3met --- Gold-Metformin Prodrug --- Treating Aggressive Breast Cancer
Hi friends, just sharing the following:
Treating aggressive breast cancer with an anti-diabetic drug
April 21, 2021
National University of Singapore (NUS) researchers developed an approach to target highly resistant triple-negative breast cancers (TNBCs) by interfering with their energy production using cytotoxic gold-metformin prodrugs.
Metformin is a widely prescribed “over-the-counter” medication for Type 2 diabetes.
There is some evidence that patients taking metformin for a long time have significantly reduced risk of developing cancer.
However, despite well-characterised anticancer effects and the low cost of metformin, its use as an anticancer agent has serious drawbacks.
Metformin is poorly taken up by cells.
In order to achieve therapeutic concentrations, it has to be taken repeatedly in high doses, which may cause serious side effects in cancer patients.
A team of researchers led by Prof ANG Wee Han from the Department of Chemistry, National University of Singapore and Prof Maria BABAK from City University of Hong Kong devised an approach to chemically conjugate metformin, as well as its analogue phenformin.
This is achieved by using a gold-based active molecular fragment to improve bioavailability and to achieve synergistic action of the two key components (metformin and gold molecules).
By taking advantage of the electrochemical activity of the gold-based molecule, the team successfully delivered metformin into cancer cells with high selectivity.
The anticancer activity of the lead drug candidate developed by the team named 3met, was found to be more than 6,000 times higher when compared to metformin.
Interfering with Metabolic Profile of Triple‐Negative Breast Cancer using Rationally‐Designed Metformin Prodrugs
First published: 23 March 2021
This sounds fabulous. But I guess it is only at the cell research phase?