Eli Lilly's First-in-Class Serotonin 1F Receptor Agonist Reyvow (Lasmiditan) Receives FDA Approval for Acute Migraine Treatment

On October 14, 2019, VCBeat (WeChat ID: vcbeat) learned from foreign media reports that U.S. pharmaceutical giant Eli Lilly announced that its acute migraine treatment drug, Reyvow (lasmiditan) tablets, had received FDA approval for market launch.

Migraine is a common chronic neurovascular disorder that predominantly affects young and middle-aged individuals, often with a genetic predisposition. It is the most prevalent type of primary headache in clinical practice, characterized primarily by episodic, moderate-to-severe, pulsating, and unilateral head pain, which may be accompanied by nausea and vomiting. The pain typically lasts from 4 to 72 hours and can be exacerbated by light or sound stimuli or by routine physical activity.

According to the National Headache Foundation (NHF), 39 million people in the United States are affected by migraines, and there are over 1 billion migraine sufferers worldwide. For decades, the primary medications for acute migraine treatment have been triptans, which work by constricting blood vessels. Their side effects include tightness in the neck and chest as well as increased heart rate; therefore, they are not suitable for patients with heart disease or hypertension.

Reyvow is currently the only FDA-approved serotonin 1F (5-HT1F) receptor agonist available on the market for the treatment of acute migraine with or without aura. Unlike triptans, Reyvow works by targeting and activating 5-HT1F receptors, thereby blocking the migraine pathway through interaction with calcitonin gene-related peptide (CGRP). Eli Lilly stated that CGRP receptors have not been found on human blood vessels; therefore, Reyvow does not cause vasoconstriction and is suitable for patients with hypertension and heart disease.

Reyvow was initially discovered in Eli Lilly’s laboratories and licensed to CoLucid Pharmaceuticals (CoLucid), a biotechnology company based in North Carolina. In 2015, the company relocated to Massachusetts and completed its initial public offering (IPO) to fund late-stage clinical trials of its migraine medication. In 2017, Eli Lilly acquired CoLucid for up to $960 million and completed the Phase III clinical studies of Reyvow.

Reyvow should be taken after the onset of a migraine attack. Two Phase III clinical trials demonstrated that the drug takes effect within two hours of administration and provides significantly superior pain relief compared to placebo. Common side effects of Reyvow include dizziness, fatigue, somnolence, and paresthesia or burning sensations on the skin. Patients are prohibited from driving or operating heavy machinery at heights for 8 hours after taking the medication.

Eli Lilly and Company, founded in 1876 and headquartered in Indiana, USA, is a global pharmaceutical research and development company. The company is primarily engaged in the research and development, manufacturing, and sales of new drugs, providing innovative healthcare solutions for people worldwide. Eli Lilly operates production facilities in 25 countries and regions, including the United States, China, and Puerto Rico, with its products sold in 135 countries globally.

In addition to Reyvow, Eli Lilly has also developed Emgality for the prevention of migraine attacks. Meanwhile, CGRP inhibitors from Amgen in the United States and Teva Pharmaceutical in Israel have also received FDA approval for preventing migraines by blocking CGRP. Clinical trials have shown that although these antibody drugs cannot cure migraines, they can significantly reduce the frequency of migraine episodes.

Prior to the official commercial launch of Reyvow, the U.S. Drug Enforcement Administration (DEA) will assign a controlled substance schedule to the drug. Due to Reyvow’s effects on the central nervous system, Eli Lilly conducted further studies to assess its potential for abuse. Compared with alprazolam, an anxiolytic associated with addiction risk, Reyvow demonstrated a lower risk of abuse.

(Compiled by Xu Xiaoxue)