新型外用药Opzelura（ruxolitinib，芦可替尼）乳膏剂是美国FDA批准的第一个也是唯一一个外用Janus激酶（JAK）抑制剂，治疗轻中度特应性皮炎，可显著减少皮肤炎症和瘙痒。
近日，美国食品和药物管理局（FDA）已批准Opzelura（ruxolitinib，芦可替尼）乳膏剂上市，Opzelura是一款外用JAK抑制剂，用于短期和非持续性慢性治疗接受外用处方疗法未能充分控制病情或当这些疗法不可取、非免疫功能低下的轻度至中度特应性皮炎（AD）青少年（年龄≥12岁）和成人患者。
特应性皮炎（AD）是一种慢性、免疫介导的皮肤疾病，影响美国2100多万12岁及以上个体，其特征是皮肤发炎和瘙痒，许多患者对现有疗法应答不佳病情很难控制。AD患者也更容易受到细菌、病毒和真菌感染。Opzelura乳膏剂的批准上市，将为患者提供一款重要的、非甾体、抗炎、外用乳膏剂。
批准日期：2021年09月22日 公司：Incyte Corporation
OPZELURA（芦可替尼[ruxolitinib]）乳膏，局部使用
美国首次批准：2011
警告：严重感染、死亡率、恶性肿瘤、主要不良心血管事件(MACE)和血栓形成有关完整的黑框警告，请参阅完整的处方信息。
• 因炎症而接受Januskinase抑制剂治疗的患者曾发生导致住院或死亡的严重感染，包括结核病和细菌、侵袭性真菌、病毒和其他机会性感染。
• 在因炎症而接受Janus激酶抑制剂治疗的患者中观察到更高的全因死亡率，包括突发性心血管死亡。
• 在因炎症而接受Janus激酶抑制剂治疗的患者中观察到淋巴瘤和其他恶性肿瘤。
• 在因炎症而接受Janus激酶抑制剂治疗的患者中观察到较高的MACE（包括心血管死亡、心肌梗塞和中风）发生率。
• 血栓形成，包括深静脉血栓形成、肺栓塞和动脉血栓形成，有些是致命的，在因炎症而接受Janus激酶抑制剂治疗的患者中发生。
最近的主要变化
黑框警告：07/2022
适应症及用法：07/2022
用法用量：07/2022
警告和注意事项：07/2022
作用机制
Ruxolitinib是一种Janus激酶(JAK)抑制剂，可抑制JAK1和JAK2，它们介导许多对造血和免疫功能很重要的细胞因子和生长因子的信号传导。JAK信号传导涉及将STAT（信号转导和转录激活因子）募集到细胞因子受体、激活和随后将STAT定位到细胞核，从而调节基因表达。目前尚不清楚特异性JAK酶的抑制与治疗效果的相关性。
适应症和用法
OPZELURA是一种Janus激酶(JAK)抑制剂，适用于：
• 局部短期和非持续慢性治疗轻度至中度特应性皮炎，适用于非免疫功能低下的成人和12岁及以上的儿童患者，这些患者的疾病无法通过局部处方疗法得到充分控制或不建议使用这些疗法。
• 12岁及以上成人和儿童患者的非节段性白癜风的局部治疗。
使用限制
不推荐将OPZELURA与治疗性生物制剂、其他JAK抑制剂或强效免疫抑制剂（如硫唑嘌呤或环孢素）联合使用。
剂量和给药
• 每周不要使用超过一根60克的试管或每两周使用一根100克的试管。
• 仅供局部使用。
• 不可用于眼内、口腔或阴道内。
• 特应性皮炎
o 每天两次在受影响的区域涂抹薄层，最多可达20%的体表面积。
• 非节段性白癜风
o 每天两次将薄层涂抹在最多10%体表面积的受影响区域。
剂型和规格
乳膏：1.5%鲁索替尼。
禁忌症
没有任何。
警告和注意事项
• 严重感染：发生了严重的细菌、分枝杆菌、真菌和病毒感染。定期监测患者感染情况并及时处理。
• 非黑色素瘤皮肤癌。已发生基底细胞癌和鳞状细胞癌。在治疗期间和治疗后酌情进行定期皮肤检查。
• 血栓形成。发生了血栓栓塞事件。
• 血小板减少症、贫血症和中性粒细胞减少症：发生了血小板减少症、贫血症和中性粒细胞减少症。根据临床指示进行 CBC 监测。
不良反应
• 在特应性皮炎中，最常见的不良反应（发生率≥1%）是鼻咽炎、腹泻、支气管炎、耳部感染、嗜酸性粒细胞计数增加，荨麻疹，毛囊炎，扁桃体炎和流涕。
• 在非节段性白癜风中，最常见的不良反应（发生率≥1%）是应用部位痤疮、应用部位瘙痒、鼻咽炎、头痛、尿路感染、应用部位红斑和发热。
要报告疑似不良反应，请致电 1-855-463-3463 联系IncyteCorporation 或致电1-800-FDA-1088或www.fda.gov/medwatch联系FDA。
在特定人群中使用
• 哺乳期：建议不要母乳喂养。
包装提供/储存和处理
供应方式
OPZELURA是一种含有1.5% ruxolitinib 的白色至灰白色乳膏，以 60克和100克管供应。
60克管：NDC 50881-007-05
100克管：NDC 50881-007-07
储存和处理
将OPZELURA储存在 20ºC 至 25ºC（68ºF至77ºF）；允许在 15ºC至30ºC（59ºF至86ºF）范围内偏移 [参见USP受控室温]。
请参阅随附的OPZELURA完整处方信息：
https://www.opzelura.com/prescribing-information.pdf
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U.S. FDA Approval of Opzelura(ruxolitinib)Cream, a Topical JAK Inhibitor, for the Treatment of Atopic Dermatitis(AD)
U.S. Food and Drug Administration(FDA)has approved Opzelura(ruxolitinib)cream for the short-term and non-continuous chronic treatment of mild to moderate atopic dermatitis (AD) in non-immunocompromised patients 12 years of age and older whose disease is not adequately controlled with topical prescription therapies, or when those therapies are not advisable.
IMPORTANT SAFETY INFORMATION
SERIOUS INFECTIONS
Patients treated with oral Janus kinase inhibitors for inflammatory conditions are at risk for developing serious infections that may lead to hospitalization or death. Reported infections include:
Active tuberculosis, which may present with pulmonary or extrapulmonary disease.
Invasive fungal infections, including candidiasis and pneumocystosis.
Bacterial, viral, and other infections due to opportunistic pathogens.
Avoid use of OPZELURA in patients with an active, serious infection, including localized infections. If a serious infection develops, interrupt OPZELURA until the infection is controlled. Carefully consider the benefits and risks of treatment prior to initiating OPZELURA in patients with chronic or recurrent infection. Closely monitor patients for the development of signs and symptoms of infection during and after treatment with OPZELURA.
No cases of active tuberculosis (TB) were reported in clinical trials with OPZELURA. Cases of active TB were reported in clinical trials of oral Janus kinase inhibitors used to treat inflammatory conditions. Consider eva luating patients for latent and active TB infection prior to administration of OPZELURA. During OPZELURA use, monitor patients for the development of signs and symptoms of TB.
Viral reactivation, including cases of herpes virus reactivation (e.g., herpes zoster), were reported in clinical trials with Janus kinase inhibitors used to treat inflammatory conditions including OPZELURA. If a patient develops herpes zoster, consider interrupting OPZELURA treatment until the episode resolves.
Hepatitis B viral load (HBV-DNA titer) increases, with or without associated elevations in alanine aminotransferase and aspartate aminotransferase, have been reported in patients with chronic HBV infections taking oral ruxolitinib. OPZELURA initiation is not recommended in patients with active hepatitis B or hepatitis C.
MORTALITY
Higher rate of all-cause mortality, including sudden cardiovascular death, has been observed in patients treated with oral Janus kinase inhibitors for inflammatory conditions.
MALIGNANCIES
Lymphoma and other malignancies have been observed in patients treated with Janus kinase inhibitors for inflammatory conditions. Patients who are current or past smokers are at additional increased risk. Non-melanoma skin cancers, including basal cell and squamous cell carcinoma, have occurred in patients treated with OPZELURA. Perform periodic skin examinations during OPZELURA treatment and following treatment as appropriate.
MAJOR ADVERSE CARDIOVASCULAR EVENTS(MACE)
Higher rate of MACE (including cardiovascular death, myocardial infarction, and stroke) has been observed in patients treated with Janus kinase inhibitors for inflammatory conditions. Consider the benefits and risks for the individual patient prior to initiating or continuing therapy with OPZELURA, particularly in patients who are current or past smokers and patients with other cardiovascular risk factors. Patients should be informed about the symptoms of serious cardiovascular events and the steps to take if these symptoms occur.
THROMBOSIS
Thrombosis, including deep venous thrombosis, pulmonary embolism, and arterial thrombosis has been observed in patients treated with oral Janus kinase inhibitors for inflammatory conditions. Many of these adverse reactions were serious and some resulted in death. Patients with symptoms of thrombosis should be promptly eva luated.
Thromboembolic events were observed in clinical trials with OPZELURA. There was no clear relationship between platelet count elevations and thrombotic events. OPZELURA should be used with caution in patients who may be at increased risk of thrombosis.
Thrombocytopenia, Anemia and Neutropenia
Thrombocytopenia, anemia and neutropenia were reported in the clinical trials with OPZELURA. Consider the benefits and risks for individual patients who have a known history of these events prior to initiating therapy with OPZELURA. Perform CBC monitoring as clinically indicated. If signs and/or symptoms of clinically significant thrombocytopenia, anemia, and neutropenia occur, patients should discontinue OPZELURA.
Lipid Elevations
Treatment with oral ruxolitinib has been associated with increases in lipid parameters including total cholesterol, low-density lipoprotein (LDL) cholesterol, and triglycerides.
Adverse Reactions
The most common adverse reactions (≥1%)are nasopharyngitis (3%), diarrhea (1%), bronchitis (1%), ear infection (1%), eosinophil count increased(1%), urticaria (1%), folliculitis (1%), tonsillitis (1%), and rhinorrhea (1%).
60 G CARTON LABEL
Opzelura™
(ruxolitinib) cream 1.5%
For Topical Use Only.
NDC 50881-007-05
60g
Rx only