MedPath

Rimegepant

Generic Name
Rimegepant
Brand Names
Nurtec, Vydura
Drug Type
Small Molecule
Chemical Formula
C28H28F2N6O3
CAS Number
1289023-67-1
Unique Ingredient Identifier
997WVV895X

Overview

Rimegepant is an oral antagonist of the CGRP receptor developed by Biohaven Pharmaceuticals. It received FDA approval on February 27, 2020 for the acute treatment migraine headache, and was subsequently approved by the European Commission in April 2022 for both the treatment and prevention of migraines. While several parenteral antagonists of CGRP and its receptor have been approved for migraine therapy (e.g. erenumab, fremanezumab, galcanezumab), rimegepant and ubrogepant were the only CGRP antagonists that possessed oral bioavailability until the approval of atogepant in 2021. The current standard of migraine therapy involves abortive treatment with "triptans", such as sumatriptan, but these medications are contraindicated in patients with pre-existing cerebrovascular and cardiovascular disease due to their vasoconstrictive properties. Antagonism of the CGRP pathway has become an attractive target for migraine therapy as, unlike the triptans, oral CGRP antagonists have no observed vasoconstrictive properties and are therefore safer for use in patients with contraindications to standard therapy.

Background

Rimegepant is an oral antagonist of the CGRP receptor developed by Biohaven Pharmaceuticals. It received FDA approval on February 27, 2020 for the acute treatment migraine headache, and was subsequently approved by the European Commission in April 2022 for both the treatment and prevention of migraines. While several parenteral antagonists of CGRP and its receptor have been approved for migraine therapy (e.g. erenumab, fremanezumab, galcanezumab), rimegepant and ubrogepant were the only CGRP antagonists that possessed oral bioavailability until the approval of atogepant in 2021. The current standard of migraine therapy involves abortive treatment with "triptans", such as sumatriptan, but these medications are contraindicated in patients with pre-existing cerebrovascular and cardiovascular disease due to their vasoconstrictive properties. Antagonism of the CGRP pathway has become an attractive target for migraine therapy as, unlike the triptans, oral CGRP antagonists have no observed vasoconstrictive properties and are therefore safer for use in patients with contraindications to standard therapy.

Indication

Rimegepant is indicated for the acute treatment of migraine with or without aura in adults. Rimegepant is also indicated for the prevention of episodic migraine in adults.

Associated Conditions

  • Episodic Migraine
  • Migraine With Aura
  • Migraine Without Aura

Clinical Trials

Phase 2
Not yet recruiting
Posted: 2025/05/28
Sponsor:
Second Affiliated Ho...
Phase 4
Not yet recruiting
Posted: 2025/05/22
Phase 2
Not yet recruiting
Posted: 2024/12/27
Sponsor:
Second Affiliated Ho...
Not yet recruiting
Posted: 2024/12/11
Sponsor:
The First Affiliated...

FDA Approved Products

NURTEC ODT
Manufacturer:Pfizer Laboratories Div Pfizer Inc
Route:ORAL
Strength:75 mg in 1 1
Approved: 2023/04/20
NDC:72618-3001
NURTEC ODT
Manufacturer:Pfizer Laboratories Div Pfizer Inc
Route:ORAL
Strength:75 mg in 1 1
Approved: 2023/04/20
NDC:72618-3000

Singapore Approved Products

NURTEC ORALLY DISINTEGRATING TABLET 75MG
Manufacturer:Catalent UK Swindon Zydis Limited
Form:TABLET, ORALLY DISINTEGRATING
Strength:75mg
Online:Yes
Approved: 2023/02/21
Approval:SIN16702P

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