Profile: Supergen Inc (SUPG.O)

SuperGen, Inc., incorporated in March 1991, is a pharmaceutical company engaged primarily to the discovery and development of therapies to treat patients with cancer. The Company acquires products developed by other companies and applies additional developmental effort to expand sales or advance these products clinically towards approval for marketing. The Company’s primary developmental efforts revolve around the products progressing out of its acquisition of Montigen Pharmaceuticals, Inc. (Montigen), a small-molecule drug discovery company. The Company initiated Phase I in-human clinical trials and Phase Ib clinical trials for the first Montigen product, MP-470, a deoxyribonucleic acid (DNA) repair suppressor. In November 2008, the Company received clearance to proceed with clinical trials for a second internally developed product, SGI-1776, a PIM kinase inhibitor.

MP-470

MP-470 is a multi-targeted Tyrosine Kinase Inhibitor that inhibits mutant forms of c-kit, PDGFRa, and FLT3. These protein kinase targets are involved in the growth and proliferation of cancer cells. MP-470 is also a suppressor of Rad 51, a repair protein, which is involved in resistance to a variety of chemotherapy agents and radiation.

SGI-1776 Pim Kinase Inhibitor

Pim kinases are proteins that play a pivotal role in cancer cells. The Company’s Pim kinase inhibitor blocks the pro-survival activity of Pim kinases, allowing these potentially malignant cells to self-abort. SuperGen, Inc.’s investigational new drug (IND) for SGI-1776 received clearance from the United States Food and Drug Administration (FDA) in November 2008, and it is initiating a Phase I clinical trial to evaluate the safety, tolerability and pharmacokinetic profile of SGI-1776.

MP-529

The ability of cancer cells to rapidly divide weighs heavily on the functional machinery of cell division, such as the centrosome and spindle apparatus. If this machinery is rendered nonfunctional, the cancer cells cannot proliferate. Aurora A kinase is a protein that regulates the organization of this cell division machinery. SuperGen, Inc.’s Aurora kinase inhibitor (MP-529) was designed to block the action of Aurora A kinase, thus disrupting the machinery of cell division vital for cancer survival.

S-110 (Formerly S-110)—DNMT1 Inhibitor

The Company has developed a compound called S-110. This targets and blocks the mechanism, by which methylation occurs, thus allowing tumor suppressor genes to remain on. SGI-110 is = in the pre-clinical development stage.

SGI-1252— JAK2 Inhibitor

Janus kinases (JAK) are a family of non-receptor intracellular tyrosine kinases that transduce signaling from type I and II cytokine receptors, which possess no catalytic kinase activity, to the signal transducers and activators of transcription (STAT) proteins, which translocate into the nucleus to initiate the growth and differentiation programs associated with the various receptor cytokine complexes. The JAK/STAT pathways play an important role in an array of cellular processes, including cell survival, proliferation, differentiation and apoptosis. Activation of JAK kinases through mutation or aberrant signaling has been associated with disease progression in immune disorders, myeloproliferative disorders, and cancers. SGI-1252 is an inhibitor of the JAK2 kinase that the Company has designed to modulate the JAK/STAT pathway in cancer cells. SGI-1252 is in the pre-clinical development stage.

The Company competes with ArQule, Array BioPharma, Astex Tx, Avalon, Crystal Genomics, Exelixis, Infinity, SGX, Millennium, Sanofi-Aventis, Bristol-Myers Squibb Company, Celgene, Eli Lilly & Co., GlaxoSmithKline, Novartis AG and Pfizer.