"extremely encouraging signs of clinical efficacy"

Robert Don PhD, Progen VP of R&D to present at the 2nd Annual Conference "Angiogenesis: New Opportunities & Solutions for Drug Development"

PI-88: Targeting angiogenesis and metastasis through heparin-binding proteins. From Discovery to Phase II.

Date: Monday, September 27, 2004

With a focused Phase II program across four indications, and demonstrated signs of efficacy, PI-88 has validated the approach of targeting heparin-binding proteins for drug discovery, especially in cancer. PI-88 is an antiangiogenic and antimetastatic agent, which exerts its influence by heparan sulfate (HS) mimicry. The angiogenic growth factors VEGF, FGF-1 and –2, as well as the matrix-degrading enzyme heparanase, bind to heparan sulfate, and PI-88 is a potent inhibitor of all of these as well as being antimetastatic. Structure-based in silico studies have shown that carbohydrate and non-carbohydrate small molecules can be designed and prepared to specifically bind to the HS-binding domains on these growth factors and disrupt activity. PI-88 is the first product from this ongoing program to identify and develop small molecule growth factor inhibitors with this novel mechanism. Coupled to the antimetastatic activity seen in PI-88, high growth factor affinity of the drug has led to extremely encouraging signs of clinical efficacy, including anti-tumor activity, partial responses and multiple cases of durable stable disease. The current Phase II clinical program includes lung cancer (NSCLC), primary liver cancer (hepatocellular carcinoma), multiple myeloma and melanoma (for which PI-88 has received Orphan Drug status from the FDA). The discovery program, PI-88’s development, and recent clinical data will be presented.

Robert Don PhD
Vice President of Research and Development
PROGEN INDUSTRIES LIMITED

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