Antitumor Activity of 1,18-Octadecanedioic Acid-Paclitaxel Complexed with Human Serum Albumin.

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ID: 3060
2019
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Abstract
We describe the design, synthesis, and antitumor activity of an 18 carbon α,ω-dicarboxylic acid monoconjugated via an ester linkage to paclitaxel (PTX). This 1,18-octadecanedioic acid-PTX () prodrug readily forms a noncovalent complex with human serum albumin (HSA). Preservation of the terminal carboxylic acid moiety on enables binding to HSA in the same manner as native long-chain fatty acids (LCFAs), within hydrophobic pockets, maintaining favorable electrostatic contacts between the ω-carboxylate of and positively charged amino acid residues of the protein. This carrier strategy for small molecule drugs is based on naturally evolved interactions between LCFAs and HSA, demonstrated here for PTX. shows differentiated pharmacokinetics, higher maximum tolerated doses and increased efficacy in multiple subcutaneous murine xenograft models of human cancer, as compared to two FDA-approved clinical formulations, Cremophor EL-formulated paclitaxel (crPTX) and Abraxane (nanoparticle albumin-bound (nab)-paclitaxel).
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callmann2019antitumorjournal Use this key to autocite in the manuscript while using SciMatic Manuscript Manager or Thesis Manager
Authors Callmann, Cassandra E;LeGuyader, Clare L M;Burton, Spencer T;Thompson, Matthew P;Hennis, Robert;Barback, Christopher;Henriksen, Niel M;Chan, Warren C;Jaremko, Matt J;Yang, Jin;Garcia, Arnold;Burkart, Michael D;Gilson, Michael K;Momper, Jeremiah D;Bertin, Paul A;Gianneschi, Nathan C;
Journal Journal of the American Chemical Society
Year 2019
DOI
10.1021/jacs.9b04272
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