|Ligand Earns $2.0 Million Milestone Payment as GlaxoSmithKline Begins Clinical Studies of Oral Drug for Thrombocytopenia|
SAN DIEGO--(BUSINESS WIRE)--Jan. 6, 2003--
SB-497115 is First Oral TPO Growth Factor to Enter Human Development to Complement EPO, G-CSF in Treatment of Blood Deficiencies
Ligand Pharmaceuticals (Nasdaq:LGND) earned in the fourth quarter of 2002 a $2.0 million milestone payment from GlaxoSmithKline (NYSE:GSK), which has begun human trials of SB-497115, an oral, small molecule drug that mimics the activity of thrombopoietin (TPO), a protein factor that promotes growth and production of blood platelets.
There are no approved TPO agents for the treatment or prevention of thrombocytopenias (decreased platelet count). Investigational use of injectable forms of recombinant human TPO has been efficacious in raising platelet levels in cancer patients undergoing chemotherapy, and has led to accelerated hematopoietic recovery when given to stem cell donors. Some of these investigational treatments have not moved forward to registration due to the development of neutralizing antibodies. Thus, Ligand believes a small molecule TPO mimic with no apparent immunogenic potential and oral activity that may facilitate dosing provides an attractive therapeutic profile for a major unmet medical need.
"GSK's decision to move an oral, small molecule TPO growth factor into the clinic is an exciting step forward for patients with thrombocytopenia," said Andres Negro-Vilar, M.D., Ph.D., Ligand's senior vice president for research and development and chief scientific officer. "An oral TPO molecule, if successful, will add a third key component to the hematopoietic factors (EPO, G-CSF) that have proven useful in the treatment of anemias and neutropenias in cancer patients and in those with different hematopoietic disorders. We are also excited about SB-497115 because it is the first product to move into clinical studies from the core technology platform we built around Signal Transducers and Activators of Transcription, or STATs, and joins nine other products currently in human clinical trials from our nuclear receptor drug discovery collaborations."
STATs are a family of proteins that play a key role in the signal transduction pathway for biologically important hormones such as the interferons, interleukins and hematopoietic growth factors. The binding of these hormones to their receptors on the surface of cells triggers the activation of specific STATs. These activated STATs enter the cell nucleus and bind to specific target genes, thereby altering gene expression and affecting physiologic functions such as hematopoiesis (the formation of blood cells) and immune response.
TPO is the major cytokine involved in the formation of megakaryocytes and thrombocytes (platelets). Megakaryocytes are the precursor bone marrow cells from which platelets are derived. TPO has multilineage effects in hematopoiesis, acting in synergy with erythropoietin (EPO) and granulocyte-colony stimulating factor (G-CSF) to enhance proliferation and survival of committed erythroid progenitors and primitive hematopoietic stem cells.
Thrombocytopenia is a common side effect of many chemotherapies and can lead to uncontrolled bleeding, thus representing a significant problem in the treatment of cancer patients. Similarly, thrombocytopenia is commonly seen in patients undergoing myelosuppressive therapies or in those with leukemias or metastatic tumors.
About the GSK-Ligand STAT Collaboration
The GSK-Ligand collaboration began in 1995 to capitalize on Ligand's STAT technology to discover small molecule drugs to control hematopoiesis and treat patients with cancer, anemia or platelet deficiencies. The research phase of the collaboration ended in 2001. GSK is responsible for the development and registration of products resulting from the collaboration, and Ligand may earn milestone payments of up to $8 million as a product moves through development. GSK has exclusive worldwide marketing rights to products resulting from the research, and will pay Ligand royalties on a sliding scale up to low double digits on sales of products that make it to market.
Ligand discovers, develops and markets new drugs that address critical unmet medical needs of patients in the areas of cancer, skin diseases, men's and women's hormone-related diseases, osteoporosis, metabolic disorders, and cardiovascular and inflammatory diseases. Ligand's proprietary drug discovery and development programs are based on its leadership position in gene transcription technology, primarily related to Intracellular Receptors (IRs) and STATs.
Caution Regarding Forward-Looking Statements
This news release contains certain forward-looking statements that involve risks and uncertainties and reflect Ligand's judgment as of the date of this release. These statements include those related to research productivity and discoveries, clinical development, and milestone and royalty payments. Actual events or results may differ from our expectations. There can be no assurance that new drug compounds will be discovered, that drugs will progress through clinical development or receive required regulatory approvals, that future milestones or royalties will be earned, or that any drugs mentioned will be successfully marketed. Additional information concerning these and other risk factors affecting Ligand can be found in prior press releases as well as in public periodic filings with the Securities and Exchange Commission, available via www.ligand.com. Ligand disclaims any intent or obligation to update these forward-looking statements beyond the date of this release. This caution is made under the safe harbor provisions of the Private Securities Litigation Reform Act of 1995.
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Ligand Pharmaceuticals Incorporated
Michael J. Watts, Director, investor relations and
corporate communications, 858/550-7850
SOURCE: Ligand Pharmaceuticals Incorporated
01/06/2003 18:35 EASTERN