Target intelligence / Profile preview

Plasma Protein Binding (Mainly Albumin) (PPB)

Target
PPB
Molecular classification
Plasma Protein, Carrier Protein
01

Overview

Plasma protein binding, primarily to human serum albumin, is a reversible interaction that influences drug distribution, efficacy, metabolism, and excretion. Only the unbound fraction of a drug is pharmacologically active. Albumin, the most abundant plasma protein, binds mainly acidic and neutral drugs at sites like Sudlow Site I and II. The degree of binding affects drug half-life, onset of action, and the potential for drug-drug interactions. Decreased albumin levels caused by disease influence drug free concentrations. Albumin also acts as a carrier for fatty acids and hormones.

Other names
Albumin bindingProtein bindingDrug-protein interactionHSA binding
02

Mechanism of action

Reversible binding of drugs to plasma proteins (mainly albumin), influencing free drug concentration and distribution.

03

Biological functions

Drug transportEndogenous compound transport (fatty acids, hormones)Maintenance of oncotic pressureRegulation of osmotic balanceDrug reservoirLigand binding
04

Disease associations

Pharmacokinetic alterations in hypoalbuminemiaDrug-drug interactions related to binding displacement
05

Safety considerations

Drug-drug interactions due to displacementAltered drug pharmacokinetics in patients with hypoalbuminemiaVariability in drug response related to binding differencesHigh inter-subject variability
06

Interacting drugs

Warfarin

5 more in the full profile.

07

Biomarkers

Serum albumin levels (indicator of binding capacity)α1-acid glycoprotein levels

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