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Pharmacy and Medication

Know your medicine and arm yourself with information about your prescription therapy to ensure effective treatment, keep you safe, and help you to be aware of potential problems.  Your Pharmacist is also an excellent medication consultant, if you have questions your Pharmacist is only a phone call away.

A recent study identified an unused psychotropic drug that might help in the fight against cancer. The molecule could help to minimize drug resistance.
Chemotherapy drugs
A new study sheds light on drug-resistant tumors.

One of the most significant stumbling blocks to effectively treating cancer is its ability to develop immunity to some drugs.

Cancer cells are capable of ridding themselves of toxic chemotherapy drugs, rendering the chemicals toothless.

Researchers at the Institut de Pharmacologie Moléculaire et Cellulaire in France have been investigating this phenomenon for some time.

They have already pinned down some of the cellular machinery that appears to be involved in the process, and their most recent findings were published in the International Journal of Cancer earlier this week.

Patched, Hedgehog, and cancer

One of the main players identified by the scientists is a receptor called Patched, which is activated by the intriguingly named Hedgehog protein.

Patched has a key role in the developing embryo; fruit fly larvae that lack the Hedgehog signaling protein do not grow correctly and end up short and spiny — hence the name Hedgehog.

Previous studies showed that Patched receptors are considerably more abundant in cancer cells than healthy cells. In a range of cancers — including melanoma, colorectal cancer, and breast cancer — the Patched protein appears to be repurposed to protect cancer cells.

In earlier work, the scientists had showed that Patched pumps chemotherapy agents back out of cancerous cells where they cannot cause any damage. This, in part, helps tumor cells to survive chemotherapy.

The researchers first showed that the Patched receptor did help tumor cells to become tolerant to a chemotherapy drug called doxorubicin. Next, they set out to finds ways of reversing the process.

In order to do this, they needed to identify a molecule that would block Patched and prevent it from flushing anticancer drugs out of tumor cells. In all, they screened 1,200 small molecules, eventually finding a good fit: methiothepin.

Repurposing methiothepin

Methiothepin works at a number of sites, including serotonin receptors. It is a “psychotropic agent,” meaning that it can alter perception, mood, cognition, or behavior. Methiothepin is also a member of the tricyclic group of drugs, some of which have been used in the treatment of conditions such as schizophrenia.

Following methiothepin’s creation in the 1960s, it was never marketed. However, this study shows that it might soon be used in an altogether different way.

The team showed that methiothepin was able to prevent Patched from pumping doxorubicin out of cancerous cells.

The researchers tested a combination of doxorubicin and methiothepin on cancerous human cells in the laboratory, and the same cells implanted in mice. In both cases, the combination of drugs was more potently anticancer than doxorubicin alone.

Importantly, they also found that the two drugs together did not increase the levels of doxorubicin found in the heart (cardiotoxicity is a major side effect of doxorubicin treatment).

Next, the researchers want to work with chemists to fine-tune methiothepin; they hope to be able to prevent it from acting on serotonin receptors and increase its activity on Patched receptors.

This information is designed for educational purposes only and should not be used in any other manner. This information is not intended to be a substitute for informed medical advice. You should not use this information to diagnose or treat a health problem or disease without consulting with a qualified health care provider. A consultation with your health care professional is the proper method to address your health concerns. You are encouraged to consult your health care provider with any questions or concerns you may have regarding your condition. Rapid advances in medicine may cause information contained here to become outdated, invalid or subject to debate. Accuracy cannot be guaranteed.

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