Reyvow ® (lasmiditan) tablets CV

50 mg, 100 mg

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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


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


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


1Reyvow [package insert]. Indianapolis, IN: Eli Lilly and Company; 2021.


5-HT1F = serotonin-1F 

CYP = cytochrome P450

Ki = inhibition constant

MAO = monoamine oxidase

Date of Last Review: November 08, 2018

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