Office of Clinical Pharmacology (OCP), Office of Translational Sciences (OTS), Center for Drug Evaluation and Research (CDER), Food and Drug Administration (FDA), Silver Spring, Maryland, USA (Dr Habet).
Int J Neuropsychopharmacol. 2022 Aug 4;25(7):567-575. doi: 10.1093/ijnp/pyac021.
This new drug application was first submitted to the US Food and Drug Administration (FDA) by the Orion Corporation from Finland on January 2, 1998. The final clinical pharmacology review was completed on September 3, 1999. Entacapone is a potent and specific peripheral catechol-O-methyltransferase inhibitor. It has been shown to improve the clinical benefits of levodopa plus an aromatic L-amino acid decarboxylase inhibitor when given to patients with Parkinson's disease and end-of-dose deterioration in the response to levodopa (the "wearing-off" phenomenon). The drug indication is for Parkinson's disease as an adjunct therapy to levodopa/carbidopa. This is a combination drug with carbidopa (aromatic amino acid decarboxylation inhibitor) and entacapone. It is rapidly absorbed after oral administration of a single dose, with peak time generally reached within 1 hour. It is noted that no accumulation of plasma entacapone was detected after 8 daily doses. The maximum daily dose is 2000 mg. In this paper, the clinical pharmacology review of the drug is presented from the perspective of a clinical pharmacologist who reviewed this new drug application at the FDA. It should be noted that all the information in this paper is publicly available on the FDA website and in its literature.
这项新药申请于 1998 年 1 月 2 日由芬兰 Orion 公司首次提交给美国食品和药物管理局（FDA）。最终的临床药理学审查于 1999 年 9 月 3 日完成。恩他卡朋是一种强效且特异的外周儿茶酚-O-甲基转移酶抑制剂。当给予帕金森病患者时，它已被证明可改善左旋多巴加芳香族 L-氨基酸脱羧酶抑制剂的临床疗效，并可改善左旋多巴的疗效（“开-关”现象）。该药物的适应证为帕金森病，作为左旋多巴/卡比多巴的辅助治疗。这是一种与卡比多巴（芳香族氨基酸脱羧酶抑制剂）和恩他卡朋的组合药物。单剂量口服后迅速吸收，一般在 1 小时内达到峰值。值得注意的是，在 8 天的每日剂量后未检测到血浆恩他卡朋的积累。最大日剂量为 2000 毫克。本文从临床药理学家的角度介绍了该药物的临床药理学审查，该临床药理学家在 FDA 审查了这项新药申请。应当注意的是，本文中的所有信息均可在 FDA 网站及其文献中公开获得。
