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BioNumerik Pharmaceuticals, Inc., San Antonio, Texas, has announced treatment of the first patient at the University of Chicago Medical Center in Phase I clinical trials of BioNumerik's anticancer drug known as karenitecin. Karenitecin represents BioNumerik's third new drug that has been brought from discovery to the clinic with the assistance of supercomputer simulations. The preclinical development time for BioNumerik's three drugs has averaged 18 to 24 months compared to the pharmaceutical industry average of 6 years. BioNumerik's karenitecin is a novel, silicon containing, anticancer compound that has demonstrated potent antitumor activity at concentrations as low as parts per trillion in laboratory testing with human cancer cell lines and in animals bearing human tumors. Karenitecin is in the drug class known as camptothecins and has been designed to avoid problems with oral bioavailability, unfavorable metabolism, toxicity and drug resistance that have been associated with other camptothecins. In commenting on these developments, Frederick H. Hausheer, M.D., who led the karenitecin discovery team for BioNumerik' stated: "This is a promising new investigational drug that has demonstrated substantial antitumor activity and reasonable safety in rigorous preclinical models involving various common types of human cancer. Karenitecin represents an entirely new class of drug, and was discovered and developed by our research team using high performance Silicon Graphics and Cray supercomputers. To engineer karenitecin, we simulated more than 12 trillion possible drug candidates using SGI/Cray supercomputing technology in less than one year, and it is clear that it would not be possible to discover and develop such a molecule without this technology operating in parallel with state-of-the-art laboratory research." Dr. Hausheer continued, "Karenitecin represents a new area of medicinal chemistry with the introduction of the element silicon into the drug molecule; it is ironic that silicon based computers played a role in helping us to discover a silicon based investigational drug. Our goals as a discovery team for karenitecin have been fulfilled to this point by creating and rapidly developing a new molecule that has promising anticancer activity. We all hope that this investigational new drug will ultimately provide benefit to patients with common types of cancer. Advancement of karenitecin from the supercomputer to the laboratory and into the clinical phase 1 trial is a major step in the evaluation process." Through an alliance with Silicon Graphics and Cray Research, a Silicon Graphics company, BioNumerik has two supercomputers on site which are capable of conducting an aggregate of 12.8 billion operations per second and hold more than 1 trillion bytes of data. BioNumerik used its supercomputer simulations to construct a detailed computational model involving the key molecular interactions of karenitecin with human cancer cell DNA and topoisomerase I, an important enzyme involved in DNA synthesis and replication. BioNumerik then used this information to guide and complement the discovery and optimization of novel karenitecin compounds for laboratory synthesis and preclinical testing. "BioNumerik's work in taking karenitecin from lab to clinical trials in record time is a testament to the unique power of supercomputers," said Todd Johnson, senior vice president of Corporate Marketing, Silicon Graphics. "This drug would simply not have been developed without supercomputers, and BioNumerik is one of the leaders in using supercomputing power to improve everyday life." In preclinical animal studies, orally administered karenitecin has demonstrated excellent antitumor activity against common human solid tumors (including prostate, colon, breast, lung, melanoma and ovary) and superior potency against a variety of common human cancers compared to existing camptothecin derivatives. BioNumerik's karenitecin has also demonstrated the ability to bypass common, tumor-mediated drug resistance mechanisms to which many other camptothecins appear to be susceptible. Because it is lipophilic (fat loving), BioNumerik believes karenitecin will have enhanced tissue penetration, drug delivery and bioavailability compared to existing water soluble camptothecins. The preclinical studies reported to date appear to strongly support these mechanism based pharmaceutical development objectives. Richard L. Schilsky, M.D., director of the University of Chicago Cancer Center and Principal Investigator for the University of Chicago karenitecin Phase I trial indicated, "Karenitecin is the most potent camptothecin yet introduced into the clinic. Its broad spectrum of antitumor activity and potential for oral administration make it very exciting. We expect the phase I trial to accrue patients very quickly." Herbert M. Pinedo, M.D., Ph.D., chief of the Department of Medical Oncology at the Free University Hospital in the Netherlands commented, "This is a very interesting compound which should be studied clinically as soon as possible. This potent compound can be administered orally. To me, this is a very important practical aspect of the drug." Susan M. Blaney, M.D., principal investigator for the karenitecin Phase I pediatric trial to be conducted at the Texas Children's Cancer Center indicated, "The excellent preclinical antitumor activity that has been observed in adult tumor cell lines has also been observed in a variety of pediatric solid and central nervous system tumors. Karenitecin has very potent activity against pediatric tumor cell lines. We are looking forward to the initiation of pediatric clinical trials with this promising new agent in the near future." In addition to karenitecin, BioNumerik has two other novel investigational agents in clinical trials. BNP7787 is a novel chemoprotecting agent that is designed to prevent or reduce the toxicity and to increase the therapeutic index of a number of widely used cancer drugs, including cisplatin, carboplatin, oxaliplatin, paclitaxel and docetaxel. MDAM is an anticancer agent that is designed to have a reduced toxicity and drug resistance profile relative to the widely used cancer drug, methotrexate. BioNumerik Pharmaceuticals, headquartered in San Antonio, Texas, is an emerging pharmaceutical company with an innovative, proprietary technology platform for the rapid discovery and clinical development of small molecule based pharmaceuticals for cancer. BioNumerik is a leader in a powerful new area called "mechanism based drug discovery" which integrates medicine, quantum physics, synthetic chemistry, pharmaceutical sciences and Silicon Graphics and Cray Research supercomputing. BioNumerik views its approach as a fourth generation technology relative to drug screening, automated screening and combinatorial chemistry, and rational drug design. BioNumerik believes its approach has the potential to greatly reduce the time to discover and bring new drugs into clinical development and to reduce the risk of failure in clinical development. For more information, call 210-614-1701.
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Publication:Mainframe Computing
Geographic Code:1USA
Date:Apr 1, 1999

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