incyclinide targets conditions other than rosacea

Written by David Pascoe on November 14, 2006 in tetracyclines with 0 Comments

Rosacea News first wrote about Col-3 in August 2005 – COL-3 new tetracycline derivative being studied. We’ve also mentioned that COL-3 was renamed to Incyclinide – Incyclinide (CollaGenex) gets NIH Funding and Incyclinide phase 2 for acne.

In a recently published paper (previously mentioned only via the Abstract – Tetracyclines: their non-antibiotic properties ) we can read some more information about Incyclinide and how it is showing promise as a treatment for other inflammatory diseases. Following are some extracts from the paper ;

Tetracyclines: nonantibiotic properties and their clinical implications. Journal of The American Academy of Dermatology, 2006 Feb;54(2):258-65, Allen N. Sapadin MD, and Raul Fleischmajer MD
…
Kaposi’s sarcoma. Kaposi’s sarcoma is characterized by proliferation of endothelial cells and increase in MMP activity. A preliminary clinical trial involved 18 patients with AIDS-related Kaposi’s sarcoma who were treated with a chemical modified tetracycline, COL-3.
Cancer. Recently, a phase I clinical trial of oral COL-3 (6-demethyl, 6-deoxy, 4-dedimethylaminotetracycline) was administered to 35 patients with multiple refractory metastasizing tumors. Although COL-3 appeared to have stabilized nonepithelial-type malignancies, additional follow-up studies are necessary to determine its true efficacy in the prevention of progression of cancer metastasis.

It is interesting to see more research being published that shows how the benefits of non-antibiotic (low dose) and chemically modified tetracyclines can be applied to rosacea and other inflammatory conditions. The research is showing that the anti-angiogenic properties, by inhibiting collagenases and gelatinases and also their antiapoptotic properties, tetracyclines and their analogues are proving useful for a wide range of diseases.

The more general applicability of Incyclinide is good news for rosacea sufferers. As well as giving Collagenex a potentially bigger market for its products, it might also might mean more studies assessing Incyclinide and how well it works for rosacea. The argument against this last point is of course that Collagenex are targeting oracea as their rosacea treatment of choice.

Note that it is a bit subtle, but at pharmacological level non-antibiotic tetracycline is not the same thing as chemically modified tetracycline. Non antibiotic refers to a low dosage that gives a therapeutic benefit but does not affect systemic flora. The so-called chemically modified tetracyclines, like Incyclinide are modifications of the structure of the compound itself. cf ;

Removal of the dimethylamino group from C4 reduces its anti-
biotic properties, but enhances nonantibiotic actions. Utilization of this strategy was the basis for the development of several chemically modified tetracyclines.

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