Dr. Stahelin Influenza

Question 1

Baloxavir

Answer 1

• MOA: inhibits viral “cap-snatching” (blocks transcription)
• influenza steals the mRNA cap from host cell mRNA and uses it to make its own mRNAs. Baloxavir binds to the PB2 subunit of the RNA polymerase of the virus and inhibits the influenza cap-dependent endonuclease and viral mRNAs can no longer be produced

Question 2

Oseltamivir

Answer 2

• prodrug converted to active form by liver esterases
• metabolite is an effective inhibitor of neuraminidase. Extensively converted by hepatic esterases to oseltamivir carboxylate.
• active against influenza A and B (less effective against B)
• resistance is associated with mutations in the active site of neuraminidase.

Question 3

Zanamavir

Answer 3

• transition state analog
• MOA: neuraminidase inhibitor
• effective agaisnt influenza A and B

Question 4

Peramivir

Answer 4

• transition state analog of sialic acid
• active against influenza A and B
• MOA: NA inhibitor
• first IV administration