The Pharmaceutical Journal
Vol 269 No 7222 p637
2 November 2002

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Enzyme inhibitor that targets cancer cells spares healthy cells

A new enzyme inhibitor, bortezomib, may be an effective way of targeting cancer cells while sparing healthy ones, according to Millennium Pharmaceuticals, the company developing the drug.

The company explains that bortezomib inhibits proteasome, an enzyme complex in the cell responsible for breaking down a variety of proteins, including many that regulate cell division. Inhibiting proteasome with bortezomib disrupts regulation of cancer cell regulatory processes, inducing programmed cell death.

Data from a phase II trial presented at the European Society of Medical Oncology in Nice last month show that myeloma protein, a marker of myeloma tumour burden, was stabilised or reduced in 77 per cent of the 70 patients with multiple myeloma treated with bortezomib for up to 24 weeks.

A total of 14 patients had a greater than 90 per cent reduction in myeloma protein levels and 33 had at least a 25 per cent reduction. Overall, the median time to progressive disease had not been reached after 6.2 months of follow-up.

Side effects of bortezomib included nausea, fatigue, diarrhoea, headache, decreased platelets and peripheral neuropathy.

The company says that bortezomib is being investigated in clinical studies for solid tumours, including colon, lung, breast, prostate and pancreatic cancers.