanthine oxidase. Xanthine oxidase is responsible for the breakdown of the purine base, hypoxanthine, to xanthine and subsequently to uric acid. By blocking this enzyme, febuxostat helps to prevent the production of uric acid, thereby reducing the elevated levels of serum uric acid.

Clinical Trials:

Three randomized, double-blind, controlled clinical studies evaluated the efficacy of daily treatment with febuxostat compared to that of allopurinol 300mg daily, or placebo in 3402 patients with hyperuricemia and gout. Hyperuricemia was defined as a baseline serum uric acid level ≥8mg/dL. In all 3 studies, patients also received naproxen 250mg twice daily or colchicine 0.6mg once or twice daily for gout flare prophylaxis.

The primary efficacy endpoint was the proportion of patients with a serum uric acid level <6mg/dL at the final visit. Febuxostat 40mg demonstrated comparable efficacy to allopurinol in lowering serum uric acid to <6mg/dL at the final visit; whereas febuxostat 80mg demonstrated superior efficacy. Of the patients treated with febuxostat 80mg, 76% achieved a serum uric acid level <6mg/dL by week 2 and 83% of these patients maintained average serum uric acid levels of <6mg/dL throughout the treatment period.

Legal Classification:

Adults:

≥18yrs: initially 40mg once daily; if serum uric acid is not <6mg/dL after 2 weeks, may increase to 80mg once daily. Gout flare prophylaxis, with an NSAID or colchicine, upon initiation of therapy and for up to 6 months, is recommended.

Children:

<18yrs: not recommended.

Contraindication(s):

Concomitant azathioprine, mercaptopurine, theophylline.

Warnings/Precautions:

Not recommended for treating asymptomatic hyperuricemia. Cardiovascular events: monitor for signs and symptoms of MI and stroke. Severe renal impairment or ESRD on dialysis. Severe hepatic impairment. Monitor liver function at 2 and 4 months after initiation and periodically thereafter. Obtain target serum uric acid levels <6mg/dL after 2 weeks of initiating therapy. Secondary hyperuricemia (eg, Lesch-Nyhan syndrome, malignant disease, or in organ transplant recipients): not recommended. Pregnancy (Cat.C). Nursing mothers.