Arcalyst（rilonacept，列洛西普）
制造商： Regeneron公司
Arcalyst属于白介素-1阻滞剂，用于治疗两种cryopyrin相关周期性综合征，即家族性寒冷型自身炎症综合征和穆-韦（Muckle-Wells）两氏综合征。cryopyrin相关周期性综合征属极罕见自身炎症疾病，患者出现反复性发热、皮疹、关节疼痛以及肾脏损伤，全球约2000人罹患此病。

ARCALYST

Indication(s):

Cryopyrin-associated periodic syndromes (CAPS) including familial cold autoinflammatory syndrome (FCAS) and Muckle-Wells syndrome (MWS).

Pharmacology:

Cryopyrin-associated periodic syndromes are rare genetic disorders that are characterized by symptoms such as fever, urticaria, arthralgia, myalgia, fatigue, and conjunctivitis. In most cases, the inflammatory system is disrupted by a mutation that results in an overproduction and release of activated interleukin-1 beta, which causes an exaggerated autoimmune response.

Clinical Trials:

A randomized, double-blind, placebo-controlled study enrolling 47 patients was conducted to evaluate the safety and efficacy of rilonacept in treating CAPS. The two parts (A and B) of the study were conducted sequentially in the same patients with FCAS and MWS.

Legal Classification:

Rx

Adults:

Give by SC inj into abdomen, thigh, or upper arm; rotate sites. ≥18yrs: Loading dose: 320mg on day 1 (split dose into 2x160mg at different sites), then 160mg as single dose once weekly.

Children:

Give by SC inj into abdomen, thigh, or upper arm; rotate sites. <12yrs: not recommended. 12–17yrs: Loading dose: 4.4mg/kg (max 320mg) in 1 or 2 inj (max 2mL/inj) on day 1; may split loading dose into 2 inj at different sites. Maintenance: 2.2mg/kg (max 160mg) once weekly.

Warnings/Precautions:

Discontinue if serious infection develops. Do not start treatment with active or chronic infection. Before starting therapy: complete recommended immunization schedules (including pneumococcal and influenza), and evaluate and treat possible latent tuberculosis. Asthma. Diabetes. HIV, hep B, or hep C infection. Renal or hepatic impairment. Monitor lipid profile. Patients <18yrs: monitor growth and development. Pregnancy (Cat.C): not recommended (may cause fetal harm). Nursing mothers.

Interaction(s):

Avoid concurrent live vaccines. Infection risk with concomitant TNF blockers (eg etanercept, infliximab, adalimumab) or other IL-1 blockers (eg, anakinra): not recommended. Monitor drugs that affect or are affected by CYP450 (eg, warfarin). Caution with other immunosuppressants (eg, corticosteroids).

Adverse Reaction(s):

Inj site reactions, infections (eg, URI; may be serious/fatal); possible increased risk of malignancies, antibody formation, changes in lipid profile.

How Supplied:

Single-dose vial—4

Last Updated:

1/14/2009

Arcalyst (rilonacept)注射剂 – 以前称Interleukin-1 Trap

批准日期：2008年2月27日美国FDA；2009年7月23日欧盟EMEA。公司：Regeneron Pharmaceuticals, Inc.。

一般描述：
Rilonacept是二聚体融合蛋白由由一种人白介素-1受体组分(IL-1R1)的胞外部分配体-结合结构区和IL-1受体辅助蛋白(IL-1RAcP)呈线性连接至人IgG1的Fc部分组成。Rilonacept分子量接近251 kDa。Rilonacept在重组中国仓鼠卵巢(CHO)细胞内表达。

适应证：
Arcalyst (rilonacept)是一种白介素-1阻断剂适用于治疗在成年和12岁以上儿童的Cryopyin蛋白-相关周期性综合征，包括家族性冷自身炎症综合征(FCAS)和Muckle-Wells(穆-韦二氏综合征:淀粉样变性-耳聋-荨麻疹-肢痛综合征，MWS)。

剂量和给药方法：

成年18岁和以上：起始治疗用负荷剂量320 mg分2次，2 mL皮下注射160 mg在同一天在2处不同部位。继续给药每周1次，单次2 mL皮下注射160 mg，不要给予Arcalyst超过比每周1次更频。
年龄12至17岁儿童患者：起始治疗用负荷剂量4.4 mg/kg，直至最大剂量320 mg，分1或2次，皮下注射，最大单次注射体积为2 mL。继续给药1周1次2.2 mg/kg，最大剂量160 mg，单次皮下注射给药至2 mL。如最初剂量为2次注射，它们应在相同天2处不同部位。不要给予Arcalyst超过比每周1次更频。

剂型规格：
消毒，单次用20 mL小瓶，玻璃含220 mg rilonacept为配制的冻干粉。

禁忌证：无

警告和注意事项：

白介素-1阻断剂可能干扰对感染的免疫反应。在用Arcalyst患者中曾报道危及生命感染。如患者发生严重感染中断治疗。有活动性或慢性感染患者中不要开始用Arcalyst治疗。
罕见伴Arcalyst给药超敏反应。如发生超敏反应，中断Arcalyst给药并开始适当治疗。
与Arcalyst不应同时给予活疫苗，开始用Arcalyst治疗前，患者应接受所有的免疫接种。

不良反应：
随CAPS用Arcalyst治疗，报道的最常见不良反应是注射部位反应和上呼吸道感染。

药物相互作用：
用Arcalyst未曾进行过正规的药物相互作用研究。

特殊人群中使用：
妊娠：无人类资料。基于动物资料，可能引起胎儿危害。