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 overwhelms 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
trials 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;
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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;
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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.
CONTACT:
Nichol Harber
Genta Investor Relations
info@genta.com
908-286-3980
