bio balance corporation
DESCRIPTION
Bio Balance Corporation. Improving Medications Using Cost-Effective Processes. Building a Broad and Flexible Technology. Enhancing the safety and efficacy of existing pharmaceuticals & Creating new pharmaceuticals. G Protein-Coupled Receptors (GPCRs). - PowerPoint PPT PresentationTRANSCRIPT
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Bio Balance Corporation
Improving Medications Using Cost-Effective Processes
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Building a Broad and Flexible Technology
Enhancing the safety and efficacy of existing pharmaceuticals
&Creating new pharmaceuticals
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G Protein-Coupled Receptors(GPCRs)
• It is conservatively estimated that 30-50% of all pharmaceuticals interact with GPCRs.
• These receptors are widely distributed within our bodies and are integral to our senses, thoughts and sensations.
• They all desensitize to continued stimulation by agonists.
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Some Common GPCRs -Their Distribution and Effector Systems
• Gs – Heart, brain,lung, neurons, kidney, liver, adrenal gland
• Gi – Brain, olfactory, heart, all tissues
• Activate Ca2+ channels, cardiac positive inotropy, contractile proteins
• Regulate K+, Ca2+ channels, inhibit cAMP and Ca/CaM actions
Distribution: Effects:
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The Problem of Desensitization
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Terminology
• Desensitization• Fade• Autoinhibition• Tachyphylaxis
• Tolerance• Down-regulation• Resistance
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The History of Desensitization
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Interesting and Historical Points:
1957 – First detailed experimental observations of receptordesensitization by del Castillo & Katz Proc.Roy. Soc. Lond.146, 369-381.
1972 – From search - one paper titled “receptor desensitization by lobeline and nicotine”
1988 – The Rose patent # 5,316,759 (May 31, 1994) refers to work dating back to 1988 on the agonist-antagonist combinationof nicotine with mecamylamine.
1991 – Geoffroy, et al. “Reduction of Desensitization of aGlutamate Ionotropic Receptor by Antagonists” MolecularPharmacology 39, 587-591.
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Patents Combining Agonists with Antagonists
USP# Inventor Date Comments4,769,372 Kreek 9/6/88 opioids5,316,759 Rose 5/31/94 nicotine5,352,680 Portoghese 10/4/94 opioids5,472,943 Crain 12/5/95 1:10-10005,580,876 Crain 12/3/96 10,000,0005,597,699 Lanzara 1/28/97 All GPCRs5,767,125 Crain 6/16/98 <100th6,096,756 Crain 8/1/00 method
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Scientific Objective:Preventing Desensitization
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MethodologyMedication
(“agonist” – e.g., isoproterenol, morphine)
+Antagonist to prevent desensitization
(“antagonist” – e.g., metoprolol, naloxone)
= New & Improved Medication
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The Heart of Bio Balance’s Technology
The determination of the optimal ratio of agonist and antagonist by our patented method. This method is based upon a biophysical model for the receptor response.
This allows Bio Balance to create patentable compositions using the “best mode” of practice.
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A Representation of the two-state model showing 5-HT binding
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Experimental vs. Theoretical curves for various receptor responses
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Applications of Bio Balance’s Technology
• Extend the patent protection of existing drugs
• Create new drugs as combinations of generic drugs
• Assist in drug development by salvaging previously discarded drug candidates because of excessive desensitization or fade
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Advantages of Bio Balance’s Technology
• Better control of the therapeutic response. • Cheaper to develop• Multiple therapeutic areas can be targeted• Can combine generic drugs• Potentially quick acceptance by physicians as a
technically superior design of previously accepted drugs.
• Multiple new drugs can be created as compositions within several therapeutic areas such as cardiovascular, pain, pulmonary, brain/memory, tocolytic, etc.
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Heart
Pain
Asthma
Premature Labor
Memory
Other GPCRs
Bio Balance’s
Therapeutic Targets
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Conclusion
Bio Balance has a broad and flexible technology to enhance existing
pharmaceuticals and to create new pharmaceuticals that work better with
fewer side-effects.