RK-251 activates inside cancer cells in response to elevated ROS levels, showing promising preclinical results against aggressive triple-negative breast cancer

Indian scientists have developed a new smart cancer drug candidate designed to become active primarily inside cancer cells, offering a potentially more targeted approach to cancer treatment and reducing the risk of damage to healthy cells. The research has been led by Dr Asis Bala of the Institute of Advanced Study in Science and Technology (IASST), an autonomous institute under the Department of Science and Technology, Government of India, in collaboration with Dr K.P. Bhabak of the Indian Institute of Technology Guwahati.
The drug candidate, named RK-251, is designed to remain relatively inactive in normal tissues and become activated inside cancer cells, according to reports. Conventional cancer treatments can affect healthy cells along with tumour cells, often resulting in significant side effects. The new approach seeks to overcome this limitation by using a biological difference between cancerous and healthy cells as a trigger for drug activation, the report noted.

Cancer cells typically generate higher levels of reactive oxygen species (ROS), molecules that can cause cellular damage but can also be exploited for targeted drug delivery. When RK-251 enters a cancer cell, the elevated ROS levels are designed to trigger activation of the compound, releasing NBDHEX, a potent anticancer agent. NBDHEX works by targeting proteins that are important for the survival and treatment resistance of several cancer cells. By releasing the compound primarily in the cancer-cell environment, RK-251 could potentially deliver its anticancer action more selectively while limiting exposure to healthy tissues.
In preclinical experiments, RK-251 showed strong activity against aggressive triple-negative breast cancer cells, while producing considerably less effect on healthy cells. The findings indicate that the ROS-responsive mechanism could help improve the selectivity of cancer treatment. The researchers also evaluated the drug candidate using zebrafish embryos (Danio rerio). The experiments did not show obvious signs of toxicity, while the compound displayed the expected fluorescence in the presence of reactive oxygen species. This provided additional evidence for the proposed mechanism of action and supported further investigation of the drug candidate. However, RK-251 is still at the preclinical research stage and is not yet available as a treatment for patients. Further laboratory studies, safety assessments and validation through appropriate clinical trials will be necessary before the drug can be evaluated for use in humans.
Disclaimer: “This story has been published from a syndicated news feed. Only the headline and subtitle have been edited by EPN.”

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