DISCODERMOLIDE

Molecular Weight: 593.792 g/mol
Molecular Formula: C₃₃H₅₅NO₈

Source: The Caribbean deep-sea sponge Discodermia dissoluta (PORIFERA)
Activity: tubule interactive agent
Status:Phase I clinical trials

Discodermolide, isolated from the Bahamian deep-sea sponge Discodermia dissoluta, is a promising marine-derived candidate for treating certain cancers. It was discovered in 1987 by scientists with the Harbor Branch Division of Biomedical Marine Research.

The drug, a macrolide (polyhydroxylated lactone), is a member of a structurallu diverse class of compounds called polyketides. It has a noteworthy chemical mechanism of action. It stabilizes the microtubules of target cells, essentially arresting them at a specific stage in the cell cycle and halting cell division. In addition to anticancer properties, discodermolide possesses immunosuppresive and cytotoxic activity.

The pharmaceutical company Novartis Pharma AG licensed discodermolide for commercial development in 1998. The drug is currently in Phase I human clinical trials and continues to show promise in combating pancreatic cancer and many other drug-resistant cancers. Recently published reports offer up the exciting finding that combination drug treatment using discodermolide and Taxol in lung cancer patients exhibits several times the tumor fighting efficacy of either drug administered on its own.

A number of synthetic discodermolide schemes have been elucidated, but so far none appear to be practical on a production-scale level. Biotech company Kosan Biosciences has used recombinant culture strategies to produce several novel discodermolide analogs currently under preclinical investigation.

NCBI PubChem compound summary page - [ LINK ]

NCBI PubMed biomedical literature citations and abstracts - [ LINK ]

References

Kijjoa A and P Sawangwong. 2004. Drugs and cosmetics from the sea (review paper). Mar. Drugs 2004:73-82.

Faulkner DJ. 2000. Marine pharmacology. van Leeuwenhoek 77:135-145.