Enhanced therapeutics of cabazitaxel via polycarboxylate conjugation: improved solubility, safety, and antitumor efficacy.

ABSTRACT:

Introduction

Cabazitaxel (CTX) is a potent anticancer agent whose clinical utility is severely limited by poor aqueous solubility and severe systemic toxicity. To overcome these challenges, we designed and synthesized two water-soluble polycarboxylate conjugates, CTX-DTPA and CTX-TTHA.

Methods

The conjugates were characterized via NMR and mass spectrometry. Their hydrophilicity was assessed by lipid-water partition coefficient. Antitumor activity was evaluated in vitro across multiple cancer cell lines and in vivo using xenograft and immunocompetent models. Mechanisms were investigated via molecular docking, immunofluorescence, and tubulin polymerization assays. Safety profiles were assessed through hemocompatibility, myelosuppression, and thymic toxicity evaluations. Pharma

SUBMITTER: Mao L 

PROVIDER: S-EPMC12689286 | biostudies-literature | 2025

REPOSITORIES: biostudies-literature