LymphoSign Inc.

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Envisioning a Cure

With revolutionary targeted therapeutics, LymphoSign has its sights set firmly on the treatment of cancer

Dr. Joseph Elliot, PhD is a man on a mission. No small feat when that mission is the development of ambitious therapeutics for cancer treatment.
Using innovative scientific research and a lean-and-mean business model, Elliot, president and CEO of LymphoSign Inc. (Markham, ON), and Dr. Helmut Thomas, his vice president, Drug Development are developing some of the industry’s most innovative novel proprietary therapeutics for cancer treatment.
Established in 2000, LymphoSign is set to emerge as a serious contender in the Canadian and international biotech industry markets, in the new class of treatments called targeted therapeutics.
LymphoSign’s lead compounds target serious blood-related cancers including acute myeloid leukemia (AML) and acute lymphoblastic leukemia (ALL).
Non-specific cancer treatments, such as chemotherapy, involve powerful drugs that attack all dividing cells including bone marrow, hair follicles and those in the digestive tract, resulting in adverse symptoms that include impaired immunity, nausea and hair loss. Despite the powerful nature of these drugs, many tumours remain untouched or recur. LymphoSign’s treatments take a different approach.
Combined with traditional cancer therapy and rational drug design using computer-assisted molecular modelling (CAMM), LymphoSign has developed a new generation of highly specific drugs called kinase inhibitors that target altered pathways in cancer cells, while dynamically exhibiting low toxicity to normal cells. LymphoSign’s program in non-ATP competitive kinase inhibitors is unique and likely to yield therapeutics whose mechanism of action is different than and complimentary to most kinase inhibitors.
The groundbreaking work of company founder Dr. Chaim Roifman, of Toronto’s Hospital for Sick Children, has enabled LymphoSign to build a solid business foundation on non-ATP competitive inhibitors of auto-inhibited kinases, such as JAK2, IGF-1R, Flt 3, BCR-ABL and VEGF receptors 1, 2 and 3. Drug candidate LS104, the most advanced of these compounds showed promise as a low-toxicity treatment for acute leukemia types AML and ALL. LymphoSign advanced LS104 from the academic laboratory to IND-readiness in 18 months. The IND for LS104 will be submitted by Q2 2006. Some of the unique features of LS104 include (see sidebar):
Furthermore, LymphoSign has screened thousands of compounds in functional assays and synthesized hundreds of NCEs, optimized using CAMM models. The best hits show activity against a panel of acute leukemia cells, as well as solid tumors and achieve cellular IC50s in the nanomolar range against a variety of leukemias. These compounds demonstrate in vivo PK properties and oral bioavailability. Currently, in vivo efficacy studies are underway with human acute leukemia and solid tumour mouse xenograft models. One or two leads will be selected and commence pre-clinical development within six months.
LymphoSign is on the verge of signing an in-licensing agreement for a Phase I clinical candidate targeting all solid tumors. The compound is being licensed from one of the top-five multinational oncology companies and addresses a multi-billion dollar market.
LymphoSign’s main competitive advantage is a world-class management team encompassing skills of molecular design of kinase inhibitors, medicinal chemistry and pre-clinical and clinical drug-development capabilities up to the end of Phase II clinical development.
“We take a great deal of pride in our team,” Elliot says. “ Drug developer Helmut Thomas and molecular modeller, Letica Toledo-Sherman (now a consultant to LymphoSign) are each highly respected individuals at the top of their fields.”
LymphoSign operates in an outsourced business model, with only three full-time employees. This model provides maximum flexibility for financing or M&A transactions.
With a strong foundation, an innovative team of pre-eminent scientific and management professionals and secure financing to assist them on its mission, LymphoSign is poised to take its place as a world leader in the production of cancer therapeutics.


•     Very low toxicity — 28-day GLP toxicity in rats and monkeys complete
•     Shows significant survival advantage in an animal model of AML with the flt3 ITD
•     Short serum half-life — long half-life in target tissues and cancer cells
•     Synergistic with cytotoxic drugs (such as Ara C) currently used to treat AML
•     Easy five-step synthesis of LS104
•     Issued U.S. and U.K. patents; other patents pending
•     IND filing in Q3 2006
•     Clinical trial sites selected — targeting adult AML and ALL

www.lymphosign.com