Tamoxifen (Nolvadex) Nipple Cream for Gynecomastia Now Available at Empower Pharmacy

[Nelson Vergel]

I have proposed to Empower Pharmacy to make this product which will be launched in a month.

What do you guys think about applying this gel on nipples if you fear that you may be developing gynecomastia? One drawback of oral tamoxifen is decreased IGF-1 that can impair muscle gains. We do not know if localized transdermal application will avoid systemic exposure, however.

This new product contains tamoxifen citrate 2% (20mg/mL) in a transdermal cream base. It is applied to the breast area once daily for the treatment of male gynecomastia, or breast tissue pain/enlargement. Typically 1mL per area is applied once per day. Doctors also prescribe Tamoxifen cream off-label for gynecomastia prevention in men who are sensitive to this condition.

Quick Facts:

Patient Type: Males who present symptoms related to gynecomastia
Account Type:

Providers who offer:

· Testosterone replacement therapies
· Anabolic therapies (nandrolone/oxandrolone)
· Men’s Health


Product Detail:

Name: Tamoxifen 2% cream
Classification: Selective estrogen receptor modulators (SERM)
Dosage Form: Transdermal cream
Container: TBD (either a pump or topiclick)
Administration: Apply 1mL to affected area. Up to 2mL daily.
Uses: Treatment or prevention of gynecomastia;

 

[Nelson Vergel]

For more information about gynecomastia:

Gynecomastia: How to Diagnose and Treat it | Discounted Labs

 

[Nelson Vergel]

Click here for more information about the use of tamoxifen for gynecomastia:

Thoughts / Experiences with Nolvadex (Tamoxifen) for hCG mono induced Gynecomastia?

 

[Nelson Vergel]

Tamoxifen for the management of breast events induced by non-steroidal antiandrogens in patients with prostate cancer: a systematic review


Metabolism. 1986 Aug;35(8):705-8.
Treatment of gynecomastia with tamoxifen: a double-blind crossover study.
Parker LN, Gray DR, Lai MK, Levin ER.

Abstract
Benign asymptomatic or painful enlargement of the male breast is a common problem, postulated to be due to an increased estrogen/testosterone ratio or due to increased estrogenic or decreased androgenic stimulation via estrogen or androgen receptor interactions. Treatment at present consists of analgesic medication or surgery. However, treatment directed against the preponderance of estrogenic stimulation would seem to represent a more specific form of therapy. In the present double-blind crossover study, one-month courses of a placebo or the antiestrogen tamoxifen (10 mg given orally bid) were compared in random order. Seven of ten patients experienced a decrease in the size of their gynecomastia due to tamoxifen (P less than 0.005). Overall, the decrease for gynecomastia for the whole group was significant (P less than 0.01). There was no beneficial effect of placebo (P greater than 0.1). Additionally, all four patients with painful gynecomastia experienced symptomatic relief. There was no toxicity. The reduction of breast size was partial and may indicate the need for a longer course of therapy. A follow-up examination was performed in eight out of ten patients nine months to one year after discontinuing placebo and tamoxifen. There were no significant changes from the end of the initial study period except for one tamoxifen responder who developed a recurrence of breast tenderness after six months, and one nonresponder who demonstrated an increase in breast size and a new onset of tenderness after ten months. Therefore, antiestrogenic treatment with tamoxifen may represent a safe and effective mode of treatment for selected cases of cosmetically disturbing or painful gynecomastia.

 

[Nelson Vergel]

The cream is now available. I think it's under $80 per month supply. Shelf life 6 months. Here is how to write the script to fax Empower Pharmacy:

Tamoxifen 2% Cream 30mL
Apply 0.5mL - 1mL to affected area once daily

 

[HealthMan]

I would definitely use it. Tamoxifen makes me feel really bad (tons of side effects). If the topical application is effective in reducing/eliminating gyno and avoiding systemic exposure at the same time I wouldn’t think twice in using it. You mentioned IGF-1. Tamoxifen also increases SHBG therefore reducing FT.
Price might be a problem. Insurance would probably not cover the cream and it does cover the pills. for me a 1 month supply of tamoxifen cost less than 7 bucks using insurance.

 

[Nelson Vergel]

Yes, you can't beat the generic price but if your IGF1 does not decrease, your SHBG does not increase AND your gynecomastia is improved, then savings on oral tamoxifen may not justify the systemic effects.

 

[HealthMan]

Agree 100%. I am very sensitive to estradiol and had gynecomastia a few times. Tamoxifen worked everytime but i felt terrible. I would definitely try the cream in case i have gyno again

 

[Nelson Vergel]

This product was launched three week ago. Doctors can write a script as follows:

Tamoxifen 2% cream, 30 grams, Apply 0.5- 1mL to affected area.

 

[Dwhit]

Oral low dose and topical tamoxifen for breast cancer prevention: modern approaches for an old drug

How does this cream work locally given that tamoxifen requires hepatic activation?

 

[econnolly]

Has anyone switched from oral to the cream and noticed a decrease in side effects?

 

[dinhoguerra]

Has anyone switched from oral to the cream and noticed a decrease in side effects?

I I'd be grateful to hear it too.

 

[Sides]

As the article mentioned above states, transdermal tamoxifen cream applied locally to the breast shouldn't work, as tamoxifen is a pro-drug and it's beneficial effects depend on conversion in the liver into it's active metabolites like 4-OHT. However, if someone were to make a transdermal cream containing 4-OHT, that has been shown to work locally on the breast while avoiding the systemic effects of tamoxifen. I wish someone had a transdermal 4-OHT cream available.

"Tamoxifen is a pro-drug, requiring conversion by the phase I drug metabolizing cytochrome P450 enzymes, predominantly CYP2D6 but also CYP3A4/5 among others, to its major anti-estrogenic metabolites [52]. Toxicity can result from systemic administration, due to the activity of tamoxifen in non-breast tissues.
Transdermal delivery has long been recognized as an effective alternative to conventional systemic therapy, including oral administration. When delivered transdermally, a drug is characterized by distinct pharmacokinetics, with longer retention in the local tissue. However, due to the effectiveness of the barrier function of the stratum corneum, only a relatively small number of lipophilic drugs with low molecular weights (< 500 Da) have been successfully formulated for these purposes.
Since tamoxifen is a pro-drug requiring hepatic activation, the transdermal approach may not be suitable per se. A more reasonable approach is to utilize its more active metabolites. Mauvais-Jarvis and colleagues [58] determined that the tamoxifen metabolite 4-OHT, like progesterone, could be concentrated directly in the breast tissue.
Following transdermal application of 4-OHT in the studies conducted so far, very low plasma concentrations of the drug have been observed. These low plasma levels in the setting of a topical approach that bypasses first-pass metabolism in the liver suggest that there should be a reduction in systemic toxicity [58,59,65,78,79]."

Oral low dose and topical tamoxifen for breast cancer prevention: modern approaches for an old drug

 

[Nelson Vergel]

Let me see if 4-OHT can be sourced.

 

[dinhoguerra]

Let me see if 4-OHT can be sourced.

And so?

 

[Nelson Vergel]

And so?

Nope

 

[HealthMan]

Nope

Any feedback about the tamoxifen cream to treat gynecomastia? Reading about it seems like @Sides is correct in saying that given tamoxifen is a prodrug a topical application might not work.

 

[Nelson Vergel]

Two guys I know tried it with good results but they complained that the cream stained their T shirts, so Empower is working on a new vehicle for the formula.

 

[HealthMan]

Two guys I know tried it with good results but they complained that the cream stained their T shirts, so Empower is working on a new vehicle for the formula.

I will give it a try. Tks Nelson!

 

[HealthMan]

As the article mentioned above states, transdermal tamoxifen cream applied locally to the breast shouldn't work, as tamoxifen is a pro-drug and it's beneficial effects depend on conversion in the liver into it's active metabolites like 4-OHT. However, if someone were to make a transdermal cream containing 4-OHT, that has been shown to work locally on the breast while avoiding the systemic effects of tamoxifen. I wish someone had a transdermal 4-OHT cream available.

"Tamoxifen is a pro-drug, requiring conversion by the phase I drug metabolizing cytochrome P450 enzymes, predominantly CYP2D6 but also CYP3A4/5 among others, to its major anti-estrogenic metabolites [52]. Toxicity can result from systemic administration, due to the activity of tamoxifen in non-breast tissues.
Transdermal delivery has long been recognized as an effective alternative to conventional systemic therapy, including oral administration. When delivered transdermally, a drug is characterized by distinct pharmacokinetics, with longer retention in the local tissue. However, due to the effectiveness of the barrier function of the stratum corneum, only a relatively small number of lipophilic drugs with low molecular weights (< 500 Da) have been successfully formulated for these purposes.
Since tamoxifen is a pro-drug requiring hepatic activation, the transdermal approach may not be suitable per se. A more reasonable approach is to utilize its more active metabolites. Mauvais-Jarvis and colleagues [58] determined that the tamoxifen metabolite 4-OHT, like progesterone, could be concentrated directly in the breast tissue.
Following transdermal application of 4-OHT in the studies conducted so far, very low plasma concentrations of the drug have been observed. These low plasma levels in the setting of a topical approach that bypasses first-pass metabolism in the liver suggest that there should be a reduction in systemic toxicity [58,59,65,78,79]."

Oral low dose and topical tamoxifen for breast cancer prevention: modern approaches for an old drug

Biotransformation of Drugs in Human Skin

Maybe the skin is able to partially metabolize tamoxifen. Seen a few medical articles talking about the existence of P450 enzymes in the skin. Any thoughts @Nelson Vergel?