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Pacritinib is primarily metabolized by CYP3A4. Concomitant use of pacritinib with strong or moderate CYP3A4 inhibitors increases pacritinib exposure, which may elevate the risk of exposure-related adverse reactions.
Concomitant use of pacritinib with strong CYP3A4 inhibitors is prohibited.
Monitor patients receiving concomitant treatment with moderate CYP3A4 inhibitors (e.g., fluconazole) for increased adverse reactions, and adjust the dose of pacritinib based on safety considerations. The concomitant use of pacritinib with fluconazole at a daily dose exceeding 200 mg has not been studied.
Pacritinib is primarily metabolized by CYP3A4. Concomitant use of pacritinib with strong CYP3A4 inducers reduces pacritinib exposure, which may diminish the therapeutic efficacy of pacritinib.
Concomitant use of pacritinib with strong CYP3A4 inducers is prohibited.
Pacritinib is an inhibitor of CYP1A2. Pacritinib increases the plasma concentrations of CYP1A2 substrates, which may raise the risk of adverse reactions associated with these substrates.
When pacritinib is used concomitantly with CYP1A2 substrates, monitor for adverse reactions related to the CYP1A2 substrates more frequently unless otherwise recommended in the prescribing information of the substrate. This monitoring is particularly critical when small changes in substrate concentrations may lead to severe adverse reactions.
Pacritinib is an inducer of CYP2C19. Pacritinib decreases the plasma concentrations of CYP2C19 substrates, which may reduce the therapeutic efficacy of these substrates.
When pacritinib is used concomitantly with CYP2C19 substrates, monitor the therapeutic efficacy of the CYP2C19 substrates more frequently unless otherwise recommended in the prescribing information of the substrate. This monitoring is particularly important when small changes in substrate concentrations may result in diminished efficacy. Dose adjustment of the CYP2C19 substrate may be required.
Pacritinib is an inducer of CYP3A4. Pacritinib decreases the plasma concentrations of CYP3A4 substrates, which may impair the therapeutic efficacy of these substrates.
When pacritinib is used concomitantly with CYP3A4 substrates, monitor the therapeutic efficacy of the CYP3A4 substrates more frequently unless otherwise recommended in the prescribing information of the substrate. This monitoring is particularly necessary when small changes in substrate concentrations may lead to reduced efficacy. Dose adjustment of the CYP3A4 substrate may be required.
Avoid concomitant use of pacritinib with hormonal contraceptives except for levonorgestrel-containing intrauterine systems. The effectiveness of hormonal contraceptives (other than levonorgestrel-containing intrauterine systems) may be reduced when co-administered with pacritinib.
If contraception is needed or desired, use an alternative contraceptive method unaffected by CYP3A4 inducers (e.g., intrauterine systems) or an additional non-hormonal contraceptive method (e.g., condoms) during concurrent treatment with pacritinib and for 30 days after the last dose of pacritinib.
Pacritinib is an inhibitor of P-glycoprotein (P-gp). Pacritinib increases the plasma concentrations of P-gp substrates, which may increase the risk of adverse reactions associated with these substrates.
When pacritinib is used concomitantly with P-gp substrates, monitor for adverse reactions related to the P-gp substrates more frequently unless otherwise recommended in the prescribing information of the substrate. This monitoring is particularly crucial when small changes in substrate concentrations may cause severe adverse reactions.
Digoxin: Measure serum digoxin concentrations before initiating concomitant use with pacritinib, and continue monitoring serum digoxin concentrations as recommended in the prescribing information of digoxin.
Pacritinib is an inhibitor of breast cancer resistance protein (BCRP). Pacritinib increases the plasma concentrations of BCRP substrates, which may elevate the risk of adverse reactions associated with these substrates.
When used concomitantly with pacritinib, monitor for adverse reactions related to the BCRP substrates more frequently, and consider reducing the dose of the BCRP substrate in accordance with its prescribing information.
Rosuvastatin: When co-administered with pacritinib, the dose of rosuvastatin should not exceed 20 mg once daily.
FDA，2025.10
