Inhibition of all-TRANS-retinoic acid metabolism by R116010 induces antitumour activity
2002

R116010: A New Drug That Helps Cancer Treatment

Sample size: 10 publication 10 minutes Evidence: high

Author Information

Author(s): Van heusden J, Van Ginckel R, Bruwiere H, Moelans P, Janssen B, Floren W, van der Leede B J, van Dun J, Sanz G, Venet M, Dillen L, Van Hove C, Willemsens G, Janicot M, Wouters W

Primary Institution: Johnson & Johnson Pharmaceutical Research & Development

Hypothesis

Can R116010 effectively inhibit all-trans-retinoic acid metabolism and enhance its antitumor activity?

Conclusion

R116010 is a highly potent and selective inhibitor of all-trans-retinoic acid metabolism, enhancing its biological activity and exhibiting antitumor effects.

Supporting Evidence

  • R116010 inhibits all-trans-retinoic acid metabolism with an IC50-value of 8.7 nM.
  • In combination with all-trans-retinoic acid, R116010 enhances its antiproliferative activity.
  • R116010 significantly inhibits the growth of murine TA3-Ha mammary tumors at doses as low as 0.16 mg/kg.

Takeaway

R116010 is a new medicine that helps another medicine work better against cancer by stopping it from being broken down too quickly.

Methodology

The study involved in vitro assays using T47D breast cancer cells and in vivo experiments with murine TA3-Ha mammary tumors.

Potential Biases

Potential bias in the selection of animal models and the specific cancer types studied.

Limitations

The study primarily focused on a specific cancer model and may not be generalizable to all cancer types.

Participant Demographics

The study used murine models, specifically A/J and C3D2F1 mice.

Statistical Information

P-Value

0.05

Statistical Significance

p<0.05

Digital Object Identifier (DOI)

10.1038/sj.bjc.6600056

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