Bacrelba Drug Interactions

Agents that may increase asciminib plasma concentrations: Strong CYP3A4 inhibitors: Physiologically based pharmacokinetic (PBPK) models predict that co-administration of Asciminib (Bacrelba) at 200 mg twice daily with a strong CYP3A4 inhibitor (clarithromycin) would increase asciminib AUC_tau and C_max by 77% and 49%, respectively. Caution should be exercised during concomitant administration of Asciminib (Bacrelba) 200 mg twice daily with strong CYP3A4 inhibitors including but not limited to clarithromycin, telithromycin, troleandomycin, itraconazole, ketoconazole, voriconazole, ritonavir, indinavir, nelfinavir or saquinavir. Dose adjustment of Asciminib (Bacrelba) is not required.
Agents that may decrease asciminib plasma concentrations: Strong CYP3A4 inducers: Co-administration of a strong CYP3A4 inducer (rifampicin) decreased asciminib AUC_inf by 14.9%, while increasing asciminib C_max by 9% in healthy subjects receiving a single Asciminib (Bacrelba) dose of 40 mg.
PBPK models predict that co-administration of asciminib at 80 mg once daily with rifampicin would decrease asciminib AUC_tau and C_max by 52% and 23%, respectively, while co-administration of asciminib at 200 mg twice daily with rifampicin would decrease asciminib AUC_tau and C_max by 63% and 47%, respectively.
Caution should be exercised during concomitant administration of Asciminib (Bacrelba) at all recommended doses with strong CYP3A4 inducers, including but not limited to carbamazepine, phenobarbital, phenytoin, or St. John's wort (Hypericum perforatum). Dose adjustment of Asciminib (Bacrelba) is not required.
Agents that may have their plasma concentrations altered by asciminib: CYP3A4 substrates with narrow therapeutic index: Co-administration of asciminib with a CYP3A4 substrate (midazolam) increased midazolam AUC_inf and C_max by 28% and 11%, respectively, in healthy subjects receiving Asciminib (Bacrelba) 40 mg twice daily.
PBPK models predict that co-administration of asciminib at 80 mg once daily would increase midazolam AUC_inf and C_max by 24% and 17%, respectively, while co-administration of asciminib at 200 mg twice daily would increase midazolam AUC_inf and C_max by 88% and 58%, respectively.
Caution should be exercised during concomitant administration of Asciminib (Bacrelba) at all recommended doses with CYP3A4 substrates known to have a narrow therapeutic index, including, but not limited to, the CYP3A4 substrates fentanyl, alfentanil, dihydroergotamine, or ergotamine (see Pharmacology under Actions). Dose adjustment of Asciminib (Bacrelba) is not required.
CYP2C9 substrates: Co-administration of asciminib with a CYP2C9 substrate (warfarin) increased S-warfarin AUC_inf and C_max by 41% and 8%, respectively, in healthy subjects receiving Asciminib (Bacrelba) 40 mg twice daily.
PBPK models predict that co-administration of asciminib at 80 mg once daily would increase S-warfarin AUC_inf and C_max by 52% and 4%, respectively, while co-administration of asciminib at 200 mg twice-daily would increase S-warfarin AUC_inf and C_max by 314% and 7%, respectively.
Caution should be exercised during concomitant administration of Asciminib (Bacrelba) at 80 mg total daily with CYP2C9 substrates known to have a narrow therapeutic index, including, but not limited to, phenytoin or warfarin (see Pharmacology under Actions). Dose adjustment of Asciminib (Bacrelba) is not required.
Concomitant administration of Asciminib (Bacrelba) at 200 mg twice daily with CYP2C9 sensitive substrates and CYP2C9 substrates known to have a narrow therapeutic index should be avoided and alternative medications should be considered (see Pharmacology under Actions). If co-administration cannot be avoided, the CYP2C9 substrates dose should be reduced. If co-administration with warfarin cannot be avoided, the frequency of international normalized ratio (INR) monitoring should be increased as the anti-coagulant effect of warfarin may be enhanced.
Substrates of OATP1B, of BCRP or of both transporters: PBPK models predict that co-administration of asciminib at 40 mg twice daily and 80 mg once daily with an OATP1B substrate (pravastatin) would increase pravastatin C_max by 43% and 63% and AUC_inf by 37% and 51%, respectively, while co-administration of asciminib at 200 mg twice daily would increase pravastatin C_max and AUC_inf by 141% and 137%, respectively.
PBPK models predict that co-administration of asciminib at 40 mg twice daily and 80 mg once daily with an OATP1B, CYP3A4 and P-gp substrate (atorvastatin) would increase atorvastatin C_max by 97% and 143% and AUC_inf by 81% and 122%, respectively, while co-administration of asciminib at 200 mg twice daily would increase atorvastatin C_max and AUC_inf by 300% and 326%, respectively.
PBPK models predict that co-administration of asciminib at 40 mg twice daily and 80 mg once daily with a BCRP substrate (sulfasalazine) would increase sulfasalazine C_max by 334% and 342% and AUC_inf by 333% and 340%, respectively, while co-administration of asciminib at 200 mg twice daily would increase sulfasalazine C_max and AUC_inf by 353% and 359%, respectively.
PBPK models predict that co-administration of asciminib at 40 mg twice daily and 80 mg once daily with a BCRP and OATP1B substrate (rosuvastatin) would increase rosuvastatin C_max by 453% and 530% and AUC_inf by 190% and 202%, respectively, while co-administration of asciminib at 200 mg twice daily would increase rosuvastatin C_max and AUC_inf by 732% and by 311%, respectively.
Caution should be exercised during concomitant administration of Asciminib (Bacrelba) at all recommended doses with substrates of OATP1B, of BCRP or of both transporters, including, but not limited to sulfasalazine, methotrexate, pravastatin, atorvastatin, pitavastatin, rosuvastatin and simvastatin. Refer to OATP1B and BCRP substrates' dose reductions, as recommended in their prescribing information.
Concomitant administration of Asciminib (Bacrelba) at all recommended doses with rosuvastatin should be avoided and alternative statins should be considered. If co-administration cannot be avoided, rosuvastatin dose should be reduced, as recommended in its prescribing information (see Pharmacology under Actions).
P-gp substrates of narrow therapeutic index: PBPK models predict that co-administration of asciminib at 40 mg twice daily and 80 mg once daily with a P-gp substrate (digoxin) would increase digoxin C_max by 30% and 38% and AUC_inf by 20% and 22%, respectively, while co-administration of asciminib at 200 mg twice daily would increase digoxin C_max and AUC_inf by 62% and 40%, respectively.
Caution should be exercised during concomitant administration of Asciminib (Bacrelba) at all recommended doses with P-gp substrates known to have a narrow therapeutic index, including but not limited to digoxin, dabigatran, and colchicine.
QT prolonging agents: Caution should be exercised during concomitant administration of Asciminib (Bacrelba) at 80 mg total daily dose and medicinal products with a known risk of torsades de pointes, including, but not limited to, bepridil, chloroquine, clarithromycin, halofantrine, haloperidol, methadone, moxifloxacin or pimozide (see Pharmacology under Actions).
Concomitant administration of Asciminib (Bacrelba) at 200 mg twice-daily dose and medicinal products with a known risk of torsades de pointes should be avoided (see Pharmacology under Actions).
Drug-food interactions: The bioavailability of asciminib decreases on consumption of food (see Dosage & Administration and Pharmacology under Actions).