Estrogen levels gradually rise leading to unwanted clinical effects in aging men. Estrogens may promote benign enlargement of the prostate called benign prostatic hyperplasia, BPH; initiate prostate cancer; and, cause gynecomastia.

Testosterone levels decrease in aging men. Testosterone is the predominant androgen in men. It is important for mental well-being and for masculine characteristics, such as muscle size and strength, bone strength, sexual interest, potency, fertility, and hair loss.

What are hormone receptors?
Hormone receptors are sites located in hormonally sensitive tissues. Once a hormone binds with its receptor, a series of intracellular events occur that results in estrogenic or androgenic tissue depending on the hormone.

What is a steroid?
Natural or synthetic hormones known as steroids, have been used to stimulate androgen or estrogen receptors.

What is a nonsteroidal receptor modulator?
A drug that is a small molecule, not a steroid, that can either block or stimulate the same hormone receptor is called a receptor modulator. If it can block or stimulate a receptor in a tissue-selective manner, it may be able to mimic the beneficial and at the same time minimize the unwanted effects of the natural or synthetic steroidal hormones.

What is a SERM?
A selective estrogen receptor modulator, or SERM, is a small molecule that binds to and selectively modulates estrogen receptors. These molecules have the ability to either stimulate or block estrogen's activity in different types of tissue:

What is a SARM?
A selective androgen receptor modulator, or SARM, is a small molecule that binds to and selectively modulates androgen receptors depending on tissue type. In men, SARMs may be able to:

What is PIN?
Precancerous prostate lesions, know as high grade prostatic intraepithelial neoplasia, or high grade PIN, are detected in approximately 10% of the patients who undergo biopsies looking for prostate cancer.

Scientific evidence has shown patients with high grade PIN are at high risk for prostate cancer. Prostate cancer is found in approximately 30%-70% of high grade PIN patients within one year of diagnosis and in 45% to 80% of high grade PIN patients within 5 years. The primary endpoint of our Phase IIb clinical trial for the prevention of prostate cancer in high risk men was the incidence of prostate cancer. This is the largest prospective study to determine the natural history of patients with high grade PIN and supports the premise that high grade PIN patients have a high risk for developing prostate cancer.

Treating men with high grade PIN reduces the incidence of prostate cancer.

What is ADT?
The standard medical treatment for patients who have advanced, recurrent or metastatic prostate cancer is androgen deprivation therapy, or ADT, which reduces blood levels of testosterone, the growth factor for prostate cancer. ADT is accomplished either surgically by removal of the testes, or chemically by treatment with luteinizing hormone releasing hormone agonists, known as LHRH agonists.

How do LHRH agonists work?
LHRH agonists work by shutting off luteinizing hormone secretion by the pituitary gland, which stops testosterone production by the testes. Examples of commercially marketed LHRH agonists are Lupron®, Zoladex® and Eligard®.

What is Cancer Cachexia?
Cancer Cachexia is defined as the unintentional loss of over 5% of a patient's original lean body weight, which can result in weakness, fatigue, immobility and even death.

Cancer causes the body to go into a starvation-like state that causes cachexia. Muscle wasting, weight loss from cancer, or cancer cachexia, is diagnosed in approximately one-third of newly-diagnosed cancer patients and accounts for approximately 20% of cancer deaths. Testosterone normally serves to increase lean body weight.