|[December 09, 2013]
Ligand Announces Positive Preclinical Data on Small-Molecule G-CSF Receptor Agonist at the 55th Annual Meeting of the American Society of Hematology
SAN DIEGO --(Business Wire)--
Ligand Pharmaceuticals Incorporated (NASDAQ: LGND) announced that
data from preclinical studies on its granulocyte colony stimulating
factor (G-CSF) receptor agonist program were featured in a poster
presentation today at the 55th Annual Meeting of the American
Society of Hematology (ASH) in New Orleans.
In preclinical studies, Ligand evaluated the ability of LGD-7455 to
stimulate neutrophil (white blood cell) counts in cynomolgus monkeys and
investigated the role that metal ions play in the activity of LGD-7455
on the G-CSF receptor (G-CSFR). Additionally, the effects and mechanisms
of LGD-7455 on tumor cell growth were examined.
The key findings include:
LGD-7455 is a novel small-molecule, selective human G-CSFR agonist
that activates the receptor in a manner distinct from native G-CSF,
but similar to the mechanism of small-molecule oral thrombopoietin
receptor (TPOR) agonists.
LGD-7455 significantly increases peripheral blood neutrophils,
demonstrating the first reported proof-of-concept for a small molecule
G-CSFR agonist in a primate model.
LGD-7455 inhibits tumor cell growth and increases apoptosis, mediated
by intracellular metal chelation and an increase in reactive oxygen
"We are pleased to present this scientifically important work from one
of Ligand's internal un-partnered programs," said Matthew W. Foehr,
Chief Operating Officer of Ligand. "Ligand's R&D team continues to make
scientific advancements like this first reported proof-of-concept for a
small molecule G-CSF in a primate model. Further optimization of the
LGD-7455 series may lead to a novel oral anticancer therapy that also
serves as a supportive care agent to treat neutropenia in patients
receiving bone-marrow suppressive treatments. The worldwide market for
injectable G-CSF is currently over $6 billion, and we believe there is a
substantial unmet medical need and market opportunity for a G-CSF
receptor agonist that offers a novel route of administration and
differentiated profile with the potential to have anti-tumor efficacy in
addition to increasing neutrophils."
About Ligand's Small-Molecule Oral G-CSF Program
G-CSF is a glycoprotein growth factor and cytokine produced by different
tissues to stimulate the bone marrow to produce granulocytes andstem
cells. G-CSF acts on its homodimeric receptor, G-CSFR, to stimulate
proliferation of granulocytic progenitor cells and induce their survival
and differentiation into neutrophils. Several biologic versions of
injectable recombinant human G-CSF (e.g., Neupogen®, Neulasta® and
Neutrogin®) are approved to treat chemotherapy-induced neutropenia,
neutropenia associated with hematopoietic stem cell transplantation and
severe chronic neutropenia. The goal of Ligand's G-CSF Program is to
provide a non-peptide, small-molecule, oral G-CSFR agonist that is a
convenient alternative to injectable G-CSF therapy for the treatment of
neutropenia with potential advantages, including anti-tumor activity,
that have not been observed with recombinant G-CSF.
Ligand has previously reported the discovery of a novel series of
molecules, exemplified by LGD-7455, that selectively activate human
G-CSFR function in a manner distinct from G-CSF, but similar to the
mechanism of small-molecule TPOR agonists, such as eltrombopag (Promacta®).
The new preclinical studies find that LGD-7455 is a metal chelator with
anti-proliferative effects on tumor cells. Ligand believes that the use
of metal chelators has potential in anti-cancer treatment, as neoplastic
cells have a high requirement for metal ions, such as iron and copper,
related to their rapid rate of replication. Limiting the availability of
these metal ions to tumor cells or reducing their intracellular content
may be an advantageous strategy to inhibit uncontrolled cancer cell
About Ligand Pharmaceuticals
Ligand is a biopharmaceutical company focused on assembling a large
portfolio of revenue-generating assets through licensing and acquisition
with the goal to generate sustainable cash-flow and profitability.
Ligand has a diverse asset portfolio addressing the unmet medical needs
of patients for a broad spectrum of diseases including thrombocytopenia,
multiple myeloma, diabetes, hepatitis, muscle wasting, dyslipidemia,
anemia and osteoporosis. Ligand's Captisol platform technology is a
patent-protected, chemically modified cyclodextrin with a structure
designed to optimize the solubility and stability of drugs. Ligand has
established multiple alliances with the world's leading pharmaceutical
companies including GlaxoSmithKline, Onyx Pharmaceuticals (a subsidiary
of Amgen Inc.), Merck, Pfizer, Baxter International, Bristol-Myers
Squibb, Lundbeck Inc., Eli Lilly & Co. and Spectrum (News - Alert) Pharmaceuticals.
Please visit www.captisol.com
for more information on Captisol or www.ligand.com
for more information on Ligand.
This news release contains certain forward-looking statements by Ligand
that involve risks and uncertainties and reflect Ligand's judgment as of
the date of this release. These statements include those related to the
use and market potential of LGD-7455 and other metal chelators in
anti-cancer treatment and to treat neutropenia in patients receiving
bone-marrow suppressive treatments. The failure to meet expectations
with respect to any of the foregoing matters may reduce Ligand's stock
price. Additional information concerning risk factors affecting Ligand's
business can be found in prior press releases available via www.ligand.com
as well as in Ligand's public periodic filings with the Securities and
Exchange Commission at www.sec.gov.
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.
Follow Ligand on Twitter (News - Alert) @Ligand_LGND.
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