Diroximel/ Vumerity | 迪罗西莫/沃美力

Diroximel/ Vumerity has approved indication for multiple sclerosis, relapsing: Treatment of relapsing forms of multiple sclerosis, including clinically isolated syndrome, relapsing-remitting disease, and active secondary progressive disease, in adults. again

Oral: Initial: 231 mg twice daily; after 7 days, increase to the maintenance dose of 462 mg twice daily.

Dosage adjustment for side effects: If maintenance dose is not tolerated (GI side effects, flushing), consider temporary dose reduction to 231 mg twice daily; resume recommended maintenance dose of 462 mg twice daily within 4 weeks. Consider discontinuation in patients who cannot tolerate return to the maintenance dose.

Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.

Diroximel fumarate and its active metabolite, monomethyl fumarate (MMF), have been shown to activate the nuclear factor (erythroid-derived 2)-like 2 (Nrf2) pathway, which is involved in cellular response to oxidative stress. The mechanism by which diroximel fumarate exerts a therapeutic effect in multiple sclerosis is unknown, although it is believed to result from its anti-inflammatory and cytoprotective properties via activation of the Nrf2 pathway. MMF has also been identified as a nicotinic acid receptor agonist in vitro.

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Diroximel/ Vumerity已被批准用于复发性多发性硬化症。治疗成人复发性多发性硬化症，包括临床孤立综合征、复发-再发性疾病、和继发性进展性疾病。

口服。初始剂量：231毫克，每日两次；7天后，增加到维持剂量462毫克，每日两次。根据副作用调整剂量。如果不能耐受维持剂量（消化道副作用，潮红），考虑临时减量至231毫克，每日两次；在4周内恢复推荐的维持剂量462毫克，每日两次。对于不能耐受恢复到维持剂量的病人，考虑停药。伴随治疗的剂量调整。存在明显的药物相互作用，需要调整剂量/频率或避免。

迪罗西莫Diroximel是富马酸二羟甲基酯, 其活性代谢物富马酸单甲酯（MMF）已被证明可激活核因子（红细胞衍生2）-like 2（Nrf2）途径，该途径参与细胞对氧化压力的反应。Diroximel在多发性硬化症中发挥治疗作用的机制尚不清楚，但据信是由于其通过激活Nrf2途径而具有抗炎和细胞保护特性。MMF在体外也被确定为烟碱酸受体激动剂。