药品信息:
--------------------------------------------------------------- 详细处方信息以本药内容附件PDF文件(201872323225512.PDF)的“原文Priscribing Information”为准 --------------------------------------------------------------- 部分中文Rydapt处方资料(仅供参考)
Rydapt(midostaurin 中文药名:雷德帕斯胶囊)-Rydapt是第一个靶向治疗与化疗联用治疗有AML患者
作用机制
Midostaurin是抑制多种受体酪氨酸激酶的小分子。 体外生物化学或细胞测定显示,midostaurin或其主要的人类活性代谢物CGP62221和CGP52421抑制野生型FLT3,FLT3突变型激酶(ITD和TKD),KIT(野生型和D816V突变体),PDGFRα/β,VEGFR2的活性 ,以及丝氨酸/苏氨酸激酶PKC(蛋白激酶C)家族的成员。
中度石蜡表现出抑制FLT3受体信号传导和细胞增殖的能力,并且其在表达ITD和TKD突变体FLT3受体或过表达野生型FLT3和PDGF受体的白血病细胞中诱导凋亡。 Midostaurin还表现出抑制KIT信号,细胞增殖和组胺释放并诱导肥大细胞凋亡的能力。
使用限制
适应症和用途
RYDAPT未被指定为用于治疗AML患者的单一药物诱导疗法。
侵袭性系统性肥大细胞增多症(ASM),伴有血液肿瘤的系统性肥大细胞增多症(SM-AHN)或肥大细胞白血病(MCL)。
RYDAPT是一种激酶抑制剂适用为成年患者和上呼吸道感染的治疗。(6.1)有:
● ASM,SM-AHN,或MCL:最常见不良反应(≥ 20%)为恶心,呕吐,腹泻,水肿,肌肉骨骼痛,腹痛,疲乏,上呼吸道感染,便秘,发热,
● 新诊断急性髓性白血病(AML)是FLT3突变阳性当用一个FDA-批准的测试检测, 标准阿糖胞苷[cytarabine]和柔红霉素[daunorubicin]联用诱导和阿糖胞苷巩固(1.1).
剂量和给药方法
AML:50毫克口服每日两次食物。
ASM,SM-AHN和MCL:100毫克口服每日两次食物。
禁忌证
对midostaurin或任何赋形剂的超敏反应
警告和注意事项
胚胎 - 胎儿毒性:当对孕妇进行管理时,RYDAPT可能会引起胎儿的伤害。建议胎儿的潜在风险。
肺部毒性:监测间质性肺病或肺炎的症状。停止RYDAPT患有肺部毒性征兆或症状的患者。发生致命案件。
不良反应
AML:最常见的不良反应(≥20%)为发热性中性粒细胞减少症,恶心,粘膜炎,呕吐,头痛,瘀点,肌肉骨骼疼痛,鼻出血,器官相关感染,高血糖症和上呼吸道感染。
ASM,SM-AHN或MCL:最常见的不良反应(≥20%)为恶心,呕吐,腹泻,水肿,肌肉骨骼疼痛,腹痛,疲劳,上呼吸道感染,便秘,发热,头痛和呼吸困难。
RYDAPT ®
Generic Name and Formulations:
Midostaurin capsule
Company: Novartis Pharmaceuticals Corp
Select therapeutic use: Leukemias, lymphomas, and other hematologic cancers
Indications for RYDAPT:
Treatment of adults with newly diagnosed FLT3 mutation-positive acute myeloid leukemia (AML) as detected by an FDA-approved test, in combination with standard cytarabine and daunorubicin induction + cytarabine consolidation. Treatment of adults with aggressive systemic mastocytosis (ASM), systemic mastocytosis with associated hematological neoplasm (SM-AHN), or mast cell leukemia (MCL).
Limitations Of use:
Not for use as single-agent induction therapy for AML.
Adult:
Swallow whole. Take with food approx. 12hrs apart. Give prophylactic antiemetics prior to initiation. AML: 50mg twice daily on Days 8–21 of each induction cycle with cytarabine and daunorubicin, and on Days 8–21 of each consolidation cycle with high-dose cytarabine. ASM, SM-AHN, MCL: 100mg twice daily until disease progression or unacceptable toxicity. Dose modifications: see full labeling.
Children:
Not established.
Warnings/Precautions:
For ASM, SM-AHN, MCL: Monitor for toxicity at least weekly for first 4 weeks, every other week for next 8 weeks, and monthly thereafter. Discontinue if low ANC, platelet count, or hemoglobin persists >21 days. Interrupt dose if Grade 3/4 nausea and/or vomiting despite antiemetics or other Grade 3/4 non-hematological toxicities; resume at reduced dose and increase if tolerated (see full labeling). Both: monitor for signs/symptoms of interstitial lung disease or pneumonitis; discontinue if pulmonary toxicity develops. Embryo-fetal toxicity. Pregnancy; exclude status within 7 days prior to initiation. Females of reproductive potential and males should use effective contraception during and for at least 4 months after last dose. Nursing mothers: not recommended (during and for at least 4 months after last dose).
Interactions:
Concomitant drugs that prolong QT interval; monitor EKG periodically. Potentiated by strong CYP3A inhibitors (eg, boceprevir, clarithromycin, cobicistat, conivaptan, danoprevir/ritonavir, diltiazem, elvitegravir/ritonavir, grapefruit juice, idelalisib, indinavir/ritonavir, itraconazole, ketoconazole, lopinavir/ritonavir, nefazodone, nelfinavir, paritaprevir/ritonavir and [ombitasvir and/or dasabuvir], posaconazole, ritonavir, saquinavir/ritonavir, tipranavir/ritonavir, troleandomycin, voriconazole); consider alternatives; if co-administration needed, monitor for increased adverse reactions. Avoid concomitant strong CYP3A inducers (eg, carbamazepine, enzalutamide, mitotane, phenytoin, rifampin, St. John's wort).
Pharmacological Class:
Kinase inhibitor.
Adverse Reactions:
AML: Febrile neutropenia, nausea, mucositis, vomiting, headache, petechiae, musculoskeletal pain, epistaxis, device-related infection, hyperglycemia, upper respiratory tract infection. ASM, SM-AHN, MCL: also diarrhea, edema, abdominal pain, fatigue, constipation, pyrexia, dyspnea; pulmonary toxicity.
--------------------------------------------------------------- 详细处方信息以本药内容附件PDF文件(201872323225512.PDF)的“原文Priscribing Information”为准 --------------------------------------------------------------- |