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Single-Dose Drug Candidate Eradicates Breast Cancer Tumors in Mice

Photo credit: www.sciencedaily.com

Despite advances in medical therapies, breast cancer continues to be a principal cause of cancer-related mortality among women. Standard treatment regimens often include surgical intervention followed by hormone therapy. However, these therapies can lead to long-term complications such as osteoporosis, sexual dysfunction, and thromboembolic events. Recently, researchers unveiled a promising new treatment method in ACS Central Science, demonstrating the potential to eliminate small breast tumors and significantly reduce the size of larger tumors in mouse models after a single dose, all while minimizing adverse effects.

The majority of breast cancers are classified as estrogen receptor positive (ER+), necessitating years of hormone therapy as part of the treatment plan. Although hormone therapies tend to be more tolerable than chemotherapeutic agents, they can still produce side effects that negatively impact patients’ quality of life and may increase the likelihood of cancer recurrence or resistance to treatment. This underscores the pressing need for targeted cancer treatments that can effectively destroy tumor cells while minimizing the associated side effects.

To tackle this issue, Paul Hergenrother and his team previously devised a small molecule known as ErSO. While this compound demonstrated effectiveness in targeting ER+ breast cancer cells, it also led to unwanted side effects. In a 2022 study, the researchers created a variety of small molecule derivatives based on ErSO, finding that these new compounds displayed enhanced potency, greater specificity for ER+ cancer cells, and improved pharmacological characteristics compared to the original molecule.

In their most recent research, the scientists concentrated on one particular derivative, ErSO-TFPy, and made several notable observations:

  • It successfully induced cell death in various human ER+ breast cancer cell lines in laboratory settings.
  • It was well tolerated by different species (mice, rats, and beagles) without evident harmful effects.
  • It reduced transplanted human breast tumors with differing genetic profiles in a mouse model.

During experiments involving dosing, the team discovered that a single administration of ErSO-TFPy led to either total or nearly total regression of both small and larger tumors in the subjects. Unlike other treatments requiring prolonged administration, the minimal circulation of ErSO-TFPy in the body after a single dose may substantially lower the chances of experiencing side effects or late-onset effects. While further studies are necessary to verify the safety and effectiveness of this treatment, the researchers propose that if these outcomes are applicable to human patients, ErSO-TFPy could revolutionize the approach to treating ER+ breast cancer.

“It is quite unusual for a compound to achieve tumor shrinkage in mouse models of breast cancer, let alone completely eliminate tumors with just one dose. We are optimistic about the potential of ErSO-TFPy in revolutionizing breast cancer treatment,” Hergenrother commented.

The authors express gratitude for the support received from the National Cancer Institute at the National Institutes of Health and the Cancer Center at Illinois.

Source
www.sciencedaily.com

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