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New derivatives of tamoxifen with less adverse effects

Scientists at CSIC and at University of La Laguna have patented new compounds derived from tamoxifen, one of the most commonly used cancer-fighting drugs. The new molecules could be used as an alternative treatment to tamoxifen, as they don't have its adverse effects, and as diagnostic biomarkers due to their fluorescence quality. They could be used also as a laser pigment.

Left: Cancer cells labeled with one of the derivatives. Right: the corresponding transmission image of the same cells.Tamoxifen is one of the most powerful fighting-cancer drugs, used commonly against breast cancer. Its efficacy has been widely demonstrated. Nevertheless, treatment with tamoxifen increases the risk of developing uterine and endometrial cancer.

According to the National Cancer Institute (EUA), two in every thousand women treated with tamoxifen will suffer of endometrial cancer – while only one in every thousand women receiving placebo will suffer this cancer. Although it doesn’t seem very high figure, it is one of the most worrying adverse effects. 

Other less severe adverse effects of tamoxifen are pain at joints, intestinal disorders, leg cramps, hot flashes, vaginal dryness, and less often blood clots, heart attacks or cataracts.

Scientists at CSIC's Instituto de Productos Naturales y Agrobiología and at University of La Laguna led by Dr. Alicia Boto and Professor Mario Diaz have developed new molecules derived from tamoxifen that could be used as an alternative treatment.

Preclinical research on animals has shown that these compounds have anti-estrogenic activity as powerful as tamoxifen but less adverse effects. Now, partners are being sought for starting clinical research, and to exploit the existing know-how through a patent License agreement.

Animal experiments in laboratory have shown that adverse effects reduction is mainly in two cases. Firstly, there is less uncontrolled endometrial cell growth, which implies less risk of endometrial cancer. Secondly, there are less intestinal disorders, an apparently minor problem that is very common and detrimental to the patient’s health and quality of life.

The new compounds, patented by the CSIC and the University of La Laguna, have another potential use as diagnostic biomarkers, as they have fluorescence properties, and as laser pigments. Scientists found this last potential use by chance, when the group led by Fernando Lahoz, at University of La Laguna, was studying the optical properties of the compounds.

As Alicia Boto says, “these molecules are one of the most powerful pigments known for laser. They can absorb a specific light wavelength and give back a laser beam that has much higher intensity than the ones obtained with conventional laser pigments”. In this sense, the compounds would be useful for electronics, medical, nanotechnology and optical applications.

Contact:

Sebastián Jiménez Reyes
Tel.: + 34 – 922 25 68 47. Ext. 205.
Fax: + 34 – 922 26 01 35
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