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2017年9月19日，靶向抗癌药copanlisib（商品名:Aliqopa 拜耳产品 60mg小瓶静脉注射）获美国FDA加速批准上市，用于治疗罹患复发性滤泡性淋巴瘤，且已经接受了至少两次系统疗法的成人患者。这也是美国FDA今年批准的第10款抗癌新药。
copanlisib是一种新颖的静脉注射型泛I类磷脂酰肌醇-3-激酶（PI3K）抑制剂，针对恶性B细胞中表达的PI3K-α和PI3K-δ异构体具有主要的抑制活性。PI3K信号通路参与细胞的生长、存活和新陈代谢，该通路的失调在非霍奇金淋巴瘤（NHL）中发挥了重要作用。
安全性方面，44例患者（26%）发生严重不良反应，最常见的严重不良反应包括肺炎（8%）、局限性肺炎（5%）、高血糖症（5%）；36例患者（21%）因不良反应降低剂量，27例（16%）因不良反应停止治疗。copanlisib治疗的患者中观察到的最常见的不良反应（发生率≥20%）包括高血糖（54%）、白细胞减少（36%）、腹泻（36%）、体力和精力下降（36%）、高血压（35%）、中性粒细胞减少（32%）、恶心（26%）、血小板减少症（22%）、下呼吸道感染（21%）。这些安全数据来自于接受copanlisib治疗的168例滤泡性淋巴瘤患者和其他血液恶性肿瘤患者。
提供：copanlisib（商品名 Aliqopa）以60mg冻干固体的形式用于单剂量小瓶
推荐：通过静脉输注给药，给药模式为：治疗3周（每周一次，每次1小时）后停药1周。
完整说明资料附件：https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=ade50241-2c10-4038-b4e9-72f6bf905f03
Aliqopa(Copanlisib for Injection, for Intravenous Use)
ALIQOPA
Leukemias, lymphomas, and other hematologic cancers Only 4 drugs may be compared at once
Generic Name and Formulations:
Copanlisib 60mg; per vial; lyophilized pwd for IV infusion after reconstitution and dilution.
Company:
Bayer Healthcare Pharmaceuticals Inc
Select therapeutic use:
RECENT UPDATES Monograph added.
Indications for ALIQOPA:
Treatment of adults with relapsed follicular lymphoma (FL) who have received at least two prior systemic therapies.
Adult:
Give 60mg as IV infusion over 1hr on Days 1, 8, and 15 of a 28-day cycle on an intermittent schedule (3 weeks on, 1 week off) until disease progression or unacceptable toxicity. Concomitant strong CYP3A inhibitors: reduce to 45mg. Dose modifications for toxicities: see full labeling.
Children:
Not established.
Warnings/Precautions:
Monitor for signs/symptoms of infection (eg, pneumonia); withhold if Grade ≥3 infection develops. Risk of serious pneumocystis jiroveci pneumonia (PJP); consider PJP prophylaxis for those at risks prior to initiation. Diabetes. Obtain optimal blood glucose and blood pressure (BP) control prior to each infusion; monitor closely. Discontinue if blood glucose ≥500mg/dL is persistent at Copanlisib 30mg dose. Discontinue if post-dose BP remains uncontrolled (>150/90mmHg) despite antihypertensives or elevated with life-threatening consequences. Withhold and treat if non-infectious pneumonitis occurs; discontinue if Grade 2 recurs or if Grade ≥3 develops. Monitor ANC at least weekly; withhold if ANC <0.5 x 103 cells/mm3; reduce to 45mg if ANC ≤0.5 x 103 cells/mm3 recurs. Monitor for severe cutaneous reactions; withhold for Grade 3 reaction; discontinue if life-threatening. Monitor for thrombocytopenia, other severe and non-life-threatening toxicities; see full labeling. Embryo-fetal toxicity. Females of reproductive potential and males (w. female partners) should use highly effective contraception during treatment and for ≥1 month after last dose. Pregnancy; exclude status prior to initiation. Nursing mothers: not recommended (during and for ≥1 month after last dose).
Interactions:
May be antagonized by strong CYP3A inducers (eg, carbamazepine, enzalutamide, mitotane, phenytoin, rifampin, St. John’s wort); avoid. 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); if concomitant use unavoidable, reduce Copanlisib dose (see Adult).
Pharmacological Class:
Kinase inhibitor.
Adverse Reactions:
Hyperglycemica, diarrhea, decreased general strength/energy, hypertension, leukopenia, neutropenia, nausea, lower respiratory tract infections, thrombocytopenia.
Generic Availability:
NO
How Supplied:
Single-dose vial—1 |
