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Reyvow ® (lasmiditan) tablets CV
50 mg, 100 mgThis information is provided in response to your request. Resources may contain information about doses, uses, formulations and populations different from product labeling. See Prescribing Information above, if applicable.
Additional Information Regarding Metabolism and Elimination
Metabolism
Lasmiditan undergoes hepatic and extrahepatic metabolism primarily by non-CYP enzymes.1
Lasmiditan is primarily eliminated via metabolism. Major metabolites of lasmiditan identified in plasma and urine are
S-M8, through ketone reduction to the alcohol (major pathway),
M7, through oxidation on piperidine ring, and
M18, through a combination of M7 and M8 pathways.1
Relative to lasmiditan, these metabolites exhibited considerably lower affinity (~1000-fold lower Ki) for the target 5-HT1F receptor and are considered pharmacologically inactive.1
The following enzymes are not involved in metabolism of lasmiditan, including
MAO-A
MAO-B
flavin monooxygenase 3
CYP450 reductase
xanthine oxidase
alcohol dehydrogenase
aldehyde dehydrogenase, and
aldo-keto reductases.1
Excretion
Renal excretion is a minor route of lasmiditan clearance with approximately 3% of the dose recovered as unchanged lasmiditan in urine. Metabolite S-M8 represented approximately 66% of the dose in urine, with the majority of recovery within 48 hours post-dose.1
Enclosed Prescribing Information
REYVOW® (lasmiditan) tablets, for oral use, CV, Lilly
1. Reyvow [package insert]. Indianapolis, IN: Eli Lilly and Company; 2020.
Glossary
5-HT1F = serotonin-1F
CYP = cytochrome P450
Ki = inhibition constant
MAO = monoamine oxidase
Date of Last Review: November 08, 2018
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