Tasimelteon: Important Drug Interactions

Tasimelteon: Important Drug Interactions

Q.2. Tasimelteon is a melatonin receptor agonist indicated for the treatment of Non-24-Hour Sleep-Wake Disorder.
Addition of which of the following medication can result in potentially large decrease in Tasimelteon exposure with reduced efficacy?
(a) Cimetidine
(b) Suboxone
(c) Modafinil
(d) Clarithromycin

Answer: (c) Modafinil


Avoid use of Tasimelteon in combination with CYP3A4 inducers because of a potentially large decrease in tasimelteon exposure with reduced efficacy:

  • Modafinil is CYP3A4 inducers
  • Cimetidine, Suboxone and Clarithromycin are CYP3A4 inhibitors. 


Second important CYP450 enzyme is 1A2:

Avoid use of Tasimelteon in combination with strong CYP1A2 inhibitors because of a potentially large increase in tasimelteon exposure and greater risk of adverse reactions: ex: Fluvoxamine.

Source: Tasimelteon package insert. 

Please do post your questions or comments below. 

Dr. Harvinder Singh, M.D. (Admin)

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