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Takecab（vonoprazan fumarate,TAK-438）富马酸沃诺拉赞片,タケキャブ錠10mg／タケキャブ錠20mg
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2015年2月27日，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。
New Drug Application Approval of TAKECAB® for the treatment of Acid-related Diseases in Japan
References
Product name TAKECAB®
Generic name Vonoprazan Fumarate
Indications Gastric ulcer, duodenal ulcer, reflux esophagitis, prevention of recurrence of gastric or duodenal ulcer during low-dose aspirin administration, prevention of recurrence of gastric or duodenal ulcer during non-steroidal anti-inflammatory drug (NSAID) administration
Adjunct to Helicobacter pylori eradication in the following settings:
Gastric ulcer, duodenal ulcer, gastric mucosa-associated lymphatic tissue (MALT) lymphoma, idiopathic thrombocytopenic purpura, the stomach after endoscopic resection of early stage gastric cancer, or Helicobacter pylori gastritis
Dosage and administration
Gastric ulcer, duodenal ulcer
The usual adult dosage for oral use is 20 mg of Vonoprazan administered orally once daily an 8 week treatment for gastric ulcer and a 6 week treatment for duodenal ulcer.
Reflux esophagitis
The usual adult dose for oral use is 20 mg of Vonoprazan administered once daily for a total of 4 weeks of treatment. If that dosing proves insufficient, the administration should be extended, but for no longer than 8 weeks of treatment.
For the maintenance therapy of reflux esophagitis showing recurrence and recrudescence, the dose for oral use is 10 mg once daily. However, when the efficacy is inadequate, the dosage may be increase up to 20 mg once daily.
Prevention of recurrence of gastric or duodenal ulcer during low-dose aspirin administration
The usual adult dosage is one tablet of 10 mg of Vonoprazan administered orally once daily.
Prevention of recurrence of gastric or duodenal ulcer during non-steroidal anti-inflammatory drug (NSAID) administration
The usual adult dosage is one tablet of 10 mg of Vonoprazan administered orally once daily
Adjunct to Helicobacter pylori eradication:
For adults, the following three-drug regimen should be administered orally at the same time twice daily for seven days: 20 mg dose of Vonoprazan, 750 mg (potency) dose of amoxicillin hydrate, and 200 mg (potency) dose of clarithromycin. The dose of clarithromycin may be increased as clinically warranted. Howe |
