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A more selective version of abiraterone that was meant to avoid the need for steroids. It delayed the cancer on scans but did not help men live longer, and was abandoned.
Orteronel is a non-steroidal, partially selective inhibitor of CYP 17,20-lyase. The selectivity was the point: abiraterone inhibits both the 17-alpha-hydroxylase and the 17,20-lyase activities of CYP17, which is why it raises mineralocorticoids and has to be given with a corticosteroid. A lyase-selective inhibitor should avoid that.
ELM-PC 4 randomised 1,560 chemotherapy-naive men with metastatic castration-resistant prostate cancer at 324 centres in 43 countries to orteronel 400 mg with prednisone twice daily or placebo with prednisone. Median radiographic progression-free survival was 13.8 months against 8.7, hazard ratio 0.71 (95 percent confidence interval 0.63 to 0.80, p<0.0001), a large and unambiguous effect. Median overall survival was 31.4 against 29.5 months, hazard ratio 0.92 (0.79 to 1.08, p=0.31), which is nothing. The companion trial in men after docetaxel, ELM-PC 5, also missed overall survival.
Grade 3 or worse increases in lipase (17 against 2 percent) and amylase (10 against 1 percent) were the characteristic toxicities, along with fatigue and pulmonary embolism. Millennium, a Takeda subsidiary, stopped developing the drug. Orteronel is the reason the field treats radiographic progression-free survival in prostate cancer with suspicion as a surrogate for survival.
Non-steroidal, partially selective inhibitor of CYP 17,20-lyase, reducing extragonadal androgen synthesis. Connects to CYP17A1 (17-alpha-hydroxylase/17,20-lyase).
1.Orteronel slips into a pocket on CYP17A1 (17-alpha-hydroxylase/17,20-lyase).
Background: ADC sequencing, Antigen escape (antigen loss, lineage switch), BCG-unresponsive, Castration-resistant prostate cancer (CRPC), Circulating tumour DNA (ctDNA). Also on OnCo: Resistance atlas · Lines of therapy.
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Query for this drug: (TITLE:"Orteronel" OR ABSTRACT:"Orteronel" OR TITLE:"TAK-700" OR ABSTRACT:"TAK-700") AND (cancer OR tumor OR tumour OR oncology OR carcinoma OR lymphoma OR leukemia OR leukaemia OR myeloma OR sarcoma OR melanoma OR glioma). Results are unfiltered search hits about Orteronel, not a curated reading list.
Shares CYP17A1 (17-alpha-hydroxylase/17,20-lyase), Androgen receptor pathway inhibitor (ARPI), Castration-resistant prostate cancer (CRPC), Metastatic castration-resistant prostate cancer.
Shares ELM-PC 4, Androgen receptor pathway inhibitor (ARPI), Castration-resistant prostate cancer (CRPC), Metastatic castration-resistant prostate cancer.
Shares CYP17A1 (17-alpha-hydroxylase/17,20-lyase), Androgen receptor pathway inhibitor (ARPI), Castration-resistant prostate cancer (CRPC), Metastatic castration-resistant prostate cancer.
Shares CYP17A1 (17-alpha-hydroxylase/17,20-lyase), Castration-resistant prostate cancer (CRPC), Metastatic castration-resistant prostate cancer, Prostate cancer.
Shares CYP17A1 (17-alpha-hydroxylase/17,20-lyase), Prostate cancer.
Shares ELM-PC 4, Castration-resistant prostate cancer (CRPC), Metastatic castration-resistant prostate cancer, Prostate cancer.
Shares Androgen receptor pathway inhibitor (ARPI), Castration-resistant prostate cancer (CRPC), Metastatic castration-resistant prostate cancer, Prostate cancer.
Shares Androgen receptor pathway inhibitor (ARPI), Castration-resistant prostate cancer (CRPC), Metastatic castration-resistant prostate cancer, Prostate cancer.