Toremifene

[John Juan]

***Click the SuperiorPeptide banner in my signature for (Toremifene) in the Research Liquids section***

Toremifene: Usually dosed around 60 mgs, some dose it up to 240 mgs. Its androgenicity:estrogenicity ratio is 5x that of Nolvadex. It is prescribed to female patients for breast cancer and has shown a high affinity for bonding to the Estrogen receptors in the breast tissue. Male patients treated with toremifene citrate 80 mg compared to placebo demonstrated statistically significant increases in bone mineral density in the lumbar spine, hip, and femur skeletal sites. It decreased the risk by up to 50%. Toremifene citrate 80 mg treatment compared to placebo also resulted in a decrease in total cholesterol, LDL, and triglycerides, and an increase in HDL. There were also statistically significant improvements in gynecomastia. This data are from an ongoing study of men receiving treatment for ADT (androgen depravation therapy). These men are receiving ADT for advanced prostate cancer. ADT removes much of the testosterone and estrogen in the body which helps the prostatic cancer cells grow. So these men were suffering from side effects from reduced estrogen and testosterone in the body. Some studies have even suggested that Torm doesn't regulate progesterone receptors and we may see in the future the possibility of using it with 19-nors.

 

[Kevlor]

What you like best? Toremifene or clomiphene?

 

[ibleedoranbla]

Is this a better option than nolvadex?

 

[John Juan]

My research rat responds real well to Clomid. It gives him a sense of well being, and incredible muscle strength and hardness. He hasn't sampled Toremifene yet.

 

[John Juan]

The beneficial effects of toremifene administration on the hypothalamic-pituitary-testicular axis and sperm parameters in men with idiopathic oligozoospermia.

AuthorsFarmakiotis D, et al. Show all Journal
Fertil Steril. 2007 Oct;88(4):847-53. Epub 2007 Apr 6.

Affiliation
Abstract
OBJECTIVE: To evaluate whether toremifene, a selective estrogen receptor modulator (SERM), has a beneficiary effect on all three main sperm parameters.

DESIGN: Prospective interventional clinical study.

SETTING: University hospital.

PATIENT(S): One-hundred subfertile men with idiopathic oligozospermia.

INTERVENTION(S): Toremifene (60 mg daily) was administered to all men for 3 months. At baseline and at the end of each month, serum concentrations of follicle-stimulating hormone (FSH), testosterone, inhibin B, and sex hormone-binding globulin (SHBG) were measured. At baseline and at the end, semen analysis was performed and sperm concentration, spermatozoal motility and normal sperm forms were determined.

MAIN OUTCOME MEASURE(S): Gonadotropin, testosterone, inhibin-B levels, total sperm count, sperm morphology and motility.

RESULT(S): Toremifene administration resulted in a significant increase in FSH, testosterone, SHBG, and inhibin B levels, as well as in sperm concentration, percentage motility and normal sperm forms. Twenty-two men's partners achieved pregnancy within 2 months of the end of treatment. At the end of the third month, serum FSH levels were significantly higher in the men whose partners did not achieve pregnancy, and total sperm count and normal sperm forms were significantly lower compared with the group of men whose partners achieved pregnancy.

CONCLUSION(S): Toremifene administration for a period of 3 months in men with idiopathic oligozoospermia is associated with significant improvements of sperm count, motility, and morphology, mediated by increased gonadotropin secretion and possibly a direct beneficial effect of toremifene on the testes. The above findings are also indicative of a better testicular exocrine (improved sperm parameters) response to treatment in men whose partners achieved pregnancy compared with those who did not. Further randomized, placebo-controlled trials should be conducted to determine whether this particular selective estrogen receptor modulator can be useful as an initial approach in men with oligozoospermia.

PMID 17412336 [PubMed - indexed for MEDLINE]
Full text: Elsevier Science

 

[John Juan]

Great for pct.

 

[SMW235]

Clomid better for hpta reboot than torem.

Torem better for hpta reboot than nolva.

Nolva is better for gyno than torem and clomid.

Ralox is the best of all for gyno.

I've used them all and that's my opinion on it only.

 

[John Juan]

Clomid better for hpta reboot than torem.

Torem better for hpta reboot than nolva.

Nolva is better for gyno than torem and clomid.

Ralox is the best of all for gyno.

I've used them all and that's my opinion on it only.

They need to make one compound that's the best of each mentioned.

 

[SMW235]

No kidding.

My cabinet looks like a drug store.

All in 1 would be great.

 

[John Juan]

No kidding.

My cabinet looks like a drug store.

All in 1 would be great.

Do you think Toremifene would keep your test production up best while on cycle?

 

[SMW235]

I've never ran a serm on cycle.

If your pinning and worried about it i would just suggest hcg.

On a oral ph cycle I think torem has the quickest recovery time overall. Also believe clomid will put your natural test levels higher but Torem will do it faster which is more important in pct.

I don't have proof of this besides how I feel after using these. But I've seen others bloodwork supporting this.

I've thought about running a serm on cycle, but never really had an issue with recovery so it's really not neccasary IMO. Unless your worried about gyno and a low dose of ralox every 3rd day might be useful as I've seen others doing when running heavy cycles.

 

[SMW235]

Edit: The stated above about Torem is for any cycle and not just a ph cycle. I worded it wrong.

Hope that makes sense.

 

[John Juan]

I've never ran a serm on cycle.

If your pinning and worried about it i would just suggest hcg.

On a oral ph cycle I think torem has the quickest recovery time overall. Also believe clomid will put your natural test levels higher but Torem will do it faster which is more important in pct.

I don't have proof of this besides how I feel after using these. But I've seen others bloodwork supporting this.

I've thought about running a serm on cycle, but never really had an issue with recovery so it's really not neccasary IMO. Unless your worried about gyno and a low dose of ralox every 3rd day might be useful as I've seen others doing when running heavy cycles.

Thank you for the reply. I haven't tried Toremifene yet. It sounds like a good candidate to try in place of hcg on cycle as hcg is difficult to find. Every 3rd day sounds good.

 

[Elvia1023]

Thank you for the reply. I haven't tried Toremifene yet. It sounds like a good candidate to try in place of hcg on cycle as hcg is difficult to find. Every 3rd day sounds good.

HCG always makes my anxiety worse. I am taking it now... first time in ages. Big balls here I come

 

[John Juan]

I have heard that Toremifene doesn't give the emotional sides that Clomid does.

 

[SMW235]

I'm using Torem now. Balls feel bigger already lol No sides as of now except shit taste lol

 

[John Juan]

I'm using Torem now. Balls feel bigger already lol No sides as of now except shit taste lol

Hahaha I hear ya on the taste. Research liquids are often diluted in grain alcohol so it tastes like a cheap shot of vodka.

 

[Elvia1023]

I'm using Torem now. Balls feel bigger already lol No sides as of now except shit taste lol

Sounds good. I have never used Torem... might have to try it out one time

 

[SMW235]

Good shit, if it's legit you'll like it.

 

[John Juan]

I'm using Torem now. Balls feel bigger already lol No sides as of now except shit taste lol

My balls/peanuts could use a little boost. Hahaha

 

[SMW235]

You on cycle?

 

[John Juan]

You on cycle?

I'm always on cycle

 

[SMW235]

Yea buddy lol

 

[John Juan]

The igf1 keeps my nuts up pretty well. It releases luetinizing hormone.

 

[John Juan]

I read on another forum that a 25mg dose of Toremifene while on a heavy cycle is strong enough to drop your testicles right down into the nut sack 90 minute after dosing it. That's similar to how my body reacts to hcg. The same post said Toremifene is more effective than simaltaniously stacking Nolvadex and Clomid.

 

[SMW235]

I been on torem for a few days now, off cycle, and by the 2nd day my balls were hanging low again, feeling fuller again. I had almost forgot what it felt like lol

 

[John Juan]

I been on torem for a few days now, off cycle, and by the 2nd day my balls were hanging low again, feeling fuller again. I had almost forgot what it felt like lol

Do you notice a sex drive increase?

 

[SMW235]

More than any other serm I've used.

 

[John Juan]

More than any other serm I've used.

Wow, that's real cool! I have only just become aware of this compound recently. It's so hard to find hcg and it sounds like Toremifene has the benefits of hcg plus some of the other AI's.
I'll have to experiment with it.

Does it dry out the joints like Adex or lethro?

 

[Elvia1023]

I plan to try torem after my current cycle

 

[John Juan]

I plan to try torem after my current cycle

Turn those raisins into walnuts.

 

[John Juan]

It sounds like Toremifene is taking over the old Clomid/Nolvadex stack in pct.

 

[John Juan]

It is recommended to use hcg the night before your testosterone shot to keep you natural test production up. I'm thinking Toremifene is the same deal. Twice a week being optimum.

 

[Elvia1023]

It sounds like Toremifene is taking over the old Clomid/Nolvadex stack in pct.

Exactly. Even taken alone it sounds great

 

[John Juan]

Exactly. Even taken alone it sounds great

It sounds like a good legal alternative to hcg.

 

[John Juan]

Toremifene/Fareston differs from Nolvadex in several ways, however- even though it’s very similar to it in others. Firstly, the risk of certain side effects (although relatively rare with Nolvadex) is actually quite a bit lower with Fareston.However unlikely these risks are in the first place, the risk of stroke, pulmonary embolism, and cataract is probably lower with Fareston than with Nolvadex. This is going to be of interest to people who have issues with “floaters” in their vision, which is sometimes caused by Nolvadex and Clomid, as this product may represent significantly less occular toxicity. It also differs slightly from Nolvadex in its potent with regards to improving lipid (cholesterol) profiles. In terms of improving bone mineral density, Fareston is roughly equal to Nolvadex.

 

[John Juan]

Randomized controlled trial of toremifene 120 mg compared with exemestane 25 mg after prior treatment with a non-steroidal aromatase inhibitor in postmenopausal women with hormone receptor-positive metastatic breast cancer.

AuthorsYamamoto Y, et al. Show all Journal
BMC Cancer. 2013 May 16;13(1):239. [Epub ahead of print]

Affiliation
Abstract
BACKGROUND: After the failure of a non-steroidal aromatase inhibitor (nsAI) for postmenopausal patients with metastatic breast cancer (mBC), it is unclear which of various kinds of endocrine therapy is the most appropriate. A randomized controlled trial was performed to compare the efficacy and safety of daily toremifene 120 mg (TOR120), a selective estrogen receptor modulator, and exemestane 25 mg (EXE), a steroidal aromatase inhibitor. The primary end point was the clinical benefit rate (CBR). The secondary end points were objective response rate (ORR), progression-free survival (PFS), overall survival (OS) and toxicity.

METHODS: Initially, a total of 91 women was registered in the study and randomly assigned to either TOR120 (n = 46) or EXE (n = 45) from October 2008 to November 2011. Three of the 46 patients in the TOR120 arm were not received treatment, 2 patients having withdrawn from the trial by their preference and one having been dropped due to administration of another SERM.

RESULTS: When analyzed after a median observation period of 16.9 months, the intention-to-treat analysis showed that there were no statistical difference between TOR120 (N = 46) and EXE (n = 45) in terms of CBR (41.3% vs. 26.7%; P = 0.14), ORR (10.8% vs. 2.2%; P = 0.083), and OS (Hazard ratio, 0.60; P = 0.22). The PFS of TOR120 was longer than that of EXE, the difference being statistically significant (Hazard ratio, 0.61, P = 0.045). The results in treatment-received cohort (N = 88) were similar to those in ITT cohort. Both treatments were well-tolerated with no severe adverse events, although the treatment of 3 of 43 women administered TOR120 was stopped after a few days because of nausea, general fatigue, hot flush and night sweating.

CONCLUSIONS: TOR120, as a subsequent endocrine therapy for mBC patients who failed non-steroidal AI treatment, could potentially be more beneficial than EXE.

 

[NoFatChicks91]

What is your opinion on a PCT including both clomid and Torem?

Clomid 50/50/25/25
Tore 120/90/90/60

Sent from my SPH-L710 using EliteFitness

 

[John Juan]

What is your opinion on a PCT including both clomid and Torem?

Clomid 50/50/25/25
Tore 120/90/90/60

Sent from my SPH-L710 using EliteFitness

Based on pct plans I've seen at various forums, that looks like a solid plan to me. I'm a bad person to ask about pct as I stay on AAS year round. I rotate various compounds in and out regularly and raise and lower doses based on my goals at the time.,

 

[John Juan]

Toremifene improves lipid profiles in men receiving androgen-deprivation therapy for prostate cancer: interim analysis of a multicenter phase III study.

AuthorsSmith MR, et al. Show all Journal
J Clin Oncol. 2008 Apr 10;26(11):1824-9. doi: 10.1200/JCO.2007.13.5517.

Affiliation
Comment in
Eur Urol. 2008 Nov;54(5):1202-3.
Abstract
PURPOSE: Androgen-deprivation therapy (ADT) is associated with greater risk of incident coronary heart disease and hospital admission for myocardial infarction; treatment-related increases in serum lipids may contribute to greater cardiovascular disease risk. We evaluated the effects of toremifene, a selective estrogen-receptor modulator, on fasting serum lipid levels in men receiving ADT for prostate cancer.

PATIENTS AND METHODS: In an ongoing, multicenter, double-blind, placebo-controlled phase III fracture-prevention study, 1,389 men receiving ADT for prostate cancer were randomly assigned to receive toremifene (80 mg/d) or placebo. In this interim analysis of 188 patients, changes in fasting serum lipids from baseline to month 12 were compared between the placebo and toremifene groups.

RESULTS: Changes in serum lipids differed significantly between the groups. Mean (+/- SE) total cholesterol decreased by 1.0% +/- 1.7% from baseline to month 12 in the placebo group and decreased by 8.1% +/- 1.4% in the toremifene group (P = .001 for between group comparison). Low-density lipoprotein (LDL) cholesterol increased by 0.8% +/- 2.5% in the placebo group and decreased by 8.2% +/- 2.5% in the toremifene group (P = .003). In contrast, high-density lipoprotein (HDL) cholesterol decreased by 4.9% +/- 1.2% in the placebo group and increased by 0.5% +/- 2.2% in the toremifene group (P = .018). Triglycerides increased by 6.9% +/- 4.2% in the placebo group and decreased by 13.2% +/- 3.6% in the toremifene group (P = .003).

CONCLUSION: Toremifene significantly decreased total cholesterol, LDL cholesterol, and triglycerides, and increased HDL cholesterol in men receiving ADT for prostate cancer.

 

[John Juan]

The beneficial effects of toremifene administration on the hypothalamic-pituitary-testicular axis and sperm parameters in men with idiopathic oligozoospermia.

AuthorsFarmakiotis D, et al. Show all Journal
Fertil Steril. 2007 Oct;88(4):847-53. Epub 2007 Apr 6.

Affiliation
Abstract
OBJECTIVE: To evaluate whether toremifene, a selective estrogen receptor modulator (SERM), has a beneficiary effect on all three main sperm parameters.

DESIGN: Prospective interventional clinical study.

SETTING: University hospital.

PATIENT(S): One-hundred subfertile men with idiopathic oligozospermia.

INTERVENTION(S): Toremifene (60 mg daily) was administered to all men for 3 months. At baseline and at the end of each month, serum concentrations of follicle-stimulating hormone (FSH), testosterone, inhibin B, and sex hormone-binding globulin (SHBG) were measured. At baseline and at the end, semen analysis was performed and sperm concentration, spermatozoal motility and normal sperm forms were determined.

MAIN OUTCOME MEASURE(S): Gonadotropin, testosterone, inhibin-B levels, total sperm count, sperm morphology and motility.

RESULT(S): Toremifene administration resulted in a significant increase in FSH, testosterone, SHBG, and inhibin B levels, as well as in sperm concentration, percentage motility and normal sperm forms. Twenty-two men's partners achieved pregnancy within 2 months of the end of treatment. At the end of the third month, serum FSH levels were significantly higher in the men whose partners did not achieve pregnancy, and total sperm count and normal sperm forms were significantly lower compared with the group of men whose partners achieved pregnancy.

CONCLUSION(S): Toremifene administration for a period of 3 months in men with idiopathic oligozoospermia is associated with significant improvements of sperm count, motility, and morphology, mediated by increased gonadotropin secretion and possibly a direct beneficial effect of toremifene on the testes. The above findings are also indicative of a better testicular exocrine (improved sperm parameters) response to treatment in men whose partners achieved pregnancy compared with those who did not. Further randomized, placebo-controlled trials should be conducted to determine whether this particular selective estrogen receptor modulator can be useful as an initial approach in men with oligozoospermia.

 

[John Juan]

Toremifene versus tamoxifen for advanced breast cancer.

AuthorsMao C, et al. Show all Journal
Cochrane Database Syst Rev. 2012 Jul 11;7:CD008926. doi: 10.1002/14651858.CD008926.pub2.

Affiliation
Abstract
BACKGROUND: Toremifene (TOR) and tamoxifen (TAM) can both be used as treatments for advanced breast cancer.

OBJECTIVES: To compare the efficacy and safety of TOR with TAM in patients with advanced breast cancer.

SEARCH METHODS: The Cochrane Breast Cancer Group's Specialised Register was searched (1 July 2011) using the codes for "toremifene", "fareston", "tamoxifen, "nolvadex, and "breast cancer". We also searched MEDLINE (via PubMed) (from inception to 1 July 2011), EMBASE (via Ovid) (from inception to 1 July 2011), The Cochrane Central Register of Controlled Trials (CENTRAL) (The Cochrane Library, Issue 7, 2011), and the WHO International Clinical Trials Registry Platform search portal (1 July 2011). In addition, we screened the reference lists of relevant trials or reviews.

SELECTION CRITERIA: Randomised controlled trials (RCTs) that compared the efficacy and safety, or both of TOR with TAM in women with advanced breast cancer. Trials that provided sufficient data on one of the following items: objective response rate (ORR), time to progression (TTP), overall survival (OS), and adverse events, were considered eligible for inclusion.

DATA COLLECTION AND ANALYSIS: Studies were assessed for eligibility and quality. Two review authors independently extracted the following details: first author, publication year, country, years of follow-up, treatment arms, intention-to-treat (ITT) population size, menopausal status of patients, hormone receptor status, response criteria, efficacy and safety outcomes of TOR and TAM arms. Hazard ratios (HR) were derived for time-to-event outcomes, where possible, and response and adverse events were analysed as dichotomous variables. We used a fixed-effect model for meta-analysis unless there was significant between-study heterogeneity.

MAIN RESULTS: A total of 2061 patients from seven RCTs were included for final analysis, with 1226 patients in the TOR group and 835 patients in the TAM group. The ORR for the TOR group was 25.8% (316/1226) whereas, the ORR for the TAM group was 26.9% (225/835). The pooled risk ratio (RR) suggested that the ORRs were not statistically different between the two groups (RR 1.02, 95% confidence interval (CI) 0.88 to 1.18, P = 0.83). The median TTP was 6.1 months for the TOR group and 5.8 months for the TAM group. The median OS was 27.8 months for the TOR group and 27.6 months for the TAM group. There were no significant differences in TTP and OS between the two therapeutic groups (for TTP: HR 1.08, 95% CI 0.94 to 1.24; for OS: HR 1.02, 95% CI 0.86 to 1.20). The frequencies of most adverse events were also similar in the two groups, while headache seemed to occur less in the TOR group than in the TAM group (RR 0.14, 95% CI 0.03 to 0.74, P = 0.02). There was no significant heterogeneity between studies in most of the above meta-analyses. Sensitivity analysis did not alter the results.

AUTHORS' CONCLUSIONS: TOR and TAM are equally effective and the safety profile of the former is at least not worse than the latter in the first-line treatment of patients with advanced breast cancer. Thus, TOR may serve as a reasonable alternative to TAM when anti-oestrogens are applicable but TAM is not the preferred choice for some reason.

 

[John Juan]

A two-year dietary carcinogenicity study of the antiestrogen toremifene in Sprague-Dawley rats.

AuthorsKarlsson S, et al. Show all Journal
Drug Chem Toxicol. 1996 Nov;19(4):245-66.

Affiliation
Abstract
The carcinogenic potential of the nonsteroidal triphenylethylene antiestrogen toremifene (Fareston) was evaluated in a standard 104-week rat dietary carcinogenicity study. The doses were 0, 0.12, 1.2, 5.0 and 12 mg/kg/day and the number of animals 50/sex/dose group. The body weight gain and food consumption were monitored once weekly (study weeks 1-16) or once every four weeks thereafter (study weeks 17-104). Blood samples were taken at weeks 34, 52 and 104 and the plasma concentrations of toremifene, as well as the two main metabolites (deaminohydroxy)toremifene and N-demethyltoremifene, were measured. All doses of toremifene reduced food intake and body weight gain. Toremifene caused a significant reduction in mortality, which was mainly due to reduced incidences of pituitary tumors. This was evident in all dose groups. Drug-related decrease of mammary tumors in females (at all doses) and testicular tumors in male rats (doses > or = 1.2 mg/kg/day) were also evident. The incidence of the preneoplastic foci of basophilic hepatocytes were significantly decreased in treated female groups. Toremifene induced no preneoplastic or neoplastic lesions. Based on histopathology, no obvious toxicity could be observed. Drug-related changes were observed in the genital organs, thyroid, spleen, mammary gland, adrenal, kidney, stomach and lung. These changes were due to hormonal disturbances or as a result of reduced food consumption or reduced incidences of pituitary, mammary or testicular tumors. This study indicates that toremifene is an efficient antiestrogen in long-term treatment, is well tolerated and has no tumorigenic potential in rats.

 

[John Juan]

Toremifene is quickly becoming a favorite over Nolvadex.

 

[John Juan]

Toremifene Improves Lipid Profiles in Men Receiving Androgen-Deprivation Therapy for Prostate Cancer: Interim Analysis of a Multicenter Phase III Study

Matthew R. Smith, S. Bruce Malkowicz, Franklin Chu, John Forrest, Paul Sieber, K. Gary Barnette, Domingo Rodriquez, and Mitchell S. Steiner
Author information ► Copyright and License information ►
The publisher's final edited version of this article is available at J Clin Oncol
See other articles in PMC that cite the published article.
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Abstract
Purpose
Androgen-deprivation therapy (ADT) is associated with greater risk of incident coronary heart disease and hospital admission for myocardial infarction; treatment-related increases in serum lipids may contribute to greater cardiovascular disease risk. We evaluated the effects of toremifene, a selective estrogen-receptor modulator, on fasting serum lipid levels in men receiving ADT for prostate cancer.
Patients and Methods
In an ongoing, multicenter, double-blind, placebo-controlled phase III fracture-prevention study, 1,389 men receiving ADT for prostate cancer were randomly assigned to receive toremifene (80 mg/d) or placebo. In this interim analysis of 188 patients, changes in fasting serum lipids from baseline to month 12 were compared between the placebo and toremifene groups.
Results
Changes in serum lipids differed significantly between the groups. Mean (± SE) total cholesterol decreased by 1.0% ± 1.7% from baseline to month 12 in the placebo group and decreased by 8.1% ± 1.4% in the toremifene group (P = .001 for between group comparison). Low-density lipoprotein (LDL) cholesterol increased by 0.8% ± 2.5% in the placebo group and decreased by 8.2% ± 2.5% in the toremifene group (P = .003). In contrast, high-density lipoprotein (HDL) cholesterol decreased by 4.9% ± 1.2% in the placebo group and increased by 0.5% ± 2.2% in the toremifene group (P = .018). Triglycerides increased by 6.9% ± 4.2% in the placebo group and decreased by 13.2% ± 3.6% in the toremifene group (P = .003).
Conclusion
Toremifene significantly decreased total cholesterol, LDL cholesterol, and triglycerides, and increased HDL cholesterol in men receiving ADT for prostate cancer.

 

[John Juan]

Toremifene for the prevention of prostate cancer in men with high grade prostatic intraepithelial neoplasia: results of a double-blind, placebo controlled, phase IIB clinical trial.

AuthorsPrice D, et al. Show all Journal
J Urol. 2006 Sep;176(3):965-70; discussion 970-1.

Affiliation
Abstract
PURPOSE: A randomized, double-blind, dose finding, placebo controlled, parallel group clinical study was done to determine the incidence of prostate cancer in men with high grade prostatic intraepithelial neoplasia treated with toremifene.

MATERIALS AND METHODS: A total of 514 patients with high grade prostatic intraepithelial neoplasia and no evidence of prostate cancer on screening biopsy were randomized to 20, 40 or 60 mg toremifene, or placebo daily for 12 months. Patients underwent re-biopsy at 6 and 12 months.

RESULTS: The number of evaluable patients, that is those with 1 on study biopsy who were compliant, was 447. The cumulative risk of prostate cancer was decreased in patients on 20 mg toremifene compared with placebo (24.4% vs 31.2%, p <0.05). The annualized rate of prevention was 6.8 cancers per 100 men treated. In patients with no biopsy evidence of cancer at baseline and 6 months, the 12-month incidence of prostate cancer was decreased by 48.2% with 20 mg toremifene compared with placebo (9.1% vs 17.4%, p <0.05). The 20 mg dose was most effective but cumulative and 12-month incidences of prostate cancer were lower for each toremifene dose vs placebo with a cumulative risk of 29.2% and 28.1%, and a 12-month incidence of 14.3% and 13.0% for 40 and 60 mg, respectively. Gleason scores were similar across treatments. The overall incidence of drug related and serious adverse events did not differ between any of the toremifene groups and the placebo group.

CONCLUSIONS: Toremifene decreased the incidence of prostate cancer by 1 year and had a tolerability profile comparable to that of placebo in a high risk population.

 

[John Juan]

Toremifene increases bone mineral density in men receiving androgen deprivation therapy for prostate cancer: interim analysis of a multicenter phase 3 clinical study.

AuthorsSmith MR, et al. Show all Journal
J Urol. 2008 Jan;179(1):152-5. Epub 2007 Nov 14.

Affiliation
Abstract
PURPOSE: We evaluated the effects of toremifene on bone mineral density, a surrogate for fracture risk, in men receiving androgen deprivation therapy for prostate cancer.

MATERIALS AND METHODS: In an ongoing, multicenter, phase 3 fracture prevention study 1,392 men 50 years or older with prostate cancer receiving androgen deprivation therapy were randomized to 80 mg toremifene per day or placebo. Bone mineral density of the lumbar spine, total hip and femoral neck was assessed using dual energy x-ray absorptiometry. In this planned interim analysis of the first 197 subjects we compared bone mineral density changes from baseline to month 12 between the placebo and toremifene groups.

RESULTS: Compared with the placebo group men in the toremifene group had significant increases in bone mineral density at each evaluated skeletal site. Lumbar spine bone mineral density decreased 0.7% in the placebo group and increased 1.6% in the toremifene group (between group comparison p <0.001). Total hip bone mineral density decreased 1.3% in the placebo group and increased 0.7% in the toremifene group (p = 0.001). Femoral neck bone mineral density decreased 1.3% in the placebo group and increased 0.2% in the toremifene group (p = 0.009). Between group differences in the change in bone mineral density from baseline to month 12 were 2.3%, 2.0% and 1.5% for the lumbar spine, total hip and femoral neck, respectively.

CONCLUSIONS: Toremifene significantly increased hip and spine bone mineral density in men receiving androgen deprivation therapy for prostate cancer. The effect of toremifene on the fracture risk is being assessed in the ongoing randomized, controlled trial.

 

[John Juan]

These studies make it seem that Toremifene offers the benefits of exemestane on cholesterol and the strength of anastrozole in estro blocking.

 

[John Juan]

It seems from all these studies posted that the health benefits in both men and women are substantial from researching Toremifene.

 

[John Juan]

I have read that Toremifene has a 5 day half-life

 

[John Juan]

Improved lipid profiles are a big plus with this compound.

 

[John Juan]

The beneficial effects of toremifene administration on the hypothalamic-pituitary-testicular axis and sperm parameters in men with idiopathic oligozoospermia

Abstract

Objective

To evaluate whether toremifene, a selective estrogen receptor modulator (SERM), has a beneficiary effect on all three main sperm parameters.

Design

Prospective interventional clinical study.

Setting

University hospital.

Patient(s)

One-hundred subfertile men with idiopathic oligozospermia.

Intervention(s)

Toremifene (60 mg daily) was administered to all men for 3 months. At baseline and at the end of each month, serum concentrations of follicle-stimulating hormone (FSH), testosterone, inhibin B, and sex hormone–binding globulin (SHBG) were measured. At baseline and at the end, semen analysis was performed and sperm concentration, spermatozoal motility and normal sperm forms were determined.

Main Outcome Measure(s)

Gonadotropin, testosterone, inhibin-B levels, total sperm count, sperm morphology and motility.

Result(s)

Toremifene administration resulted in a significant increase in FSH, testosterone, SHBG, and inhibin B levels, as well as in sperm concentration, percentage motility and normal sperm forms. Twenty-two men's partners achieved pregnancy within 2 months of the end of treatment. At the end of the third month, serum FSH levels were significantly higher in the men whose partners did not achieve pregnancy, and total sperm count and normal sperm forms were significantly lower compared with the group of men whose partners achieved pregnancy.

Conclusion(s)

Toremifene administration for a period of 3 months in men with idiopathic oligozoospermia is associated with significant improvements of sperm count, motility, and morphology, mediated by increased gonadotropin secretion and possibly a direct beneficial effect of toremifene on the testes. The above findings are also indicative of a better testicular exocrine (improved sperm parameters) response to treatment in men whose partners achieved pregnancy compared with those who did not. Further randomized, placebo-controlled trials should be conducted to determine whether this particular selective estrogen receptor modulator can be useful as an initial approach in men with oligozoospermia.

 

[John Juan]

Toremifene PCT dosing schedule:

150 3 days
100 3 days
50 until PCT is over

 

[John Juan]

Has anyone here run Toremifene while on cycle?

 

[John Juan]

Toremifene to reduce fracture risk in men receiving androgen deprivation therapy for prostate cancer.

AuthorsSmith MR, et al. Show all Journal
J Urol. 2013 Jan;189(1 Suppl):S45-50. doi: 10.1016/j.juro.2012.11.016.

Affiliation
Abstract
PURPOSE: Androgen deprivation therapy is associated with fracture risk in men with prostate cancer. We assessed the effects of toremifene, a selective estrogen receptor modulator, on fracture incidence in men receiving androgen deprivation therapy during a 2-year period.

MATERIALS AND METHODS: In this double-blind, placebo controlled phase III study 646 men receiving androgen deprivation therapy for prostate cancer were assigned to toremifene (80 mg by mouth daily) and 638 were assigned to placebo. Subjects were followed for 2 years. The primary study end point was new vertebral fractures. Secondary end points included fragility fractures, bone mineral density and lipid changes.

RESULTS: The 2-year incidence of new vertebral fractures was 4.9% in the placebo group vs 2.5% in the toremifene group, a significant relative risk reduction of 50% (95% CI -1.5 to 75.0, p = 0.05). Toremifene significantly increased bone mineral density at the lumbar spine, hip and femoral neck vs placebo (p <0.0001 for all comparisons). There was a concomitant decrease in markers of bone turnover (p <0.05 for all comparisons). Toremifene also significantly improved lipid profiles. Venous thromboembolic events occurred more frequently with toremifene than placebo with 7 subjects (1.1%) in the placebo group experiencing a venous thromboembolic event vs 17 (2.6%) in the toremifene group. Other adverse events were similar between the groups.

CONCLUSIONS: Toremifene significantly decreased the incidence of new vertebral fractures in men receiving androgen deprivation therapy for prostate cancer. It also significantly improved bone mineral density, bone turnover markers and serum lipid profiles.

 

[John Juan]

Toremifene citrate 80 mg treatment compared to placebo resulted in a decrease in total cholesterol, LDL, and triglycerides, and an increase in HDL.

 

[John Juan]

Toremifene is a great substitute for Nolvadex

 

[John Juan]

Toremifene and testicular enlargement...

 

[John Juan]

[Regulation mechanism of breast cancer resistance protein by toremifene to reverse BCRP-mediated multidrug resistance in breast cancer cells].

AuthorsZhang YH, et al. Show all Journal
Zhonghua Zhong Liu Za Zhi. 2011 Sep;33(9):654-60. Article in Chinese.

Affiliation
Abstract
OBJECTIVE: To explore the regulation mechanism of the reversal of breast cancer resistance protein-mediated multidrug resistance by toremifene.

METHODS: Two recombinant plasmids (pcDNA3-promoter-BCRP and pcDNA3-CMV-BCRP) were designed to express the wild-type full-length BCRP cDNA enforced driven by its endogenous promoter containing a functional ERE and a CMV promoter as control, respectively. Two recombinant plasmids were transfected into ERα-positive MCF-7 and ERα-negative MDA-MB-231 breast cancer cell lines. Four kinds of BCRP expressing cell lines of MCF-7/Promoter-BCRP, MCF-7/CMV-BCRP, MDA-MB-231/Promoter-BCRP and MDA-MB-231/CMV-BCRP were established in which BCRP was promoted by the BCRP promoter and a CMV promoter as control, respectively. The drug resistant cells were treated with toremifene. Then RT-PCR, Western blot, mitoxantrone efflux assays and cytotoxicity assay were performed to detect the reversal function of BCRP by toremifene on the drug resistance cell lines.

RESULTS: Toremifene significantly downregulated BCRP mRNA levels in a dose-dependent manner in ERα-positive MCF-7/Promoter-BCRP cells than that of untreated control cells. In MCF-7/Promoter-BCRP cells, toremifene at the dose of 0.1, 1 and 10 µmol/L decreased BCRP mRNA expression by 29.5% (P < 0.05), 68.1% (P < 0.01) and 97.4% (P < 0.01), respectively. After being treated with toremifene and 17β-estradiol, the BCRP mRNA level in MCF-7/Promoter-BCRP cells was 64.2% ± 1.3%, significantly higher than that of toremifene treatment control cells (3.8% ± 0.2%,P < 0.01). Furthermore, the effect of toremifene on BCRP protein is similar in BCRP mRNA. Toremifene obviously increased the mitoxantrone fluorescence intensity and decreased the efflux activity by 47.3% (P < 0.05) in MCF-7/promoter-BCRP cells when compared with the untreated control, whereas intracellular accumulation of mitoxantrone obviously decreased and the efflux activity increased by 61.5% were observed in combination with 17β-estradiol when compared with toremifene treatment alone. The results therefore suggested that toremifene reversed mitoxantrone resistance in MCF-7/Promoter-BCRP cells. However, in MCF-7/CMV-BCRP, MDA-MB-231/Promoter-BCRP and MDA-MB-231/CMV-BCRP cells, toremifene or in combination with 17β-estradiol did not affect intracellular mitoxantrone uptake.

CONCLUSION: Taken together, our findings indicate that expression of BCRP is downregulated by toremifene, via a novel transcriptional mechanism which might be involved in the ERE of BCRP promoter through ER-mediated to inactivate the transcription of BCRP gene.

 

[John Juan]

Post from another forum...

"I used tor in last pct. 120 MG's for a WK, then 60 MG's for 2 wks overlapped by 50 MG's clomid weeks 2-4. Administration of Tor led to an noticeable increase in sex drive, very similar to a mild dose of test."

 

[John Juan]

Toremifene is said to kick the sex drive up big time during pct...

 

[John Juan]

Toremifene for breast cancer: a review of 20 years of data.

AuthorsVogel CL, et al. Show all Journal
Clin Breast Cancer. 2014 Feb;14(1):1-9. doi: 10.1016/j.clbc.2013.10.014. Epub 2013 Oct 31.

Affiliation
Abstract
Endocrine therapy is a cornerstone of medical treatment for estrogen receptor-positive breast cancer. The discovery of selective estrogen receptor modulators (SERMs) > 40 years ago represented a revolutionary advance in the treatment of breast cancer. As a therapeutic class, SERMs have either estrogenic or antiestrogenic activity, depending on the target tissue and the hormonal environment. In breast tissue, SERMs are antiestrogenic, making them a major treatment option for women with hormone-sensitive breast cancer. Toremifene citrate was developed > 20 years ago with the goal of achieving efficacy similar to that of tamoxifen and with an improved safety profile. Although studies to date have not confirmed a clear safety advantage or disadvantage for toremifene, clinical data support the efficacy and safety of toremifene for the treatment of breast cancer in postmenopausal patients. Toremifene also has a pharmacokinetic profile and metabolic pathway different from that of tamoxifen, which may provide a therapeutic advantage in certain patients. In addition, because of the selective estrogenic effects of SERMs in bone and on lipid levels along with a different side effect profile compared with the aromatase inhibitors (AIs), toremifene is a viable option to the AIs for some patients. Despite a number of clinical trials and over 500,000 patient years of use, many oncologists have limited familiarity with toremifene data. This article will examine the rationale for the use of toremifene in the treatment of women with breast cancer and review data from 20 years of clinical experience with this agent.

 

[John Juan]

Three pivotal phase III trials conducted in North America and Europe served as the basis for the application for approval of toremifene (Fareston) by the FDA. These trials demonstrated that 60 mg/d of toremifene is safe and effective in the treatment of advanced breast cancer in postmenopausal women. The studies also indicated that, on the basis of antitumor efficacy, as well as safety, toremifene is at least equivalent to tamoxifen and may have some long-term advantages.

 

[John Juan]

Toremifene improves lipid profiles in men receiving androgen-deprivation therapy for prostate cancer: interim analysis of a multicenter phase III study.

AuthorsSmith MR, et al. Show all Journal
J Clin Oncol. 2008 Apr 10;26(11):1824-9. doi: 10.1200/JCO.2007.13.5517.

Affiliation
Comment in
Eur Urol. 2008 Nov;54(5):1202-3.
Abstract
PURPOSE: Androgen-deprivation therapy (ADT) is associated with greater risk of incident coronary heart disease and hospital admission for myocardial infarction; treatment-related increases in serum lipids may contribute to greater cardiovascular disease risk. We evaluated the effects of toremifene, a selective estrogen-receptor modulator, on fasting serum lipid levels in men receiving ADT for prostate cancer.

PATIENTS AND METHODS: In an ongoing, multicenter, double-blind, placebo-controlled phase III fracture-prevention study, 1,389 men receiving ADT for prostate cancer were randomly assigned to receive toremifene (80 mg/d) or placebo. In this interim analysis of 188 patients, changes in fasting serum lipids from baseline to month 12 were compared between the placebo and toremifene groups.

RESULTS: Changes in serum lipids differed significantly between the groups. Mean (+/- SE) total cholesterol decreased by 1.0% +/- 1.7% from baseline to month 12 in the placebo group and decreased by 8.1% +/- 1.4% in the toremifene group (P = .001 for between group comparison). Low-density lipoprotein (LDL) cholesterol increased by 0.8% +/- 2.5% in the placebo group and decreased by 8.2% +/- 2.5% in the toremifene group (P = .003). In contrast, high-density lipoprotein (HDL) cholesterol decreased by 4.9% +/- 1.2% in the placebo group and increased by 0.5% +/- 2.2% in the toremifene group (P = .018). Triglycerides increased by 6.9% +/- 4.2% in the placebo group and decreased by 13.2% +/- 3.6% in the toremifene group (P = .003).

CONCLUSION: Toremifene significantly decreased total cholesterol, LDL cholesterol, and triglycerides, and increased HDL cholesterol in men receiving ADT for prostate cancer.