Scientists May Have Improved Overall Efficacy of Two Common Chemo Drugs

A better version of vinblastine could be on the way.

According to a study published in the journal ACS Medicinal Chemistry Letters, researchers from The Scripps Research Institute (TSRI) are reporting that they have modified the drug and created a version of vinblastine that is 10 to 200 times more potent, has the ability to overcome drug resistance, and might increase the efficacy of a similar drug, vincristine.

About Vinblastine and Vincristine

Vinblastine is one of the oldest and most reliable drugs in chemotherapy. It is used to treat a broad range of cancers, from blood cancers to cancers of the ovaries, breast, lung and bladder. The same is true of vincristine, although it is more limited, generally reserved for the treatment of blood cancers.

Vinblastine and vincristine come from the Madagascar periwinkle (a pink-flowered herb) and they work in the same way – by binding to a certain cellular protein, which disrupts cell division and leads to cell death.

Overcoming Drug Resistance in Long-Term Use

Both vinblastine and vincristine suffer from the same problem: When used for too long, drug resistance develops, making them worthless to the patient.

Since vinblastine comes from a plant, investigators from TSRI couldn't recreate them through biotechnology, so they created a so-called "three-step preparation process" by taking commercially available chemicals and applying chemistry tricks they created solely for this purpose. These modifications resulted in analogues that were not only more effective than the originals but also able to overcome drug resistance.

According to lead author Dale L. Boger, professor and chair at TSRI:

The potency of these analogues is extraordinary. They show activity down at the 100 picomolar level (100 trillionths of a mole) against some cell lines. So we have something here that's really unique, and we discovered it only because of the novel chemistry we developed. These new compounds should improve on what are already superb anticancer drugs.

Source: MNT