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Bicalutamide

Androgen Receptor InhibitorAndrogen Receptor Antagonists

Route: Oral

7 interactions on record

Bicalutamide has 7 known drug interactions based on U.S. FDA drug labeling data. 2 are classified as major interactions requiring close medical supervision. Notable interactions include combinations with Oral Anticoagulants, Warfarin Sodium, Midazolam. Patients taking Bicalutamide should inform their healthcare provider of all current medications — including over-the-counter drugs and supplements — to avoid potentially harmful combinations. Data sourced from OpenFDA and the NIH National Library of Medicine.

Total: 7
Major: 2
Moderate: 1
Minor: 2

Major (2)

Bicalutamide + Oral Anticoagulants— Bicalutamide can displace coumarin anticoagulants from protein binding sites. PT/INR should be closely monitored and ant…
Bicalutamide + Warfarin Sodium— CYP3A4 inhibitor that increases warfarin effect and INR; requires close monitoring.

Moderate (1)

Bicalutamide + Midazolam— Bicalutamide co-administration increases midazolam levels 1.5-fold (Cmax) and 1.9-fold (AUC). Caution should be exercise…

Minor (2)

Bicalutamide + Goserelin— Clinical studies have shown no drug interactions between bicalutamide and goserelin.
Bicalutamide + Leuprolide— Clinical studies have shown no drug interactions between bicalutamide and leuprolide.

Bicalutamide + Oral Anticoagulants⚠️Major

Bicalutamide can displace coumarin anticoagulants from protein binding sites. PT/INR should be closely monitored and anticoagulant dose adjustment may be necessary.

Bicalutamide + Warfarin Sodium⚠️Major

CYP3A4 inhibitor that increases warfarin effect and INR; requires close monitoring.

Bicalutamide + Midazolam🟡Moderate

Bicalutamide co-administration increases midazolam levels 1.5-fold (Cmax) and 1.9-fold (AUC). Caution should be exercised when co-administered.

Bicalutamide + Goserelin🟢Minor

Clinical studies have shown no drug interactions between bicalutamide and goserelin.

Bicalutamide + Leuprolide🟢Minor

Clinical studies have shown no drug interactions between bicalutamide and leuprolide.

Bicalutamide + Lomitapide Mesylateℹ️Unknown

7.2 Weak CYP3A4 Inhibitors Weak CYP3A4 inhibitors (such as alprazolam, amiodarone, amlodipine, atorvastatin, bicalutamide, cilostazol, cimetidine, cyclosporine, fluoxetine, fluvoxamine, ginkgo, goldenseal, isoniazid, lapatinib, nilotinib, pazopanib, ranitidine, ranolazine, ticagrelor, zileuton) can increase lomitapide exposure approximately 2-fold [see Clinical Pharmacology (12.3) ] .

Bicalutamide + Warfarinℹ️Unknown

Table 2: Examples of CYP450 Interactions with Warfarin Enzyme Inhibitors Inducers CYP2C9 amiodarone, capecitabine, cotrimoxazole, etravirine, fluconazole, fluvastatin, fluvoxamine, metronidazole, miconazole, oxandrolone, sulfinpyrazone, tigecycline, voriconazole, zafirlukast aprepitant, bosentan, carbamazepine, phenobarbital, rifampin CYP1A2 acyclovir, allopurinol, caffeine, cimetidine, ciprofloxacin, disulfiram, enoxacin, famotidine, fluvoxamine, methoxsalen, mexiletine, norfloxacin, oral contraceptives, phenylpropanolamine, propafenone, propranolol, terbinafine, thiabendazole, ticlopidine, verapamil, zileuton montelukast, moricizine, omeprazole, phenobarbital, phenytoin, cigarette smoking CYP3A4 alprazolam, amiodarone, amlodipine, amprenavir, aprepitant, atorvastatin, atazanavir, bicalutamide, cilostazol, cimetidine, ciprofloxacin, clarithromycin, conivaptan, cyclosporine, darunavir/ritonavir, diltiazem, erythromycin, fluconazole, fluoxetine, fluvoxamine, fosamprenavir, imatinib, indinavir, isoniazid, itraconazole, ketoconazole, lopinavir/ritonavir, nefazodone, nelfinavir, nilotinib, oral contraceptives, posaconazole, ranitidine, ranolazine, ritonavir, saquinavir, telithromycin, tipranavir, voriconazole, zileuton armodafinil, amprenavir, aprepitant, bosentan, carbamazepine, efavirenz, etravirine, modafinil, nafcillin, phenytoin, pioglitazone, prednisone, rifampin, rufinamide 7.3 Drugs that Increase Bleeding Risk Examples of drugs known to increase the risk of bleeding are presented in Table 3.

Data sourced from U.S. FDA drug labeling via openFDA and the NIH National Library of Medicine. For informational purposes only. Always consult your pharmacist or physician.