Carlito
New Member
Sup bros, I've been intrigued by this compound since Promatrix cameout with their oral version of formestne named Primobolan Acetate, I tried and liked it pretty much, the downside was that I had to take 6 to 8 tabs a day for it to work, it gave me lean mass gain and hardness and it helped me recover from a cycle I did not used Clomid or Nolva!...lol, yeah I always do things like this I am the guinea pig...ya know. I think if we could use this compund as an injectable it would be more efficient and less expensive, I will post some info on its anti-progesterone activity and later as I find more info I will post more.
Thanks
Carlito
Chemical Structure
<FONT face=Arial size=2>Invalid Embedded Image Removed
Effect of 4-hydroxyandrostenedione on murine Leydig tumor cell steroidogenesis.
Zimniski SJ, Brandt ME, Melner MH, Brodie AM, Puett D.
Department of Biochemistry and Molecular Biology, University of Miami School of Medicine, Florida 33101.
The murine Leydig cell tumor (M5480A) possesses high levels of estrogen receptor and is known to produce estrogens. In these studies we examined the effects of the potent aromatase inhibitor 4-hydroxyandrostenedione (4-OHA) on Leydig tumor cell steroidogenesis both in vitro and in vivo. The addition of 4-OHA to Leydig tumor cells in primary culture resulted in a dose- and a time-dependent decrease in media progesterone levels. The observed decrease was most likely due to impaired synthesis of progesterone, inasmuch as no alteration in progesterone metabolism was seen when progesterone levels were diminishing. However, 4-OHA inhibited progesterone conversion to testosterone following 1 h of incubation, but this effect disappeared coincident with 4-OHA metabolism. Analysis of pregnenolone production revealed a biphasic dose-dependent effect of 4-OHA. At low doses (0.01-0.1 microM), 4-OHA was found to decrease pregnenolone concentrations, while at higher doses (1-10 microM) pregnenolone levels were elevated. Therefore, the actions of 4-OHA on Leydig cell steroidogenesis in vitro appear to be multifocal. Other experiments were performed to evaluate the effects of 4-OHA on tumor-bearing male mice in vivo. In these studies, the predominant effects of 4-OHA were to act as an aromatase inhibitor and to inhibit progesterone production. Thus, while 4-OHA is a potent aromatase inhibitor, we have found that this compound may alter steroidogenesis in Leydig tumor cells at several sites prior to aromatization.
PMID: 2065323 [PubMed - indexed for MEDLINE]
Is there a benefit by the sequence anastrozole-formestane for postmenopausal metastatic breast cancer women?
Carlini P, Ferretti G, Di Cosimo S, Colella E, Tonachella R, Romiti A, Tomao S, Frassoldati A, Papaldo P, Fabi A, Ruggeri EM, Cognetti F.
Department of Medical Oncology, Regina Elena Cancer Institute, Via Elio Chianesi 53, Rome, Italy. pcarlini@iol.it
To explore the different sequence interactions between reversible non-steroidal (anastrozole, ANZ and letrozole, LTZ) and non-reversible steroidal aromatase inhibitors (formestane, FOR and exemestane, EXE), we evaluated the clinical benefit (CB) in postmenopausal breast cancer patients, who had previously received anastrozole and subsequently formestane. In 19 out of 21 patients (90.5%), a clinical benefit response was achieved by anastrozole, with a median duration of 12 months. Out of the 21 women progressing on anastrozole, 12 achieved stable disease (SD)>/=6 months by formestane only. The overall clinical benefit was 66.5%. The median duration of clinical benefit was 11 months with a time to progression of 6.5 months. The median duration of clinical benefit in our series is similar to that reported in two phase II trials with the sequence aminogluthetimide-->formestane and aminogluthetimide-->exemestane as third-line hormonal therapy, suggesting a non-cross-resistance between the two classes of inhibitors.
Publication Types:
Clinical Trial
PMID: 12943750 [PubMed - indexed for MEDLINE]
Thanks
Carlito
Chemical Structure
<FONT face=Arial size=2>Invalid Embedded Image Removed
Effect of 4-hydroxyandrostenedione on murine Leydig tumor cell steroidogenesis.
Zimniski SJ, Brandt ME, Melner MH, Brodie AM, Puett D.
Department of Biochemistry and Molecular Biology, University of Miami School of Medicine, Florida 33101.
The murine Leydig cell tumor (M5480A) possesses high levels of estrogen receptor and is known to produce estrogens. In these studies we examined the effects of the potent aromatase inhibitor 4-hydroxyandrostenedione (4-OHA) on Leydig tumor cell steroidogenesis both in vitro and in vivo. The addition of 4-OHA to Leydig tumor cells in primary culture resulted in a dose- and a time-dependent decrease in media progesterone levels. The observed decrease was most likely due to impaired synthesis of progesterone, inasmuch as no alteration in progesterone metabolism was seen when progesterone levels were diminishing. However, 4-OHA inhibited progesterone conversion to testosterone following 1 h of incubation, but this effect disappeared coincident with 4-OHA metabolism. Analysis of pregnenolone production revealed a biphasic dose-dependent effect of 4-OHA. At low doses (0.01-0.1 microM), 4-OHA was found to decrease pregnenolone concentrations, while at higher doses (1-10 microM) pregnenolone levels were elevated. Therefore, the actions of 4-OHA on Leydig cell steroidogenesis in vitro appear to be multifocal. Other experiments were performed to evaluate the effects of 4-OHA on tumor-bearing male mice in vivo. In these studies, the predominant effects of 4-OHA were to act as an aromatase inhibitor and to inhibit progesterone production. Thus, while 4-OHA is a potent aromatase inhibitor, we have found that this compound may alter steroidogenesis in Leydig tumor cells at several sites prior to aromatization.
PMID: 2065323 [PubMed - indexed for MEDLINE]
Is there a benefit by the sequence anastrozole-formestane for postmenopausal metastatic breast cancer women?
Carlini P, Ferretti G, Di Cosimo S, Colella E, Tonachella R, Romiti A, Tomao S, Frassoldati A, Papaldo P, Fabi A, Ruggeri EM, Cognetti F.
Department of Medical Oncology, Regina Elena Cancer Institute, Via Elio Chianesi 53, Rome, Italy. pcarlini@iol.it
To explore the different sequence interactions between reversible non-steroidal (anastrozole, ANZ and letrozole, LTZ) and non-reversible steroidal aromatase inhibitors (formestane, FOR and exemestane, EXE), we evaluated the clinical benefit (CB) in postmenopausal breast cancer patients, who had previously received anastrozole and subsequently formestane. In 19 out of 21 patients (90.5%), a clinical benefit response was achieved by anastrozole, with a median duration of 12 months. Out of the 21 women progressing on anastrozole, 12 achieved stable disease (SD)>/=6 months by formestane only. The overall clinical benefit was 66.5%. The median duration of clinical benefit was 11 months with a time to progression of 6.5 months. The median duration of clinical benefit in our series is similar to that reported in two phase II trials with the sequence aminogluthetimide-->formestane and aminogluthetimide-->exemestane as third-line hormonal therapy, suggesting a non-cross-resistance between the two classes of inhibitors.
Publication Types:
Clinical Trial
PMID: 12943750 [PubMed - indexed for MEDLINE]
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