Loperamide is a common medicine. It is used against diarrhea. Sjoerd van Wijk from the Institute for Experimental Tumor Research in Pediatrics at Goethe University has discovered another possible application. The preparation works against brain tumors, which are difficult to fight with conventional therapies such as radiation. In certain tumor cells, loperamide leads to a stress reaction in the endoplasmic reticulum (ER), the cell organelle that is responsible for essential steps in protein synthesis in the body. That in turn has an unusual effect. To a certain extent, the tumor cells commit suicide, they eat themselves up. This is called autophagy.
Healthy cells are not attacked
“Our experiments with cell lines show that autophagy could support the treatment of glioblastoma brain tumors,” says van Wijk. Glioblastoma is a very aggressive and usually fatal form of cancer in children and adults that reacts poorly to previous therapies. Therefore, researchers are looking for new treatment options.
It could be the diarrhea medicine. It only acts on cancer cells, not on healthy tissue. In the intestine, for example, it only works at certain binding sites and is not really absorbed by the body. The loperamide-induced cell death of glioblastoma cells could help to develop new therapeutic approaches for the treatment of this serious cancer. “Our findings also open up new, exciting possibilities for other diseases in which ER breakdown is impaired, such as nerve cell diseases or dementia diseases and other types of tumors.”, so van Wijk.
The blood-brain barrier has to be crossed
Before loperamide can actually be used in the treatment of glioblastomas or other diseases, van Wijk’s researchers have to find a way how loperamide can be transported into the brain and penetrate the blood-brain barrier. This prevents foreign substances from the blood from entering the brain. Loperamide would be identified as a pest, so it would not be allowed through. The researchers believe that nanoparticles could still be used as transporters. So it will be a while before loperamide can be used as a cancer killer.
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