Future Discovery

Our current Product Pipeline is based on single chemical entities and mixtures.  In the future we expect to integrate new technologies, such as proteomics, in our drug discovery efforts.  Specifically, our strategy is to expand the use of cytokines in in vitro assays into the development of cytokine fingerprints.  We also want to integrate information from proteomic services and published disease spectra to establish novel TCM-validating approaches that will ultimately lead to generation of new prescription drugs.

Single Chemical Entities

We will continue to search for natural products as single chemical entities from TCM exhibiting hematopoiesis, immune modulation and cancer bioactivities.  Collaborators have historically constituted a major source of our natural products.

Natural products with hematopoiesis, immune modulation and cancer bioactivities described in the scientific literature will be evaluated in-house for bioactivity.  These natural products may be obtained as in the past, through arrangements with collaborators.  However, for the future we believe that we can purchase interesting natural products from vendors.  Indeed, chemical vending is a growth industry in China.  We can obtain quantities of natural products ranging from research supplies to bulk amounts of cGMP material.

Once a natural product from TCM with an optimal therapeutic profile has been identified, it can be modified. to produce a derivative as a single chemical entity.  With the derivative strategy, we start with a natural product that has a desired therapeutic.  The objective of a derivative strategy is to chemically modify the lead structure to increase potency, reduce toxicity and/or optimize bioavailability.  When a series of chemically modified derivatives are prepared and tested, a structure activity profile is generated that can lead to further improvements or can provide a development candidate.  In addition, we can obtain a composition of matter IP position for a development candidate.

Screening

We currently use primary in vitro screens when assessing bioactivity including the induction of cytotoxicity in Jurkat T lymphoid tumor cells as an indicator of anticancer activity (MTT assay), and inhibition of IL-2 production in Jurkat cells as an immune suppression read-out.  Secondary in vitro screens allow more precise determination of the activities of test compounds and include both anticancer and immune suppression assays.

New technologies bridging Eastern and Western medicines

Chemically complex extracts as drugs are a basis of success of TCM.  Water extracts of a single plant or preferably multiple plants have been traditionally used in TCM.  Spray drying or precipitation of these aqueous extracts and formulating the resulting solid in tablet or capsules is a recent variation.  The value of these mixtures appears to be that a combination of weakly acting molecules is a better medicine than a single chemical entity that is potently active.  In addition, TCM based extracts are thought to be less toxic in general than single chemical entities.

The Western drug paradigm has been ‘one molecule affecting one receptor or one enzyme.' This approach is less effective when more complex diseases are targeted.

Recently, however, pharmaceutical technology has advanced its capabilities for defining mixtures medically.  These technologies, genomics and proteomics, will soon be used to define single chemical entities as potential prescription drugs.  Traditional pharmaceutical discovery has employed single receptors or single enzymes to characterize single chemical agents.  Proteomics is a powerful new tool in pharmaceutical discovery because proteins are effectors of health/disease on a molecular level.  As a tool, proteomics can be used to characterize the state of complex biological systems.  The proteomic tool combined with Pharmagenesis unique expertise will allow for the first time the characterization of mixtures. Currently, proteomics is being used in detection of certain cancers, which emit specific proteins, such as, HER-2/neu and PSA.

Many different proteomic tools are now available.  As a result of the availability of these tools, Clinical Proteomic Databases are emerging becoming available.  In the very near future, clinical proteomic databases will characterize disease spectra. For example, the NIH (National Institute of Health), FDA (Food and Drug Administration) and NCI (National Cancer Institute) have both Prostate Spectra and Ovarian Spectra.

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