” …significant reduction in the Kupperman index following 12 weeks of treatment, which was sustained throughout the 12 months of treatment.”
Efficacy and safety of standard versus low-dose Femarelle (DT56a) for the treatment of menopausal symptoms.
In both groups there was a significant reduction in the Kupperman index following 12 weeks of treatment, which was sustained throughout the 12 months of treatment (p < 0.01). Seventy-six percent of the patients in the SD group reported a decrease in vasomotor symptoms and seventy-eight % in the LD group (NS). This decrease was sustained following 12 months of treatment. There was no change in TSH and sex hormone levels or endometrial thickness during the study period.
“Femarelle treatment in postmenopausal women increases BMD without unwanted estrogenic effect.”
Tofupill/Femarelle (DT56a): a new phyto-selective estrogen receptor modulator- like substance for the treatment of postmenopausal bone loss.
After 12 months of treatment, BMD had increased in the study group by 3.6% in the lumbar spine (P = 0.039) and by 2.0% in the femoral neck (NS). In the low-dose group, BMD had decreased in the lumbar spine by 0.6% (NS) and by 0.6% in the femoral neck (NS). Comparison of the change in bone density between the groups yielded a significant difference for the lumbar spine (P = 0.037). Neither group showed a change in endometrial thickness and sex hormone levels nor reported any side effects of treatment.
“DT56a … unique nature compared to the compounds currently used for postmenopausal osteoporosis by being bone-forming and not only an anti-resorptive agent.”
DT56a stimulates gender-specific human cultured bone cells in vitro.
DT56a stimulated CK and DNA synthesis in both pre- and post-menopausal female Ob with maximal effect at 100 ng/ml for both age groups. In addition, DT56a stimulated ALP in Ob from both pre- and post-menopausal women with maximal effect at lower dose of 50 ng/ml, with higher response of pre-menopausal cells. Raloxifene (Ral) inhibited all DT56a-stimulated changes in Ob from both age groups. DT56a, when given together with E2, completely antagonized E2-stimulated effects demonstrating its nature as a phyto-SERM. DT56a also, dose dependency, stimulated the intracellular levels of [Ca(2+)](i) with maximal effect at 10 ng/ml. Male-derived Ob did not respond to DT56a in any parameter. In summary, DT56a stimulated sex-specifically female-derived Ob, indicating its unique nature
compared to the compounds currently used for postmenopausal osteoporosis by being bone-forming and not only an anti-resorptive agent.
“Treatment with DT56a resulted in a significant reduction in the number and intensity of hot flushes in postmenopausal women… observed within the first month of treatment.”
A prospective study of DT56a (Femarelle®) for the treatment of menopause symptoms.
A statistically significant (p < 0.01) reduction in the number and intensity of hot flushes was experienced after 2 and 4 weeks of DT56atreatment. After 4 weeks of treatment with DT56a, 80.7% of the patients reported that their hot flushes were ‘better’ or ‘much better’. The severity of hot flushes was also reduced by 38% in all study participants and by 36% in women who had experienced more than seven hot flushes per day initially, before treatment.
“DT56a prevents postmenopausal osteoporosis.”
DT56a (Femarelle) stimulates bone formation in female rats.
OVX rats developed noticeable signs of osteoporosis, namely, significant decrease in trabecular bone volume and in trabecular and cortical thickness. DT56a, like oestrogen, restored the bone structure measurements of all tested parameters in the OVX rats to the values obtained in the intact rats. In skeletal tissues, CK activity was elevated in both treatment groups. However, in the uterus DT56a did not activate oestrogen receptors while oestrogen did elevate CK activity.
“Femarelle … inhibits menopausal symptoms without thrombogenicity…”
The selective estrogen receptor modulator DT56a (Femarelle) does not affect platelet reactivity in normal or thrombophilic postmenopausal women
Pretreatment study of all seven women with shortened closure times confirmed abnormalities associated with thrombophilia: four women were heterozygous for the factor V Leiden gene mutation, one was heterozygous for the prothrombin gene mutation, one was found to have protein S deficiency, and one had increased anticardiolipin antibodies. All participants reported improved symptoms during the treatment period. No significant change in closure times was found in the normally clotting participants after 3 or 8 weeks of Femarelle therapy (P > 0.26). No significant change in closure time was seen in the seven thrombophilic women after 3 or 8 weeks or 1 year of Femarelle treatment (P > 0.26). The regression curve for measures over time was not significant (P = 0.26).
” DT56a was effective against symptomatic vulvo-vaginal atrophy (vaginal dryness)…”
A Prospective Study of DT56a (Femarelle®) for the Treatment of Postmenopausal
The main bothersome symptoms were: Dyspareunia- 5 Patients, Vaginal soreness- 3 Patients, Vaginal dryness- 2 Patients, Vaginal irritation-1 Patient and Bleeding with coitus-1 Patient. All patients reported significant improvement in their most bothersome symptom. All women had a significant reduction in vaginal pH. The average pH went from baseline 7.7±2.2 to 4.9±1.4 on week 12, p< 0.0001. The maturation index also improved as shown in the figure below: Parabasal cells that were 100% at entry were 43% following 12 weeks of treatment, Intermediate cells were changed from 0 to 47% and Superficial cells that were 0 at entry, were 10% following 12 weeks of treatment with DT56a (all statistically significant, p< 0.001). A significant improvement was found in UQoL index from mean pre-treatment of 75.4±22.7 points to mean post-treatment of 88.9±26.8, p< 0.001. In the sexual domains of the UQoL there was a significant improvement from 6.5±2 points (mean pre-treatment) to 10.6± 3.2 (mean post-treatment), p< 0.001.
“DT56a decreased menopausal symptoms significantly and in the same degree as HT.”
Efficacy and safety of DT56a compared to hormone therapy in Greek post-
Patients receiving HT and DT56a showed a significant and independent decrease in menopausal symptoms (mean difference in Kupperman score, DT56a group: -3.98, HT group -5.601, no treatment group +1.76, p-value <0.001). Lumbar spine BMD T-score was significantly lower in women receiving no treatment, as opposed to the two treatment arms which showed no significant change (No treatment, baseline: -0.60, final: -0.85, p=0.001; HT, baseline: -84, final -0.99, p=0.79; DT56a, baseline -0.51, final: -0.76, p=0.75). No differences in femoral bone density, ET or mammography classification were detected in any of the treatment arms. Likewise, serum lipids or lipoproteins did not differ between the three