Dosing and uses of Custirsen
Prostate Cancer
Pending FDA approval for metastatic castrate-resistant prostate cancer (CRPC)
It is administered in combination with cabazitaxel/prednisone for CRPC following prior treatment with a docetaxel-containing regimen
Pharmacology of Custirsen
Mechanism of action
Custirsen is an antisense oligodeoxynucleotide that blocks the production of the protein clusterin, which may play a fundamental role in cancer cell survival and treatment resistance
Clusterin is upregulated in tumor cells in response to treatment interventions such as chemotherapy, hormone ablation and radiation therapy
In patients with prostate cancer, custirsen inhibits testosterone-repressed prostate message-2 (TRPM-2), which is an anti-apoptotic clusterin that is overexpressed by prostate cancer cells and is associated with chemoresistance
