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The binding of drugs to plasma proteins greatly influences the drug distribution. Human serum albumin (HSA) and a1-acid glycoprotein (AGP) are the most important plasma proteins, which act as drug carriers, with drug pharmacokinetic implications.<br />HSA has several binding pockets where various ligands such as fatty acids, ions can bind to, providing drugs the option for non-covalent binding sites. Meanwhile, two terminal ends of albumin and certain amino acid residues provide more choices for drug targeting