近日，美国FDA批准Orilissa（elagolix），用于女性患者子宫内膜异位症相关的中度至重度疼痛的治疗。此次批准，成为首个也是唯一一个获准专门治疗EMs相关中重度疼痛的口服促性腺激素释放激素（GnRH）受体拮抗剂，同时也是过去10多年来FDA批准治疗EMs相关中重度疼痛的首个口服药物。
批准日期：2018年7月24日 公司：艾伯维（AbbVie）
ORILISSATM（elagolix)片剂，用于口服
美国最初批准：2018年
作用机制
ORILISSA是一种GnRH受体拮抗剂，通过与垂体腺中的GnRH受体竞争性结合来抑制内源性GnRH信号传导。 ORILISSA的施用导致对黄体生成素（LH）和促卵泡激素（FSH）的依赖性抑制，导致卵巢性激素，雌二醇和孕酮的血液浓度降低。
适应症和用法
ORILISSA是一种促性腺激素释放激素（GnRH）受体拮抗剂，用于治疗与子宫内膜异位症相关的中度至重度疼痛。
剂量和给药
正常肝功能或轻度肝功能损害：150mg每日一次，最多24个月或200mg，每日两次，最长6个月。中度肝功能损害：每日一次150毫克，最长可达6个月。
剂量形式和强度
口服片剂：150毫克和200毫克。
禁忌症
•怀孕。
•已知骨质疏松症。
•严重肝功能损害。
•强有机阴离子转运多肽（OATP）1B1抑制剂。
警告和注意事项
•骨丢失：骨矿物质密度（BMD）的剂量和持续时间依赖性降低可能不是完全可逆的。评估BMD女性患有骨质流失的其他风险因素。
•降低识别妊娠的能力：ORILISSA可能会改变经期出血，这可能会降低识别妊娠的能力。怀疑怀孕时进行测试。如果确认怀孕则停止。
•自杀意念和情绪障碍：建议患者寻求自杀意念，自杀行为，新发病或恶化抑郁，焦虑或其他情绪变化的医疗保健。
•肝转氨酶升高：血清明腺素氨基转移酶（ALT）的剂量依赖性升高。咨询患者肝脏损伤的体征和症状。
•含有雌激素的避孕药具有降低疗效的可能性：在治疗期间和停止使用ORILISSA后一周内使用非激素避孕药。
不良反应
临床试验中最常见的不良反应（>5％）包括潮热和盗汗，头痛，恶心，失眠，闭经，焦虑，关节痛，抑郁相关的不良反应和情绪变化。
要报告疑似不良反应，请联系AbbVie Inc.at 1-800-633-9110或FDA，电话1-800-FDA-1088或www.fda.gov/medwatch
药物相互作用
查看完整的处方信息，了解临床重要的脑组织清单。
如何提供/存储和处理
ORILISSA片剂有两种强度：150毫克和200毫克，分别相当于155.2毫克和207.0毫克的elagolix钠。
ORILISSA 150毫克片剂是浅粉色，长方形，薄膜包衣片剂，“EL 150”在一侧凹陷。 ORILISSA 150毫克片剂包装在每周泡罩包装中。 每个泡罩包装
含有7片药片，供应药物一周。 将四个泡罩包装（总共28片）包装到纸箱中，该纸箱提供药物产品4周（NDC 0074-003828）。
ORILISSA 200毫克片剂为浅橙色，长方形，薄膜包衣片剂，一侧有“EL 200”凹陷。 将200mg片剂包装在每周泡罩包装中。 每个泡罩包装包含14片供应药物一周。 将四个泡罩包装（总共56片）包装在纸箱中，提供药物产品4周（NDC 0074-0039-56）。存储在2°C至30°C（36°F至86°F）。

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ORILISSA (elagolix) 150mg and 200mg oral tablets
ORILISSA™ (elagolix) is a prescription medicine used to treat moderate to severe pain associated with endometriosis.
It is not known if ORILISSA is safe and effective in children under 18 years of age.
IMPORTANT SAFETY INFORMATION
What is the most important information I should know about ORILISSA?
Take ORILISSA exactly as your Healthcare Provider (HCP) tells you.
ORILISSA may cause serious side effects, including:
Bone Loss (decreased Bone Mineral Density [BMD])
While you are taking ORILISSA, your estrogen levels will be low. This can lead to BMD loss. Your BMD may improve after stopping ORILISSA, but may not recover completely. It is unknown if these bone changes could increase your risk for broken bones as you age. Your HCP may order a DXA scan to check your BMD.
Effects on Pregnancy
Do not take ORILISSA if you are trying to become or are pregnant, as your risk for early pregnancy loss may increase. If you think you are pregnant, stop taking ORILISSA right away and call your HCP. ORILISSA may change your menstrual periods (irregular bleeding or spotting, a decrease in menstrual bleeding, or no bleeding at all), making it hard to know if you are pregnant. Watch for other signs of pregnancy, such as breast tenderness, weight gain, and nausea. ORILISSA does not prevent pregnancy. You will need to use effective hormone-free birth control (such as condoms or spermicide) while taking ORILISSA and for one week after stopping ORILISSA. Birth control pills that contain estrogen may make ORILISSA less effective. It is unknown how well ORILISSA works while on progestin-only birth control.
Do not take ORILISSA if you:
Are or may be pregnant, have osteoporosis, have severe liver disease, or take medicines known as strong OATP1B1 inhibitors, such as cyclosporine or gemfibrozil. If you are unsure if you are taking one of these medicines, ask your HCP.
What should I tell my HCP before taking ORILISSA?
Tell your HCP about all of your medical conditions, including if you:
Have or have had broken bones, have other conditions, or take medicines that may cause bone problems; have or have had depression, mood problems, or suicidal thoughts or behavior; have liver problems; think you may be pregnant; or are breastfeeding or plan to be. It is unknown if ORILISSA passes into breast milk. Talk to your HCP about the best way to feed your baby if you take ORILISSA.
Tell your HCP about all of the medicines you take, including prescription and over-the-counter medicines, vitamins, and herbal supplements.
Especially tell your HCP if you take birth control pills. Your HCP may advise you to change the pills you take or your method of birth control.
What are the possible side effects of ORILISSA?
ORILISSA can cause serious side effects including:
Suicidal thoughts, actions, or behavior, and worsening of mood. Call your healthcare provider right away, or call 911 if an emergency, if you have any of these symptoms, especially if they are new, worse, or bother you: thoughts about suicide or dying, try to commit suicide, new or worse depression or anxiety, or other unusual changes in behavior or mood. You or your caregiver should pay attention to any changes, especially sudden changes in your mood, behaviors, thoughts, or feelings.
Abnormal liver tests. Call your HCP right away if you have any of these signs and symptoms of liver problems: yellowing of the skin or the whites of the eyes (jaundice), dark amber-colored urine, feeling tired, nausea and vomiting, generalized swelling, right upper stomach area pain, or bruising easily.
The most common side effects of ORILISSA include: hot flashes or night sweats, headache, nausea, difficulty sleeping, absence of periods, anxiety, joint pain, depression, and mood changes.
These are not all of the possible side effects of ORILISSA. This is the most important information to know about ORILISSA. For more information, talk to your doctor or healthcare provider.
Tell your HCP if you have any side effect that bothers you or that does not go away. Call your HCP for medical advice about side effects.