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Alpha1-acid glycoprotein (AGP), also known as orosomucoid, is a highly glycosylated plasma protein and a member of the lipocalin family [3, 13]. It serves as a major acute-phase reactant, with its concentration increasing significantly in response to systemic inflammation, infection, and malignancy [7, 12]. AGP plays a critical role in the pharmacokinetics of many drugs, particularly basic and neutral lipophilic compounds, by acting as a high-affinity, low-capacity transport protein [1, 4]. Its biological functions extend beyond transport to include immunomodulation, anti-inflammatory effects, and maintenance of capillary barrier function [16, 17]. In clinical settings, AGP is a valuable biomarker for monitoring inflammatory status and predicting drug disposition [10, 20]. Fluctuations in AGP levels can lead to significant variability in the free fraction of bound drugs, such as imatinib or lidocaine, potentially impacting therapeutic efficacy and safety [14, 15]. Consequently, understanding AGP-drug interactions is essential for dose optimization and managing drug-drug interactions in patients with acute or chronic diseases [4, 10].
Binding and sequestration of basic and neutral drugs in plasma, which regulates the free fraction and bioavailability of these compounds.
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