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