Modeling and Simulation to Inform Apixaban Dosing in Pediatrics With Acute Lymphoblastic Leukemia or Lymphoblastic Lymphoma Treated With Asparaginase

利用建模和仿真指导接受天冬酰胺酶治疗的急性淋巴细胞白血病或淋巴细胞淋巴瘤患儿的阿哌沙班给药方案

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Abstract

Apixaban could be a potential treatment option for the prevention of venous thromboembolism (VTE) in children with acute lymphoblastic leukemia (ALL) or lymphoblastic lymphoma (LL). This analysis describes an updated two-compartment population pharmacokinetic (PPK) model that characterizes the PK variability of apixaban in pediatric patients with ALL or LL treated with asparaginase using PK data from a phase III study (PREVAPIX). Patient type of ALL or LL was found to be a significant covariate on the apparent central volume of distribution (Vc/F) and first-order absorption rate (Ka). Pediatric patients (aged 9 months to < 18 years) with ALL or LL had a 52.4% lower Ka compared with adults; this was 81.1% lower than other pediatric patients (9 months to < 18 years) at risk of VTE. Apixaban Vc/F was estimated to be 43.1% lower in pediatric patients compared with adult patients. The updated PPK model was used to simulate and confirm apixaban fixed-dose by weight-tiered regimen-achieved target exposures in pediatric patients (aged 28 days to < 18 years) with ALL or LL. In addition, a PK/pharmacodynamic (PD) analysis was performed using a linear regression model to characterize the relationship between anti-FXa activity (AXA) and apixaban concentration in pediatric patients with ALL or LL. The characterization of apixaban PK and PK/PD in this analysis contributes to evidence that apixaban could be a potential antithrombotic option in pediatric patients.

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