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英文药名：Amnolake（Tamibarotene Tablets）
中文药名：他米巴罗汀片
生产厂家：日本新药
药品介绍
-复发性或难治性急性早幼粒细胞白血病的治疗剂-
批准上市日期：2005年6月
商標名
Ａｍｎｏｌａｋｅ
一般名：
タミバロテン（JAN） （英名）Tamibarotene（JAN）
化学名：
4-[(5,6,7,8-Tetrahydro-5,5,8,8-tetramethyl-2-naphthyl)carbamoyl]benzoic acid
構造式：
分子式：
Ｃ22Ｈ25ＮＯ3
分子量：
351.45
性状：
它是一种结晶性粉末或白色结晶。 N，它是易溶于二甲基甲酰胺N - ，容易给微溶于乙醇或甲醇（95），和微溶于乙醚，微溶于乙腈中，并在水中几乎不溶。
熔点
约232℃
分配系数：
>63900[1 - 辛醇/缓冲液（pH4.23,25℃）]
854[1 - 辛醇/缓冲液（pH7.07,25℃）]
审批条件
的进行上市后监测和寄存器的使用情况的所有实施例，以及进行调查的有效性和安全性，视黄酸综合征，弥散性血管内凝血综合征，总胆固醇值，上市后的一定期间，甘油三酯水平，对这种药物的肌酸激酶值，淀粉酶水平，皮肤症状，肝功能障碍，视力障碍，骨骼疼痛，高血脂剂，以及它的相互作用，将主要影响。
适应症：
复发或难治性急性前骨髓细胞性白血病（急性早幼粒细胞白血病，APL）。
用法用量：
缓解导入疗法，1日6mg/m2，分2次给药，早上及晚饭后口服，直至得到骨髓缓解。从开始给药到结束不超过8周
制造厂商
日本新药
Information is based on approvals granted in Japan. In some cases, the approved details may vary in countries other than Japan.
In deciding to use a medicine, the risk (side effects) of taking the medicine must be weighed against the benefit (effects) it will do. The patient's cooperation is indispensable here.
Brand name : Amnolake Tablets 2mg
Active ingredient: Tamibarotene
Dosage form: white tablet, diameter 7mm, thickness 3mm
Printings on wrapping: (face) 402, (back) アムノレイク錠 2mg
Effects of this medicine
This medicine has therapeutic action to differentiate myeloid cell.
It is used to treat relapsed or refractory acute promyelocytic leukemia.
Before using this medicine, tell your doctor/pharmacist
•If you ever experienced any allergic reaction (itch, rash, etc.) to any medicines.
Woman who has a possibility of being pregnant, or getting pregnant.
If you are patient with hypervitaminosis A, hyperlipemia, disorders in liver/kidney, or reduced gastric acid secretion.
If you are elderly patient, or 25 years or under.
•If you are pregnant or breastfeeding.
•If you are using any other prescription or nonprescription (OTC) medicine. (It is important to reduce the risk of drug interactions.)
Dosage regimen (proper use of this medicine)
•Your dosage regimen is:(order of your doctor)
•General dosage regimen: Take 6mg/m2 in 2 divided doses a day after breakfast and dinner. This tablet contains 2mg of the active ingredient. Strictly follow the instructions of dosage regimen.
•Swallow the medicine without breaking this tablet into small pieces or chewing.
•Missed dose: If you missed a dose, skip the missed dose and continue your regular dosing schedule. DO NOT take a double dose to make up for the missed dose.
•Overdose: If you took too much of this medicine (more than ordered), check with your doctor/pharmacist.
•Others: Do not stop taking this medicine without the instructions of your doctor.
Precautions while using this medicine
•Woman make sure to avoid pregnancy for at least 1 month before starting this medication, during taking this medicine and for at least 2 years after discontinuing it.
•Man make sure to avoid pregnancy during taking this medicine, and for at least 6 month after discontinuing it.
•Note that the grapefruit juice might strengthen the action of this medicine.
•Note that St. John's wort-containing food might weaken the action of this medicine.
•If you are taking vitamin A product (Chocola A etc.) or fibrate drug, tell your doctor/pharmacist before using this medicine.
Side effects of this medicine
Common side effects are reported as below. If any of them occurs, check with your doctor/pharmacist:
rash, bone pain, fever, dry skin, etc.
In rare cases, symptoms described below may be the sign of side effects indicated in brackets [ ]. If they occur, stop taking your medicine and check with your doctor immediately.
•high fever of over 38℃, chest pain, breathlessness[retinoic acid syndrome]
•cold-like symptoms, lassitude, vomiting[infection]
•fever, dry cough, breathlessness[interstitial lung disease]
•fever, chest pain, swallowing difficulty[mediastinitis]
•muscle pain of the hands and feet, stiffness, numbness, lassitude, red/brown urine [rhabdomyolysis]
Other side effects not listed here may occur. Check with your doctor/pharmacist if you have any worrisome symptom.
Storage and other information
•Keep out of the reach of baby and children. Store away from direct sunlight, high temperature and humidity.
•Pay close attention to storage, not to lose this medicine.
•Do not share this medicine with any other person, and make sure that any other person do not take it by mistake.
•Discard the remainder. Do not store them. Ask the pharmacist how to discard
Manufacturer's name : Nippon Shinyaku Co., Ltd。
他米巴罗汀（Tamibarotene）系由日本新药株式会社研制开发，于2005年6月13日在日本首次上市（商品名：Amnolake Tablets 2mg）
急性前骨髓细胞性白血病(APL)约占同期白血病的3.3％～17.4％。尽管1986年国内首创的全反式维甲酸(all trans retinoic acid,ATRA)诱导分化疗法可使其完全缓解(CR)率达85％以上，但快速发展的耐药与高复发率仍是影响长期疗效的两大障碍，随着临床进一步应用，发现其可形成耐药性并使复发患者难以再次获得缓解。全反式维甲酸（ATRA）与化疗药物联合应用是当前APL的一线及标准治疗方法。ATRA可并发视黄酸综合征，这种并发症是严重的且有时可致命，在患者中出现的比例已达25％。不幸的是，ATRA单独治疗诱导的缓解持续时间比较短暂。另外，患者经常对ATRA的二次治疗应答失败。如今，ATRA基础治疗失败的患者采用三氧化二砷治疗，此化合物由静脉内给药且具有明显的毒性（包括心搏不齐）。
他米巴罗汀针对ATRA的耐药性而开发，是一个新的RARα促进剂，对急性前骨髓细胞性白血病复发患者具有显著分化诱导能力的药品。本品显示对ATRA缓解后复发的APL 具有显著有效性，对ATRA应答困难患者的有效性也可期待。
药理特点：急性前骨髓细胞性白血病（APL）由一种特殊的染色体易位[t(15;17)]所导致。这种易位使前骨髓细胞（PML）白血病基因和视黄酸受体α (RARα)基因产生融合，从而阻止使处于前骨髓细胞期的骨髓细胞成熟，导致了前骨髓细胞的增殖。这些细胞在骨髓和外周血中蓄积，代替了正常的血液细胞。APL以原始细胞的一种特殊形态为特征且伴随特殊的凝血障碍。
他米巴罗汀是一个新的RARα促进剂，其在体外可成功地诱导PML分化和成熟，制止PML增殖。在体内试验中，他米巴罗汀显示了抗肿瘤活性和较好的耐受性。
他米巴罗汀导致APL细胞分化和死亡的体外有效性约超过ATRA（全反式维甲酸）10倍。另外，他米巴罗汀对细胞维甲酸结合蛋白具有较低的亲和力，因此本品给药期间可维持持久的血浆浓度。他米巴罗汀不与RAR-α受体（皮层内的主要的视黄酸受体）结合。
临床评价：在APL 患者中进行了他米巴罗汀1 日 3~12 mg/m2 分2次口服给药，给药时间为11 天~57天评价治疗效果的临床试验，有效性分析对象为39 例，结果见下表。39例患者包括先前没有接受过治疗和先前接受过治疗的患者，这些患者中的全部缓解率为61.5%。复发性患者中的全部缓解率为81%。7.3%的患者报告了RAS。
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产地国家: 日本
原产地英文商品名:
Amnolake （アムノレイク錠）2mg/tablet 10tablets/box
原产地英文药品名:
Tamibarotene
中文参考商品译名:
Amnolake（アムノレイク錠） 2毫克/片 10片/盒
中文参考药品译名:
他米巴罗汀
完整处方附件：http://www.info.pmda.go.jp/go/pack/4291014F1021_1_09/ |
