Revelutamide,a second-generation androgen receptor antagonist for the treatment of metastatic hormone-sensitive prostate cancer
Revelutamide is a new type of second-generation androgen receptor(AR)antagonist independently developed in China,which can inhibit the activation of AR signaling pathway through a triple potent inhibition mechanism,thus effectively inhibiting the proliferation of prostate cancer cells.Revelutamide binds to the ligand-binding domain of AR,competitively inhibits the binding of androgen to AR,prevents androgen-induced AR activation,and inhibits AR nuclear translocation.It also inhibits the expression of genes that regulate prostate cancer cell proliferation by binding to DNA and reduces AR-mediated gene transcription.In addition,revelutamide introduces a double hydroxyl group,increasing its water solubility by nearly 20-fold compared to its counterparts enzalutamide and apalutamide,which is less likely to cross the blood-brain barrier,resulting in a reduced risk of seizures and lethargy.In June 2022,revilutamide was approved in China for the treatment of patients with metastatic hormone-sensitive prostate cancer(mHSPC)with high tumor burden.This article mainly reviews the mechanism of action,pharmacokinetics,safety and clinical efficacy evaluations of revirutamide,aiming to provide theoretical references for new drug development and clinical application of revirutamide.
revelutamideandrogen receptor antagonistprostate cancer
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