Here's the press release for the Phgase II diabetes trial:
Ligand Announces Start of Phase II Targretin(TM) Trial In Diabetic Patients Six Months
From Preclinical Data to Human Trials
SAN DIEGO, Calif., March 20 /PRNewswire/ -- Ligand Pharmaceuticals
Incorporated (Nasdaq: LGND) announced today it had initiated Phase II clinical
trial with Targretin(TM) (LGD1069) for type II diabetic patients in Europe.
The purpose of this 12-week trial is to assess the metabolic efficacy,
safety and tolerability of four dose levels of Targretin Oral Capsules in 48
patients with non-insulin dependent diabetes mellitus (NIDDM or type II
diabetes). The trial, to be conducted at multiple sites in Belgium and the
Netherlands, is designed to determine Targretin's potential to positively
impact carbohydrate and lipid metabolism in type II diabetic patients. In
order to determine ideal dosing levels, patients will be randomly assigned to
one of six groups, and will take Targretin in doses ranging from 150 mg to 600
mg per day.
"Ligand's intensive preclinical and clinical trial programs are rapidly
uncovering Targretin's broad range of activity," according to Steven D. Reich,
Senior Vice President, Clinical Research, Ligand Pharmaceuticals. "Clinical
researchers have already explored Targretin's safety and efficacy in over 300
cancer patients and we are eager to more fully explore the compound's
mechanism of action in the management of type II diabetes. We are especially
pleased that in less than six months from reporting key animal data, we have
activated human trials."
"We are excited to be conducting a study involving a new drug to treat
non-insulin dependent type II diabetes," according to Professor Luc Van Gaal
from the University Hospital Antwerp, Belgium, and one of the trial's
principal investigators. "Targretin may act as an insulin sensitizer; insulin
insensitivity or insulin resistance is one of the recently developed pathways
playing a role in the pathophysiology of type II diabetes and is probably
involved in the diabetes associated morbidity. Treating our patients with
this new drug may offer significant benefits over conventional diabetes
treatments." Dr. Van Gaal is also the president of the Belgium Diabetes
Association.
In in vivo preclinical studies, Targretin acted as an "insulin
sensitizer," enabling diabetic mice to use insulin more efficiently and
resulting in 40% glucose reduction, 20% insulin reduction and 30% reduction in
triglyceride levels. These beneficial effects were comparable to those
observed with the thiazolidinedione (TZD) class of drugs, one of which was
found to be efficacious in diabetic patients and recently approved for
marketing in the U.S. by the FDA earlier this year.
Targretin Mechanism of Action
Targretin, a small organic compound discovered by Ligand scientists,
selectively activates a subclass of retinoid receptors called retinoid X
receptors (RXRs). RXR receptors play an important role in regulating cellular
activities, including the enhancement of insulin action and lipid metabolism.
When the RXR receptor is paired to another unique cell receptor,
peroxisome proliferator activated receptor (PPAR) gamma, which is known to be
a target for antidiabetic therapies, activation of the pair causes increased
insulin sensitivity which impacts glucose metabolism and creates an anti-
diabetic effect. Since Targretin binds to the RXR receptor, which is part of
the paired heterodimer RXR/PPAR complex, it, too, influences the way the body
uses insulin, glucose and lipids.
Ligand is developing Targretin in both topical and oral formulations. In
addition to affecting glucose and lipid metabolism, RXRs also play an
important role in other cellular activities, such as programmed cell death or
"apoptosis," a natural process by which the body eliminates unwanted cells.
This unique activity may be involved in the actions of Targretin as an anti-
cancer agent. During the last three years, Targretin has been tested in over
300 cancer patients.
In the oncology arena, Topical Targretin is in pivotal Phase III clinical
trials for the treatment of cutaneous T-cell lymphoma (CTCL). In addition,
Oral Targretin is in pivotal Phase II/III trials for the treatment of CTCL and
is in Phase II/III trials in lung cancer and in Phase II trials for head and
neck cancer, Kaposi's sarcoma, ovarian cancer, prostate cancer and renal cell
cancer.
Ligand Pharmaceuticals, Inc., founded in 1987, is a leader in gene
transcription technology, particularly intracellular receptor (IR) technology,
including retinoids like Targretin, and Signal Transducers and Activators of
Transcription (STATs). Ligand applies IR and STATs technology to the
discovery and development of small molecule drugs to enhance therapeutic and
safety profiles and to address major unmet patient needs in cancer, women's
health and skin diseases, as well as osteoporosis, cardiovascular and
inflammatory diseases.
This statement may contain certain forward looking statements by Ligand
and actual results could differ materially from those described as a result of
factors, including, but not limited to the following. There can be no
assurance that: (a) human clinical trials will result from the preclinical
studies discussed herein; (b) that the preclinical results described herein
will be observed in human patients; (c) that these or any new products under
development by Ligand or any of its partners will receive approval from the
U.S. Food and Drug Administration or other authorities to market any of these
products; (d) that, if approved, there will be a market for the drugs; (e)
that preclinical results will be predictive of any final results. Targretin
is the trademark of Ligand Pharmaceuticals Inc.
If you would prefer to receive Ligand press releases via email, please
inform Ligand at investors@ligand.com and request to be placed on the priority
email list.
SOURCE Ligand Pharmaceuticals Incorporated
CONTACT: Susan Atkins of Ligand Pharmaceuticals, Inc.,
619-550-7687; John Bluth of Fleishman-Hillard, 212-265-9150 |
