Reyvow ® (lasmiditan) tablets CV

50 mg, 100 mg

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How is Reyvow® (lasmiditan) metabolized and eliminated?

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.

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Pharmacokinetic Properties

Metabolism

Lasmiditan undergoes hepatic and extrahepatic metabolism primarily by non-cytochrome P450 enzymes.1

The following enzymes are not involved in metabolism of lasmiditan, including

  • monoamine oxidase-A
  • monoamine oxidase-B
  • flavin monooxygenase 3
  • cytochrome P450 reductase
  • xanthine oxidase
  • alcohol dehydrogenase
  • aldehyde dehydrogenase, and
  • aldo-keto reductases.1

Major metabolites of lasmiditan identified in plasma and urine are

  • S-M8, through ketone reduction to 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 are considered pharmacologically inactive.1

Excretion

Lasmiditan is primarily eliminated via metabolism.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

Reference

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

Date of Last Review: August 12, 2021


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