Jina Pharmaceuticals Inc, Libertyville, IL, USA.
Intas Pharmaceuticals Ltd, Ahmedabad, Gujarat, India.
Bipolar Disord. 2021 Sep;23(6):595-603. doi: 10.1111/bdi.13041. Epub 2021 Jan 9.
Endoxifen is a protein kinase C inhibitor. The objective of the present phase III study was to demonstrate the safety and efficacy of endoxifen in treating bipolar I disorder (BPD I) patients.
A multicenter, double-blind, active-controlled study was conducted using a daily dose of 8 mg endoxifen compared to 1000 mg divalproex, the current standard treatment, in patients with BPD I acute manic episodes with/without mixed features. The primary endpoint of our study was the mean change in total Young Mania Rating Scale (YMRS) score at day 21.
Endoxifen (n = 116) significantly (p < 0.0001) reduced total YMRS score (from 33.1 to 17.8. A significant (p < 0.001) improvement in Montgomery-Åsberg Depression Rating Scale (MADRS) score was observed for endoxifen (4.8 to 2.5). Early time to remission of the disease was observed with endoxifen compared to divalproex. None of the patients required rescue medication and there was no drug-associated withdrawals. Changes in Clinical Global Impressions-Bipolar Disorder and Clinical Global Impression-Severity of Illness scores showed that treatment with endoxifen was well-tolerated.
Endoxifen at a low daily dose of 8 mg was as efficacious and safe in patients with BPD I acute manic episodes with/without mixed features.
依西美坦是一种蛋白激酶 C 抑制剂。本 III 期研究的目的是证明依西美坦治疗双相 I 型障碍（BPD I）患者的安全性和疗效。
采用多中心、双盲、活性对照研究，使用每日 8mg 依西美坦与目前的标准治疗 1000mg 丙戊酸钠相比，治疗 BPD I 急性躁狂发作伴/不伴混合特征的患者。我们研究的主要终点是第 21 天总 Young Mania Rating Scale（YMRS）评分的平均变化。
依西美坦（n=116）显著（p<0.0001）降低了总 YMRS 评分（从 33.1 降至 17.8。依西美坦观察到 Montgomery-Åsberg 抑郁评定量表（MADRS）评分显著（p<0.001）改善（从 4.8 降至 2.5）。与丙戊酸钠相比，依西美坦更早达到疾病缓解。没有患者需要抢救药物，也没有与药物相关的停药。临床总体印象-双相障碍和临床总体印象-疾病严重程度评分的变化表明，依西美坦治疗耐受性良好。
依西美坦每日低剂量 8mg 对 BPD I 急性躁狂发作伴/不伴混合特征的患者同样有效且安全。
