AR mutations | Resistance to | Domain | Reference | Mechanisms |
E463G | abiraterone/dutasteride | NTD | [42] | unknown |
C595X | abiraterone | DBD | [42] | unknown |
S613F | abiraterone/dutasteride | DBD | [42] | unknown |
S646R | ketoconazole | Hinge region | [42] | unknown |
Q670R | hydroxyflutamide | Hinge region | [43] | unknown |
I672T | hydroxyflutamide | Hinge region | [43] | unknown |
L701H | abiraterone, bisphenol A | LBD | [43] [45] | receptor promiscuity |
E709Y | bicalutamide | LBD | [46] | unknown |
V715M | bicalutamide, bisphenol A, flutamide, hydroxyflutamide | LBD | [10] [47] | receptor promiscuity |
V731M | bicalutamide, flutamide | LBD | [48] | receptor promiscuity |
W741C/L | abiraterone, bicalutamide, flutamide, hydroxyflutamide | LBD | [24] [40] [49] | antagonist-to-agonist switch |
M749I | bicalutamide | LBD | [45] | unknown |
V866M | abiraterone | LBD | [42] | unknown |
G872Q | cyproterone acetate | LBD | [45] | unknown |
E873Q | abiraterone, cyproterone acetate | LBD | [49] | receptor promiscuity |
H874Y/Q | abiraterone, bisphenol A, flutamide, hydroxyflutamide, nilutamide | LBD | [40] [44] | receptor promiscuity, antagonist-to-agonist switch |
F876L | ARN-509, bicalutamide, enzalutamide, hydroxyflutamide, MDV3100 | LBD | [24] [51] [52] [53] | antagonist-to-agonist switch |
T877A/S/C/G | abiraterone, bicalutamide, bisphenol A, cyproterone acetate, hydroxyflutamide, flutamide, nilutamide, | LBD | [10] [44] [48] | receptor promiscuity, antagonist-to-agonist switch |
D879G | bicalutamide | LBD | [54] | antagonist-to-agonist switch (controversial) |
D880E | enzalutamide | LBD | [2] | unknown |