Melanoma medicine is being tested on volunteers
Experimental cancer drug successfully tested on humans
Denis Strigun, Naked Science
Scientists from the University of Virginia have confirmed the effectiveness of pevonedistat in the treatment of melanoma in human studies. The results of the study are published in the journal EBioMedicine (Benamar et al., Inactivation of the CRL4-CDT2-SET8/p21 ubiquitylation and degradation axis underlies the therapeutic efficacy of pevonedistat in melanoma).
Pevonedistat (pevonedistat) is a selective inhibitor of the Nedd8-activating enzyme, considered as an antitumor drug. It was developed in 2015 and is currently undergoing clinical trials. Until now, the mechanism of action of pevonedistat has been unclear, since it is designed to "turn off" hundreds, if not thousands of proteins.
In a new study, the authors identified one of these proteins – it provides rapid replication of cancer cells, in particular melanoma. The protein inhibited by the drug was associated with the CDT2 gene. Its high content is characteristic of various tumors, for example, tumors of the brain, liver, breast. In the case of melanoma, CDT2 expression is more pronounced, as a result, there is an increased sensitivity of this type of tumor to the drug. By blocking the production of CDT2 protein, pevonedistat stops the replication of cancer cells, and they are destroyed.
"We really hope that the drug will play a big role in the fight against melanoma. Tests show that it is effective against all types of melanoma, including resistant ones," said University representative Terek Abbas. He added that if approved by the FDA, pevonedistat can be used as part of a second-line therapy.
Melanoma is a malignant tumor, often localized on the skin. Melanoma is characterized by a high frequency of relapses and metastases, and therefore its treatment is associated with significant difficulties. The main method of treatment of initial melanoma is surgical removal, with metastatic immunotherapy, polychemotherapy and radiation therapy are used. The survival rate as a result of first-line therapy at stage III of melanoma is 20-45 percent.
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08.09.2016