Basic Information
ID DDInter1622 and DDInter107
Interaction Coadministration with apalutamide may decrease the plasma concentrations and therapeutic effects of drugs that are substrates of CYP450 3A4, 2C9, 2C19, breast cancer resistance protein (BCRP), uridine diphosphate glucuronosyltransferase (UGT), organic anion transporting polypeptide 1B1 (OATP1B1), and/or P-glycoprotein (P-gp) efflux transporter. The proposed mechanism involves accelerated clearance via these routes due to apalutamide-mediated induction. The resulting plasma concentrations will depend on the sensitivity of the affected drugs to these isoenzymes.
Management Caution is advised when apalutamide is used concomitantly with drugs that are substrates of CYP450 3A4, 2C9, 2C19, BCRP, UGT, OATP1B1, and/or P-gp, particularly those with a narrow therapeutic range. Dosage adjustments as well as clinical and laboratory monitoring may be appropriate for some drugs whenever apalutamide is added to or withdrawn from therapy.
References [1] "Product Information. Erleada (apalutamide)." Janssen Biotech, Inc., Horsham, PA, PA. [2] Cerner Multum, Inc. "UK Summary of Product Characteristics." O 0 [3] Yoovathaworn KC, Sriwatanakul K, Thithapandha A "Influence of caffeine on aspirin pharmacokinetics." Eur J Drug Metab Pharmacokinet 11 (1986): 71-6 [4] "Grapefruit juice interactions with drugs." Med Lett Drugs Ther 37 (1995): 73-4 [5] Maish WA, Hampton EM, Whitsett TL, Shepard JD, Lovallo WR "Influence of grapefruit juice on caffeine pharmacokinetics and pharmacodynamics." Pharmacotherapy 16 (1996): 1046-52
Alternative for Rosuvastatin C10B
Ramipril Lisinopril Perindopril Acetylsalicylic acid Niacin Bempedoic acid
Indapamide Fenofibrate

C10A
Fenofibric acid Mipomersen Evinacumab
More
Alternative for Apalutamide L02B
Fulvestrant Toremifene Abarelix Flutamide Relugolix Degarelix
Nilutamide Aminoglutethimide Abiraterone
Potential Metabolism Interactions
Substrate-Substrate Interaction：If more than one drug is metabolized by the same CYP, it is possible that its metabolism is inhibited because of the competition between the drugs. That means, it can be useful to lower the dosage of the drugs in the drug-cocktail because they remain longer in the organism than in monotherapy.
Inhibitor-Inhibitor Interaction：Combining two or more inhibitors of one CYP, should be compensated by lowering the dosage of these drugs because the metabolism is reduced and the drugs remain longer in the organism than in monotherapy. Not adapting the dosage bears the risk of even more side effects.
Inhibitor-Substrate Interaction：Combining drugs that have inhibitory effect and are substrates of one particular CYP, should be compensated by lowering the dosage. They rest longer in the organism than in monotherapy. Not adapting the dosage bears the risk of even more side effects.