Conţinutul numărului revistei |
Articolul precedent |
Articolul urmator |
563 0 |
SM ISO690:2012 DURAN, Ignacio, CARLES, J., BULAT, Iurie, HELLEMANS, Peter, MITSELOS, Anna, WARD, Peter D., JIAO, James Juhui, ARMAS, Danielle, CHIEN, Caly. Pharmacokinetic Drug–Drug Interaction of Apalutamide, Part 1: Clinical Studies in Healthy Men and Patients with Castration-Resistant Prostate Cancer. In: Clinical Pharmacokinetics , 2020, nr. 9(59), pp. 1135-1148. ISSN 0312-5963. DOI: https://doi.org/10.1007/s40262-020-00882-2 |
EXPORT metadate: Google Scholar Crossref CERIF DataCite Dublin Core |
Clinical Pharmacokinetics | |
Numărul 9(59) / 2020 / ISSN 0312-5963 /ISSNe 1179-1926 | |
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DOI:https://doi.org/10.1007/s40262-020-00882-2 | |
Pag. 1135-1148 | |
Rezumat | |
Background and Objectives: Two phase I studies assessed the drug–drug interaction potential of apalutamide as a substrate and perpetrator. Methods: Study A randomized 45 healthy men to single-dose apalutamide 240 mg alone or with strong inhibitors of cytochrome P450 (CYP)3A4 (itraconazole) or CYP2C8 (gemfibrozil). In study B, 23 patients with castration-resistant prostate cancer received probes for CYP3A4 (midazolam), CYP2C9 (warfarin), CYP2C19 (omeprazole), and CYP2C8 (pioglitazone), and transporter substrates for P-glycoprotein (P-gp) (fexofenadine) and breast cancer resistance protein (BCRP)/organic anion transporting polypeptide (OATP) 1B1 (rosuvastatin) at baseline and after repeat once-daily administration of apalutamide 240 mg to steady state. Results: Systemic exposure (area under the plasma concentration–time curve) to single-dose apalutamide increased 68% with gemfibrozil but was relatively unchanged with itraconazole (study A). Apalutamide reduced systemic exposure to midazolam ↓92%, omeprazole ↓85%, S-warfarin ↓46%, fexofenadine ↓30%, rosuvastatin ↓41%, and pioglitazone ↓18% (study B). After a single dose, apalutamide is predominantly metabolized by CYP2C8, and less by CYP3A4. Conclusions: Co-administration of apalutamide with CYP3A4, CYP2C19, CYP2C9, P-gp, BCRP or OATP1B1 substrates may cause loss of activity for these medications. Therefore, appropriate mitigation strategies are recommended. |
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Cuvinte-cheie Abiraterone Acetate, MDV 3100, Cabazitaxel |
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Cerif XML Export
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