Bortezomib in the treatment of cancer

Aldo M. Roccaro, Angelo Vacca, Domenico Ribatti

Research output: Contribution to journalArticlepeer-review


Bortezomib (Velcade, formerly PS-341) represents the first proteasome inhibitor to have shown anti-tumor activity in both solid and haematological malignancies. It blocks activation of nuclear factor-kappa B (NF-kB), resulting in increased apoptosis, decreased angiogenic cytokine production, and inhibition of tumor cell adhesion to stroma. Additional mechanisms of action include c-Jun N-terminal kinase activation, effects on growth factor expression and antiangiogenic properties. Multiple myeloma is the prototype of cancer where bortezomib has shown marked in vitro activity, which was followed by rapid translation to phase I, II and III clinical trials, and resulted in accelerated approval by the FDA for the treatment of patients with relapsed refractory disease. Different clinical trials are currently ongoing in multiple myeloma as well as in many others haematologic and solid tumors (mantle cell and follicular non-Hodgkin's lymphoma; peripheral T-cell lymphoma; Waldenström's macroglobulinemia, chronic lymphocytic leukemia; head and neck / gastroesophageal junction / stomach /colo-rectal / prostate / non-small cell lung cancer).

Original languageEnglish
Pages (from-to)397-403
Number of pages7
JournalRecent Patents on Anti-Cancer Drug Discovery
Issue number3
Publication statusPublished - 2006


  • Anti-tumor activity
  • Bortezomib
  • Proteasome inhibition

ASJC Scopus subject areas

  • Oncology
  • Cancer Research
  • Pharmacology (medical)
  • Drug Discovery


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