Sunday, January 26, 2025

Drug candidate eliminates breast cancer tumors in mice in a single dose

Good news! Cancer is history (soon)!

"Now, researchers ... have created a novel treatment that eliminated small breast tumors and significantly shrank large tumors in mice in a single dose, without problematic side effects. ...

Most breast cancers are estrogen receptor positive (ER+) ...

In 2022, the researchers synthesized a series of small molecules similar to ErSO. That prior study demonstrated that these derivatives have higher potency, greater selectivity for ER+ cancer cells and better pharmacological properties than the original compound.

Now, in the latest study, the researchers further evaluated one derivative, ErSO-TFPy, and found that it:
  • Effectively killed multiple human ER+ breast cancer cell lines in culture.
  • Was well tolerated, with no obvious deleterious effects, by multiple species (mice, rats and beagles).
  • Shrank transplanted human breast tumors of various genetic backgrounds in mice.
...
"It is very rare for a compound to shrink tumors in mouse models of breast cancer, let alone completely eradicate those tumors with a single dose, so we are eager for ErSO-TFPy to advance for treatment of breast cancer," ..."

From the abstract:
"Patients with estrogen receptor α positive (ERα+) breast cancer typically undergo surgical resection, followed by 5–10 years of treatment with adjuvant endocrine therapy. This prolonged intervention is associated with a host of undesired side effects that reduce patient compliance, and ultimately therapeutic resistance and disease relapse/progression are common.
An ideal anticancer therapy would be effective against recurrent and refractory disease with minimal dosing; however, there is little precedent for marked tumor regression with a single dose of a small molecule therapeutic. Herein we report ErSO-TFPy as a small molecule that induces quantitative or near-quantitative regression of tumors in multiple mouse models of breast cancer with a single dose. Importantly, this effect is robust and independent of tumor size with eradication of even very large tumors (500−1500 mm3) observed. Mechanistically, these tumor regressions are a consequence of rapid induction of necrotic cell death in the tumor and are immune cell independent. If successfully translated to human cancer patients, the benefits of such an anticancer drug that is effective with a single dose would be significant."

Drug candidate eliminates breast cancer tumors in mice in a single dose


Something similar was apparently already reported in 2021 by some of the same researchers:


Graphical abstract

Figure 4. A single dose of ErSO-TFPy induces complete tumor regressions in mouse models.


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