2. Academic Validation
  3. Triptolide and Its Derivatives as Cancer Therapies

Triptolide and Its Derivatives as Cancer Therapies

  • Trends Pharmacol Sci. 2019 May;40(5):327-341. doi: 10.1016/j.tips.2019.03.002.
Pawan Noel 1,  Daniel D Von Hoff 2,  Ashok K Saluja 3,  Mohana Velagapudi 4,  Erkut Borazanci 2,  Haiyong Han 5
Affiliations

Affiliations

  • 1 Molecular Medicine Division, Translational Genomics Research Institute, Phoenix, AZ, USA.
  • 2 Molecular Medicine Division, Translational Genomics Research Institute, Phoenix, AZ, USA; HonorHealth Research Institute, Scottsdale, AZ, USA.
  • 3 Department of Surgery, Miller School of Medicine, Sylvester Pancreatic Cancer Research Institute, University of Miami, Miami, FL, USA.
  • 4 Minneamrita Therapeutics LLC, Moline, IL, USA.
  • 5 Molecular Medicine Division, Translational Genomics Research Institute, Phoenix, AZ, USA. Electronic address: hhan@tgen.org.
PMID: 30975442 DOI: 10.1016/j.tips.2019.03.002
Abstract

Triptolide, a compound isolated from a Chinese medicinal herb, possesses potent antitumor, immunosuppressive, and anti-inflammatory properties, but is clinically limited due to its poor solubility, bioavailability, and toxicity. Recently, Minnelide, a water-soluble prodrug of triptolide, was shown to have potent antitumor activity in various preclinical Cancer models. Minnelide is currently in Phase II clinical trials for treatment of advanced pancreatic Cancer, which has fueled increased interest in this promising agent. Here, we review the recent advances in the biological activity of triptolide and its analogs, their mechanisms of actions, and their clinical developments. A special emphasis is given to proteins and pathways within the tumor and stromal compartments that are targeted by triptolide and its analogs as well as the ongoing clinical trials.

Keywords

Minnelide; stroma; transcription regulation; triptolide; tumor microenvironment.

Figures
Products