英文药名：DELTYBA tablets(delamanid)

中文药名：迪拉马尼片

生产厂家：大冢制药

デルティバ錠50mg

治疗类别名称
结核病化疗药物
商標名
DELTYBA tablets
一般名
デラマニド〔Delamanid （JAN）〕
化学名
(2R)-2-Methyl-6-nitro-2-[(4-{4-[4-(trifluoromethoxy)phenoxy]piperidin-1-yl}phenoxy)methyl]-2, 3-dihydroimidazo[2, 1-b]oxazole
構造式

分子式
C25H25F3N4O6
分子量
534.48
性　状
白色至是浅黄色的晶体或结晶粉末。N，N-二甲基乙酰胺是可溶的，并且是易溶略微四氢呋喃，略少溶于乙腈，略溶于甲醇，极微溶于乙醇（99.5），并且几乎不溶于水。
熔点
约195℃（分解）
审批条件
从在日本的施用经验已经非常有限的一段时间后，制造和销售，通过进行的所有的情况下的利用效果的调查，所以能够理解这种用药患者的背景资料，这种药物在安全性和有效性的早期收集的数据，采取必要的措施，正确使用此药。
薬効薬理
1. 薬理作用
(1) 抗菌作用
耐多药结核分枝杆菌，并显示在结核杆菌，包括耐药结核分枝杆菌的抗菌活性，也表现出对细胞内的结核杆菌和休眠结核杆菌厌氧条件下的抗菌活性。
(2) 治療効果
在小鼠慢性肺结核模型，剂量相关降低活菌通过口服给药的肺数观察，表明有治疗效果。另外，在免疫应答和免疫缺陷小鼠结核模型，表现出治疗效果相媲美。
(3) 抗结核药物联合作用
在小鼠和豚鼠慢性肺结核模型，观察治疗期间与现有抗结核药物联合用药的缩短。另外，在慢性结核病的豚鼠模型中，表明在厌氧环境对结核分枝杆菌的治疗作用。
2. 作用机序
抑制结核杆菌特异性霉菌酸生物合成。
3. 耐性
突变抵抗由具有结核杆菌辅酶F420相关基因获得。在体外试验中，Deramanido天然耐药菌出现频率高于利福平，它比得上异烟肼。然而，跨电阻与其它抗结核药是不允许。
疗效或作用
<适应的物种>
感性的结核杆菌对本药
<主治>
多耐药结核病
剂量和给药方法
成人一天两次，一次100毫克，早晨，晚上餐后口服给药。
包装规格
片剂
50毫克：[PTP] 20片（10片×2），60片（10片×6）

生产厂商
大冢制药有限公司
注：使用以原处方为准：http://www.info.pmda.go.jp/go/pack/6222006F1029_1_04/
Deltiva: New TB treatment for 40 years
On July 4, 2014, the manufacture and sale of tuberculosis chemotherapeutic drug Delamanide (trade name DELTIBA tablet 50 mg) was approved. The indication is "multidrug-resistant pulmonary tuberculosis", once 100 mg twice daily, after morning and dinner.
Currently, in standard treatment of tuberculosis, Rifampicin (RFP: trade name Rifagin et al.), Isoniazid (INH: trade name Iscochin, Isoniazid, Hydra et al.), Ethambutol (EB: Esambutol, Ebutol, etc.), Pirazinamide (PZA: Pyramid), followed by two months of intensification therapy, followed by 4 months of maintenance therapy using a combination of RFP and INH. The cure rate in this treatment program is about 90% for drug-sensitive tuberculosis patients.
On the other hand, for patients with multidrug-resistant pulmonary tuberculosis who are resistant to the first-line drugs RFP and INH, according to the WHO guidelines, two drugs for EB and PZA, one for injection and one for tuberculosis for injection such as kanamycin and levofloxacin And a fluoroquinolone antimicrobial agent such as Cravit et al.), Etc., are strongly recommended. However, even if these treatment programs are carried out, it is reported that the cure rate is 50 to 70% and the mortality rate is about 25%.
In Japan, 110 to 120 cases of multidrug-resistant pulmonary tuberculosis patients occur every year. In addition to INH and RFP, the proportion of "supermulti-drug resistant pulmonary tuberculosis" that is resistant to anti-tuberculosis drugs for injection and fluoroquinolone antibiotics is higher than those in other countries, and in 2006, patients with multidrug-resistant pulmonary tuberculosis The survey results show that about 29% of the patients were suffering from multidrug resistance.
Delramanide suppresses the biosynthesis of mycolic acid specific to mycobacteria including Mycobacterium tuberculosis and exerts anti-tuberculosis action. In nonclinical studies and early clinical phase II studies, the minimum inhibitory concentration is lower than INH and RFP, and it has been confirmed to have strong antituberculous activity.
In an international joint study for patients with multidrug - resistant pulmonary tuberculosis including Japanese, delamanide was added to the standard therapy for 2 months, and the sputum idiotization rate was significantly higher than that in the placebo group. Furthermore, the proportion of patients with effective treatment outcome in the final treatment outcome after 2 years was reported to be 74.5% in the group treated with Delamanide more than 2 months in the standard treatment, and 55.0% in the group in which the addition was 2 months or less Has been done.
In addition, DELAMANIDE does not show cross-resistance with existing anti-tuberculosis drugs, has anti-tuberculosis activity against Mycobacterium tuberculosis under aerobic and anaerobic environments, and also has a bactericidal action against intracellular Mycobacterium tuberculosis Has been approved. Overseas it was approved in Europe in April 2014 and was released in the UK in May. In Japan, on February 8, 2008, we received designation of drugs for rare diseases.
Please note that 52.7% of adverse reactions (including clinical laboratory test abnormalities) are recognized in the international joint test until approval. Main side effects are insomnia (12.2%), headache (10.4%), QT prolongation (7.1%), somnolence (6.3%) and the like, and the expression of QT prolongation is reported as a serious side effect.
In addition, in order to prevent the appearance of resistant bacteria and to promote proper use, at a registered medical institution/pharmacy with a doctor/pharmacist registered in a RAP (Responsible Access Program) conducted by a pharmaceutical company, only for patients registered by a doctor Can be used.