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Fourteen-step synthesis of ingenol to aid analog design

A 14-step process for ingenol synthesis could facilitate the generation of analogs for therapeutic evaluation. Ingenol is a diterpenoid, and analogs of the molecule are marketed to treat cancer. However, ingenol currently is obtained directly from its plant source with an isolation yield of about 0.028% by weight. In the new approach, a 2-phase, 14-step chemical synthesis, starting from the inexpensive commodity chemical 3-carene, generated ingenol with a 1.2% overall yield. Next steps include optimizing the final steps of the process and trying to further decrease the number of synthesis steps.
Leo Pharma A/S markets Picato ingenol mebutate gel, an ingenol 3-angeloyl topical formulation, to treat actinic keratosis. The topical drug also is in Phase II testing to treat basal cell carcinoma (BCC).

SciBX 6(34); doi:10.1038/scibx.2013.938
Published online Sept. 5, 2013

Provisional patent application filed; licensing details available from Leo Pharma

Jørgensen, L. et al. Science;
published online Aug. 1, 2013;
Contact: Phil S. Baran, The Scripps Research Institute, La Jolla, Calif.
Contact: Steve J. McKerrall,
same affiliation as above