Over the past decades,
albumin has emerged as a versatile carrier for therapeutic and diagnostic agents, primarily for diagnosing and treating diabetes,
cancer,
rheumatoid arthritis and
infectious diseases. Market approved products include
fatty acid derivatives of human
insulin or the glucagon-like-1
peptide (
Levemir(®) and
Victoza(®)) for treating diabetes, the
taxol albumin nanoparticle
Abraxane(®) for treating metastatic
breast cancer which is also under clinical investigation in further
tumor indications, and (99m)Tc-aggregated
albumin (
Nanocoll(®) and Albures(®)) for diagnosing
cancer and
rheumatoid arthritis as well as for lymphoscintigraphy. In addition, an increasing number of
albumin-based or
albumin-binding drugs are in clinical trials such as antibody fusion
proteins (MM-111) for treating HER2/neu positive
breast cancer (phase I), a camelid
albumin-binding nanobody anti-HSA-anti-TNF-α (ATN-103) in phase II studies for treating
rheumatoid arthritis, an
antidiabetic Exendin-4 analog bound to recombinant
human albumin (phase I/II), a
fluorescein-labeled
albumin conjugate (AFL)-
human serum albumin for visualizing the malignant borders of
brain tumors for improved surgical resection, and finally an
albumin-binding
prodrug of
doxorubicin (INNO-206) entering phase II studies against
sarcoma and
gastric cancer. In the preclinical setting, novel approaches include attaching
peptides with high-affinity for
albumin to
antibody fragments, the exploitation of
albumin-binding
gadolinium contrast agents for magnetic resonance imaging, and physical or covalent attachment of
antiviral, antibacterial, and anticancer drugs to
albumin that are permanently or transiently attached to
human serum albumin (HSA) or act as
albumin-binding
prodrugs. This review gives an overview of the expanding field of preclinical and clinical drug applications and developments that use
albumin as a
protein carrier to improve the pharmacokinetic profile of the drug or to target the drug to the pathogenic site addressing diseases with unmet medical needs.