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taccalonolide AJ + hydroxypropyl-beta-cyclodextrin
- Development stage
- Preclinical
- Lead developer
- Nanjing University of Chinese Medicine
- Modality
- Small Molecules
- Administration
- Intravenous, Oral
01
Overview
Taccalonolide AJ + hydroxypropyl-beta-cyclodextrin is a supramolecular inclusion complex consisting of the semi-synthetic microtubule-stabilizing agent taccalonolide AJ and the cyclodextrin carrier hydroxypropyl-beta-cyclodextrin (HP-beta-CD). Taccalonolide AJ, derived from the Tacca genus, is a potent antineoplastic agent that binds covalently to the D226 residue of beta-tubulin, circumventing common mechanisms of taxane resistance such as P-glycoprotein overexpression and tubulin mutations. The HP-beta-CD formulation was developed to address the parent drug's poor aqueous solubility and chemical instability caused by the hydrolysis of its C-22,23 epoxide moiety. Preclinical studies in clear-cell renal-cell carcinoma (ccRCC) models demonstrate that this complex improves kidney deposition, reduces toxicity, and allows for a weekly dosing schedule, thereby significantly widening the therapeutic window compared to free taccalonolide AJ.
- Other names
- taccalonolide AJ-hydroxypropyl-beta-cyclodextrin inclusion complexAJ-HP-beta-CD inclusion complex
02
Targets
TUBB (Tubulin (alpha and beta subunits))
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