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Drug interactions of Alpelisib

1.Effect of Other Drugs on Alpelisib 

CYP3A4 Inducer

Coadministration of Alpelisib with a strong CYP3A4 inducer decreases alpelisib concentration, which may reduce alpelisib efficacy. Avoid concomitant use of strong CYP3A4 inducers and consider an alternative concomitant drug with no or minimal potential to induce CYP3A4. 

Breast Cancer Resistance Protein Inhibitors

Coadministration of Alpelisib with a breast cancer resistance protein (BCRP) inhibitor may increase alpelisib concentration, which may increase the risk of toxicities. Avoid the use of BCRP inhibitors in patients treated with Alpelisib. If unable to use alternative drugs, when Alpelisib is used in combination with BCRP inhibitors, closely monitor for increased adverse reactions. 

2.Effect of Alpelisib on Other Drugs

CYP2C9 Substrates

Coadministration of Alpelisib with CYP2C9 substrates (e.g., warfarin) 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.

from FDA,2022.11

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