Evaluation of pharmacokinetics of intravenous protein C concentrate in protein C deficiency: implications for treatment initiation and maintenance

Background: Dosing of intravenous protein C concentrate (Ceprotin) in patients with protein C deficiency is guided by pharmacokinetics (PK) of plasma protein C activity. Objectives: This study aimed to characterize PK of intravenous Ceprotin in patients with severe congenital protein C deficiency (S...

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Bibliographic Details
Main Authors: Zhaoyang Li, Inmaculada C. Sorribes, Jennifer Schneider, Adekemi Taylor
Format: Article
Language:English
Published: Elsevier 2025-03-01
Series:Research and Practice in Thrombosis and Haemostasis
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Online Access:http://www.sciencedirect.com/science/article/pii/S2475037925001839
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Summary:Background: Dosing of intravenous protein C concentrate (Ceprotin) in patients with protein C deficiency is guided by pharmacokinetics (PK) of plasma protein C activity. Objectives: This study aimed to characterize PK of intravenous Ceprotin in patients with severe congenital protein C deficiency (SCPCD) and severe acquired protein C deficiency (SAPCD). Methods: An exploratory analysis was conducted to assess effects of demographic and disease-related factors on PK of Ceprotin (n = 35 patients with SCPCD or SAPCD), followed by a population PK analysis on data from 4 prospective clinical trials of Ceprotin in SCPCD or SAPCD (n = 58). Model-based simulations were conducted across 3-stage or 1-stage dosing scenarios based on label-recommended doses in acute or maintenance settings. Results: Age, body weight, and symptomatic state of disease appeared to influence PK of Ceprotin, including endogenous production of (active) protein C. Model-based simulations predicted that after the first doses, 15% to 76% of patients in the 3-stage dosing scenarios (initial dose: 60-120 IU/kg) and 15% of patients in the 1-stage dosing scenario (60 IU/kg every 12 hours) would attain the recommended target Cmax of >100 IU/dL. At steady state, ≥86% of patients were predicted to attain the recommended maintenance Ctrough of >25 IU/dL. The steady-state protein C concentration was driven by the maintenance dose, regardless of the level of initial loading doses. Conclusion: Age, body weight, and symptomatic disease state should be considered in dose optimization. Model-based simulations support the use of various combined loading and maintenance regimens to quickly and effectively achieve target protein C plasma levels.
ISSN:2475-0379