TABLE 1
Reported IC50 values for inhibitors of CYP17A1 that have undergone clinical trials
| Inhibitor | FDA Approval Status | Reported 17,20-Lyase IC50 | Reported 17α-Hydroxylase IC50 | Reported 17,20-Lyase Selectivitya |
|---|---|---|---|---|
| nM | nM | |||
Abiraterone | Approved | 2.9–800 (Potter et al., 1995; Handratta et al., 2005; Yamaoka et al., 2012; Rafferty et al., 2014) | 1.5–72 (Potter et al., 1995; Jagusch et al., 2008; Yamaoka et al., 2012; Al-Masoudi et al., 2014; Rafferty et al., 2014) | 0.1- to 1.4-fold (Potter et al., 1995; Yamaoka et al., 2012; Rafferty et al., 2014) |
Galeterone
(TOK-001 or VN/124-1) | Phase III clinical trials | 47–300 (Handratta et al., 2005; Bruno et al., 2011) | N/R | N/R |
(S)-orteronel (TAK-700) | Discontinued after phase III clinical trials | 19–140 (Kaku et al., 2011; Yamaoka et al., 2012) | 760 (Yamaoka et al., 2012) | 5-fold (Yamaoka et al., 2012) |
(S)-seviteronel (VT-464) | Phase II clinical trials | 69 (Rafferty et al., 2014) | 690 (Rafferty et al., 2014) | 10-fold (Rafferty et al., 2014) |
FDA, Food and Drug Administration; N/R, not reported.
↵a Versus progesterone or pregnenolone hydroxylation.