Tubulin polymerization inhibitors in early clinical studies as cancer therapeutics.

[INTRODUCTION] Microtubules are essential to cancer therapy as key cytoskeletal components that regulate cell division, intracellular transport, and mitotic spindle formation. Tubulin polymerization inhibition is a critical target in anticancer drug development. This review evaluates tubulin polymerization inhibitors (TPIs) in early clinical stages. Using pertinent keywords on tubulin polymerization inhibitors and related trials, literature from January 2018 to January 2026 was obtained from PubMed, Scopus, Embase, Web of Science, ClinicalTrials.gov, and Google Scholar.

[AREA COVERED] TPIs are classified by their tubulin binding sites into colchicine, vinca alkaloid, and taxane categories. Preclinical data demonstrate strong antiproliferative activity, tumor regression in models, and synergism with DNA-damaging agents, targeted therapies, and immunotherapy. Clinical investigations assess efficacy, identify dose-limiting toxicities, and guide biomarker-based patient selection. Challenges such as drug resistance and pharmacokinetics are addressed through nanoparticle delivery and combination strategies.

[EXPERT OPINION] TPIs are evolving from traditional cytotoxic agents to precision medicines that exploit molecular differences between cancerous and normal tissues. Advances such as βIII-tubulin as a predictive biomarker enable personalized therapy. Despite challenges, integrating nanotechnology and immunotherapy offers transformative potential. TPIs are emerging as potent agents in precision oncology with enhanced efficacy and reduced toxicity, marking a pivotal shift in targeted cancer treatment.