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ASCEND Therapeutics, Inc. Acquires North American Product Rights; New Estrogen Inhibitor In Phase II Clinical Development

10/19/2005 5:09:56 PM

HERNDON, Va.--(BUSINESS WIRE)--Feb. 5, 2004--ASCEND Therapeutics, Inc. (ASCEND) announced today that it has obtained exclusive North American development, marketing and commercialization rights to the developmental pharmaceutical product, TamoGel(TM) (4-hydroxytamoxifen gel), a new estrogen inhibitor under investigation for a variety of estrogen-dependent conditions, including cyclic breast pain and gynecomastia. TamoGel(TM) is formulated using Enhanced Hydroalcoholic Gel (EHG(TM) Technology. This technology enables percutaneous delivery of drugs that cannot be delivered orally.

TamoGel(TM) is an example of how a patient-friendly percutaneous gel can deliver the clinical promise of undeveloped molecules. 4-hydroxytamoxifen, the active ingredient in TamoGel(TM), is a potent estrogen inhibitor that cannot be taken orally due to high first-pass liver metabolism. The use of the innovative EHG(TM) technology as a delivery vehicle for 4-hydroxytamoxifen has enabled the clinical development of this promising, but previously undeveloped molecule, now in Phase II trials. TamoGel(TM), along with its intellectual property, was acquired by ASCEND from Besins International Holdings, the leading manufacturer of prescription gels in the world.

"We are very pleased to announce the acquisition of TamoGel(TM)," noted Jay Bua, Chief Executive Officer of ASCEND Therapeutics, "as we firmly believe that we have the potential to create a standard of care for two large areas of unmet medical need: cyclic breast pain in premenopausal women and gynecomastia in men receiving therapy for prostate cancer. Both of these conditions are estrogen-dependent diseases of the breast."

A New Estrogen Inhibitor in Transdermal Gel Form

TamoGel(TM) is a percutaneously applied gel formulation of the anti-estrogen 4-hydroxytamoxifen (4-OHT), the most active metabolite of tamoxifen. 4-OHT has been shown to be up to 100 times more potent than tamoxifen in inhibiting breast cancer cell proliferation in vitro. 4-OHT cannot be delivered orally, however, because it is rapidly inactivated by the liver following oral administration. Using EHG(TM) Technology, 4-OHT has been formulated for transdermal delivery as a gel. The gel is applied daily by the patient to the surface of the breast. The EHG(TM) gel is fast-drying (less than 2 minutes), non-greasy and can easily be incorporated into morning hygiene habits. EHG(TM) Technology enhances the penetration of 4-OHT into the skin and allows the skin itself to become the reservoir of drug release.

EHG(TM) is a proven technology that is currently used in AndroGel®, the leading testosterone replacement therapy in the world. EHG(TM) Technology effectively creates an "invisible patch" that patients can apply almost anywhere on the body. Unlike transdermal patches, which need to be concealed and can cause skin irritation, EHG(TM) gels are completely invisible after drying. The advantages of percutaneous administration of 4-OHT include avoidance of first-pass liver metabolism, greater bioavailability and the ability to target the desired tissue/area of medical need. Local, transdermal application of TamoGel(TM) may be able to provide adequate tissue concentration of 4-OHT while keeping systemic levels low, thus avoiding unwanted side effects.

Cyclic Breast Pain

Menstrual-cycle related cyclic breast pain (also called cyclical mastalgia) is a common problem in both primary care and breast surgery clinics. Studies have indicated that approximately 68% of women ages 18-44 experience cyclic breast symptoms, and 22% of women suffer from moderate to severe breast pain. While mild premenstrual discomfort lasting 1-4 days per month is considered normal, moderate to severe cyclic breast pain is a more prolonged and debilitating disorder which can disrupt daily activities.

Tamoxifen, which is taken orally and is approved for the treatment and prevention of breast cancer, has been shown to be effective in treating cyclic breast pain in clinical studies. However, safety and tolerance concerns limit its acceptance for the treatment of benign disease, particularly among premenopausal women. Tamoxifen is taken orally and circulates systemically throughout the body. Systemic tamoxifen can result in the onset of serious adverse events, such as deep vein thrombosis, pulmonary embolism, endometrial cancer and the premature onset of menopausal symptoms.

TamoGel(TM) is currently being evaluated in an international multicenter Phase II trial to assess its efficacy in reducing or eliminating cyclic breast pain. Previous clinical trials for TamoGel(TM) have shown it to be biologically active in the breast tissue of women with locally invasive breast cancer, with systemic exposure that is 9-fold lower than that of oral tamoxifen.

Mr. Bua commented, "We believe that an estrogen inhibitor that can be locally effective in the breast tissue while minimizing systemic exposure may provide a safe, tolerable and more effective option for cyclic breast pain. Because of this local activity and low systemic exposure, there is a strong clinical rationale for assessing TamoGel(TM) in a variety of estrogen-dependent conditions."

TamoGel(TM) Clinical Development Program

An international multicenter Phase II trial is currently underway to assess the effect of TamoGel(TM) on cyclic breast pain. A second multicenter, Phase II trial is evaluating the ability of TamoGel(TM) to reduce breast density. Both trials are scheduled for completion in mid-2004. In addition to the treatment of cyclic breast pain, ASCEND plans to investigate the use of TamoGel(TM) for the treatment and prevention of certain other estrogen-dependent benign breast diseases in both women and men. As part of this program, ASCEND is currently launching its development plan to assess the effect of TamoGel(TM) in reducing gynecomastia in men receiving hormonal therapy for prostate cancer.

Approximately 1.6 million men in the U.S. have prostate cancer, the majority of whom will receive hormonal therapy as adjuvant therapy for locally advanced disease or as primary therapy for metastatic disease. These regimens commonly cause breast enlargement (gynecomastia) and/or breast pain. Rates of these adverse effects vary by regimen, but can be as high as 73% in some patient groups). ASCEND plans to evaluate the efficacy of TamoGel(TM) in treating gynecomastia associated with anti-androgen prostate cancer therapy.

ASCEND Therapeutics

Formed in 2001, ASCEND ( is an emerging biopharmaceutical company focused on the use of transdermal drug delivery technology to overcome therapeutic barriers and thereby raise the standard of care for certain chronic conditions.

BESINS International Holdings

Besins International Holdings is a successful European pharmaceutical company, focused in women's and men's health. Besins, the largest manufacturer of prescription hydroalcoholic gels in Europe, is a privately-held company headquartered in Belgium, with revenue of more than $100 million and 300 employees, including manufacturing and sales. Among the company's products approved and marketed in the U.S. and/or Europe are: AndroGel® (first FDA-approved testosterone gel, sold by Solvay), Oestrogel® (HRT), Prometrium® (HRT), Andractim® (Hypogonadism and Gynecomastia), Progestogel(TM) (Cyclic Breast Pain) and Percutalgine(TM) (Sports Therapy).


LaVoie Strategic Communications Group, Inc. Paul Kidwell, 781-596-0200 X104 Sr. Vice President

Source: ASCEND Therapeutics

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