Ligand Presents First-in-Human Phase I Data on Lead SARM Molecule LGD-4033 at the International Congress of Endocrinology
SAN DIEGO--
Ligand Pharmaceuticals Incorporated (NASDAQ: LGND) today
announced that data from a Phase I study with its selective androgen
receptor modulator (SARM) LGD-4033 was featured today in a poster
presentation at the 14th International Congress of
Endocrinology in Kyoto, Japan. This Phase I clinical trial was the first
study in humans of LGD-4033, and evaluated the safety, tolerability and
pharmacokinetic profiles of the molecule in a single escalating dose,
double blind, placebo-controlled study in 48 healthy volunteers.
The key findings include:
-- LGD-4033 was well tolerated by healthy male volunteers after single oral
doses up to 22 mg, the highest dose tested. No serious adverse events
(SAE) or clinically significant dose-related adverse events were
reported.
-- Systemic exposure of LGD-4033 increased proportionally with the dose
level after a single oral dose. Sustained systemic exposure was observed
with appreciable plasma levels of LGD-4033 detectable a week post-dose.
LGD-4033's half-life was consistent with a regimen of once-daily oral
dosing.
According to Martin D. Meglasson, Ph.D., Ligand's Vice President
of Discovery Research, "This study with LGD-4033 shows encouraging
safety and pharmacokinetic data in humans consistent with once-daily
oral dosing. Based on this favorable profile, a Phase I multi-dose
clinical trial is being conducted. SARMs are promising drugs to treat
the serious problem of muscle wasting that occurs in patients with a
variety of disorders including frailty, cachexia and sarcopenia in the
elderly."
About LGD-4033
LGD-4033 is a non-steroidal selective androgen receptor modulator
(SARM), expected to produce the therapeutic benefits of testosterone
with improved safety, tolerability and patient acceptance due to
tissue-selective mechanisms of action and oral routes of administration.
Ligand has discovered several orally active, non-steroidal SARM
compounds based on tissue-specific gene expression and other functional,
cell-based technologies. LGD-4033 exhibited desirable in vivo
efficacy on skeletal muscle and bone measurements in animal models of
male hypogonadism and postmenopausal osteoporosis. The clinical
applications for SARMs include the treatment of multiple muscle wasting
disorders (e.g., sarcopenia, cachexia and frailty), the treatment of
osteoporosis, male hypogonadism and female sexual dysfunction.
To view the poster visit Ligand's Web site at http://investors.ligand.com/events.cfm.
About Ligand Pharmaceuticals
Ligand discovers and develops new drugs that address critical unmet
medical needs of patients for a broad spectrum of diseases including
hepatitis, muscle wasting, Alzheimer's, inflammatory diseases, anemia,
COPD, asthma, rheumatoid arthritis and osteoporosis. Ligand's
proprietary drug discovery and development programs are based on
advanced cell-based assays, gene-expression tools, ultra-high throughput
screening and one of the world's largest combinatorial chemical
libraries. Ligand has strategic alliances with major pharmaceutical and
biotechnology companies, including GlaxoSmithKline, Merck, Pfizer,
Roche, Bristol-Myers Squibb, and Cephalon and more than 30 programs are
in various stages of development by its partners.
Caution Regarding Forward-Looking Statements
This news release contains 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 clinical
trials of LGD-4033, other SARM-related drugs, market size and potential,
LGD-4033's profile, efficacy, potency, selectivity, and competitiveness,
and the strength of Ligand's product portfolio. Actual events or results
may differ from our expectations. For example, there can be no assurance
that LGD-4033 or other potential drugs will progress through clinical
development or receive required regulatory approvals within the expected
time lines or at all, that clinical trials will confirm any safety or
other characteristics or profile described in this press release, that
there will be a market of any size for LGD-4033, or that LGD-4033 or any
drugs will be beneficial to patients or 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.
Source: Ligand Pharmaceuticals Incorporated
Released March 29, 2010