NEW aromatase inhibitor

[~HOUNDOG~]

MPV-2213ad
Synonyms:

Finrozole
Drug Class:

Hormonal Agents
Drug Approval Status:

Phase 1
Description:

MPV-2213ad blocks the activity of aromatase, a protein needed for the conversion of testosterone and other androgens to estrogen, and could be useful in the treatment of estrogen-dependent diseases like breast cancer. In two Phase I clinical trials, varying doses of MPV-2213ad were given to healthy male volunteers. A significant decrease in estrogen levels was noted in the volunteers. An increase in testosterone and follicle-stimulating hormone levels was also observed. There is no clinical data regarding its potential role in the treatment of estrogen-responsive breast cancer.
Side Effects:

Overall, MPV-2213ad appears to be well-tolerated. Side effects included hot flashes, nausea, dizziness, acne and gastrointestinal discomfort.
How Taken:

This drug can be taken orally.
Pharmaceutical Companies:

 

[Mike P.T.]

hmmm wonder if its more powerful that arimidex or aromasin?(i think thats how u spell it)

 

[Diesil]

bump fo rmore knowledge on the product vs. arimidex

 

[ORANGE_JUICER]

bump, i love all these new aromatise inhibitors, i know one of them will eventually help my mild gyno.

 

[Zyglamail]

There are a lot of em out that are as good if not better than anastrozole, they are just hard to come by. FOr those interested, here is more reading.

Acute inhibition of oestrogen biosynthesis does not affect serum leptin levels in young men.

Luukkaa V, Rouru J, Ahokoski O, Scheinin H, Irjala K, Huupponen R.

Department of Pharmacology, University of Turku, and Clinical Pharmacology Unit, Turku University Central Hospital, FIN-20520 Turku, Finland. [email protected]

OBJECTIVE: Leptin plays an important role in the regulation of reproduction. To explore the contribution of oestradiol to serum leptin levels in men, we measured the concentrations of serum leptin and insulin after inhibition of oestrogen biosynthesis by selective blockade of the aromatase enzyme. DESIGN: The study had a double-blind parallel group design. METHODS: The aromatase inhibitor, MPV 2213ad, was given to eight healthy male volunteers as a single dose of 100mg. Eight men received placebo. Serum leptin and insulin were determined from blood samples collected at 0800h, 1600h and 2000h both on the actual test day (day 0) and on the previous day (day -1), and from single blood samples taken in the morning of days 1, 2, 4 and 7. Changes in serum leptin were correlated with those seen in serum oestradiol, testosterone, LH, FSH, cortisol and aldosterone, which were determined earlier. RESULTS: After the aromatase inhibitor administration, mean serum oestradiol concentration was reduced by 74% from the baseline compared with a 19% reduction in the placebo group (P for difference <0.001), and returned to pre-treatment levels within four days. Despite marked changes in serum oestradiol and sustained elevations in serum testosterone, LH and FSH concentrations, serum leptin concentrations were similar in the group receiving the aromatase inhibitor and in the placebo group. We found a weak correlation between serum oestradiol and leptin, which could not be reproduced when the percentage changes in these variables were analysed. CONCLUSION: Marked short-term reduction in serum oestradiol concentration has no effect on serum leptin levels in young men.

and more...........

A double-blind study of MPV-2213ad, a novel aromatase inhibitor, in healthy male subjects.

Ahokoski O, Irjala K, Huhtala S, Salminen E, Scheinin H, Huupponen R.

Department of Pharmacology and Clinical Pharmacology, University of Turku, Turku University Central Hospital, Finland. [email protected]

OBJECTIVE: Novel aromatase inhibitors are developed with requirements of high potency and selectivity for the aromatase enzyme. The hormonal effects of a new, non-steroidal competitive inhibitor of the aromatase enzyme, MPV-2213ad, were investigated in this study. METHODS: The study was conducted as a double-blind, placebo controlled phase I study, where 32 healthy male volunteers were randomized to receive a single oral dose of either 0.3, 3 or 100 mg of MPV-2213ad or placebo. Serum concentrations of estradiol (E2), testosterone, follicle stimulating hormone (FSH), luteinizing hormone (LH), cortisol and aldosterone were determined from samples taken 0, 4, 8 h and 12 h during the day of drug administration and 1, 2, 4 and 7 days after drug intake. The individual diurnal variation of circulating hormone concentrations was determined in all participants at 0, 4, 8 h and 12 h on the day before drug intake. Specimens for hematological and biochemical analyses were also collected. RESULTS: A dose-dependent and statistically significant (P < 0.001) decrease in serum E2 concentrations was induced by MPV-2213ad. Lowest mean values were observed 8-12 h after drug administration and at 24 h the reductions were 10%, 34% and 69% from baseline in the 0.3-mg, 3-mg and 100-mg groups, compared with an 18% increase in the placebo group. Serum E2 concentrations returned to baseline within 4 days in all study subjects. A significant increase was observed in the serum concentrations of testosterone (P = 0.016), LH (P = 0.002) and FSH (P < 0.001) after administration of MPV-2213ad. Serum concentrations of cortisol and aldosterone were unaffected by MPV-2213ad. The drug was well tolerated. CONCLUSION: Single oral doses of MPV-2213ad, given to healthy male subjects, induced hormonal effects typical for a specific and selective inhibitor of the aromatase enzyme. Importantly, this study design with the determination of the diurnal rhythm in the levels of the corresponding hormones gives additional validity on the results.

and yet another......

Hormonal effects of MPV-2213ad, a new selective aromatase inhibitor, in healthy male subjects. A phase I study.

Ahokoski O, Irjala K, Huupponen R, Halonen K, Salminen E, Scheinin H.

Department of Pharmacology and Clinical Pharmacology, University of Turku, Turku University Central Hospital, Finland.

AIMS: A novel non-steroidal competitive inhibitor of the aromatase enzyme, MPV-2213ad, was entered into an open dose-escalation study. The objective of this study was to investigate the tolerability and efficiency of this new compound with assessment of the hormonal effects after study drug administration. METHODS: MPV-2213ad was given to 39 healthy male volunteers. Single increasing oral doses of 0.003, 0.03, 0.3, 3, 9, 30 and 100 mg were given to three subjects at each dose level, after which ten subjects received the 300 mg dose and eight subjects the highest 600 mg dose of MPV-2213ad. RESULTS: Serum oestradiol levels were suppressed by 58-65% when MPV-2213ad was given at doses between 0.3 and 30 mg. A reduction in serum oestradiol levels by 83% from baseline was achieved with the 300 mg dose. No additional decrease was seen with the highest dose. The suppression lasted longer with higher doses of MPV-2213ad. After the 300 and 600 mg doses serum oestradiol returned to baseline within 4 days. Marked increases in serum concentrations of testosterone, androstenedione, 17-OH-progesterone, LH and FSH were also observed at doses between 100 and 600 mg of MPV-2213ad. The drug was well-tolerated and the adverse events were mild or moderate including hot flushes, mild vertigo, nausea, acne and gastrointestinal discomfort. CONCLUSIONS: MPV-2213ad has a potent, dose-dependent inhibitory effect on serum oestradiol. It was selective for the aromatase enzyme with no signs of adreno-cortical suppression or haematological or biochemical toxicity.