By Mary Welch

With one product about to enter Phase III trials, BioNumerik Pharmaceuticals Inc. raised $12 million in its second self-managed private placement. "We were targeting $4 million, but there was more interest than we thought," said Frederick Hausheer, BioNumerik's chairman and CEO. "So we took the money."

Since its founding in May 1992, the company has raised more than $45 million, and closed its fiscal year on March 31 with more than $20 million in cash.

"The market has been very interesting and with the recent downturn, it's good to be a private company," Hausheer said. BioNumerik's placement attracted both institutional investors as well as some "significant high-net-worth individuals," he said.

The proceeds will be used to fund the Phase III trial as well as advance other products in development. Other uses include funding drug discovery operations, drug manufacture and supply operations, and patent filing, as well as hiring additional personnel.

In addition, the San Antonio-based company expanded its alliance with Tokyo-based Grelan Pharmaceutical Co. for the development and commercialization of BioNumerik's chemoprotecting agent, BNP7787, in Japan. The new expansion deal allows for Grelan to fund the research and development of additional uses of BNP7787, including paclitaxel and radiation toxicity prevention.

"It's a great collaboration," Hausheer said. "Japan is the second-largest oncology market in the world. Grelan distributes through Takeda Chemical Industries, which provides us with excellent access to this major territory. In addition, Grelan will bear all the development costs for the product in Japan."

As part of the expansion, Grelan purchased $2 million worth of stock in the recent private placement and may participate in future rounds, he said.

BioNumerik's technology involves a mechanism-based drug discovery platform that integrates medicine, quantum physics, synthetic chemistry and pharmaceutical sciences with an advanced supercomputer. Combining these disciplines allows BioNumerik to rapidly optimize key structural, targeting, safety and delivery requirements for small molecules, Hausheer said.

The company has successfully used its approach to reduce the preclinical development time for three new drugs to approximately 18 to 24 months, compared to the industry average of 6.1 years. At the same time, it is generating new compounds that are aimed at having a higher degree of clinical success, he said.

BioNumerik views its approach as a fourth-generation technology relative to drug screening, automated screening and combinatorial chemistry and rational drug design, said Hausheer, who pioneered the technology.

Because its approach permits an advanced understanding of a compound's mechanism of action, safety and delivery requirements, BioNumerik believes it can avoid and overcome many potential problems at an earlier stage and avoid costly false starts.

In addition, the company's computational combinatorial approach does not exclude or select compounds by a limited set of experimental conditions. Rather, it assumes that most new compounds can eventually be synthesized, especially those with blockbuster potential.

As if to offer further evidence of the technology's success in rapidly advancing compounds to the clinic, Hausheer noted, "We have three compounds in clinical trials and eight more in preclinical product areas. We also have 220 patents or patents pending."

Ready to start Phase III trials later this year is BNP7787, a novel agent for the prevention of major and serious toxicities that are associated with widely used oncology drugs, including cisplatin, paclitaxel and carboplatin. BNP7787 is designed to reduce the kidney and bone marrow toxicities, emesis and neurotoxicities associated with paclitaxel and platinum chemotherapy drugs. It also makes the drugs easier and safer to give to patients, Hausheer said.

BNP7787 recently received fast-track status for the prevention of paclitaxel-associated nerve damage. Based on a positive interim analysis of ongoing Phase I trials, BNP7787 will skip Phase II and go directly into Phase III testing for breast and non-small-cell lung cancer, and possibly ovarian cancer.

The company also finished Phase I trials of racemic MDAM, a nonpolyglutamylatable antifolate, whose parent, methotrexate, is one of the most widely used anticancer agents. The company was successful in synthesizing and testing L-MDAM and found that it has excellent oral anti-tumor activity and safety. An abbreviated Phase I trial with L-MDAM for patients with solid tumors will start this year.

BioNumerik's third compound currently in the clinic is Karenitecin, which was developed in 24 months. Karenitecin is part of a new class of novel oral and parenteral highly lipophilic camptothecin derivatives and has shown broad activity against several cancers, including prostate, pancreas, lung, breast, brain, melanoma, colon, ovary, and head and neck. It has met early trial expectations and is scheduled to enter Phase II trials later this year. It was designed to address metabolism, bioavailability, toxicity and resistance problems associated with other camptothecins.

Hausheer said BioNumerik is in "serious discussions" with many pharmaceutical companies regarding a strategic alliance for BNP7787.

"We hold the rights to all our compounds except BNP7787 in Japan," he said. "We intend to develop and commercialize our drugs in the U.S. and we have thus far been able to advance these products on our own, which is another reason why investors appreciate us. "

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