英文药名: Xolair(Omalizumab)
中文药名: 索雷尔注射剂, 乐无喘, 柯耐尔
生产厂家: Novartis
药品介绍
诺华公司（Novartis）宣布，欧盟委员会已经批准其抗哮喘药omalizumab（Xolair）在欧盟25个成员国上市。本品有望在未来几周内在欧盟国家上市。许多专家认为，本品是最近15年中哮喘治疗方面最重要的进步之一，欧盟是在考虑了这些专家意见之后给予本品上市授权的。
本品的独特作用机制为哮喘患者提供了一种新型注射疗法，能够有效控制哮喘发作以及现有疗法尚未控制的症状。
作为首个获准用于哮喘治疗的单克隆抗体，本品具有独特的治疗途径——能够阻断IgE的作用。
在欧洲，本品获准作为附加疗法用于改善严重持续性变应性哮喘患者的哮喘控制。
适用本品的患者应是成人和12岁及以上青少年，除了接受高剂量吸入糖皮质激素加长效吸入β2-激动剂治疗，还应具备下列条件：
1、皮肤试验或体外检测显示对常年性气源性致敏原呈阳性；
2、肺功能降低（FEV1<80%）；
3、频发日间症状或夜间觉醒；
4、多次记录严重哮喘加重发作。
此外，本品仅考虑用于确诊的IgE介导型哮喘。
本品通过皮下注射给药，每二周或四周注射1次。临床研究显示，本品能显著降低哮喘加重发作率，并使严重哮喘患者的急诊率减半。即使是采用现有最好疗法仍未能得到足够控制（甚至因此而出现致命性发作）的哮喘患者，在使用本品后仍可以获得治疗益处。本品已于2003年6月获得了美国FDA的批准。
上述这些资料取自546例中重度过敏哮喘患者的III期临床试验。尽管受试者每日吸入糖皮质激素，但仍存在哮喘症状。他们被随机分为两组：每隔2到4周，分别皮下注射omalizumab或安慰剂。在开始16周疗程中，治疗上将丙酸倍氯米松（BDP）浓度控制在420到840mcg/d范围（此期称为激素治疗稳定期）。在BDP减量8周后，紧接12周的激素减量期，维持最小有效BDP剂量4周。在激素减量期，病人继续接受omalizumab或安慰剂。在试验中，omalizumab剂量由病人的IgE水平和体重决定，共有274例病人接受omalizumab治疗，272例接受安慰剂。
加利福尼亚大学儿科变态反应和免疫学临床教授William Berger指出：在稳定治疗期，接受omalizumab治疗的病人中12.8％出现一次或多次病情加重，而安慰剂组则有30.5％；在激素减量期，omalizumab组加重病人中占15.7％，而安慰剂组占20.8％。
研究人员发现，应用omalizumab的病人，病情改善，伴随用药明显减少，BDP减量和无须使用BDP患者的百分数明显高于安慰剂组。而且，在随访结束后的５个月，患者未出现哮喘加重或重新吸入BDP的反弹现象。
该药最常见的副作用是病毒感染和头疼，未见与药物相关的严重副作用报道。
IMPORTANT SAFETY INFORMATION
Injection site reactions of any severity occurred at a rate of 45% in XOLAIR-treated patients compared with 43% in placebo-treated patients.
The types of injection site reactions included: bruising, redness, warmth, burning, stinging, itching, hive formation, pain, indurations, mass, and inflammation.
INDICATION
XOLAIR(omalizumab) for subcutaneous use is indicated for adults and adolescents (12 years of age and above) with moderate to severe persistent asthma who have a positive skin test or in vitro reactivity to a perennial aeroallergen and whose symptoms areinadequatelycontrolledwithinhaledcorticosteroids.
XOLAIR has been shown to decrease the incidence of asthma exacerbations in these patients.
Important Limitations of Use
XOLAIR is not indicated for treatment of other allergic conditions
XOLAIR is not indicated for the relief of acute bronchospasm or status asthmaticus
XOLAIR is not indicated for use in pediatric patients less than 12 years of age
IMPORTANT SAFETY INFORMATION
WARNING: Anaphylaxis
Anaphylaxis presenting as bronchospasm, hypotension, syncope, urticaria, and/or angioedema of the throat or tongue, has been reported to occur after administration of XOLAIR. Anaphylaxis has occurred as early as after the first dose of XOLAIR, but also has occurred beyond 1 year after beginning regularly administered treatment. Because of the risk of anaphylaxis, observe patients closely for an appropriate period of time after XOLAIR administration.
Health care providers administering XOLAIR should be prepared to manage anaphylaxis that can be life-threatening.
Inform patients of the signs and symptoms of anaphylaxis and instruct them to seek immediate medical care should symptoms occur (see Warnings and
Precautions: Anaphylaxis).
XOLAIR should only be administered in a healthcare setting by healthcare providers prepared to manage anaphylaxis that can be life-threatening.
XOLAIR should not be administered to patients who have experienced a severe hypersensitivity reaction to XOLAIR or any ingredient of XOLAIR(see Warnings and Precautions). XOLAIR should be discontinued in patients who experience a severe hypersensitivity reaction.
Malignant neoplasms were observed in 20 of 4127 (0.5%) XOLAIR-treated patients compared with 5 of 2236 (0.2%) control patients in clinical studies of asthma and other allergic disorders.
XOLAIR has not been shown to alleviate asthma exacerbations acutely. Do not use XOLAIR to treat acute bronchospasm or status asthmaticus.
A constellation of signs and symptoms including arthritis/arthralgia, rash (urticaria or other forms), fever and lymphadenopathy similar to serum sickness have been reported in post-approval use of XOLAIR in some patients. Physicians should stop XOLAIR if a patient develops this constellation of signs and symptoms.
Patients should be given and instructed to read the accompanying Medication Guide before starting treatment and before each subsequent treatment.
Do not abruptly discontinue corticosteroid use upon initiation of XOLAIR therapy. Decrease corticosteroids gradually under the direct supervision of a physician.
In patients >12 years of age, the most commonly observed adverse reactions (>1% more frequent in XOLAIR-treated patients) from 4 placebo-controlled asthma studies were arthralgia (8%), pain (general)(7%), leg pain (4%), fatigue (3%), dizziness (3%), fracture (2%), arm pain (2%), pruritus (2%), dermatitis (2%), and earache (2%).
The adverse events most frequently resulting in clinical intervention(e.g. discontinuation of XOLAIR, or the need for concomitant medication to treat an adverse event), in either placebo-controlled or other controlled asthma studies, were injection site reaction (45%), viral infections (23%), upper respiratory tract infection (20%), sinusitis (16%), headache (15%), and pharyngitis (11%). These events were observed at similar rates in XOLAIR-treated patients and control patients.
XOLAIR Rx
Generic Name and Formulations:
Omalizumab 150mg/vial; pwd for SC inj after reconstitution; preservative-free.
Company:
Genentech and Novartis
Indications for XOLAIR:
Moderate to severe persistent asthma in patients with a (+) skin test or in vitro reactivity to a perennial aeroallergen and whose symptoms are inadequately controlled by inhaled corticosteroids.
Adult Dose for XOLAIR:
Base dose and frequency on baseline serum total IgE level and body weight; see literature. Give by SC inj over 5–10 seconds; max 150mg per inj site. 150–375mg every 2 or 4 weeks. Reevaluate periodically.
Children's Dose for XOLAIR:
Not recommended.
Pharmacological Class:
Antiasthmatic (IgE blocker).
Warnings/Precautions:
Not for treating acute attacks. Have medications for treating anaphylaxis available, monitor for at least 2 hours after inj; may have delayed reaction. Elevated serum IgE levels may persist for up to 1 year after stopping therapy. Patients at risk of malignancy. Pregnancy (Cat.B). Nursing mothers.
Adverse Reactions:
Inj site reactions, viral infections, upper respiratory tract infections (eg, sinusitis, pharyngitis), headache; hypersensitivity reactions (discontinue if severe), anaphylaxis (may be fatal), antibody formation, malignancies.
How Supplied:
Single-use vial—1