Treatment of cancer with bortezomib

The drug is given intravenously over three to five seconds, and it's scheduled on, for example, Monday, Thursday, Monday, Thursday, two weeks in a row. Then there is a 10-day break, so it's a 21-day cycle. It's very important that 72 hours elapse between the doses so that normal cells can recover from the effect of protease inhibition. Proteasomes are present in every single cell, and the protease inhibition results in far more damage to the cancer cell, thankfully, than to the normal cells. But if you didn't keep that 72-hour interval, even the normal cells would start showing bad effects of treatment.

These new drugs, such as thalidomide and bortezomib, can be combined to increase response rates. Bortezomib overcame resistance to thalidomide. Patients who had had previous treatment [with] thalidomide and were now progressing on it or had not responded, the simple act of adding bortezomib to their treatment resulted in responses. This really leads to hope. One drug brings another new similar drug, and that new drug can be combined with older drugs and newer drugs, so you end up with having so many more treatment options.

Bortezomib functions as a garbage disposal unit for waste proteins generated within the cells. Bortezomib was designed to inhibit protease. It effectively chokes or blocks the garbage disposal unit, resulting in build-up of waste products which then kill the cell inside which the waste products are built up. It's a very simple and elegant way of killing off the malignant cell.

The cancer cells have more intercellular activity so more waste products are generated within these cells and, therefore, they die much more easily than normal cells. Although it's one simple blocking of the protease, multiple things happen, eventually resulting in the death of the cancer cells.

As far as myeloma, bortezomib blocks a protein called NF-kB in the malignant cells. This protein is important in gene regulation, and by sticking it, the bortezomib stops it from working and promotes apotosis.