Administer with food at approximately the same time each day. Swallow tablets whole (tablets should be intact prior to ingestion); do
not chew, crush, or split.
Unable to swallow tablets, may administer as an oral suspension (with food). Place tablets in a glass containing 60 to 120 mL of water
(use water only) and let stand ~5 minutes, then crush tablets with a spoon and stir until a suspension forms. Administer suspension
immediately after preparation (discard if not administered within 60 minutes). After administering the initial suspension, add another
30 to 45 mL of water to the same glass and stir to resuspend remaining particles and administer contents. Repeat if particles remain.
Accounting for missed doses
it can be taken with food within 9 hours after the time it is usually taken. After more than 9 hours, skip the dose for that day. The
next day, take alpelisib at the usual time.
If the patient vomits after taking the dose, advise the patient not to take an additional dose on that day, and to resume the dosing
schedule the next day at the usual time
Drug interactions
CYP3A4 inducer (eg, rifampin, carbamazepine, phenytoin)
Coadministration of alpelisib with a strong CYP3A4 inducer may decrease alpelisib concentration, which may decrease alpelisib
BCRP inhibitors (eg, cyclosporine A)
Coadministration of alpelisib with a BCRP inhibitor may increase alpelisib concentration, which may increase the risk of toxicities
If unable to use alternative drugs, when alpelisib is used in combination with BCRP inhibitors, closely monitor for increased
adverse reactions
CYP2C9 substrates (eg, S-warfarin, fluoxetine, losartan, phenytoin)
Coadministration of alpelisib with CYP2C9 substrates may reduce plasma concentration of these drugs
Closely monitor when alpelisib is used in combination with CYP2C9 substrates where decreases in the plasma concentration of
CYP2C9 substrates may reduce activity of these drugs