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. 2022 Aug 24;25(6):795–809. doi: 10.1007/s11102-022-01268-2

Table 2.

Concomitant medications with potential to interact with osilodrostat [2]

Interaction with	Medication		Rationale
CYP3A4 substrates	Atorvastatin^a Aprepitant^a Buspirone^a Conivaptan^a Cyclosporine Eletriptan^a Eplerenone^a Ergot alkaloids Erythromycin Fentanyl Glucocorticoids Ibrutinib^a Midazolam^a Nifedipine Omeprazole	Ondansetron Propranolol Quetiapine^a Quinidine Ritonavir Sildenafil^a Sirolimus^a Testosterone Ticagrelor^a Verapamil Vincristine Voriconazole Warfarin Zolpidem	Osilodrostat is a weak CYP3A4 inhibitor and may increase plasma concentrations of CYP3A4 substrates
CYP3A4 inhibitors	Amiodarone Aprepitant Atomoxetine Cimetidine Clarithromycin^b Conivaptan Diltiazem Erythromycin Grapefruit juice^b	Itraconazole^b Ketoconazole^b Metyrapone Nefazodone^b Omeprazole Ritonavir^b Verapamil Voriconazole^b	Osilodrostat dose should be increased when discontinuing a strong CYP3A4 inhibitor
CYP3A4 inhibitors			Osilodrostat dose should decrease by 50% when co-administering with a strong CYP3A4 inhibitor
CYP3A4 inducers	Carbamazepine^c Dexamethasone^c Enzalutamide Mitotane^c Nevirapine Oxcarbazepine	Phenobarbital^c Phenytoin^c Pioglitazone^c Rifampin^c St. John’s wort	Osilodrostat dose may need to be increased when co-administered with a strong CYP3A4 inducer
CYP3A4 inducers			Osilodrostat dose may need to be decreased when discontinuing a strong CYP3A4 inducer
CYP2B6 inducers	Carbamazepine^c Insulin Modafinil Nafcillin	Omeprazole Rifampin Tobacco	Osilodrostat dose may need to be increased when co-administered with a strong CYP2B6 inducer
CYP2B6 inducers	Carbamazepine^c Insulin Modafinil Nafcillin	Omeprazole Rifampin Tobacco	Osilodrostat dose may need to be decreased when discontinuing a strong CYP2B6 inducer
CYP1A2 and CYP2C19 substrates	CYP1A2 Acetaminophen Amitriptyline Caffeine^a Clozapine Duloxetine^a Estradiol Haloperidol Imipramine Melatonin^a Naproxen Ondansetron Propranolol Ramelteon^a Theophylline Tizanidine^a Verapamil Warfarin Zolmitriptan	CYP2C19 Amitriptyline Citalopram Clobazam Clopidogrel Diazepam Indomethacin Labetalol Omeprazole^a Phenytoin^a Progesterone Propranolol Warfarin	Osilodrostat may increase plasma concentrations of drugs metabolized by CYP1A2 and CYP2C19
CYP2D6 and CYP2E1 substrates	CYP2D6 Amitriptyline Atomoxetine^a Carvedilol Chlorpromazine Citalopram Dextromethorphan^a Donepezil Haloperidol Imipramine Lidocaine Metoclopramide Oxycodone Propafenone Propranolol Tolterodine^a Venlafaxine^a	CYP2E1 Acetaminophen Ethanol Halothane Isoflurane Theophylline	Osilodrostat may increase plasma concentrations of drugs metabolized by CYP2D6 and CYP2E1

^aSensitive substrate

^bStrong inhibitor

^cStrong inducer