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Updated: Jul 10, 2026

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Small-Molecule Mitotic Inhibitors as Anticancer Agents: Discovery, Classification, Mechanisms of Action, and Clinical

Yazmin Salinas1, Subhash C Chauhan2,3, Debasish Bandyopadhyay1,4

  • 1School of Integrative Biological and Chemical Sciences, The University of Texas Rio Grande Valley, 1201 West University Drive, Edinburg, TX 78539, USA.

International Journal of Molecular Sciences
|April 17, 2025
PubMed

Insights

Small-molecule mitotic inhibitors target cancer cell replication by disrupting microtubule proteins or kinases. This review classifies these drugs by mechanism, exploring clinical trials and antibody-drug conjugates for improved cancer treatment.

Area of Science:

  • Oncology
  • Pharmacology
  • Cell Biology

Background:

  • Cancer remains a significant global health concern, causing millions of deaths annually.
  • Small-molecule mitotic inhibitors are a crucial class of anticancer drugs.
  • These drugs impede cancer cell division (mitosis), hindering proliferation and promoting cell death.

Purpose of the Study:

  • To review and classify small-molecule mitotic inhibitors.
  • To explore their discovery, chemistry, and mechanisms of action.
  • To discuss their anticancer activity, clinical trials, and future prospects, including antibody-drug conjugates.

Main Methods:

  • Literature review and classification of small-molecule mitotic inhibitors.
  • Analysis of mechanisms targeting microtubule-related proteins, Checkpoint Kinase 1, and mitotic kinases.
  • Examination of clinical trial data and antibody-drug conjugate strategies.

Main Results:

  • Small-molecule mitotic inhibitors exhibit diverse anticancer activities through various mechanisms.
  • Clinical trials are actively investigating these agents, with some showing promise.
  • Antibody-drug conjugates offer a potential strategy for targeted delivery and reduced toxicity.

Conclusions:

  • Small-molecule mitotic inhibitors represent a vital therapeutic strategy in oncology.
  • Continued research and clinical investigation are essential for optimizing their use.
  • Novel delivery systems like antibody-drug conjugates may enhance efficacy and minimize side effects.
Keywords:
antibody–drug conjugatesanticancer agentclinical trialscytotoxickinase proteinsmicrotubule-associated proteinsmitosismitotic proteinssmall-molecule inhibitorstaxanes

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