Genta Completes Initial Clinical Dosing of G4544, a New Oral Drug for Bone Diseases Safety Analysis Shows Good Tolerance with No Serious Adverse Reactions
BERKELEY HEIGHTS, NJ – November 15, 2007 – Genta
Incorporated (NASDAQ: GNTA) released findings from the initial
clinical dosing of G4544, the Company’s proprietary small
molecule that is intended as a treatment for diseases associated
with accelerated bone loss. The Phase 1 study, which was conducted
in normal volunteers, has shown good tolerance with oral
bioavailability of the active ingredient, and an excellent safety
profile without serious adverse reactions. The findings were
released in an abstract published in the proceedings of the
upcoming annual meeting of the American Society of
Hematology.
G4544 is a new tablet formulation using delivery technology
developed by Emisphere Technologies, Inc. that enables oral
absorption of the active ingredient contained in Ganite®
(gallium nitrate injection). Ganite® is marketed by Genta and
approved in the U.S. for treatment of cancer-related hypercalcemia
that is resistant to hydration. Low doses of the active ingredient
in Ganite administered by intravenous or subcutaneous injections
have shown clinical activity in a range of skeletal diseases,
including hypercalcemia, bone metastasis (myeloma and breast
cancer), Paget’s disease, and osteoporosis.
The initial clinical trial was a Phase 1 study of escalating single
doses of G4544 in 30 normal volunteers. The endpoints of the study
were to determine safety and to assess pharmacokinetics and oral
bioavailability. The drug was tested over a dosing range of the
active ingredient from 30 to 150 mg, and no adverse effects
attributable to G4544 were observed in this study. Initial analysis
of plasma samples of low doses showed that the active ingredient
was absorbed after oral administration. Complete pharmacokinetic
assessment of higher dose levels is pending further analyses.
“G4544 offers both ease of administration and patient
convenience that could considerably expand the usefulness of this
highly active class of compounds,” said Dr. Raymond P.
Warrell, Jr., Chairman and Chief Executive Officer of Genta.
“Further analysis of these data, combined with additional
preclinical and toxicology work, should enable the multi-dose
studies that will be needed to seek regulatory approval in a range
of bone diseases. Obviously, the previously published clinical
activity of the active ingredient at low doses is a major advantage
for future clinical development.”
About G4544
G4544 is one of a class of gallium-containing compounds that were
originally developed by the U.S. National Cancer Institute. In
investigational studies, high doses of gallium nitrate demonstrated
consistent antitumor activity in patients with non-Hodgkin’s
lymphoma. However, experimental work by Genta personnel and others
established that lower doses of gallium directly inhibited calcium
release from bone, principally by decreasing bone resorption and
possibly by also stimulating bone formation.
Many diseases are associated with accelerated bone loss, including
osteoporosis, cancer, and Paget’s disease. In some diseases,
the rate of loss is slow and subtle, while in others the rate is
rapid and acutely life-threatening. In osteoporosis, the most
prevalent bone- losing condition, the process of bone loss extends
over many years before the disease becomes evident. Conversely, in
cancer-related hypercalcemia, bone loss is so rapid that it overwhe
lms the kidney’s ability to eliminate calcium from the blood,
and this condition can quickly become lethal. In patients with
cancer-related hypercalcemia who were resistant to hydration,
randomized double-blind trials have been conducted with Ganite
compared with calcitonin and with two bisphosphonates (etidronate
[Didronel®; Proctor and Gamble] and pamidronate [Aredia®;
Novartis, Inc.]). G4544 was developed to enable extended
administration of the active ingredient in Ganite, which may
greatly improve patient convenience and avoid the current need for
intravenous pumps or hospitalization. The initial focus of clinical
studies with G4544 will be to evaluate bioequivalence with the
intravenous product, potentially enabling rapid regulatory approval
of the oral formulation. Genta holds or has exclusively licensed
the intellectual property related to G4544.
About Genta
Genta Incorporated is a biopharmaceutical company with a
diversified product portfolio that is focused on delivering
innovative products for the treatment of patients with cancer. Two
major programs anchor the Company’s research platform:
DNA/RNA-based Medicines and Small Molecules. Genasense®
(oblimersen sodium) Injection is the Company's lead compound from
its DNA/RNA Medicines program. Genta is currently recruiting
patients to the AGENDA Trial, a global Phase 3 trial of Genasense
in patients with advanced melanoma. The leading drug in
Genta’s Small Molecule program is Ganite® (gallium
nitrate injection), which the Company is exclusively marketing in
the U.S. for treatment of symptomatic patients with cancer related
hypercalcemia that is resistant to hydration. The Company has
developed G4544, an oral formulation of the active ingredient in
Ganite, that has recently entered clinical tria ls as a potential
treatment for diseases associated with accelerated bone loss.
Ganite® and Genasense® are available on a
“named-patient” basis in countries outside the United
States. For more information about Genta, please visit our website
at: www.genta.com.
Safe Harbor
This press release may contain forward-looking statements with
respect to business conducted by Genta Incorporated. By their
nature, forward-looking statements and forecasts involve risks and
uncertainties because they relate to events and depend on
circumstances that will occur in the future. Forward-looking
statements include, without limitation, statements about:
· the Company’s ability to obtain
necessary regulatory approval for Genasense® from the U.S. Food
and Drug Administration (“FDA”) or European Medicines
Agency (“EMEA”);
· the safety and efficacy of the Company’s
products or product candidates;
· the Company’s assessment of its clinical
trials;
· the commencement and completion of clinical
trials;
· the Company’s ability to develop,
manufacture, license and sell its products or product
candidates;
· the Company’s ability to enter into and
successfully execute license and collaborative agreements, if
any;
· the adequacy of the Company’s capital
resources and cash flow projections, and the Company’s
ability to obtain sufficient financing to maintain the
Company’s planned operations;
· the adequacy of the Company’s patents
and proprietary rights;
· the impact of litigation that has been brought
against the Company and its officers and directors and any proposed
settlement of such litigation;
· the Company’s ability to retain
compliance with the NASDAQ’s listing qualifications;
and
· the other risks described under Certain Risks
and Uncertainties Related to the Company’s Business, as
contained in the Company’s Annual Report on Form 10-K and
Quarterly Report on Form 10-Q.
The Company does not undertake to update any forward-looking
statements. There are a
number of factors that could cause actual results and developments
to differ materially. For a
discussion of those risks and uncertainties, please see the
Company's Annual Report on Form
10-K for 2006 and its most recent quarterly report on Form
10-Q.
SOURCE: Genta Incorporated
CONTACT:
Nichol Harber
Genta Investor Relations
info@genta.com
Brian Korb
The Trout Group
908-286-3980
Posted: November 2007
