AN INTERVENTIONAL EFFICACY AND SAFETY, PHASE 3, DOUBLE-BLIND, 3-ARM, STUDY TO INVESTIGATE PAIN RESPONSE WITH INTRANASAL ZAVEGEPANT COMPARED WITH PLACEBO IN THE ACUTE TREATMENT OF MULTIPLE MIGRAINE ATTACKS IN ADULT PARTICIPANTS

The purpose of this study to show that zavegepant 10 milligrams given through the nose provides:
* freedom from pain, 2 hours after taking the medicine for the first migraine attack.
* consistent freedom from pain, 2 hours after taking the medicine across 4 separate migraine attacks.
This study is seeking participants who:
* are 18 years of age or older.
* have migraine attacks present for at least 1 year with age onset before 50 years old.
* have migraine attacks, on average, lasting about 4 to 72 hours if not treated.
* have 3 to 8 attacks per month but less than15 headache days per month.
If the participant is fit to take part in the study, the participant will receive either the study medicine zavegepant or placebo. A placebo looks like zavegepant but does not contain active ingredients. The study medicine will be given using nasal spray device containing a single amount of zavegepant or matching placebo.
The participants will be instructed to take the study medicine at home if participants have a migraine headache which reaches moderate or severe pain intensity. The participants are expected to treat up to 4 migraines of moderate to severe intensity.
After taking the study medicine, the participant is not allowed to take any other medications for at least 2 hours after taking the study medicine or placebo. Participant can take other medicines after the 2 hours if the migraine is still present. The participant is expected to record on a paper log all medications taken throughout the study.
The study duration is around 26 weeks. This includes a 28-day screening window, up to 20 weeks of treatment period, and a follow up visit at about 4 weeks after taking the study medicine the last time.
The participant is expected to come into the study center up to 4 times. There will be up to 3 telephone contacts including one after taking the study medicine the first time or Month 1 whichever comes first, at Month 3 if the participant is still in the study, and a safety follow-up.
During the study, the participant is expected to complete two sets of questions in an app on a smartphone. This step is done before and after taking the study medicine. The participants must rate:
* Pain
* Pain symptoms
* How the participants are feeling
* General well-being

开始日期2025-09-15

申办/合作机构

Pfizer Inc.

NCT06985342

/ Not yet recruiting临床4期IIT

A Prospective, Open-Label Study Examining the Use of Rimegepant ODT 75 mg or Zavegepant Nasal Spray 10 mg for Acute Treatment of Migraine in the Emergency Department Setting

This study evaluates the effectiveness of rimegepant 75 mg orally disintegrating tablet (ODT) single-dose or zavegepant 10 mg nasal spray single-dose as acute migraine treatments during Emergency Department (ED) encounters. Although these two calcitonin gene-related peptide receptors (CGRP) receptor antagonists are FDA-approved for the indication of acute migraine treatment, past studies have been limited to the outpatient setting. If these medications are effective in the Emergency Department, their delivery methods alone may have advantages over intravenous medications commonly used for acute migraine in EDs, including quicker time to treatment delivery, faster pain relief, and reduced ED length of stay. This investigation is a pilot study to examine rimegepant and zavegepant in an ED, to gain insight on effectiveness in this setting.
This study will administer rimegepant 75 mg ODT single-dose or zavegepant 10 mg nasal spray single-dose as acute migraine treatments to 100 patients in the Emergency Department. It is a single center, open-label, non-controlled 2-group clinical trial (allocated 1:1 to rimegepant or zavegepant via pseudo-random assignment). The study will enroll adults in the ED meeting ICHD-3 criteria for migraine or probable migraine, with or without aura.

开始日期2025-05-01

申办/合作机构

Icahn School of Medicine at Mount Sinai

[+1]

NCT06453356

/ Completed临床1期

A PHASE 1 SINGLE INTRANASAL DOSE, OPEN-LABEL PHARMACOKINETIC STUDY OF ZAVEGEPANT IN HEALTHY LACTATING WOMEN

The purpose of the study is to look at the amount of zavegepant that is present in breast milk after single dose of zavegepant is sprayed through the nose in healthy breast-feeding women. This would allow to see if there are any possible risk to infants from medicines during breast-feeding.
The study is seeking for about 12 healthy breast-feeding females who are:
* 18 to 55 years of age.
* actively breast-feeding or producing breast milk.
* at least 2 weeks post-partum and not pregnant at present. Participants will not be allowed to breast-feed their infant from the evening of the day before to the first dose till 48 hours (2 days) after the dose.
Eligible participants will check into the clinical research unit (CRU) on Day -1. Participants will receive the zavegepant dose sprayed into the nose at the CRU on Day 1. The participants will stay at the CRU until the morning of Day 2. There will be collections of breast milk and plasma over 24 hours. Participants will be sent from the CRU on Day 2 and may begin to breastfeed their infant 48 hours (2 days) after the dose. A safety follow-up call will be done at about 28 to 35 days from the day the first dose of study medicine was given.

开始日期2024-06-10

申办/合作机构

Pfizer Inc.

100 项与 Zavegepant 相关的临床结果

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100 项与 Zavegepant 相关的转化医学

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100 项与 Zavegepant 相关的专利（医药）

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项与 Zavegepant 相关的文献（医药）

2025-05-04·Pain Management

Head-to-head relief: ubrogepant, rimegepant, and zavegepant in migraine treatment

Review

作者: Al-Abdullah, Samah ; Pellesi, Lanfranco ; Jedie, Budour ; Xiao, Zheman ; Barhum, Fadia ; Martelletti, Paolo

Migraine, a significant cause of disability worldwide, heavily impacts daily functioning and quality of life. Despite various acute treatment options, including nonsteroidal anti-inflammatory drugs (NSAIDs) and triptans, patients experience limited relief or adverse effects. This review examines the efficacy and safety of gepants - ubrogepant, rimegepant, and zavegepant - in the acute treatment of migraine. We assessed phase II and III clinical trials, focusing on clinically relevant endpoints such as pain freedom and freedom from the most bothersome symptom at two hours post-treatment. We calculated the number needed to treat (NNT) to achieve significant endpoints for each gepant. Gepants are recommended for the acute treatment of migraine in individuals who do not respond to triptan monotherapy or combination therapy, who experience only partial effectiveness, or who cannot tolerate or have contraindications to triptans. The NNT values for achieving pain freedom at two hours were 9 for rimegepant, 11 for zavegepant, and 12 for ubrogepant, which are comparable to NSAIDs such as naproxen (NNT = 11). Paracetamol, although not an NSAID, showed similar efficacy (NNT = 12). Triptans demonstrated lower NNTs, indicating higher efficacy. Gepants offer effective, well-tolerated alternatives with no significant cardiovascular risk and minimal potential for medication-overuse headache.

2025-03-01·HEADACHE

Comparative bioavailability of single‐dose zavegepant during and between migraine attacks: A phase 1, randomized, open‐label, fixed‐sequence, two‐period study

Article

作者: Kamen, Lisa ; Bhardwaj, Rajinder ; Madonia, Jennifer ; Liu, Jing ; Matschke, Kyle T. ; Collins, Julie L. ; Bertz, Richard J.

Abstract:

Objective:

To compare the rate and extent of absorption of zavegepant 10 mg (therapeutic dose) or 20 mg (supratherapeutic dose) nasal spray during a migraine attack versus non‐migraine period, assess safety, and explore efficacy and the relationship between zavegepant concentration and therapeutic response.

Background:

Physiologic changes occurring during a migraine attack could affect the pharmacokinetics of treatments for migraine.

Methods:

This was a Phase 1, multicenter, open‐label, randomized, single‐dose, two‐period, fixed‐sequence, comparative bioavailability study. Participants with a history of 2–8 migraine attacks per month of moderate or severe pain intensity were randomized to a single dose of zavegepant 10 or 20 mg, administered intranasally during a migraine attack (Period 1) and in a non‐migraine period (Period 2). Blood samples were collected pre‐dose and at pre‐specified intervals up to 24 h post‐dose for plasma zavegepant concentration measurement. Safety was monitored throughout, and efficacy (migraine pain intensity score, nausea, photophobia, phonophobia, aura, and functional disability) assessed during Period 1. Plasma zavegepant pharmacokinetic parameters were calculated by standard noncompartmental methods, including maximum plasma concentration (Cmax), area under plasma concentration–time curve from time zero to infinity (AUC0–inf), and time of Cmax (Tmax).

Results:

A total of 37 participants were evaluable for pharmacokinetics. Following administration of zavegepant 10 mg, geometric mean ratios for Period 1/Period 2 were 82.8% (90% confidence interval [CI] 60.5–113.2) for Cmax and 90.1% (90% CI 70.2–115.5) for AUC0–inf. Following administration of zavegepant 20 mg, geometric mean ratios for Period 1/Period 2 were 72.5% (90% CI 57.9–90.8) for Cmax and 73.4% (90% CI 58.8–91.7) for AUC0–inf. Averaging over the study period, geometric mean ratios for zavegepant 20 mg/10 mg were 142.5% (90% CI 118.6–171.4) for Cmax and 157.0% (90% CI 133.6–184.5) for AUC0–inf. Median Tmax was 0.5 h for both doses regardless of Period. Zavegepant was well tolerated in both study periods and effective during Period 1 at both dose levels. There was no apparent correlation between concentration at 0.5 h or 2 h post‐dose and efficacy outcomes.

Conclusion:

Zavegepant exposure was comparable during a migraine attack and a non‐migraine period, particularly at the therapeutic dose of 10 mg. When averaging over migraine and non‐migraine periods, there was a less‐than‐dose proportional increase in zavegepant exposure when the dose was doubled from 10 to 20 mg. The median Tmax was 0.5 h regardless of migraine attack or dose. Zavegepant 10 and 20 mg exhibited favorable safety profiles during migraine attacks and non‐migraine periods, and were effective to relieve pain, associated symptoms, and functional disability during migraine attacks, with no apparent correlation between zavegepant concentration and efficacy outcomes.

2025-02-01·HEADACHE

Assessment of pharmacokinetic and pharmacodynamic interactions between zavegepant and sumatriptan: A phase 1, randomized, placebo‐controlled study in healthy adults

Article

作者: Donohue, Mary K. ; Bertz, Richard ; Matschke, Kyle ; Bhardwaj, Rajinder ; Anderson, Matt S. ; Madonia, Jennifer ; Morris, Beth ; Croop, Robert ; Liu, Jing

Abstract:

Objective:

To evaluate the pharmacodynamic (PD) and pharmacokinetic (PK) interactions between zavegepant and sumatriptan in healthy adults.

Background:

Zavegepant is a high‐affinity, selective, small‐molecule calcitonin gene–related peptide receptor antagonist administered as a nasal spray approved in the United States for the acute treatment of migraine. Triptans, including sumatriptan, are a different class of drugs for acute migraine treatment and are associated with a risk of increased blood pressure (BP). Hence, it is important to study the drug–drug interactions between zavegepant and sumatriptan due to potential coadministration in clinical settings.

Methods:

This was a Phase 1, single‐center, partially blind, randomized, placebo‐controlled, single‐arm study. Eligible participants were males aged ≥ 18 and ≤ 40 years or females aged ≥ 18 and ≤ 50 years. On Day 1, participants received sumatriptan 2 × 6 mg subcutaneous injections (1 h apart) and were then randomized (6:1 ratio) to receive zavegepant 2 × 10 mg nasal spray (1 in each nostril) or placebo on Days 2 and 3. On Day 4, zavegepant or placebo was coadministered with sumatriptan after the second sumatriptan injection. BP, PK, and safety were evaluated at pre‐specified time points.

Results:

Forty‐two participants enrolled in the study received at least one dose of any treatment and were included in the safety analyses. Forty‐one participants who completed the study were included in the BP and PK analyses. The mean (standard deviation) time‐weighted average (TWA) of mean arterial pressure (MAP [sumatriptan + zavegepant 87.2 (6.8) vs. sumatriptan 86.9 (6.0)]), diastolic BP (DBP [sumatriptan + zavegepant 72.3 (6.8) vs. sumatriptan 72.1 (6.2)]), and systolic BP (SBP [sumatriptan + zavegepant 116.8 (10.2) vs. sumatriptan 116.2 (8.6)]) did not change following zavegepant and sumatriptan coadministration on Day 4 compared to sumatriptan alone on Day 1. Statistical comparisons of the TWA of MAP, DBP, and SBP between sumatriptan and zavegepant coadministration and sumatriptan alone were similar; the differences observed were 0.04 mmHg for MAP (90% confidence interval [CI]: −0.69, 0.77 mmHg), 0.00 mmHg for DBP (90% CI: −0.76, 0.76 mmHg), and 0.33 mmHg for SBP (90% CI: −0.97, 1.63 mmHg). Sumatriptan PK after sumatriptan and zavegepant coadministration versus sumatriptan alone was similar; the comparison ratios were 102.5% (90% CI: 100.7%, 104.2%) for AUC0‐inf and 104.1% (90% CI: 98.0%, 110.6%) for Cmax. A small difference in zavegepant PK exposure after sumatriptan and zavegepant coadministration versus zavegepant alone was not considered clinically relevant: the comparison ratios were 112.4% (90% CI: 103.4%, 122.3%) for AUC0–24 and 96.7% (90% CI: 88.9%, 105.2%) for Cmax. Overall, 90% (38/42) of participants experienced ≥ 1 treatment‐emergent adverse event that was mild or moderate in severity. All treatments were generally safe and well tolerated.

Conclusion:

Coadministration of zavegepant with sumatriptan was safe and without PD or PK interactions in healthy adults.

177

项与 Zavegepant 相关的新闻（医药）

2025-05-16

·ETPharma

US FDA approves Amneal's self-administered migraine treatment

Bengaluru: The U.S. Food and Drug Administration has approved Amneal Pharmaceuticals ' self-administered migraine drug , giving way to a quick and more convenient treatment option for patients. The treatment, branded as Brekiya , delivers a single dose of the drug called dihydroergotamine mesylate via an autoinjector. It is approved for the treatment of acute cases of migraine and severe, one-sided pain in the head called cluster headaches in adults, the drugmaker said on Thursday. Migraine, characterized by recurrent attacks of throbbing pain on one side of the head, causes symptoms such as nausea, vomiting and sensitivity to light. The treatment offers a beneficial alternative to those who respond poorly to oral therapies, Amneal said. Oral migraine treatments include Axsome Therapeutics' recently approved Symbravo and Pfizer's Nurtec ODT. Pfizer also sells a nasal spray, Zavzpret, for the treatment of acute migraine. Amneal's single-dose drug can be administered by patients into the middle of the thigh and does not require refrigeration or assembly of the device. Brekiya will be available in the U.S. by the second half of the year and Amneal will disclose price details close to the launch, it said. The FDA had previously declined to approve the application citing issues at a third-party manufacturing site. The company said last year it had transferred production to an in-house facility. (Reporting by Mariam Sunny and Puyaan Singh in Bengaluru; Editing by Devika Syamnath)

上市批准

2025-01-26

·化学经纬

新药研发新趋势：融合氮杂环的使用

药物研发新趋势：融合氮杂环的兴起在现代药物研发的舞台上，融合氮杂环化合物正逐渐成为一颗耀眼的新星。随着科学技术的不断进步，药物的结构和性质也在快速演变。最近美国亚利桑那大学的一项研究对2013年至2023年间美国FDA批准的小分子药物进行了深入分析，揭示了融合氮杂环化合物在新药研发中的重要性。本文将为您系统总结这项研究的主要内容，带您走进药物化学的新视野。研究背景 2013年至2023年间，FDA批准了321种新小分子药物，其中82%含有至少一个氮杂环，这一比例相较于过去几十年的59%有了惊人的增长。此外，每种药物的氮杂环数目也显著增加，大量药物含有两个(33%)、三个(23%)或四个(8%)氮杂环，并且有两个药物含六个氮杂环的结构。 From:J. Med. Chem. 2024, 67, 11622–11655 下图是美国FDA批准的独特新小分子药物集中出现的前35个氮杂环，排名前五位的是吡啶，哌啶，吡咯烷，哌嗪和嘧啶。与从FDA成立到2012年12月的前25种氮杂环化合物进行比较，揭示了一些显著变化。在前五种最常见的氮杂环化合物中，吡啶已经取代了哌啶，成为第一位，后者降至第二位；吡咯烷已经从第五位跃升至与哌啶并列的第二位；哌嗪从第三位降至第四位；而嘧啶则是一个新面孔，跻身第五位，较之前的第十位大幅上升。 From:J. Med. Chem. 2024, 67, 11622–11655 融合氮杂环对2013年到2023年间美国FDA批准的小分子药物中的氮杂环结构分析表明，一个关键的新的显著增长趋势是使用不同类型的融合氮杂环，其中大多数在早期的研究中是不存在的，这一趋势主要受到新批准的抗癌药物的推动。融合氮杂环的优势融合氮杂环化合物因其在药物中的多功能性和结构多样性而备受青睐。这些化合物不仅增强了药物的效力和选择性，还提高了药物的生物利用度和稳定性。在新批准的药物中，融合氮杂环的出现频率和多样性都有显著提升，尤其是在抗癌领域。融合氮杂环的应用实例在这项研究中，多个新药的成功案例展示了融合氮杂环化合物的巨大潜力。以下是融合氮杂环在最近十年FDA批准药物中的具体应用： 01 吡咯并嘧啶共有六种新的吡咯并嘧啶类药物获得批准，所有这些药物都是激酶抑制剂，其中三种用于治疗癌症。Abrocitinib（2022年1月批准）和Baricitinib（2018年5月批准）分别包含张力性环丁烷和氮杂环丁烷环作为其结构的一部分，其中Abrocitinib用于治疗湿疹，Baricitinib用于治疗类风湿性关节炎。Ritlecitinib（2023年6月批准），其结构中含有活性丙烯酰胺取代基和4-取代的吡咯并嘧啶，与Abrocitinib和Baricitinib类似，用于治疗斑秃（脱发）。 From:J. Med. Chem. 2024, 67, 11622–11655 02 吡唑并嘧啶五种新的含有吡唑并嘧啶的药物已经获得批准，它们都是用于治疗癌症的激酶抑制剂。值得注意的是，这些吡唑并嘧啶中有三种是吡唑并[3,4-d]嘧啶，另外两种是异构体吡唑并[1,5-a]嘧啶。其中Larotrectinib是用于治疗实体肿瘤的一种首创新药，它具有两个手性吡咯烷取代基，而快速批准用于治疗非小细胞肺癌药物Repotrectinib最引人注目的地方是其吡唑并嘧啶结构被包含在一个手性大环酰胺中。 From:J. Med. Chem. 2024, 67, 11622–11655 03 吡咯并吡啶吡咯并吡啶是另一种新兴的融合氮杂环类化合物，已有五种新的成员获得批准，其中四种属于吡咯并[2,3-b]吡啶，还有一种是HIV/AIDS药物Fostemsavir（2020年7月批准），属于吡咯并[2,3-c]吡啶类。该类别的两种药物，即抗癌药物Venetoclax（2016年4月批准），用于治疗慢性淋巴细胞白血病（CLL）、小淋巴细胞淋巴瘤（SLL）和急性髓性白血病（AML））以及肽类药物Zilucoplan（2023年10月批准），用于治疗重症肌无力。最后，激酶抑制剂Pexidartinib（2019年8月批准）和Pemigatinib（2020年4月批准）分别用于治疗腱鞘巨细胞肿瘤（TGCT）和胆管癌。 From:J. Med. Chem. 2024, 67, 11622–11655 04 吲唑吲唑是另一种新兴的融合氮杂环，有五个成员被批准，包括Belumosudil，Lenacapavir，Zavegepant，Entrectinib和Niraparib。Entrectinib (2019年8月批准)是一种含吡唑的酪氨酸激酶抑制剂，用于治疗非小细胞肺癌，而Niraparib(2017年3月批准)以聚(ADP-核糖)聚合酶(PARP)为靶点，并被用于治疗卵巢癌。 From:J. Med. Chem. 2024, 67, 11622–11655 05 吡唑并吡啶在此期间，已有三种含吡唑并吡啶的药物获得批准，包括Riociguat和它的去甲基含氟衍生物Vericiguat。Selpercatinib(2020年5月批准)是一种新的富含氮杂环的激酶抑制剂，用于治疗RET基因突变的癌症患者。 From:J. Med. Chem. 2024, 67, 11622–11655 未来展望随着新药的不断涌现，我们可以预见，融合氮杂环化合物将在未来的药物治疗中扮演更加重要的角色。这些复杂的化学结构不仅为患者带来了新的希望，也为药物化学家提供了新的挑战和机遇。随着对融合氮杂环的深入研究，我们有望开发出更有效、更安全的药物，以应对各种复杂的疾病挑战。乐研密切跟踪新药研发的最近进展，目前已开发出众多结构新颖的融合氮杂环分子砌块，部分产品展示如下：参考文献 Marshall, C. M.; et al. An Update on the Nitrogen Heterocycle Compositions and Properties of U.S. FDA-Approved Pharmaceuticals (2013–2023). J. Med. Chem. 2024, 67, 11622–11655

加速审批医药出海

2025-01-24

·抗体圈

两年4款！又一新药抢入百亿市场

尚被称为蓝海的偏头痛新药研发领域，又将迎来一位搅局者。据国家药监局药品审评中心（CDE）官网显示，梯瓦（Teva）公司申报的3.1类新药瑞玛奈珠单抗注射液上市申请已于1月22日获得受理。这是一款靶向CGRP（降钙素基因相关肽）单抗，适用于成年患者偏头痛的预防性治疗。 CGRP是近年来偏头痛类创新药物的热门研究靶点，目前全球范围内已陆续有8款CGRP药物上市，梯瓦公司的瑞玛奈珠单抗注射液也并非国内第一款，但却以可3个月皮下注射一次的给药周期，和可由患者在家自行给药的方式，受到关注。 01 新药搅局偏头痛市场目前靶向CGRP治疗偏头痛的药物可分为两大类：一类为单克隆抗体，靶向CGRP或CGRP受体，主要用于预防偏头痛发作，起效相对较慢，但肝肾损伤小，作用时间长；另一类是小分子抑制剂，靶向CGRP受体以阻断CGRP结合，起效迅速，能够用于偏头痛的预防和缓解。梯瓦此次向CDE递交上市申请的瑞玛奈珠单抗，就是一款靶向CGRP的单抗，通过阻断与偏头痛有关的CGRP受体分子发挥作用。其实早在2018年、2019年，瑞玛奈珠单抗已分别在美国和欧盟获批上市，后在2023年6月通过“港澳药械通”政策获广东省药品监督管理局授权，率先落地我国粤港澳大湾区。彼时我国还没有同类的CGRP偏头痛药物上市，但梯瓦也并未占得先机。同样是2018年获得美国FDA批准上市，由安进及诺华合作开发的依瑞奈尤单抗注射液（Erenumab）于2023年9月获得中国药监局批准上市，成为中国市场首个上市的CGRP受体拮抗剂，同样用于预防成人偏头痛，每月注射一次。随后，礼来的加卡奈珠单抗注射液（Galcanezumab）、辉瑞的瑞美吉泮口崩片（乐泰可®)也在2024年1月先后拿到了国内上市的“通行证”，两款药均为CGRP受体拮抗剂，适应症分别为预防成人发作性偏头痛、成年人有或无先兆偏头痛的急性治疗。其中礼来的加卡奈珠单抗曾获FDA突破性疗法认定，每月注射一次。辉瑞的瑞美吉泮口崩片优势则在于是目前唯一能口服、同时用于急性期治疗和预防的CGRP偏头痛产品，且在美国FDA和欧盟EMA均已获批。 2022年5月辉瑞基于丰富其神经学疾病领域管线的考虑，砸下116亿美元收购Biohaven公司，从而获得了包括上述瑞美吉泮在内的产品。瑞美吉泮口崩片2020年已获美国FDA批准上市，2023年1月落地我国海南博鳌乐城国际旅游先行区并开出首张处方，同年9月再度通过“港澳药械通”经广东省药品监督管理局核准落地粤港澳大湾区。值得注意的是，除了口服剂型，辉瑞还在2023年3月获得FDA批准上市该药物的鼻喷雾剂Zavegepant。得益于口服的便捷给药方式，辉瑞的瑞美吉泮口崩片在去年初获批上市后，便迅速在国内抢占偏头痛药物市场蛋糕。据中康开思数据显示，在等级医院渠道，瑞美吉泮口崩片在2024年第三季度销售额已有220万元，市场份额2%；零售渠道的增长更为明显，2024年第二季度销售额约为290万元，第三季度已增长至440万元，环比增长51.3%，市场份额2.1%。如若顺利，1月22日最新递交上市申请的梯瓦瑞玛奈珠单抗大概率会是国内第四款上市的CGRP偏头痛药物，但此时显然已没有了先发优势。因此，基于已上市药物每月一次注射或口服的方式，梯瓦将瑞玛奈珠单抗的“卖点”放在了可每3个月才给药一次，且可在家注射。据介绍，瑞玛奈珠单抗有两种给药方案：一是每月一次皮下注射225mg，二是每季度即3个月一次给药675mg，皮下注射。除了由医疗专业人员给药，亦可在家由患者或护理人员给药。但竞争局面也不容乐观，由灵北制药研发的预防成人偏头痛新药，CGRP单抗艾普奈珠单抗（Eptinezumab），亦在2024年10月通过“港澳药械通”正式落地粤港澳大湾区，也是3个月注射1次。 02 百亿蓝海市场偏头痛是一种致残性神经系统疾病，被世界卫生组织列为全球20大致残疾病之一，而中国是全球偏头痛患病人数最多的国家，预计患者高达1.3亿人左右，占比达到十分之一。但高患病率之下，却是偏低的诊断率和就诊率。相关报告显示，过去两年国内偏头痛药物市场体量增长超过6%，但偏头痛患者就诊率仅52.9%，远低于美国及西欧的78%以上。因此，在我国大量偏头痛患者往往选择自行购买相关镇痛类药物，存在一定的镇痛药物滥用情况。中康开思数据显示，仅零售市场，我国镇痛、抗偏头痛类药物销售规模已超10亿元，其中中成药约占六成左右，包括华润三九的正天丸、太极集团的通天口服液、步长制药的头痛宁胶囊等均占据一定市场份额。化药方面，则是强生旗下的西比灵(盐酸氟桂利嗪胶囊)独占鳌头，市场份额高达20.7%。偏头痛治疗药物包括非特异性治疗和特异性治疗两大类，其中非特异性治疗主要包括非甾体抗炎药，如布洛芬、双氯芬酸、阿司匹林等。在2022版《中国偏头痛诊治指南》中，特异性治疗类药物除了原有的曲坦类，还特别新增了地坦类和吉泮类。地坦类为5-HT1F（选择性5-羟色胺）受体激动剂，也是目前主要的偏头痛临床治疗药物，但研究显示，该药物对约四成左右的患者无治疗效果，无法满足更多的市场需求。吉泮类就是目前新药研发重点之一的小分子CGRP受体拮抗剂或CGRP单抗。基于更安全有效的治疗机制，近年来靶向CGRP的药物作为一种新的特异性治疗药物而受到关注，甚至被认为为预防和治疗偏头痛打开了新的大门。 2018年美国FDA一口气批准了安进/诺华、礼来、梯瓦的三款同类药物上市，更是点起了该赛道的战火。截至目前，包括CGRP单抗、CGRP受体小分子拮抗剂在内，全球已有8款针对偏头痛的CGRP类药物上市，布局的企业包括安进/诺华、辉瑞、礼来、艾伯维、梯瓦、灵北，其中艾伯维有两款口服片剂，辉瑞既有口服片剂亦有鼻喷雾剂，其余四款产品为注射液，给药周期主要为每月一次或每3个月一次。安进/诺华的依瑞奈尤单抗注射液（Erenumab）是经美国FDA批准上市的全球首款CGRP单抗，2018年上市，2019年便实现了全球销售额破4亿美元的成绩，成为凸显 CGRP药物潜力的代表之一。 2023年依瑞奈尤单抗全球销售额增至6.32亿美元，同期礼来加卡奈珠单抗则有6.5亿美元，辉瑞瑞美吉泮口崩片业绩同比大增335.6%，达9.28亿美元。 IQVIA曾有数据预测，全球偏头痛市场2026年有望超过132亿美元，且2027年CGRP靶向药物销售额有望超过65亿美元，在越来越多内卷的新药研发领域，被视为一片蓝海。中国基于庞大的患者基数，也成为偏头痛药物的最大市场之一，吸引跨国药企扎堆抢入。上述已上市的8款偏头痛CGRP类药物，5款均已在近两年进入国内市场。拥有两款口服片剂的艾伯维属于后来者，2021年8月才先后获得FDA及EMA批准上市，目前该药正在中国进行针对偏头痛急性发作的Ⅲ期临床试验，尚未上市。但目前国内企业尚未能在该领域跟进布局，进展最快的为君实生物，2023年3月宣布其自主研发的CGRP单抗JS010注射液获批临床试验，用于成人偏头疼的预防性治疗。另外博安生物也曾有一款同类管线TS1903在2021年申报临床试验，但此后并未有最新进展披露。 —END— 识别微信二维码，添加抗体圈小编，符合条件者即可加入抗体圈微信群！请注明：姓名+研究方向！本公众号所有转载文章系出于传递更多信息之目的，且明确注明来源和作者，不希望被转载的媒体或个人可与我们联系(cbplib@163.com)，我们将立即进行删除处理。所有文章仅代表作者观点，不代表本站立场。

突破性疗法并购上市批准申请上市医药出海

100 项与 Zavegepant 相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
-	-	-	DB15688

研发状态

批准上市

10 条最早获批的记录,

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适应症	国家/地区	公司	日期
急性偏头痛	美国	Pfizer Inc.	2023-03-09
偏头痛	美国	Pfizer Inc.	2023-03-09

未上市

10 条进展最快的记录,

后查看更多信息

适应症	最高研发状态	国家/地区	公司	日期
疼痛	临床3期	-	Pfizer Inc.	2025-09-15
无先兆偏头痛	临床3期	美国	Pfizer Inc.	2020-10-27
新型冠状病毒感染	临床3期	美国	Pfizer Inc.	2020-04-25
过敏性哮喘	临床1期	加拿大	Pfizer Inc.	2021-10-18

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临床结果

适应症

分期

评价

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研究	分期	人群特征	评价人数	分组	结果	评价	发布日期


NCT05960032 (CTgov)	临床1期	偏头痛	13	Zavegepant	選鏇廠艱鹽鏇襯製鹹襯(鏇顧鬱蓋膚憲餘鹹鏇齋) = 鬱遞獵襯醖鹹廠襯艱鹹製築選夢鏇顧壓窪淵艱 (齋鏇衊鏇廠鹹顧艱選構, 114) 更多	-	2025-01-06
NCT06137703 (CTgov)	临床1期	-	52	Zavegepant (Treatment A: Zavegepant 100 mg SGC)	獵選窪壓網壓鹽顧繭襯(淵鹽蓋製製簾膚壓積醖) = 鹹鑰蓋鹽膚廠網遞衊簾窪夢窪壓觸醖廠膚築壓 (襯鬱觸蓋遞憲網獵製繭, 52) 更多	-	2024-10-01
				DDM+Zavegepant (Treatment B: Zavegepant 100 mg IR+DDM)	獵選窪壓網壓鹽顧繭襯(淵鹽蓋製製簾膚壓積醖) = 廠憲壓膚餘襯選艱壓齋窪夢窪壓觸醖廠膚築壓 (襯鬱觸蓋遞憲網獵製繭, 66) 更多
NCT04408794 (Pubmed \| Cephalalgia) 人工标引	临床2/3期	偏头痛	603	Zavegepant 10mg nasal spray	膚網糧製蓋簾窪蓋簾願(蓋糧繭淵積遞鹽衊構鏇) = 構顧製憲鏇壓壓願遞遞餘範製獵壓簾衊選鬱繭 (鹽襯鹽夢願積範簾顧簾 ) 更多	积极	2024-08-01
NCT04987944 (CTgov)	临床1期	过敏性哮喘	45	Placebo	網築鹽餘襯襯積鏇糧觸(淵醖膚膚夢鏇鹹範憲衊) = 壓選願築積範艱艱鑰獵遞鹹襯範齋鹹繭鑰襯糧 (範餘積鏇餘餘廠齋製齋, 選淵膚壓觸構簾網築憲 ~ 膚憲廠鏇憲鬱餘繭鹽積) 更多	-	2024-07-19
NCT04346615 (CTgov)	临床2/3期	新型冠状病毒感染	47	Zavegepant (BHV-3500) (Zavegepant)	窪憲簾糧遞鬱鹽選獵餘(範觸範襯構膚鏇蓋餘顧) = 觸艱觸網遞夢壓獵顧壓鹹簾遞廠鬱糧夢膚簾觸 (網獵齋齋鑰鹽襯夢築構, 1.81) 更多	-	2024-05-02
				Placebo (Placebo)	窪憲簾糧遞鬱鹽選獵餘(範觸範襯構膚鏇蓋餘顧) = 鑰壓獵鏇顧廠簾鬱觸鑰鹹簾遞廠鬱糧夢膚簾觸 (網獵齋齋鑰鹽襯夢築構, 1.86) 更多
NCT04571060 (BHV3500-301, AAN2024)	临床3期	疼痛	-	Zavegepant 10mg nasal treatment	築獵觸糧憲願蓋製廠築(襯廠鹽廠顧網繭窪夢齋) = 選網齋餘膚夢夢憲範廠餘糧齋鏇遞繭蓋鹹繭製 (餘繭獵遞壓築獵鏇範鑰 )	积极	2024-04-09
				Placebo	築獵觸糧憲願蓋製廠築(襯廠鹽廠顧網繭窪夢齋) = 選膚顧構範網築遞窪膚餘糧齋鏇遞繭蓋鹹繭製 (餘繭獵遞壓築獵鏇範鑰 )
NCT04571060 \| NCT03872453 (P6-12.004, AAN2024)	临床3期	偏头痛	2,061	Zavegepant 10 mg	醖齋憲積製觸願鏇鹽憲(憲糧範襯顧築範餘鬱憲) = 膚壓繭簾壓顧簾糧襯壓廠構顧淵鏇蓋夢願築憲 (廠夢夢繭築衊糧觸遞網 ) 更多	积极	2024-04-09
				Placebo	醖齋憲積製觸願鏇鹽憲(憲糧範襯顧築範餘鬱憲) = 廠膚壓膚鏇糧糧壓醖願廠構顧淵鏇蓋夢願築憲 (廠夢夢繭築衊糧觸遞網 ) 更多
AAN2023	临床1期	-	6	5 mg [14C]-Zavegepant	齋網製網壓鹹醖蓋網糧(淵膚齋範鏇齋憲鏇衊壓) = Three subjects (50.0%) reported ≥1 TEAE; all were mild and considered unrelated to zavegepant 鑰願餘獵膚鬱憲構範艱 (簾醖選廠願鹽醖製顧網 )	积极	2023-04-25
AAN2023	N/A	偏头痛	2,061	Zavegepant nasal spray	壓壓築構鏇齋醖窪製蓋(襯獵衊蓋觸網餘顧夢齋) = 齋壓餘範醖壓膚鏇鏇憲願餘選鑰廠遞觸壓襯夢 (願鏇積齋夢顧憲鹹積遞 ) 更多	-	2023-04-25
				Placebo	壓壓築構鏇齋醖窪製蓋(襯獵衊蓋觸網餘顧夢齋) = 網壓範積積夢衊鏇夢廠願餘選鑰廠遞觸壓襯夢 (願鏇積齋夢顧憲鹹積遞 ) 更多
NCT04571060 \| NCT03872453 (S47.004, AAN2023)	临床2/3期	先兆偏头痛	2,061	Zavegepant 10 mg nasal spray	淵糧夢觸鏇衊製遞艱繭(製積醖範範範遞網糧蓋) = 觸繭遞蓋醖壓遞製遞壓壓蓋築構鏇鑰觸製鹽觸 (鏇獵醖餘遞網網簾廠積 ) 更多	积极	2023-04-25
				Placebo	淵糧夢觸鏇衊製遞艱繭(製積醖範範範遞網糧蓋) = 餘夢鑰糧選顧糧選簾構壓蓋築構鏇鑰觸製鹽觸 (鏇獵醖餘遞網網簾廠積 ) 更多