更新于：2023-05-28
Vazegepant
更新于：2023-05-28
概要
基本信息
药物类型 小分子化药 |
别名 Zavegepant hydrochloride、Zavegepant、1-piperidinecarboxamide, 4-(1,2-dihydro-2-oxo-3-quinolinyl)-n-((1r)-1-((7-methyl-1h-indazol-5-yl)methyl)-2-(4-(1-methyl-4-piperidinyl)-1-piperazinyl)-2-oxoethyl)- + [7] |
靶点 CGRP(降钙素基因相关肽) |
作用机制 CGRP拮抗剂(降钙素基因相关肽拮抗剂) |
治疗领域 神经系统疾病、免疫系统疾病、呼吸系统疾病 |
在研适应症 偏头痛、哮喘 |
非在研适应症 新型冠状病毒感染 |
非在研机构- |
最高研发状态(全球)批准上市 |
首次获批日期(全球) 美国 (2023-03), 偏头痛 |
最高研发状态(中国)临床1期 |
特殊审评- |
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结构
分子式C36H46N8O3 |
InChIKeyJJVAPHYEOZSKJZ-JGCGQSQUSA-N |
CAS号1337918-83-8 |
关联
7
项与 Vazegepant 相关的临床试验A Phase 1b, Double-blind, Placebo-controlled, Parallel-group Study to Evaluate Safety and Efficacy of Oral Zavegepant in Subjects With Mild Allergic Asthma
A Phase 2/3 Randomized, Double-Blind, Placebo Controlled Study to Evaluate the Efficacy and Safety of Oral Zavegepant in Migraine Prevention
Double-Blind, Randomized, Placebo-controlled, Safety and Efficacy Trial of BHV-3500 (Zavegepant) Intranasal for the Acute Treatment of Migraine
100 项与 Vazegepant 相关的专利（医药）
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18
项与 Vazegepant 相关的文献（医药）2023-04-12Expert opinion on pharmacotherapy
The pharmacotherapeutic management of episodic and chronic migraine with gepants.
Article
作者: János Tajti ; Délia Szok ; Anett Csáti ; László Vécsei
INTRODUCTION:
The small molecule non-peptide calcitonin gene-related peptide (CGRP) receptor antagonists named gepants offer a breakthrough novel approach in migraine acute and prophylactic drug treatment. This review aimed to determine the place of gepants in the treatment of episodic and chronic migraine.
AREAS COVERED:
The new generation gepants are ubrogepant, atogepant, rimegepant, and zavegepant. Ubrogepant is ratified for acute migraine treatment, atogepant is validated for preventive therapy, whereas rimegepant is ratified for both indications, all via oral administration and while zavegepant is administered intranasally for migraine attacks. Gepants are effective, safe, and well-tolerated in acute or prophylactic therapy. The PubMed literature search included randomized controlled trials, meta-analyses, real-world data, and review articles published in English until January 2023.
EXPERT OPINION:
Whether gepants will be real game changers in the acute treatment of migraine compared to triptans and ditans or in the prophylactic therapy compared to standard-of-care preventive drugs or CGRP-targeting monoclonal antibodies cannot be answered yet based on the available literature data.
2023-04-03Nature reviews. Neurology
Zavegepant for the acute treatment of migraine: look before leaping.
Article
作者: Håkan Ashina ; Peer Tfelt-Hansen
2023-03-01The Lancet. Neurology
Safety, tolerability, and efficacy of zavegepant 10 mg nasal spray for the acute treatment of migraine in the USA: a phase 3, double-blind, randomised, placebo-controlled multicentre trial.
Article
作者: Richard B Lipton ; Robert Croop ; David A Stock ; Jennifer Madonia ; Micaela Forshaw ; Meghan Lovegren ; Linda Mosher ; Vladimir Coric ; Peter J Goadsby
BACKGROUND:
Intranasal formulations can provide treatment options for people with migraine in whom oral drugs are ineffective, slow-acting, or intolerable because of nausea and vomiting. Zavegepant, an intranasally administered small molecule calcitonin gene-related peptide (CGRP) receptor antagonist, was previously assessed in a phase 2/3 trial. This phase 3 trial aimed to compare the efficacy, tolerability, safety, and timecourse of response for zavegepant nasal spray with placebo in the acute treatment of migraine.
METHODS:
This double-blind, randomised, placebo-controlled, multicentre phase 3 trial, conducted at 90 academic medical centres, headache clinics, and independent research facilities in the USA, recruited adults (aged ≥18 years) with a history of two to eight moderate or severe migraine attacks per month. Participants were randomly assigned (1:1) to zavegepant 10 mg nasal spray or matching placebo and self-treated a single migraine attack of moderate or severe pain intensity. Randomisation was stratified by the use or non-use of preventive medication. Study centre personnel entered eligible participants into the study using an interactive web response system that was operated and managed by an independent contract research organisation. All participants, investigators, and the funder were masked to group assignment. The coprimary endpoints, freedom from pain and freedom from the most bothersome symptom at 2 h after the treatment dose, were assessed in all randomly assigned participants who took the study medication, had a migraine attack of moderate or severe pain intensity at baseline, and provided at least one evaluable post-baseline efficacy datapoint. Safety was analysed in all randomly assigned participants who received at least one dose. The study is registered with ClinicalTrials.gov, number NCT04571060, and is closed to accrual.
FINDINGS:
Between Oct 27, 2020, and Aug 20, 2021, 1978 participants were recruited and assessed for eligibility. 1405 participants were eligible (703 were assigned to zavegepant and 702 to placebo), and 1269 were included in the efficacy analysis set (623 in the zavegepant group and 646 in the placebo group). 2 h after the treatment dose, more participants in the zavegepant group than in the placebo group had pain freedom (147 [24%] of 623 participants vs 96 [15%] of 646 participants, risk difference 8·8 percentage points, 95% CI 4·5-13·1; p<0·0001) and freedom from their most bothersome symptom (247 [40%] vs 201 [31%], risk difference 8·7 percentage points, 3·4-13·9; p=0·0012). The most common adverse events in either treatment group (≥2%) were dysgeusia (129 [21%] of 629 in the zavegepant group vs 31 [5%] of 653 in the placebo group), nasal discomfort (23 [4%] vs five [1%]), and nausea (20 [3%] vs seven [1%]). No signal of hepatotoxicity due to zavegepant was identified.
INTERPRETATION:
Zavegepant 10 mg nasal spray was efficacious in the acute treatment of migraine, with favourable tolerability and safety profiles. Additional trials are needed to establish the long-term safety and consistency of effect across attacks.
FUNDING:
Biohaven Pharmaceuticals.
95
项与 Vazegepant 相关的新闻（医药）2023-05-15
2023-05-03
临床2期上市批准临床3期疫苗临床结果
外链
| KEGG | Wiki | ATC | Drug Bank |
|---|---|---|---|
| - | - | - |
研发状态
| 适应症 | 最高研发状态 | 国家/地区 | 公司 |
|---|---|---|---|
| 偏头痛 | 批准上市 | 美国 更多 | |
| 哮喘 | 临床1期 | 加拿大 更多 | |
| 新型冠状病毒感染 | 终止 | 美国 更多 |
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