ABSTRACT: Introduction: Microtubules represent one of the most logical and strategic molecular targets amongst the current targets for chemotherapy, alongside DNA. In the past decade, tubulin inhibitors as cancer therapeutics have been an area of focus due to the improved understanding and biological relevance of microtubules in cellular functions. Fueled by the objective of developing novel chemotherapeutics and with the aim of establishing the benefits of tubulin inhibition, several clinical trials have been conducted with others ongoing. Area covered: At present, the antitubulin development pipeline contains an armful of agents under clinical investigation. This review focuses on novel tubulin inhibitors as cancer therapeutics. The article covers the agents which have completed the phase II studies along with the agents demonstrating promising results in phase I studies. Expert opinion: Countless clinical trials evaluating the efficacy, safety and pharmacokinetics of novel tubulin inhibitors highlights the scientific efforts being paid to establish their candidature as cancer therapeutics. Colchicine binding site inhibitors as vascular disrupting agents (VDAs) and new taxanes appear to be the most likely agents for future clinical interest. Numerous agents have demonstrated clinical benefits in terms of efficacy and survival in phase I and II studies. However conclusive benefits can only be ascertained on the basis of phase III studies.

Original languageEnglish
Pages (from-to)917-936
Number of pages20
JournalExpert Opinion on Investigational Drugs
Issue number8
Publication statusPublished - Aug 2 2016


  • colchicine
  • efficacy
  • microtubules
  • objective response
  • overall survival
  • progression free survival
  • solid tumors
  • taxanes
  • Tubulin inhibitors

ASJC Scopus subject areas

  • Pharmacology
  • Pharmacology (medical)


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