CIBINQO 9 Drug Interactions

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9.2 Drug Interactions Overview

When indicated dose is 100 mg or 200 mg CIBINQO dose should be reduced by half to 50 mg or 100 mg once daily respectively in patients receiving strong inhibitors of cytochrome P450 (CYP) 2C19 (e.g., fluconazole, fluvoxamine, fluoxetine) and in patients receiving one or more concomitant medicinal products that result in both moderate inhibition of CYP2C9 (e.g., amiodarone, fluconazole) as well as strong inhibition of CYP2C19. The use of CIBINQO is not recommended concomitantly with strong inducers of CYP enzymes (e.g., rifampin).

9.4 Drug-Drug Interactions

The drugs listed in table 5 are based on either drug interaction case reports or studies, or potential interactions due to the expected magnitude and seriousness of the interaction (i.e., those identified as contraindicated).

Potential for Other Drugs to Affect Pharmacokinetics of Abrocitinib:

Abrocitinib is metabolized predominantly by CYP2C19 and CYP2C9 enzymes, and its active metabolites are renally excreted and are substrates of the organic anion transporter 3 (OAT3). Therefore, exposures of abrocitinib and/or its active metabolites may be affected by medicinal products that strongly inhibit or induce CYP2C19 or CYP2C9 or inhibit the OAT3 transporter. Dose adjustments, as appropriate, based on these results are outlined below.

Table 5 - Established or Potential Drug-Drug Interactions
Legend: C = Case Study; CT = Clinical Trial; T = Theoretical
Proper/Common name Source of Evidence Effect Clinical comment




When CIBINQO 100 mg was administered concomitantly with fluvoxamine (a strong CYP2C19 and moderate CYP3A inhibitor) or fluconazole (a strong CYP2C19, moderate CYP2C9 and CYP3A inhibitor), the extent of exposure of abrocitinib active moiety increased by 91% and 155%, respectively, compared with administration alone.

Caution should be exercised when administering CIBINQO with dual strong CYP2C19/ and moderate CYP2C9 inhibitors, or strong CYP2C19 inhibitors alone.

Dosage reduction of CIBINQO is recommended

[see 4.2 Recommended Dose and Dosage Adjustment, 10 ACTION AND CLINICAL PHARMACOLOGY]



Administration of CIBINQO 200 mg after multiple dosing with rifampin, a strong inducer of CYP enzymes, resulted in reduction of abrocitinib active moiety exposures by approximately 56%.

Coadministration of CIBINQO with strong or moderate CYP2C19/CYP2C9 inducers is not recommended




When CIBINQO 200 mg was administered concomitantly with probenecid, an OAT3 inhibitor, abrocitinib active moiety exposures increased by approximately 66%.

This is not clinically significant, and a dose adjustment is not needed.

Potential for Abrocitinib to Affect Pharmacokinetics of Other Drugs:

In vitro, abrocitinib or its metabolites were not significant inhibitors or inducers of CYPs (CYP1A2, CYP2B6, CYP2C8, CYP2C9, CYP2C19, CYP2D6, and CYP3A4) or of uridine diphosphate-glucuronyltransferases (UGTs) (UGT1A1, UGT1A4, UGT1A6, UGT1A9, and UGT2B7). In vitro, abrocitinib is an inhibitor of P-glycoprotein (P-gp), organic anion transporter (OAT)3, organic cation transporter (OCT)1, multidrug and toxin compound extrusion protein (MATE)1/2K and breast cancer resistance protein (BCRP) but is not an inhibitor of organic anion transporting polypeptide (OATP)1B1/1B3, bile salt export pump (BSEP), OAT1 or OCT2 at clinically meaningful concentrations. The metabolites do not change the transporter inhibition risk compared to abrocitinib. 

No clinically significant effects of CIBINQO were observed in drug interaction studies with oral contraceptives (e.g., ethinyl estradiol/levonorgestrel), or with substrates of BCRP and OAT3 (e.g., rosuvastatin), MATE1/2K (e.g., metformin) and CYP3A4 (e.g., midazolam). 

Coadministration of dabigatran etexilate (a P-gp substrate), with a single dose of CIBINQO 200 mg increased dabigatran AUCinf and Cmax by approximately 53% and 40%, respectively, compared with administration alone.  

9.5 Drug-Food Interactions

CIBINQO was administered without regard to food.

9.6 Drug-Herb Interactions

Interactions with herbal products have not been evaluated.

9.7 Drug-Laboratory Test Interactions

Interactions with laboratory tests have not been evaluated.