Seviteronel racemate is the racemate form of Seviteronel and is a potent inhibitor of CYP17 lyase.

CYP17 Lyase (human):69 nM

The MDA-PCa-133 xenograft, originating from a clinical castration-resistant prostate cancer (CRPC) bone metastasis, exhibits expression of PSA, the full-length androgen receptor (AR), and the AR-V7 isoform subcutaneously. In a study involving castrated male mice bearing the MDA-PCa-133 tumor, subjects were divided into three groups and underwent 25 days of oral treatment with either a vehicle, Seviteronel (VT-464) at 100 mg/kg twice daily, or Abiraterone Acetate (AA) at 100 mg/kg twice daily. Results demonstrated that both Seviteronel (VT-464) and AA significantly reduced tumor volume by more than two-fold relative to the vehicle group (p<0.05). The study highlights that Seviteronel’s (VT-464) selective CYP17 lyase inhibition is comparably effective to AA’s CYP17 inhibition in reducing tumor volume in this model [2].