Biological Activity & Performance
| Endpoint | Model / source | Reported finding |
|---|---|---|
| Protein degradation | 22Rv1 cells; Fig. 1B [1] | BRD2/3/4 degradation DC50 <5 nM; this measures protein depletion, not binding affinity. |
| Mechanistic control | VHL recruitment; Fig. 1 [1] | The VHL-inactive stereoisomer ARV-766 served as a negative control. |
| Cellular activity | Prostate cancer models [1] | Suppressed c-MYC and cell growth in 22Rv1, VCaP and LNCaP95 models. |
| Tumor pharmacodynamics | 22Rv1 xenografts; Fig. 4A [1] | After three daily 10 mg/kg subcutaneous doses, tumor BRD4 decreased 37% and c-MYC 76%. |
| Animal efficacy | 22Rv1 xenografts; Fig. 5 [1] | Daily 30 mg/kg subcutaneous treatment produced regression; 2/10 mice had no palpable mass at treatment end. |
How to interpret the evidence
ARV-771 degrades BET proteins; downstream androgen-receptor effects do not make it a direct AR degrader. Absence of a palpable mass does not establish cure.