The effect of aprepitant and race on the pharmacokinetics of cyclophosphamide in breast cancer patients

Abstract

Aprepitant altered the exposure of cyclophosphamide and DCE but not the active 4-OH metabolite, making it unlikely that aprepitant would change the clinical efficacy of cyclophosphamide. African Americans were also found to have altered PK compared with Caucasian patients.

Antiemetic effectiveness and safety of aprepitant in patients with hematologic malignancy receiving multiday chemotherapy

“…34 However, no study has shown serious drug interactions between aprepitant and etoposide or vincristine, both of which are metabolized by CYP3A4. 27,31 Walko et al 35 reported that aprepitant did not influence the area under the concentration-time curve (AUC) of 4-hydroxycyclophosphamide, the active metabolite of cyclophosphamide, in patients with breast cancer. In another study, Bubalo et al 36 reported that the AUC of 4-hydroxycyclophosphamide decreased by approximately 5% in the presence of aprepitant in patients who underwent cyclophosphamide therapy (1.5 g/m 2 /day for four days) for hematopoietic stem cell transplantation.…”

Management of highly emetogenic chemotherapy

“…From a safety perspective, the moderate inhibition of cytochrome P450 3A4 by aprepitant was demonstrated not to significantly impact upon the pharmacokinetics of moderate [21] or high-dose cyclophosphamide [22]. This adds to the previous literature of lack of interactions with other intravenous medications such as vinorelbine and docetaxel [23 & ].…”

Effectiveness and Safety of Antiemetic Aprepitant in Japanese Patients Receiving High-Dose Chemotherapy Prior to Autologous Hematopoietic Stem Cell Transplantation

“…Bubalo et al 29) reported that the area under the concentration-time curve (AUC) of 4-hydroxycy clophosphamide, the active metabolite of cyclophosphamide, decreased by approximately 5% in the presence of aprepitant in patients who underwent cyclophosphamide therapy (1.5 g/m 2 /d×4 d) as pre-transplant conditioning regimen, and this was not clinically significant. In another study, Walko et al 30) reported that aprepitant did not influence the AUC of cyclophosphamide in patients with breast cancer. Recently, we reported that the addition of aprepitant to granisetron improved antiemetic control without influencing AdEs in patients with hematologic malignancies receiving multiday conventional chemotherapy.…”