From: Changing paradigms in management of metastatic Castration Resistant Prostate Cancer (mCRPC)
Agent | Mechanism of action | Phase of development | Side effects | Ongoing trials |
---|---|---|---|---|
Orteronel (TAK-700) | Non-steroidal, selective inhibitor of 17, 20lyase, an enzyme required for androgen biosynthesis. | The results of Phase III trial (ELM-PC 4) did not show any survival benefit in chemotherapy naïve patients. An improvement in rPFS was seen. | Fatigue, GI toxicity | RTOG and SWOG- TAK + LHRH agonist to test whether improvement in OS or not |
Galeterone (TOK-001) | Next generation AR antagonist and CYP17A1 inhibitor | ARMOR 1- phase I study showed the drug is well tolerated [42] | Fatigue, Nausea, Diarrhea | ARMOR 2 is underway in 4 distinct populations |
1. Metastatic and treatment naïve | ||||
2. Non metastatic and treatment naïve | ||||
3. Patients who have progressed on abiraterone | ||||
4. Patients who have progressed on enzalutamide | ||||
ARN-509 | Inhibits AR translocation and AR binding to DNA, does not exhibit agonist properties in the context of AR over-expression | Results from phase I studies showed that the drug is well tolerated and PSA decline at 12 weeks (>50% from the baseline) were observed in 46.7% of the patients. [38] | Fatigue, nausea, pain | Phase II study is underway in patients with mCRPC (NCT01171898) |