Case Studies on Breast Cancer and RAD 140: Where to Buy RAD 140 For Research

Case Studies on Breast Cancer and RAD 140
Table of Contents

RAD 140 and Cancer

The American Cancer Society estimates that in 2022, around 287,850 women will receive a diagnosis of invasive breast cancer (BC). That number feels startling; however, the good news is that there is ongoing research looking at new methods of treating BC [1].

One potential treatment for this disease includes RAD 140. Keep reading to learn more about the research being done with SARMs and BC. 

RAD 140 in BC Models

A study from 2017 , looked at the androgen receptors (AR) and estrogen receptor (ER) positive (AR/ER+) breast cancer cells. Because steroidal androgens had been successful in suppressing these cells, researchers wanted to determine if oral selective androgen receptor modulators like RAD 140 would be effective as well [3]. 

To determine this, they looked at both in vitro and in vivo models of androgen receptors and estrogen receptor-positive BC for their research purposes [3]. 

Methods

For the in vivo portion of this test, researchers used female athymic nude mice. They implanted tumor fragments subcutaneously in the flank [3]. 

Researchers administered agents in three groups being the RAD 140, Dihydrotestosterone (DHT), or fulvestrant as a single agent or in combination with palbociclib to the female and male rats [3]. 

Researchers administered the RAD 140, palbociclib, and the vehicle 0.5 percent carboxymethyl cellulose orally. The fulvestrant was administered as a subcutaneous injection, and the DHT was given as subcutaneously implanted pellets [3]. 

This occurred from the day of randomization to the end of the study, and body weight, and tumor volume measurements occurred two times per week [3]. 

For the in vitro study, well plates were used. The cells were seeded in a medium with 10 percent CSS at 30,000 cells per well in 24 well plates. These were then treated for fourteen days with RAD 140, DHR, or DMSO. The treatments were renewed every three days [3]. 

At the end of the fourteen-day treatment period, the trypsinized cells were stained with Trypan blue. Researchers used a Nexcelom Cellometer for live cell counting [3]. 

Results and Conclusions

The results of this study showed that RAD 140 is an AR in breast cancer cells. It has a distinct mechanism of action; this includes the AR-mediated repression of ESR1 [3]. 

In addition, RAD 140 inhibits the growth of multiple androgen receptor and estrogen receptor-positive BC PDX models. It does this in combination with palbociclib and as a single entity [3]. 

Because of the results of this study further clinical investigation of RAD 140 as a treatment for AR/ER+ BC subjects should be completed and the androgenic side effects should be studied [3]. 

RAD 140 in Metastatic BC

The following study we’ll look at was published in January of 2021. This study was the first that tested subject phase one study for using RAD 140 in for ER+/HER2- metastatic BC [1]. 

The goal of this study was to assess the following from RAD 140 [1 Below]. :

  • Safety
  • Tolerability
  • Antitumor activity
  • Maximum tolerated quantity
  • Pharmacokinetic profile

Method

This study was an escalation study regarding various test amounts. Researchers used a 3 + 3 design. The female subjects enrolled were premenopausal vs post menopausal women and diagnosed with ER+ and epidermal growth factor receptor 2 metastatic BC [1]. 

Researchers used serum sex hormone-binding globulin and a prostate-specific antigen as surrogate markers of AR engagement. Overall, 22 heavily pretreated female subjects with metastatic BC enrolled in the study [1]. 

Women received once daily administration. The test levels included [1 below]. 

  • 50 mg (six women) 
  • 100 mg (13 women)
  • 150 mg (three women) 

Results and Conclusions

There were some treatment-emergent adverse events. The most frequent consisted of elevated [1]

  • Aspartate Aminotransferase (59.1 percent) 
  • Alanine Transaminase (45.5 percent) 
  • Total blood bilirubin (27.3 percent) 

In addition, some subjects experienced side effects including vomiting, decreased appetite, and weight (27.3 percent each). The half-life of 44.7 hours supported the once-a-day scheduling [1]. 

One subject receiving the 100 mg a day testing had a partial response at baseline, this subject had an ESR1 mutation. Overall, at 24 weeks, the clinical benefit rate was 18.2 percent [1]. 

The median progression-free survival for participants was 2.3 months. The paired baseline and biopsies during the study showed AR engagement with this [1]. 

Researchers determined that RAD 140 has potential in treating AR+/ER+/HER2- metastatic BC with an acceptable safety profile. More research is needed to test the side effects of using RAD 140 in this manner [1]. 

RAD 140 in ER+/HER2- BC

The final study was published in 2019 and looked at RAD140 in ER+/HER- BC. AR is expressed in about 90 percent of estrogen receptor-positive BC [2].

Therapies that are androgen-based have had response rates up to 20 to 25 percent. However, because of poor tissue selectivity, potential aromatization to estrogen, and the emergence of ER-targeted agents, these therapies aren’t in common use. Researchers used this phase one escalation study to look at the nonsteroidal SARM RAD 140 [2].

Methods

Researchers used a 3 + 3 design for this study. Their primary objective was to determine the safety, and the maximum tolerated test amount. Secondary objectives included pharmacokinetics and antitumor activity [2]. 

The eligibility requirements for subjects included the following [2]:

  • ER+/HER2- and inoperable metastatic BC
  • Post-menopausal
  • Ineligible for standard therapy

AR engagement was assessed using sex hormone-binding globulin and serum prostate-specific antigen. The study included 16 subjects. Testing levels were as follows [2]

  • 50 mg (six participants) 
  • 100 mg (seven participants) 
  • 150 mg (three participants) 

Each subject was given test amounts daily, and the median amount of time for testing length was eight weeks. 

Results and Conclusions

The most frequent side effects or adverse events of this test include [2]:

  • Elevated Aspartate Aminotransferase and Alanine Transaminase
  • Decreased appetite and weight 
  • Constipation

There were no deaths related to the study. One subject receiving a test amount of 100 mg had a partial response. Two subjects showed stable disease at greater than or equal to 12 weeks [2]

It took 15.9 weeks to achieve a partial response. Sex hormone-binding globulin decreased in 12 out of 12 subjects. While prostate-specific antigens increased in 10 out of 14 subjects, including the subject with a partial response [2].

Researchers concluded that the maximum tolerated test amount for RAD 140 is 100 mg once a day but that there is still a high risk of elevated liver enzymes. In addition, they determined that it has an acceptable safety profile for disease and that there is preliminary evidence of antitumor activity and target engagement [2].

Continued Need for Research With RAD 140

There have been promising results, but at the same time, there is a continued need for research with RAD140. Are you preparing to do your own SARMs research? If so, you can buy RAD 140 here at Sports Technology Labs or browse our selection of additional SARMs and peptides for sale

Where to Find RAD 140

Looking for the best place to buy RAD 140 online? RAD 140 is for laboratory research use only. RAD 140 is not approved for human consumption and is currently used for clinical research only as it is not FDA approved. Sports Technology Labs offers the highest quality SARMs for research and needs for clinical trials. Contact Sports Technology Labs today to discuss your SARMs needs.

We offer great customer service that makes us stand apart from all other companies, so feel free to message us today. We also have the new RAD 150 for sale as well.

Scientific References:

1. Hamilton E, Vidula N, Ma C, LoRusso P, Bagley RG, Yu Z, Annett M, Weitzman A, Conlan MG, Weise A. Phase I dose escalation study of a SARM RAD140 in estrogen receptor positive (ER+), HER2 negative (HER2-) breast cancer (BC). Annals of Oncology. 2020 Jan 8 [accessed 2022 Apr 22]. 

2. LoRusso P, Hamilton E, Ma C, Vidula N, Bagley RG, Troy S, Annett M, Yu Z, Conlan MG, Weise A. A first-in-human phase 1 study of a novel SARM, RAD140, in er+/her2- metastatic breast cancer. Clinical Breast Cancer. 2021 Aug 20 [accessed 2022 Apr 22].

3. Yu Z, He S, Wang D, Patel HK, Miller CP, Brown JL, Hattersley G, Saeh JC. Selective androgen receptor modulator RAD140 inhibits the growth of androgen/estrogen receptor–positive breast cancer models with a distinct mechanism of action. American Association for Cancer Research. 2017 Dec 14 [accessed 2022 Apr 22].

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