A New Compound Discovered For The Treatment Of Head And Neck Cancers

Kevetrin, our lead product candidate, is a small molecule compound proprietary to the Company.  Its structure is distinct from other anti-cancer agents currently on the market.  While we are initially planning to develop Kevetrin to treat head and neck cancers, there is a potential for its use in multiple epithelial tumors. Kevetrin was discovered by the Company’s founder, Dr. Krishna Menon and has been studied extensively demonstrating potent anti-cancer activity against various cancer cell lines in both in vitro and in vivo studies.  Kevetrin has been shown to be primarily an AKT inhibitor but also acts as an alkylating agent and LTB4 inhibitor with anti-angiogenic properties. Some of the highlights of the data we have compiled to date:

  • Small molecule drug that is structurally different from anti-cancer agents currently on the market
  • Primary mechanism of action is AKT inhibition
  • Potent in vitro cytotoxicity against a panel of human tumor cell lines
  • Demonstrated success in more than 5,000 small animal tests, achieving significant delays in tumor growth compared to controls in breast, prostate and colon cancer tumors.  
  • In animal tests of a head and neck cancer cell line, delay in tumor growth was significantly increased by 13 days with Kevetrin alone (about the same as with radiation alone) but when Kevetrin was administered in conjunction with radiation, tumor growth delay increased by 37 days, more than two-fold compared to controls
  • In small animal tests, Kevetrin was well tolerated.

 

The story behind Kevetrin

Because cancer is a pain in the neck

Few words have the immediately mind-numbing, life-altering effect that "cancer" does. Few diseases have cancer's indiscriminant, murderous streak. And few prospects are more daunting than trying to find an answer that works and safely. Most large pharmaceutical companies use high throughput screening, a scattershot approach that involves testing thousands of potential answers against a particular target, and rational drug design, which puts large teams of scientists and powerful computers at work on the problem.

Dr. Krishna Menon, one of the founders of Cellceutix and its Chief Scientific Officer, didn't have the luxury of being able to throw compounds at the cancer wall and to see which would stick, nor did he have teams of researchers to do the thinking for him. What he did have, however, was 35 years of governmental, academic, and pharmaceutical industry experience, including leading the development of two ”BLOCKBUSTER” drugs. He also had access to a very valuable bull.

Prior to obtaining his degrees in medicine and pharmacology, Dr. Menon was trained as a veterinarian. The story behind Kevetrin dates back to this early experience, when he was working for the government of Jamaica as the chief veterinarian of a Parish. Dr. Menon watched as this prized bull was mistakenly sprayed with a cytotoxic agent to kill ticks. Unfortunately the animal was killed, but subsequent examination also showed that there were some cancers present under the bull's skin which had also been eliminated. This gave rise to the thought in Dr. Menon's mind that there had to be a way to develop cytotoxic agents that eliminated cancer cells while minimizing toxicity.

Fast forward 15 years… Dr. Menon was working with certain types of compounds called indoles, which appeared to have modest anti-cancer activity and to be relatively safe for humans. He thought this might be the road to a new compound that would have the same safety profile but greater activity against cancer cells. Unfortunately, because of other projects, he was unable to start out on this road for another 10 years.

In 2003, Dr. Menon finally had the opportunity to put his experience to work. This was the beginning of several years of trial and error and more trial and error and the frustration that often attends it, as Menon hunted for a new structure that would have better efficacy than indoles but would be no less safe. He was also acutely aware of the fact that a simple derivative of an existing compound would be unlikely to be considered very innovative. He needed something really novel.

After trying many structures. Dr. Menon finally hit on Kevetrin's. He immediately tried it in some in vitro screens and found it to be quite active. Originally, Dr. Menon focused on Kevetrin's activity as an AKT4 inhibitor. Since then, he's tested it in over 5000 laboratory animals and confirmed earlier results -- that Kevetrin [restate success of early screens]. Menon also discovered that the compound works along several pathways, not just a single one, including inhibition of tumor growth by inhibition of VEGF, a protein involved in vascular growth. Based on these 5,000-plus animal tests, Dr. Menon has determined that Kevetrin has special potential in treating head and neck cancers. He and the Cellceutix team are now working on completing the preclinical development work on Kevetrin..

 

Summary of Kevetrin Data

 

In test tube studies, Kevetrin showed potent cytotoxicity against a number of human cell lines.  In animal studies of selected cell lines in breast, prostate and colon cancer, Kevetrin significantly delayed tumor growth compared to controls and was well tolerated at efficacious doses, as indicated by weight loss of less than 7%.  In a selected head and neck cancer cell line, Kevetrin alone reduced tumor volume by more than 60% compared to controls (about the same as radiation alone) and more than 90% when administered along with radiation, the standard treatment. In combination with other drugs, it is well tolerated and showed potential for some synergistic activity.  We are now conducting additional studies to allow us to request permission from FDA to begin studies in humans.

 


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