carfilzomib (YU101, CFZ, Kyprolis)

Indications

• relapsed & refractory multiple myeloma

Adverse effects

• thrombocytopenia
• anemia
• lymphopenia
• neutropenia
• pneumonia
• fatigue
• hyponatremia

Mechanism of action

• inhibits proteasome
• irreversibly binds to and inhibits the chymotrypsin-like activity of the 20S proteasome
• inhibition of proteasome-mediated proteolysis results in a build-up of polyubiquinated proteins, which may cause:
  • cell cycle arrest
  • apoptosis
  • inhibition of tumor growth

Notes

• cost: $10,000 per 28 day cycle

More general terms

• small inhibitory antineoplastic agent (ib drug)

Database

• PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=11556711