Next to AP-325 Algiax has discovered novel GABAA receptor modulator
compounds called Thioacrylamide derivatives.
(19,20) However, because estrogen administration can increase the risk of breast and uterine cancer, researchers are instead investigating selective estrogen receptor modulators
A novel selective progesterone receptor modulator
asoprisnil (J867) inhibits proliferation and induces apoptosis in cultured human uterine leiomyoma cells in the absence of comparable effects on myometrial cells.
Pharmacopeia (Princeton, CA), an innovator in the discovery and development of novel small molecule therapeutics, announced that it has licensed from Bristol-Myers Squibb (New York, NY) a selective androgen receptor modulator
(SARM) program, including a lead compound in Phase 1 clinical development and back-up compounds.
"Progesterone receptor modulator
CDB-2914 down regulates proliferative cell nuclear antigen and Bcl-2 protein expression and up-regulates caspase-3 and poly(adenosine 5'-diphosphateribose) polymerase expression in cultured human uterine leiomyoma cells," Journal of Clinical Endocrinology& Metabolism 90(2): 953-961.
Raloxifene is a selective estrogen receptor modulator
, specifically developed to maintain beneficial estrogenic activity on bone and lipids and antiestrogenic activity on endometrial and breast tissue.
Clomiphene, a selective estrogen receptor modulator
(SERM) is one of the most widely used infertility drugs and has long been used to induce ovulation in women trying to conceive.
Today, several medications are available for the prevention or treatment of osteoporosis, such as Evista (raloxifene), a selective estrogen receptor modulator
, or SERM, which is protective against vertebral fractures.
Bristol-Myers was developing a thyroid hormone receptor modulator
for the treatment of obesity.
Many companies hope to develop a designer estrogen, or selective estrogen receptor modulator
(SERM), that men can take to prevent heart disease.
In addition to retaining an ownership interest representing approximately 22.5% of the outstanding shares of common stock of the combined company, the GTx stockholders of record as of immediately prior to the effective time of the merger received contingent value rights entitling the holders to receive, in the aggregate, 75% of any net proceeds derived from the grant, sale or transfer of rights to GTx's selective androgen receptor degrader and selective androgen receptor modulator
technology during the term of the CVR and, if applicable, to receive royalties on the sale of any SARD products by the combined company during the term of the CVR.