股票配资咨询交易急性髓系白血病创新靶向药：艾伏尼布（Ivosidenib）中英说明书，适合情况、用法用量、注意事项

艾伏尼布股票配资咨询交易

Ivosidenib、Tibsovo

艾伏尼布（Ivosidenib）是全球首个且目前国内唯一获批的异柠檬酸脱氢酶1（IDH1）抑制剂，用于治疗携带IDH1突变的复发性或难治性急性髓系白血病（R/R AML）成人患者。

每年的新发病例中约有6～10%的AML患者携带IDH1突变，而当IDH1突变时，就会产生大量的D-2-HG，使得其浓度升高，从而导致细胞增殖、分化异常等现象。而艾伏尼布的作用机制则是有效抑制IDH1的活性，从而减少D-2-HG的产生，达到治疗白血病的效果。

展开剩余92%

01适应症

TIBSOVO is an isocitrate dehydrogenase-1 (IDH1) inhibitor indicated for patients with a susceptible IDH1 mutation as detected by an FDA-approved test with:

Newly Diagnosed Acute Myeloid Leukemia (AML)

In combination with azacitidine or as monotherapy for the treatment of newly diagnosed AML in adults 75 years or older, or who have comorbidities that preclude use of intensive induction chemotherapy.

Relapsed or refractory AML

For the treatment of adult patients with relapsed or refractory AML.

Relapsed or refractory Myelodysplastic Syndromes (MDS)

For the treatment of adult patients with relapsed or refractory myelodysplastic syndromes.

Locally Advanced or Metastatic Cholangiocarcinoma

For the treatment of adult patients with locally advanced or metastatic cholangiocarcinoma who have been previously treated.

中文翻译

TIBSOVO是一种异柠檬酸脱氢酶-1（IDH1）抑制剂，适用于易感IDH1突变的患者，通过FDA批准的测试检测到：

新诊断的急性髓细胞白血病（AML）

联合阿扎胞苷或作为单一疗法治疗75岁或以上的成年人新诊断的AML，或患有排除使用强化诱导化疗的合并症的患者。

复发或难治性AML

用于治疗复发或难治性AML的成年患者。

复发或难治性骨髓增生异常综合征（MDS）

用于治疗复发或难治性骨髓增生异常综合征的成年患者。

局部晚期或转移性胆管癌

用于治疗先前接受过治疗的局部晚期或转移性胆管癌的成年患者。

02用法用量

500 mg orally once daily with or without food until disease progression or unacceptable toxicity. Avoid a high-fat meal.

中文翻译

500 mg口服，每日1次，随食或空腹服用，直至疾病进展或出现不可接受的毒性。避免高脂肪食物。

03特殊人群

Pregnancy: Based on animal embryo-fetal toxicity studies, TIBSOVO may cause fetal harm when administered to a pregnant woman. There are no available data on TIBSOVO use in pregnant women to inform a drug-associated risk of major birth defects and miscarriage. In animal embryo-fetal toxicity studies, oral administration of ivosidenib to pregnant rats and rabbits during organogenesis was associated with embryo-fetal mortality and alterations to growth starting at 2 times the steady state clinical exposure based on the AUC at the recommended human dose. If this drug is used during pregnancy, or if the patient becomes pregnant while taking this drug, advise the patient of the potential risk to a fetus.

Lactation： There are no data on the presence of ivosidenib or its metabolites in human milk, the effects on the breastfed child, or the effects on milk production. Because many drugs are excreted in human milk and because of the potential for adverse reactions in breastfed children, advise women not to breastfeed during treatment with TIBSOVO and for 1 month after the last dose.

Pediatric Use： The safety and effectiveness of TIBSOVO in pediatric patients have not been established.

Geriatric Use： No overall differences in effectiveness or safety were observed between patients who were 65 years and older compared to younger patients.

Hepatic Impairment： No modification of the starting dose is recommended for patients with mild or moderate (Child-Pugh A or B) hepatic impairment. The pharmacokinetics and safety of ivosidenib in patients with severe hepatic impairment (Child-Pugh C) are unknown. For patients with pre-existing severe hepatic impairment, consider the risks and potential benefits before initiating treatment with TIBSOVO.

Renal Impairment： No modification of the starting dose is recommended for patients with mild or moderate renal impairment (eGFR ≥ 30 mL/min/1.73m2 , MDRD). The pharmacokinetics and safety of ivosidenib in patients with severe renal impairment (eGFR < 30 mL/min/1.73m 2 , MDRD) or renal impairment requiring dialysis are unknown. For patients with pre-existing severe renal impairment or who are requiring dialysis, consider the risks and potential benefits before initiating treatment with TIBSOVO.

中文翻译

妊娠：根据动物胚胎-胎儿毒性研究，TIBSOVO给孕妇服用时可能会造成胎儿伤害。没有关于孕妇使用TIBSOVO的可用数据来告知与药物相关的重大出生缺陷和流产风险。在动物胚胎-胎儿毒性研究中，在器官发生过程中向怀孕大鼠和兔子口服艾伏尼布与胚胎-胎儿死亡率和生长改变相关，从推荐人类剂量下基于AUC的稳态临床暴露的2倍开始。如果在怀孕期间使用这种药物，或者如果患者在服用这种药物时怀孕，请告知患者对胎儿的潜在风险。

哺乳期：没有关于母乳中是否存在伊沃替尼或其代谢物、对母乳喂养儿童的影响或对产奶量的影响的数据。由于许多药物是从母乳中排出的，并且母乳喂养的儿童可能会出现不良反应，因此建议女性在使用TIBSOVO治疗期间以及最后一次给药后1个月内不要母乳喂养。

儿童使用：TIBSOVO在儿科患者中的安全性和有效性尚未确定。

老年使用：与年轻患者相比，65岁及以上患者的有效性或安全性没有总体差异。

肝功能不全：对于轻度或中度（Child-Pugh A或B）肝损伤的患者，不建议修改起始剂量。严重肝功能不全（Child-Pugh C）患者的艾伏尼布药代动力学和安全性尚不清楚。对于先前存在严重肝功能损害的患者，在开始使用TIBSOVO治疗之前，请考虑其风险和潜在益处。

肾功能不全：对于轻度或中度肾功能损害（eGFR≥30 mL/min/1.73m2，MDRD）的患者，不建议修改起始剂量。严重肾功能不全（eGFR<30 mL/min/1.73m 2，MDRD）或需要透析的肾功能不全患者的艾伏尼布药代动力学和安全性尚不清楚。对于先前存在严重肾功能不全或需要透析的患者，在开始使用TIBSOVO治疗之前，请考虑其风险和潜在益处。

04不良反应

The most common adverse reactions including laboratory abnormalities (≥ 25%) in patients with AML are leukocytes decreased, diarrhea, hemoglobin decreased, platelets decreased, glucose increased, fatigue, alkaline phosphatase increased, edema, potassium decreased, nausea, vomiting, phosphate decreased, decreased appetite, sodium decreased, leukocytosis, magnesium decreased, aspartate aminotransferase increased, arthralgia, dyspnea, uric acid increased, abdominal pain, creatinine increased, mucositis, rash, electrocardiogram QT prolonged, differentiation syndrome, calcium decreased, neutrophils decreased, and myalgia.

The most common adverse reactions including laboratory abnormalities (≥ 25%) in patients with relapsed or refractory MDS are creatinine increased, hemoglobin decrease, arthralgia, albumin decreased, aspartate aminotransferase increased, fatigue, diarrhea, cough, sodium decreased, mucositis, decreased appetite, myalgia, phosphate decreased, pruritus, and rash.

The most common adverse reactions (≥ 15%) in patients with cholangiocarcinoma are fatigue, nausea, abdominal pain, diarrhea, cough, decreased appetite, ascites, vomiting, anemia, and rash.

The most common laboratory abnormalities (≥ 10%) in patients with cholangiocarcinoma are hemoglobin decreased, aspartate aminotransferase increased, and bilirubin increased.

中文翻译

AML患者最常见的不良反应包括实验室异常（≥25%），包括白细胞减少，腹泻，血红蛋白减少，血小板减少，血糖增加，疲劳，碱性磷酸酶增加，水肿，钾减少，恶心，呕吐，磷酸盐减少，食欲下降，钠减少，白细胞增多，镁减少，天冬氨酸氨基转移酶增加，关节痛，呼吸困难，尿酸增加，腹痛，肌酐增加，粘膜炎，皮疹，心电图QT延长，分化综合征，钙减少，中性粒细胞减少，肌痛。

复发或难治性MDS患者最常见的不良反应包括实验室异常（≥25%）是肌酐升高，血红蛋白降低，关节痛，白蛋白降低，天冬氨酸转氨酶升高，疲劳，腹泻，咳嗽，钠减少，粘膜炎，食欲下降，肌痛，磷酸盐减少，瘙痒和皮疹。

胆管癌患者最常见的不良反应（≥15%）是疲劳，恶心，腹痛，腹泻，咳嗽，食欲下降，腹水，呕吐，贫血和皮疹。

胆管癌患者最常见的实验室异常（≥10%）是血红蛋白降低，天冬氨酸转氨酶升高和胆红素升高。

05注意事项

QTc Interval Prolongation: Monitor electrocardiograms and electrolytes. If QTc interval prolongation occurs, dose reduce or withhold, then resume dose or permanently discontinue TIBSOVO.

Guillain-Barré Syndrome: Monitor patients for signs and symptoms of new motor and/or sensory findings. Permanently discontinue TIBSOVO in patients who are diagnosed with Guillain-Barré syndrome.

中文翻译

QTc间期延长：监测心电图和电解质。如果QTc间期延长，剂量减少或停止，然后恢复剂量或永久停止TIBSOVO。

吉兰-巴雷综合征：监测患者新的运动和/或感觉发现的体征和症状。被诊断患有吉兰-巴雷综合征的患者永久停用TIBSOVO。

06禁忌

None.

中文翻译

无。

07药物保存

Store TIBSOVO at room temperature between 68°F to 77°F (20°C to 25°C). Do not remove the desiccant canister from the bottle.

中文翻译

TIBSOVO储存于68°F至77°F（20°C至25°C）的室温下。不要将干燥剂罐从瓶中取出。

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