Protein Kinase C enzyme “PKC”

Focused on one goal: Developing Novel Therapeutics to tame Cancer

Pharmagap Inc. Profile

PharmaGap Inc., Ottawa, Ontario. TSX.V : GAP, is pursuing pre-clinical development of its lead drug candidate, PhGα1, for use in treating cancer.

PhGα1 selectively targets Protein Kinase C (PKC), a validated target for potentially treating certain types and stages of cancer.

PhGα1’s compelling bioactivity, efficacy and excellent safety profile has been demonstrated in vitro and in animal models. PhGα1 has been developed by way of computer assisted rational drug design.

PharmaGap’s researchers have deep knowledge of cell signaling pathways involved in the onset of cancer, particularly those controlled by the PKC family.

Work is also being pursued developing a pipeline of drug modulators targeting PKC isoforms important in other disease conditions, such as heart disease and diabetes.

PharmaGap’s business model strategy is to out-license its drug compounds targeting PKC prior to commencement of later-stage clinical trials in humans. Management and the board are pursuing this strategy to maximize sustainable value for shareholders.

Founded in 1999, PharmaGap is a spin-out from the National Research Council of Canada, Canada’s premier biological research organization.

The Company’s development activities take place in labs and offices located in Ottawa, Ontario, Canada.

Drug Development

PharmaGap’s Target: Protein Kinase C

PKC is a family of calcium and lipid-activated serine-threonine protein kinases which play a central role in intracellular signal transduction.

PKC isoforms plays a key role in cell replication and differentiation, as well as a key regulatory role at various checkpoints in the cell cycle.

Interest in PKC isoforms and their role in cancer were elevated after the discovery in the late 1980s that PKC is a receptor for tumor-promoting phorbol esters. PKC is implicated in many types and stages of cancer, including the chemotherapy-resistant cancer phenotype (multi-drug resistance, or MDR).

With MDR, cancer cells effectively become immune to chemotherapy over time. MDR is the major cause of chemotherapy failure and manifests itself in all types of cancer. Approximately 500,000 new cases of MDR cancer are expected to develop in the U.S. alone every year.

PKCalpha and Cancer

In healthy tissue, PKC isoforms are widely expressed in normal levels and are necessary and important signaling molecules. However, aberrant over-expression of PKC occurs in many types and stages of cancer, including non-small cell lung cancer, ovarian, breast, colon, certain leukemia’s, neuroblastoma, prostate, non-Hodgkin’s lymphoma, bladder and pancreatic cancer.

In cancer, over-expression of PKC is implicated in malignant transformation and proliferation, faulty apoptosis (cells become effectively immortalized), increased cell migration and cell activation, and desensitizing tumor cells to chemotherapeutic agents (MDR).

Numerous independent studies worldwide have validated PKC as a potential target for cancer therapeutics.

PharmaGap’s Lead Drug Targets PKC

The Company’s lead drug candidate, PhGα1, targets and inhibits the activity of PKC in cancer cells.

This novel drug is representative of a new class of targeted therapeutics now in development by the pharmaceutical industry that are designed to specifically target molecular defects within a cancer cell, rather than killing cancer cells in general via traditional toxic chemotherapeutics.

Last changed at 11-Feb-2009 05:22AM by Highgrader