英文药名：TARGRETIN capsules(Bexarotene)

中文药名：贝沙罗汀胶囊

生产厂家：美能药业

タルグレチンカプセル75mg

治疗类别名称
抗肿瘤药
商標名
TARGRETIN capsules 75mg
一般名
ベキサロテン（JAN）　（英名）Bexarotene（JAN）
化学名
4-[1-(3,5,5,8,8-Pentamethyl-5,6,7,8-tetrahydronaphthalen-2-yl)ethenyl]benzoic acid
分子式
C24H28O2
分子量
348.48
構造式

融　点
約225～227℃
性　状
白色粉末。
N，易溶于N-二甲基甲酰胺，甲醇或乙醇（95）微溶，在乙腈极微溶于，和几乎不溶于水。
条件批准
1.建立药品风险管理计划的顶部，要正确实施。
2.由于试验病人在日本是非常有限的，上市后，直至有关一定数量的病例数据集成，通过实现对一切案件的使用，结果调查显示，这使得它能够及早发现这种药物的使用患者的背景资料，数据收集这种药物的安全性和有效性，采取必要的措施，正确使用这种药物。
药效药理
1.作用机制
贝沙罗汀结合类视黄醇X受体（RXRα，RXRβ和RXRγ），通过激活转录，表明凋亡诱导和细胞周期阻滞活性，据估计，抑制肿瘤生长。
2.抗肿瘤作用
(1) 体外（In vitro）
从蓓萨罗丁HH和HUT78细胞抑制CTCL的增殖。
(2) 体内（In vivo）
贝沙罗汀是，在小鼠中的HH细胞系皮下植入，显示出肿瘤生长的抑制作用。
适应病症
皮肤T细胞淋巴瘤
用法与用量
成人；每天一次300毫克/平方米（体表面积），以餐后口服给药。应当指出的是，根据该状态的患者用药。
包装规格
75毫克：14胶囊（14粒×1）（PTP），100粒（瓶）

制造厂商
美能药业有限公司
本品完整资料附件：http://www.info.pmda.go.jp/go/pack/4291042M1022_1_02/
TARGRETIN capsules 75mg（Bexarotene）タルグレチンカプセル75mg
Skin T cell lymph of the second component of bexarotene (targretin)
On January 22, 2016, the manufacture and sale of bexarotene (product name Targretin capsule 75mg) as an antineoplastic agent was approved. Adaptation is "cutaneous T cell lymphoma", orally administered 300mg/m 2 once a day after meals.
Skin T cell lymphoma (CTCL) is a type of non-Hodgkin's lymphoma that often develops in organs other than lymph nodes, such as gastrointestinal tract, skin, brain, among malignant lymphomas. T-cell lymphomas are collectively referred to as primary skin lymphomas that do not have lesions in organs other than skin at the time of initial visit.
In mycosis fungoides occupying the majority of CTCL, it reaches the "tumor stage" which is mainly composed of multifocal dermatomas after a slow period of "erythemal stage" and "flat invasive stage". In patients with tumor stage, complications such as organ infiltration, infections, etc. are extremely poor and even if they do not die, the patient's quality of life suddenly decreases due to frequent occurrence of tumor masses and recurrence, and this will interfere with social life There are many. Oral remedy for tumor
In Japan, however, the number of affected patients with CTCL is smaller than in other countries, and the incidence of CTCL occurrence in Japan is estimated to be about 10 to 20% of white Americans and Americans. Therefore, clinical trials to develop new drugs are difficult, introduction of therapeutic drugs widely used in Europe and the United States has been delayed, but finally in September 2011 the oral drug which inhibits histone deacetylase (HDAC) Vorinostat (trade name Zolinza) has been used clinically.
This approved Bexarotene is also one of CTCL therapeutic drugs widely used in the West. Ezetimibe is a kind of retinoid, selectively binds to the retinoid X receptor to activate transcription, thereby inducing apoptosis and cell cycle arrest, suppressing tumor growth.
Overseas, it has been approved in 39 countries around the world as of August 2015, including the United States in 1999, and it is recommended as one of the therapeutic agents for CTCL in major Western guidelines (NCCN, EORTC).
In Japan, in March 2013, the Ministry of Health, Labor and Welfare received designation of drugs for rare diseases, efficacy and safety were confirmed from domestic phase I / II clinical trials (B-1101 test) and overseas clinical trials That's what we approved this time.
In domestic clinical trials, side effects (including abnormal laboratory test values) are recognized in all cases. The main adverse reactions are hypothyroidism (93.8%), hypercholesterolemia (81.3%), hypertriglyceridemia (75.0%) etc, and serious side effects are dyslipidemia, pancreatitis, pituitary thyroid function decline Disease, hypoglycemia, leukopenia, neutropenia, anemia, liver failure, liver dysfunction, infection, interstitial lung disease, thromboembolism, rhabdomyolysis are reported.
With regard to bevacizumab, attention is drawn to the serious side effects of bexarotene preparation from the Ministry of Health, Labor and Welfare. Also, since it has teratogenicity, administration to pregnant women is contraindicated, so patient selection has to be done sufficiently.