Hey guys, just been scanning the web reading up on things and I came across this new product. I will copy the website jargon cos i cant post links. Any further information you may have would be handy as i haven't dug further.
Fispemifene is a new, selective estrogen receptor antagonist that is being developed as an oral treatment for testosterone deficiency and associated disorders in men. Symptoms of low testosterone include sexual dysfunction, muscle wasting, reduced bone density, lowered energy levels and glucose intolerance. Unlike testosterone replacement therapies, fispemifene utilizes the body's normal feedback mechanism to increase testosterone levels into, but not beyond, the normal range. By blocking estrogen feedback to the pituitary with a drug like fispemifene, the pituitary increases LH and FSH secretion which increases testosterone secretion. As these rising testosterone levels feedback on the pituitary, LH and FSH secretion return toward normal and testosterone reaches a new, albeit higher, steady state level. Based on this mechanism of action, fispemifene is being studied for the treatment of androgen deficiency and associated symptoms. We believe that increased production of testosterone may treat many of the symptoms of low testosterone. In a Phase II study we conducted in hypogonadal men, fispemifene increased total testosterone levels by 78% over 28 days of treatment.
Fispemifene is a selective estrogen antagonist that blocks estrogen effects on pituitary, prostate and breast, but is an estrogen agonist on bone.
Advantages over existing therapies include:
¤ Naturally stimulates testosterone release without blocking regulatory feedback
¤ Blocks adverse estrogen effects on the prostate
¤ Protects and potentially improves bone density
Status: Phase II
Fispemifene's direct effect on tissues other than the hypothalamus and pituitary gland may provide additional benefits in patients with low testosterone. Because fispemifene has selective tissue effects, it has estrogen-blocking effects in some tissue, while having estrogen-like effects in other tissue. For example, fispemifene's direct estrogen blocking effects on breast may be useful in treatment of breast enlargement, while its direct estrogen-like effect on bone may increase bone mass. In addition, we have demonstrated preclinically the estrogen blocking effects of fispemifene on the prostate, which may help reduce certain risks associated with estrogen, including prostate cancer and increase in prostate size.
Clinical Development Program
Fispemifene has completed two Phase I clinical studies in Europe and one Phase II clinical study in the US.
The Phase II study was a randomized, double-blind, placebo-controlled, parallel group study of fispemifene in the treatment of low testosterone in older men. This study enrolled 77 men with low testosterone levels at 23 study sites in the U.S. The primary efficacy parameter was testosterone increases relative to baseline. Safety parameters included assessment of prostate volume in addition to routine safety monitoring. In this study, patient groups treated with 100, 200 and 300 mg doses of fispemifene showed a 60%, 60% and 78% increase in testosterone levels, respectively, compared to baseline, while patients treated with placebo showed a 14% increase in testosterone levels (p<0.05, p<0.01, p<0.001 (fispemifene vs. placebo), respectively). Actual increases in total testosterone ranged from 28.3 ng/dL for placebo to 196.5 ng/dL for 300 mg fispemifene. In all dose-groups the mean testosterone level increased into the normal range of 300 ng/dl to 900 ng/dl. All primary endpoints defined by the study protocol were met and no safety issues were observed.
QuatRx is now conducting additional Phase II studies with fispemifene in patient populations where testosterone has been shown to have a clinical benefit.