Target intelligence / Profile preview

Alpha1-acid glycoprotein (AGP)

Target
AGP
Molecular classification
Lipocalin family, Immunocalin subfamily, Acute-phase protein, Plasma protein, Transporter
01

Overview

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].

Other names
OrosomucoidORMAAGAlpha-1-acid glycoprotein 1Alpha-1-acid glycoprotein 2ORM1ORM2
02

Mechanism of action

Binding and sequestration of basic and neutral drugs in plasma, which regulates the free fraction and bioavailability of these compounds.

03

Biological functions

Transport of basic and neutral lipophilic compoundsImmune response modulationAnti-inflammatory activityProtection against tissue damageRegulation of metabolismMaintenance of capillary barrier function
04

Disease associations

InflammationCancerInfectionSepsisCardiovascular diseaseLiver diseaseRheumatoid arthritis
05

Safety considerations

Variability in drug free fraction due to fluctuating AGP levels in disease statesPotential for drug-drug interactions via displacement from binding sitesUnpredictable pharmacokinetics in patients with acute inflammation or malignancy
06

Interacting drugs

Propranolol

12 more in the full profile.

07

Biomarkers

Acute phase reactantMarker of systemic inflammationPrognostic marker for cancer progressionSepsis mortality predictorMarker for drug binding variability

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