武田在日本推出新型口服抗胃酸药物Takecab

日本制药企业武田（Takeda）及合作伙伴大冢（Otsuka）近日宣布，在日本推出新型口服抗胃酸药物Takecab（vonoprazan fumarate，富马酸沃诺拉赞），用于酸相关疾病的治疗。

Takecab由武田发现，该药属于钾离子（K+）竞争性酸阻滞剂（P-CAB）的新一类抑制剂，具有速效、强劲、持久的胃酸分泌抑制作用；同时，在胃壁细胞胃酸分泌的最后一步中，通过抑制K+对H+,K+—ATP酶（质子泵）的结合作用，对胃酸分泌也具有提前终止作用。在临床试验中，Takecab在治疗糜烂性食管炎、胃溃疡、十二指肠溃疡、幽门螺杆菌根除等疾病方面，表现出了强大的疗效，同时耐受性和安全性良好。

根据武田官网文件，Takecab适应症包括：（1）胃溃疡，十二指肠溃疡，反流性食管炎，预防服用低剂量阿司匹林期间胃溃疡或十二指肠溃疡的复发，预防服用非甾体类抗炎药（NSAID）期间胃溃疡或十二指肠溃疡的复发；（2）辅助幽门螺杆菌根除用于如下情况：胃溃疡，十二指肠溃疡，胃粘膜相关淋巴组织（MALT）淋巴瘤，特发性血小板减少性紫癜，早期胃癌内窥镜切除术后，幽门螺杆菌胃炎。

目前，质子泵抑制剂（PPIs）已被广泛处方用于酸相关疾病的一线治疗。但PPI并不总是能够提供足够的疗效，同时，胃酸分泌抑制效果可能也会因人而异，这是由于参与PPI代谢的一种蛋白CYP-2C19，其编码基因在不同个体中具有基因多态性。但Takecab并不主要由CYP2C19代谢，同时Takecab对质子泵的抑制作用无需酸的激活，该药以高浓度进入胃中，在首次给药时便能产生最大的抑制效应，而且该效应可持续24小时。

此外，Takecab在酸中稳定，而速效配方现成，无需优化配方设计（如肠溶包衣），药效起效剂量在不同患者中的差异并于不显著。基于这些优点，TAK-438有望显著改善当前酸相关疾病治疗中存在的问题。

英文原文：TAKECAB Now Available for the Treatment of Acid-related Diseases in Japan

Release date- 26022015 - Osaka and Tokyo, Japan,--Takeda Pharmaceutical Company Limited (Head office: Chuo-ku, Osaka; President and COO: Christophe Weber; 'Takeda') and Otsuka Pharmaceutical Company, Limited (Head office: Chiyoda-ku, Tokyo; President and Representative Director: Tatsuo Higuchi; 'Otsuka') announced today that TAKECAB 10 mg and TAKECAB 20 mg (generic name: Vonoprazan fumarate, hereafter 'TAKECAB'), discovered by Takeda for the treatment of acid-related diseases, is now available in Japan.

TAKECAB, discovered by Takeda, is a new medicine for treating acid-related diseases with a novel mechanism of action called potassium-competitive acid blockers (P-CABs) which competitively inhibits the binding of potassium ions to H+,K+-ATPase (also known as the proton pump) in the final step of gastric acid secretion in gastric parietal cells. Vonoprazan fumarate has fast-acting, strong and sustained acid secretion inhibitory effects. Takeda and Otsuka executed an agreement at the end of March 2014 to co-promote TAKECAB in Japan.

'Ever since our company launched TAKEPRON more than two decades ago, we have been supporting patients suffering from acid-related diseases and healthcare professionals who are providing them with treatment,' said Masato Iwasaki, Ph.D., Director and President, Japan Pharma Business Unit of Takeda. 'I am delighted that together with Otsuka, an excellent co-promotion partner, we are able to offer a new treatment option to address the unmet medical needs in the gastrointestinal field. Through TAKECAB, we will make further contributions to the treatment of acid-related disease.'

'From diagnosis through to treatment Otsuka is contributing broadly in the gastrointestinal field - Mucosta is a novel medicine for gastric ulcers and our diagnostic system for helicobacter pylori infections is an excellent complement to it,' said Susumu Tamai, Executive Director and Executive Operating Officer, Pharmaceutical Marketing Headquarters of Otsuka. 'We are very enthusiastic about entering this collaboration with Takeda in Japan on TAKECAB, an eagerly awaited new treatment for acid-related diseases. We strive to develop innovative medicines and diagnostic drugs to improve the quality of life of many patients.'