Mytesi(crofelemer 125mg delayed-release tablets)是一种获FDA批准的为抗腹泻处方药，用于抗逆转录病毒治疗（ART）的艾滋病毒/艾滋病成人非感染性腹泻症状缓解。
批准日期：公司：Napo Pharmaceuticals Inc.
MYTESI（crofelemer）缓释片，用于口服
美国最初批准：2012年
最近的重大变化
剂量和管理02/2018
作用机制
Crofelemer是环状腺苷一磷酸（cAMP）刺激的囊性纤维化跨膜传导调节因子（CFTR）氯离子（Cl）通道的抑制剂，以及肠细胞腔膜上的钙激活的Cl¯通道（CaCC）。CFTRCl通道和CaCC调节肠上皮细胞的Cl和液体分泌。Crofelemer通过阻断Cl分泌并伴随腹泻中的大量水分流失，使胃肠道中的Cl和水的流动正常化而起作用。
适应症和用法
MYTESI是一种抗腹泻药，适用于抗逆转录病毒治疗的成人HIV/AIDS患者非感染性腹泻的症状缓解。
剂量和给药
在开始MYTESI之前，排除腹泻的传染病因。
推荐的成人剂量是125毫克，每天口服两次，有或没有食物。
不要压碎或咀嚼片剂。。
剂量形式和强度
延迟释放片剂：125mg
禁忌症
没有
警告和注意事项
传染性腹泻患者的治疗风险：在开始治疗前考虑腹泻的传染病因，以降低不适当治疗和疾病恶化的风险。
不良反应
最常见的不良反应（≥3％）是上呼吸道感染，支气管炎，咳嗽，胃肠胀气和胆红素升高。
包装提供/存储和处理
MYTESI（crofelemer）125mg缓释片剂是白色，椭圆形片剂，一面印有125SLXP。
它们有以下包装尺寸：
60瓶：NDC 70564-802-60
储存在20°C-25°C（68°F-77°F）; 允许的偏差在15°C-30°C（59°F-86°F）之间。 参见USP受控室温。
完整说明附件：
https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=45584fba-8081-4cd1-a21e-3ea8237f62ff
MYTESI(crofelemer) delayed-release tablets for oral use
General Information
Mytesi (crofelemer) is extracted from the latex of the Croton lechleri tree. it reduces excess chloride ion secretion via the cystic fibrosis transmembrane conductance regulator (CFTR) channel. The chloride channel CFTR regulates water balance in the intestines through control of chloride ion secretion and sodium absorption.
Mytesi is specifically indicated for symptomatic relief of non-infectious diarrhea in adult patients with HIV/AIDS on anti-retroviral therapy.
Mytesi is supplied as a delayed-release tablet for oral administration. The recommended dose is one 125 mg delayed-release tablet taken orally two times a day, with or without food. Tablets should not be crushed or chewed. Tablets should be swallowed whole.
Clinical Results
FDA Approval
The FDA approval of Mytesi was based on a randomized, double-blind, placebo-controlled (one month) and placebo-free (five month), multi center study.
The study enrolled 374 HIV-positive patients on stable anti-retroviral therapy (ART) with a history of diarrhea for one month or more. The study had a two-stage adaptive design.
In both stages, patients received placebo for 10 days (screening period) followed by randomization to crofelemer or placebo for 31 days of treatment (double-blind period). Only patients with 1 or more watery bowel movements per day on at least 5 of the last 7 days in the screening period were randomized to the double-blind period.
Each stage enrolled patients separately; the dose for the second stage was selected based on an interim analysis of data from the first stage. In the first stage, subjects were randomized to one of three crofelemer dose regimens (125, 250, or 500 mg twice daily) or placebo.
In the second stage, subjects were randomized to crofelemer 125 mg twice daily or placebo. Each study stage also had a five month period (placebo-free period) that followed the double blind period. Patients treated with crofelemer continued the same dose in the placebo-free period. In the first stage, patients that received placebo were re-randomized to one of the three crofelemer dose regimens (125, 250, or 500 mg twice daily) in the placebo-free period.
In the second stage, patients that received placebo were treated with crofelemer 125 mg twice daily in the placebo-free period. The primary efficacy endpoint was the proportion of patients with a clinical response, defined as less than or equal to 2 watery bowel movements per week during at least 2 of the 4 weeks of the placebo-controlled phase.
A significantly larger proportion of patients in the crofelemer 125 mg twice daily group experienced clinical response compared with patients in the placebo group (17.6% vs. 8.0%, 1-sided p < 0.01).
Side Effects
Adverse events associated with the use of Mytesi may include, but are not limited to, the following:
upper respiratory tract infection
bronchitis
cough
flatulence
increased bilirubin
Mechanism of Action
Mytesi (crofelemer) is extracted from the latex of the Croton lechleri tree. It is an inhibitor of both the cyclic adenosine monophosphate (cAMP)-stimulated cystic fibrosis transmembrane conductance regulator (CFTR) chloride ion (Cl-) channel, and the calcium-activated Clc hannels (CaCC) at the luminal membrane of enterocytes.
The CFTR Cl channel and CaCC regulate Cl-and fluid secretion by intestinal epithelial cells.
Crofelemer acts by blocking Cl secretion and accompanying high volume water loss in diarrhea, normalizing the flow of Cl and water in the GI tract.