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The role of drug-receptor desensitization (tolerance, fade

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The role of drug-receptor desensitization (tolerance, fade
"The role of drug-receptor desensitization (tolerance, fade, tachyphylaxis or down-

regulation) for future drug development." Richard Lanzara, Ph.D. Bio Balance, Inc. 30

W. 86th St. NY, NY USA 10024-3600, e-mail: rlanzara@bio-balance.com



One of the perils of drug development is the occurrence of desensitization, which is also

called tolerance, fade, tachyphylaxis or down-regulation. Many in the industry believe

that by selecting the proper dosage regime drug-receptor desensitization can be

minimized or prevented. Rightly or wrongly, they create a tightrope that patients and

doctors must walk when utilizing these types of medications. This may affect anywhere

from 30 to 50 percent of all pharmaceuticals and be a fertile area for drug development

and improvement in the future. Given some of the disturbing reports that shown upwards

of 90,000 cases per year of reported medical errors, the production of safer drugs should

be a top priority in the pharmaceutical field. Yet why haven't the major companies done

more to produce safer drugs? A partial explanation would be that it is much more

expensive to ensure safer drugs, but an alternative explanation may be that they lack the

technology to understand and correct the problem. Certainly, the major companies would

want the safest product on the market. This would not only make sense from a medical

standpoint, but a marketing one as well. Safer drugs require that all of the variables of

drug development be evaluated and adjusted for the greatest number of people using

these medications. Surprisingly, the safest drugs may come from using

agonist/antagonist combinations in ways to prevent, diminish or control drug-receptor

desensitization. This would be analogous to creating designer partial agonists in ways

that have been previously overlooked, but would offer a new technology for enhancing

the safety and efficacy of many pharmaceuticals.



Sincerely,

Richard Lanzara

President & Principal Scientific Officer

Bio Balance™, Inc.

www.bio-balance.com

30 West 86th Street

New York, NY 10024

rlanzara@bio-balance.com





Bio Balance (www.bio-balance.com) is an early stage drug development company that

has developed the only tested method to prevent drug desensitization at the receptor

level. This phenomenon, also known as down-regulation, tolerance or fade, occurs with

a large number of very commonly used drugs such as dobutamine for heart failure,

isoproterenol for shock or asthma, L-dopa for Parkinson’s Disease, and morphine for

pain. Notably, desensitization cannot be remedied by taking larger dosages. With more

and more drug, efficacy diminishes and the drug essentially stops working. By using a

patented approach, we create new, combination drug candidates that sustain the

therapeutic response with a better side-effects profile than the original drugs.


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