San Francisco, CA; April 6, 2000 -- BioNumerik Pharmaceuticals, Inc. presented data at the 91st Annual Meeting of the American Association of Cancer Research (AACR) being held in San Francisco this week on two novel high performance computer engineered agents that have been designed to help address common and important unmet needs in cancer therapy. BioNumerik's BNP7787 is a unique chemoprotectant utilized to prevent the common and often severe toxicities associated with platinum and taxane administration without inhibiting the antitumor activity of these agents. BioNumerik's Karenitecin BNP1350 is a silicon-containing camptothecin-like agent that has demonstrated potent antitumor activity in several preclinical models including human cancer cell lines and animal bearing human tumor models. Karenitecin has been specifically crafted to overcome known problems of commercially available camptothecins such as lack of oral bioavailability, lactone instability, toxicity and drug resistance.
Further data from animal and laboratory studies was presented at AACR that establishes the ability of BNP7787 to protect against platinum and taxane induced toxicities. It has been determined that BNP7787 and its metabolites selectively conjugate with monohydrated platinum species which is thought to be the overriding mechanism for platinum toxicity. This unique activity of platinum detoxification by BNP7787 was elucidated through the marriage of high performance computing and application of basic sciences.
An ongoing Phase 1 study of BNP7787 at doses of 41g/m2 in Europe and 27.6g/m2 in the U.S. has demonstrated excellent safety results with only 3 out of 46 patients treated with standard doses of cisplatin +/- paclitaxel experiencing clinically significant grade 2 nerve damage (neurotoxicity). This number is substantially less than the expected number of patients with grade 2 nerve damage, based on historical studies of patients who were treated with the same chemotherapy drugs without BNP7787. These results also appear to indicate that while the toxic side effects of cisplatin and paclitaxel are alleviated , the tumor specific programmed cell death (apoptosis) associated with this therapy remains intact.
The Company plans to initiate Phase 3 trials later this year for BNP7787 which has been granted U.S. Food and Drug Administration "Fast Track" designation for the prevention or reduction of the nerve damage associated with paclitaxel.
Additional data presented at AACR further indicates that BioNumerik's goal of being the first to discover, synthesize, formulate, patent and develop a new class of silicon containing semisynthetic camptothecins has been accomplished. Karenitecin BNP1350 is a member of a novel class of specifically developed lipophilic camptothecins. Antitumor activity of BNP1350 has been confirmed in in vitro models of human prostate, breast, lung, colon, melanoma, glioblastoma and ovarian cancer cell lines. Experimental observations suggest the presence of a BNP1350 dimer complex that is believed to be responsible for protecting a key chemical "lactone ring" on the camptothecin molecule. These findings were confirmed in the ongoing Phase 1 study where an impressive 90% or greater lactone ring stability has been measured in patients receiving doses ranging from 0.15- 1.2mg/m2 daily times five days of karenitecin.
Based on these encouraging results and scientific findings, BioNumerik is planning to proceed with Phase 2 clinical trials in gliomas and lung cancer later this year. Additionally, a pediatric Phase 1 study has been initiated and an oral formulation of karenitecin BNP1350 is expected to be introduced into the clinic in the coming months.
BioNumerik Pharmaceuticals, headquartered in San Antonio, Texas, is an emerging cancer technoceutical company with a unique and powerful drug discovery technology platform known as "mechanism based" drug discovery. The Company has expertise in clinical oncology drug development, drug formulation and GMP manufacturing, and has established and maintained a large pipeline of its own novel drug candidates for commercial development.