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2.5 Grams of Opterone, Applied to Upper Arms and Shoulders, Raised Average
Serum Testosterone Levels of All Patients Into Physiologic Range
LEXINGTON, Mass., May 12 /PRNewswire-FirstCall/ -- MacroChem Corporation
(Nasdaq: MCHM) today announced positive results of a bioavailability study of
Opterone, its investigational topical cream for treatment of male
hypogonadism. Opterone combines 1% testosterone with MacroChem's patented
drug-absorption enhancer, SEPA(R), in a proprietary cream formulation.
According to MacroChem, the results of this randomized, crossover, single-dose
trial in three treatment groups showed that:
-- A single 2.5 gram dose of Opterone (25 mg testosterone), applied to the
upper arms and shoulders, raised the averaged circulating testosterone
levels of all patients into the physiologic range over a 24-hour
period. A 2.5 gram Opterone dose contains half the testosterone in half
the volume of the starting dose of the marketed gels.
-- Average maximum circulating total testosterone level in this 2.5 gram
treatment group was 577 ng/dL, and ranged from 408 to 577 ng/dL across
all three treatment groups. Normal circulating total testosterone
levels typically range from 300 to 1000 ng/dL.
-- Opterone was well tolerated in this trial. All reported adverse events
were mild, with the most common being headache and mild application
site reaction.
(Photo: http://www.newscom.com/cgi-bin/prnh/20050512/NYTH074 )
"The 2.5 gram dose of Opterone, applied to the upper arms and shoulders,
normalized the averaged serum testosterone values in all patients in our trial
over a 24-hour period," said Thomas Chan, PhD, vice president of R & D and
chief technology officer of MacroChem. "By comparison, the lowest doses of
the marketed gels start at 5 grams. To achieve normal serum testosterone
levels with those gel products, some patients may require as much as a 10 gram
dose."
Dr. Chan will present Opterone pharmacokinetic data, including those from
this study, at the 8th International Congress of Andrology, to be held June
12-16, in Seoul, Korea.
"The positive results announced today represent not only a major advance
for the Company's nearest-to-market product and our SEPA technology, but also
validate our new cream formulation as a drug delivery vehicle," noted Robert
J. DeLuccia, president and chief executive officer of MacroChem. "The next
step in our Opterone development plan is a Phase 3 trial."
Mr. DeLuccia said the Company is working to secure the financial resources
necessary to advance the Opterone development program.
* A digital photograph of Opterone is available to the media upon email
request to info@macrochem.com
Opterone Study Details
Study design and population. This Opterone trial was a randomized,
single-dose, crossover study designed to determine the pharmacokinetics (how a
drug is delivered, absorbed, distributed, metabolized and excreted) of
testosterone following administration of 2.5 gm and 5.0 gm of Opterone in
hypogonadal adult males. Other objectives of the clinical trial were to
determine the effects of application surface area and skin site on
bioavailability (extent to which a drug is absorbed into the body) of
testosterone, and to evaluate the safety and local tolerability of Opterone
when applied under the conditions of the trial.
The trial compared one dose of 2.5 gm Opterone applied to the upper arms
and shoulders and one dose each of 2.5 gm and 5.0 gm Opterone applied to the
abdomen. Investigators at two US sites recruited 10 hypogonadal subjects who
ranged in age from 34 to 68 years (mean = 47.9 years), with testosterone
levels between 200 and 300 ng/dL. Mean pretreatment total testosterone level
of the subjects was 241.7 ng/dL. Subjects received one dose of each of the
three test regimens separated by a six-day washout period.
Summary of trial results. All ten patients in the trial were determined
to have attained 24-hour average serum total testosterone concentrations
(Cave) equal to or greater than 300 ng/dL following application of a 2.5 gm
Opterone dose to their upper arms and shoulders, with a mean Cave of 382
ng/dL. A 2.5 gm dose applied to the abdomen normalized Cave values of
circulating testosterone in four of ten patients, with a mean serum total
testosterone Cave of 308 ng/dL. A 5 gm dose applied to the abdomen normalized
Cave values of circulating testosterone in nine of the ten patients, with a
mean serum total testosterone Cave of 366 ng/dL. Across all treatment groups,
mean total testosterone Cmax (maximum observed serum concentration) values
ranged from 408 to 577 ng/dL, and mean Tmax (time to Cmax) values ranged from
11 to 19 hours.
Hypogonadism: Description, prevalence. Testosterone is the male hormone
essential for sperm production and the development and maintenance of male
sexual characteristics, including muscle mass and strength, fat distribution,
bone mass and sex drive. Male hypogonadism is most often defined as having
total testosterone serum levels of 300 ng/dL or less, with associated
symptoms. Hypogonadal men are typically treated either with topical
testosterone gels or patches, or injections. There is currently no oral
testosterone product approved in the U.S. for treating hypogonadism.
The Endocrine Society estimates that between 4 and 5 million men in the
U.S. suffer hypogonadism, although only about 5% currently receive replacement
therapy. Despite the historically low rates of hypogonadism diagnosis, annual
sales of testosterone replacement products have been estimated at about one-
half billion dollars in the U.S. alone.
About MacroChem
MacroChem is a specialty pharmaceutical company that innovates, develops
and commercializes pharmaceuticals administered in novel ways, to treat
important medical conditions. MacroChem is developing two products containing
its patented enhancer, SEPA(R): Opterone(R), and EcoNail(TM), a SEPA-enhanced
antifungal nail lacquer to treat a common and potentially debilitating nail
infection known as onychomycosis. For more information on MacroChem, and its
technology and products, please visit our website at:
http://www.macrochem.com .
Forward-Looking Statements
With the exception of historical information contained in this press
release, the matters described herein are forward-looking statements that
involve risks and uncertainties. MacroChem's actual results may differ
significantly from the results discussed in the forward-looking statements.
Factors that might cause such a difference include, but are not limited to,
those discussed or referred to in the section entitled "Risk Factors" in
MacroChem's Annual Report on Form 10-K, as well as those discussed elsewhere
therein, and include, without limitation, risks regarding product development,
the timing and results of clinical trials, the regulatory approval process,
capital requirements, financial condition, patent protection and dependence on
third parties for development and licensing arrangements. Readers are
cautioned not to place undue reliance on these forward-looking statements,
which speak only as of the date hereof. MacroChem undertakes no obligation to
update publicly any forward-looking statements, whether as a result of new
information, future events or otherwise. For more information visit our
website, http://www.macrochem.com
SOURCE MacroChem Corporation
Web Site: http://www.macrochem.com
Serum Testosterone Levels of All Patients Into Physiologic Range
LEXINGTON, Mass., May 12 /PRNewswire-FirstCall/ -- MacroChem Corporation
(Nasdaq: MCHM) today announced positive results of a bioavailability study of
Opterone, its investigational topical cream for treatment of male
hypogonadism. Opterone combines 1% testosterone with MacroChem's patented
drug-absorption enhancer, SEPA(R), in a proprietary cream formulation.
According to MacroChem, the results of this randomized, crossover, single-dose
trial in three treatment groups showed that:
-- A single 2.5 gram dose of Opterone (25 mg testosterone), applied to the
upper arms and shoulders, raised the averaged circulating testosterone
levels of all patients into the physiologic range over a 24-hour
period. A 2.5 gram Opterone dose contains half the testosterone in half
the volume of the starting dose of the marketed gels.
-- Average maximum circulating total testosterone level in this 2.5 gram
treatment group was 577 ng/dL, and ranged from 408 to 577 ng/dL across
all three treatment groups. Normal circulating total testosterone
levels typically range from 300 to 1000 ng/dL.
-- Opterone was well tolerated in this trial. All reported adverse events
were mild, with the most common being headache and mild application
site reaction.
(Photo: http://www.newscom.com/cgi-bin/prnh/20050512/NYTH074 )
"The 2.5 gram dose of Opterone, applied to the upper arms and shoulders,
normalized the averaged serum testosterone values in all patients in our trial
over a 24-hour period," said Thomas Chan, PhD, vice president of R & D and
chief technology officer of MacroChem. "By comparison, the lowest doses of
the marketed gels start at 5 grams. To achieve normal serum testosterone
levels with those gel products, some patients may require as much as a 10 gram
dose."
Dr. Chan will present Opterone pharmacokinetic data, including those from
this study, at the 8th International Congress of Andrology, to be held June
12-16, in Seoul, Korea.
"The positive results announced today represent not only a major advance
for the Company's nearest-to-market product and our SEPA technology, but also
validate our new cream formulation as a drug delivery vehicle," noted Robert
J. DeLuccia, president and chief executive officer of MacroChem. "The next
step in our Opterone development plan is a Phase 3 trial."
Mr. DeLuccia said the Company is working to secure the financial resources
necessary to advance the Opterone development program.
* A digital photograph of Opterone is available to the media upon email
request to info@macrochem.com
Opterone Study Details
Study design and population. This Opterone trial was a randomized,
single-dose, crossover study designed to determine the pharmacokinetics (how a
drug is delivered, absorbed, distributed, metabolized and excreted) of
testosterone following administration of 2.5 gm and 5.0 gm of Opterone in
hypogonadal adult males. Other objectives of the clinical trial were to
determine the effects of application surface area and skin site on
bioavailability (extent to which a drug is absorbed into the body) of
testosterone, and to evaluate the safety and local tolerability of Opterone
when applied under the conditions of the trial.
The trial compared one dose of 2.5 gm Opterone applied to the upper arms
and shoulders and one dose each of 2.5 gm and 5.0 gm Opterone applied to the
abdomen. Investigators at two US sites recruited 10 hypogonadal subjects who
ranged in age from 34 to 68 years (mean = 47.9 years), with testosterone
levels between 200 and 300 ng/dL. Mean pretreatment total testosterone level
of the subjects was 241.7 ng/dL. Subjects received one dose of each of the
three test regimens separated by a six-day washout period.
Summary of trial results. All ten patients in the trial were determined
to have attained 24-hour average serum total testosterone concentrations
(Cave) equal to or greater than 300 ng/dL following application of a 2.5 gm
Opterone dose to their upper arms and shoulders, with a mean Cave of 382
ng/dL. A 2.5 gm dose applied to the abdomen normalized Cave values of
circulating testosterone in four of ten patients, with a mean serum total
testosterone Cave of 308 ng/dL. A 5 gm dose applied to the abdomen normalized
Cave values of circulating testosterone in nine of the ten patients, with a
mean serum total testosterone Cave of 366 ng/dL. Across all treatment groups,
mean total testosterone Cmax (maximum observed serum concentration) values
ranged from 408 to 577 ng/dL, and mean Tmax (time to Cmax) values ranged from
11 to 19 hours.
Hypogonadism: Description, prevalence. Testosterone is the male hormone
essential for sperm production and the development and maintenance of male
sexual characteristics, including muscle mass and strength, fat distribution,
bone mass and sex drive. Male hypogonadism is most often defined as having
total testosterone serum levels of 300 ng/dL or less, with associated
symptoms. Hypogonadal men are typically treated either with topical
testosterone gels or patches, or injections. There is currently no oral
testosterone product approved in the U.S. for treating hypogonadism.
The Endocrine Society estimates that between 4 and 5 million men in the
U.S. suffer hypogonadism, although only about 5% currently receive replacement
therapy. Despite the historically low rates of hypogonadism diagnosis, annual
sales of testosterone replacement products have been estimated at about one-
half billion dollars in the U.S. alone.
About MacroChem
MacroChem is a specialty pharmaceutical company that innovates, develops
and commercializes pharmaceuticals administered in novel ways, to treat
important medical conditions. MacroChem is developing two products containing
its patented enhancer, SEPA(R): Opterone(R), and EcoNail(TM), a SEPA-enhanced
antifungal nail lacquer to treat a common and potentially debilitating nail
infection known as onychomycosis. For more information on MacroChem, and its
technology and products, please visit our website at:
http://www.macrochem.com .
Forward-Looking Statements
With the exception of historical information contained in this press
release, the matters described herein are forward-looking statements that
involve risks and uncertainties. MacroChem's actual results may differ
significantly from the results discussed in the forward-looking statements.
Factors that might cause such a difference include, but are not limited to,
those discussed or referred to in the section entitled "Risk Factors" in
MacroChem's Annual Report on Form 10-K, as well as those discussed elsewhere
therein, and include, without limitation, risks regarding product development,
the timing and results of clinical trials, the regulatory approval process,
capital requirements, financial condition, patent protection and dependence on
third parties for development and licensing arrangements. Readers are
cautioned not to place undue reliance on these forward-looking statements,
which speak only as of the date hereof. MacroChem undertakes no obligation to
update publicly any forward-looking statements, whether as a result of new
information, future events or otherwise. For more information visit our
website, http://www.macrochem.com
SOURCE MacroChem Corporation
Web Site: http://www.macrochem.com
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