MedKoo product information:

Incyclinide

incyclinide is a chemically-modified tetracycline with potential antineoplastic activity. Incyclinide inhibits matrix metalloproteinases (MMPs), thereby inducing extracellular matrix degradation, and inhibiting angiogenesis, tumor growth and invasion, and metastasis. This agent also causes mitochondrial depolarization in tumor cells and induces both cellular apoptosis and tissue necrosis. Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus).

The chemically modified tetracycline (CMT) incyclinide (COL-3, CMT-3) has been extensively studied as a potential new therapeutic agent for allergic conditions, inflammatory (i.e., arthritis, acute respiratory distress syndrome [ARDS], septic shock syndrome, acne and rosacea), neoplastic (i.e., Kaposi's sarcoma, colon carcinoma, melanoma, prostate cancer) and infectious (fungal) diseases. The most prominent characteristic of CMTs is their lack of antibacterial properties, accompanied by retention, or even enhancement, of metalloproteinase (MMP) inhibition. Studies have demonstrated that incyclinide is a modulator of MMP-2, MMP-9 and serine proteases, as well as cytokines and interleukins that are crucial in the development of inflammation, angiogenesis and tumorigenesis. Furthermore, toxicology studies have demonstrated that incyclinide is relatively safe. See Drugs Fut 2007, 32(3): 209.

Current developer:    CollaGenex Pharmaceuticals, Inc.

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55: Liu Y, Tortora G, Ryan ME, Lee HM, Golub LM. Potato dextrose agar antifungal susceptibility testing for yeasts and molds: evaluation of phosphate effect on antifungal activity of CMT-3. Antimicrob Agents Chemother. 2002 May;46(5):1455-61. PubMed PMID: 11959582; PubMed Central PMCID: PMC127172.

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81: McCann UG 2nd, Gatto LA, Searles B, Carney DE, Lutz CJ, Picone AL, Schiller HJ, Nieman GF. Matrix metalloproteinase inhibitor: differential effects on pulmonary neutrophil and monocyte sequestration following cardiopulmonary bypass. J Extra Corpor Technol. 1999 Jun;31(2):67-75. PubMed PMID: 10724645.

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83: Carney DE, Lutz CJ, Picone AL, Gatto LA, Ramamurthy NS, Golub LM, Simon SR, Searles B, Paskanik A, Snyder K, Finck C, Schiller HJ, Nieman GF. Matrix metalloproteinase inhibitor prevents acute lung injury after cardiopulmonary bypass. Circulation. 1999 Jul 27;100(4):400-6. PubMed PMID: 10421601.

84: Eklund KK, Sorsa T. Tetracycline derivative CMT-3 inhibits cytokine production, degranulation, and proliferation in cultured mouse and human mast cells. Ann N Y Acad Sci. 1999 Jun 30;878:689-91. PubMed PMID: 10415809.

85: Tjäderhane L, Sulkala M, Sorsa T, Teronen O, Larmas M, Salo T. The effect of MMP inhibitor metastat on fissure caries progression in rats. Ann N Y Acad Sci. 1999 Jun 30;878:686-8. PubMed PMID: 10415808.

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88: Zhu B, Block NL, Lokeshwar BL. Interaction between stromal cells and tumor cells induces chemoresistance and matrix metalloproteinase secretion. Ann N Y Acad Sci. 1999 Jun 30;878:642-6. PubMed PMID: 10415796.

89: Lokeshwar BL. MMP inhibition in prostate cancer. Ann N Y Acad Sci. 1999 Jun 30;878:271-89. Review. PubMed PMID: 10415736.

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