Rimegepant

Products

Rimegepant was approved in the United States in 2020 in the form of meltable tablets that disintegrate in the oral cavity (Nurtec ODT). ODT stands for Orally Disintegrating Tablets.

Structure and properties

Rimegepant exists in the drug as rimegepant sulfate (hemisulfate and sesquihydrate), a white crystalline solid that is sparingly soluble in water.

Effects

Rimegepant is effective against the symptoms of migraine. The effects are due to antagonism at the CGRP receptor. The half-life is in the range of 11 hours. CGRP (Calcitonin Gene-Related Peptide) is a neuropeptide that plays an important role in triggering migraine attacks. It consists of 37 amino acids and is expressed in the peripheral and central nervous systems. Two isoforms exist, CGRP-α (Figure) and CGRP-β, which differ in three amino acids. Both are agonists at the CGRP receptor. CGRP has potent vasodilatory properties and plays a central role in pain initiation as well as neurogenic inflammation. Migraineurs have been found to have elevated levels of CGRP during an attack, and intravenous administration of the peptide can induce attacks in migraine patients.

Indications

For the acute treatment of migraine, with or without aura. Rimegepant is not approved for prevention.

Dosage

According to the prescribing information. The tablets are melted in the mouth once daily on or under the tongue. They may be taken without liquid.

Contraindications

  • Hypersensitivity

For complete precautions, see the drug label.

Interactions

Rimegepant is metabolized primarily by CYP3A4 and to a lesser extent by CYP2C9. It is a substrate of P-glycoprotein and BCRP. Corresponding interactions must be taken into account.

Adverse effects

Nausea occurs as the most common potential adverse effect.