MCHM Macrochem (MM)

MacroChem Reports Positive Results From Clinical Trial of Opterone(R) Topical Testosterone Cream* 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 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/ http://www.newscom.com/cgi-bin/prnh/20050512/NYTH074 http://photoarchive.ap.org/ DATASOURCE: MacroChem Corporation CONTACT: Investor, Bernard Patriacca - VP/CFO of MacroChem Corporation, +1-781-862-4003; Media, Donna L. LaVoie, (LaVoie Group), +1-781-596-0200 ext. 103, for MacroChem Corporation Web site: http://www.macrochem.com/

Copyright