My research activity for Bioprojet over 30 years contributed:
- to enhance the scientific knowledge in the histamine receptor pharmacology bringing particularly evidence for in vivo constitutive activity for the histamine H3 receptor (H3R),
- to develop new pharmacological tools for H3R studies such as imetit a reference agonist, [125I]-iodoproxyfan a specific radioligand, and ciproxifan a reference antagonist,
- to the selection of several H3R antagonist or agonist as drug candidates leading to the introduction into clinics of several candidates including pitolisant (BF2.649), a potent and selective H3R antagonist/inverse agonist.
In line with this research activity, I am co-author of 74 peer-reviewed articles and co-inventor of 99 submitted patents related to histamine H3 or H4 ligands, dopamine D3 ligands and enkephalinase inhibitors.
Finally, I have been one contributor to preclinical regulatory investigations (including toxicity, reproductive and developmental toxicity, safety pharmacology and carcinogenicity studies) on pitolisant. It was granted the orphan drug status by the EMA for narcolepsy in 2007 and found to be efficient in clinics for the treatment of symptoms of narcolepsy with or without catalepsy reducing significantly the excessive diurnal sleepiness and cataplectic episodes. Since, Wakix® (pitolisant) was approved by the EMA (2016) and the US-FDA (2019-2020) for the treatment of narcolepsy with and without cataplexy, becoming a first in class drug now available for narcoleptic patients in Europe and in the USA.
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日期 | 时间 | 会场 | Session | 角色 | 讲题 |
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2021-05-15 | 16:35-16:55 | 多功能会议室5AB-1F |
嗜睡与发作性睡病,促醒疗法,对H3受体反向激动剂Pitolisant 的聚焦 |
讲者 | Overview of Preclinical Studies with Pitolisant, Histamine H3-receptor Inverse Agonist |