Carfilzomib:from natural product to drug
NIU Jun-xing
XU Xing-yu
HU Li-hong
Abstract：Natural products and their derivatives have been invaluable as a source of therapeutic agents. Carfilzomib,a potential chemotherapy drug for patients with multiple myeloma,was developed from a microbial natural product Epoxomicin. Epoxomicin was found to exhibit potent anti - cancer activity,which might attribute to its inhibitory activity against proteasome. Because of its unique two- step binding mode,Epoxomicin has a clear advantage compared to other proteasome inhibitors with their substantial off - target activi-ty. With a more pontecy and better drug - like properties,Carfilzomib was developed from the lead compound Epoxomicin and approved by FDA as a second - generation proteasome inhibitor in 2012.
Keywords：Proteasome inhibitorCarfilzomibEpoxomicin
Publication Date：2015-01-01
Online Publishing Date：2025-08-15(First online date of this platform, not the publication date of the document)
Pages：6( 559-563,583 )