ArticleJournal of natural products2017
Pharmacokinetic Analysis and in Vivo Antitumor Efficacy of Taccalonolides AF and AJ.
Article in Journal of natural products, 2017. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 16 papers.
What it found
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.
Who cites it
16 citing papers in PubMed.
- Pharmacokinetic and Biodistribution Studies of [ACS medicinal chemistry letters · 2025Article
- Drugs That Changed Society: Microtubule-Targeting Agents Belonging to Taxanoids, Macrolides and Non-Ribosomal Peptides.Molecules (Basel, Switzerland) · 2022Review
- Characterization of Caerulomycin A as a dual-targeting anticancer agent.European journal of pharmacology · 2022Article
- Taccalonolides: Structure, semi-synthesis, and biological activity.Frontiers in pharmacology · 2022Review
- Efficacy of a Covalent Microtubule Stabilizer in Taxane-Resistant Ovarian Cancer Models.Molecules (Basel, Switzerland) · 2021Article
- Taccalonolide C-6 Analogues, Including Paclitaxel Hybrids, Demonstrate Improved Microtubule Polymerizing Activities.Journal of natural products · 2021Article
- Review
- Synthesis and Biological Evaluations of Electrophilic Steroids Inspired by the Taccalonolides.ACS medicinal chemistry letters · 2020Article
- Development of Taccalonolide AJ-Hydroxypropyl-β-Cyclodextrin Inclusion Complexes for Treatment of Clear Cell Renal-Cell Carcinoma.Molecules (Basel, Switzerland) · 2020Article
- Review
- Elucidating target specificity of the taccalonolide covalent microtubule stabilizers employing a combinatorial chemical approach.Nature communications · 2020Article
- Taccalonolide Microtubule Stabilizers.Progress in the chemistry of organic natural products · 2020Review
- Unravelling the covalent binding of zampanolide and taccalonolide AJ to a minimalist representation of a human microtubule.Journal of computer-aided molecular design · 2019Article
- Identification of C-6 as a New Site for Linker Conjugation to the Taccalonolide Microtubule Stabilizers.Journal of natural products · 2019Article
- Taccalonolide Microtubule Stabilizers Generated Using Semisynthesis Define the Effects of Mono Acyloxy Moieties at C-7 or C-15 and Disubstitutions at C-7 and C-25.Journal of natural products · 2018Article
- The Search for Anticancer Agents from Tropical Plants.Progress in the chemistry of organic natural productsReview
Corrections and comments
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Authors and funding
8 authors.
Funding
Abstract
The taccalonolides are microtubule stabilizers that covalently bind tubulin and circumvent clinically relevant forms of resistance to other drugs of this class. Efforts are under way to identify a taccalonolide with optimal properties for clinical development. The structurally similar taccalonolides AF and AJ have comparable microtubule-stabilizing activities in vitro, but taccalonolide AF has excellent in vivo antitumor efficacy when administered systemically, while taccalonolide AJ does not elicit this activity even at maximum tolerated dose. The hypothesis that pharmacokinetic differences underlie the differential efficacies of taccalonolides AF and AJ was tested. The effects of serum on their in vivo potency, metabolism by human liver microsomes and in vivo pharmacokinetic properties were evaluated. Taccalonolides AF and AJ were found to have elimination half-lives of 44 and 8.1 min, respectively. Furthermore, taccalonolide AJ was found to have excellent and highly persistent antitumor efficacy when administered directly to the tumor, suggesting that the lack of antitumor efficacy seen with systemic administration of AJ is likely due to its short half-life in vivo. These results help define why some, but not all, taccalonolides inhibit the growth of tumors at systemically tolerable doses and prompt studies to further improve their pharmacokinetic profile and antitumor efficacy.
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Registered trials
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