Tubulin inhibitor-based antibody-drug conjugates for cancer therapy

Hao Chen, Zongtao Lin, Kinsie E. Arnst, Duane Miller, Wei Li

Research output: Contribution to journalReview article

17 Citations (Scopus)

Abstract

Antibody-drug conjugates (ADCs) are a class of highly potent biopharmaceutical drugs generated by conjugating cytotoxic drugs with specific monoclonal antibodies through appropriate linkers. Specific antibodies used to guide potent warheads to tumor tissues can effectively reduce undesired side effects of the cytotoxic drugs. An in-depth understanding of antibodies, linkers, conjugation strategies, cytotoxic drugs, and their molecular targets has led to the successful development of several approved ADCs. These ADCs are powerful therapeutics for cancer treatment, enabling wider therapeutic windows, improved pharmacokinetic/pharmacodynamic properties, and enhanced efficacy. Since tubulin inhibitors are one of the most successful cytotoxic drugs in the ADC armamentarium, this review focuses on the progress in tubulin inhibitor-based ADCs, as well as lessons learned from the unsuccessful ADCs containing tubulin inhibitors. This review should be helpful to facilitate future development of new generations of tubulin inhibitor-based ADCs for cancer therapy.

Original languageEnglish (US)
Article number1281
JournalMolecules
Volume22
Issue number8
DOIs
StatePublished - Aug 1 2017

Fingerprint

Tubulin Modulators
antibodies
inhibitors
therapy
drugs
cancer
Antibodies
Pharmaceutical Preparations
Neoplasms
Therapeutics
warheads
Pharmacodynamics
Pharmacokinetics
Oncology
lessons learned
Drug-Related Side Effects and Adverse Reactions
conjugation

All Science Journal Classification (ASJC) codes

  • Analytical Chemistry
  • Chemistry (miscellaneous)
  • Molecular Medicine
  • Pharmaceutical Science
  • Drug Discovery
  • Physical and Theoretical Chemistry
  • Organic Chemistry

Cite this

Tubulin inhibitor-based antibody-drug conjugates for cancer therapy. / Chen, Hao; Lin, Zongtao; Arnst, Kinsie E.; Miller, Duane; Li, Wei.

In: Molecules, Vol. 22, No. 8, 1281, 01.08.2017.

Research output: Contribution to journalReview article

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