Lasmiditan

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REYVOW™ (lasmiditan): Metabolism and Elimination

Reyvow (lasmiditan) undergoes hepatic and extrahepatic metabolism primarily by non-cytochrome P450 enzymes. Recovery of unchanged lasmiditan in urine was low and accounted for approximately 3% of the dose.

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, Lilly

References

1. Reyvow [package insert]. Indianapolis, IN: Eli Lilly and Company; 2019.

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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