A peptide nucleic acid derivative represented by Formula I, or a pharmaceutically acceptable salt thereof: wherein, n is an integer between 11 and 21; the compound of Formula I possesses at least a 9-mer complementary overlap with a 17-mer RNA sequence of [(5' —> 3') CCUUGCCUGGUAAGGAA] within the human androgen receptor pre-mRNA; S 1 , S 2 , ..., S n-1 , S n , T 1 , T 2 , ..., T n-1 , and T n independently represent deuterido, hydrido, substituted or non-substituted alkyl, or substituted or non-substituted aryl radical; X and Y independently represent hydrido [H], formyl [H-C(=O)-], aminocarbonyl [NH 2 -C(=O)-], substituted or non-substituted alkyl, substituted or non-substituted aryl, substituted or non-substituted alkylacyl, substituted or non-substituted arylacyl, substituted or non-substituted alkyloxycarbonyl, substituted or non-substituted aryloxycarbonyl, substituted or non-substituted alkylaminocarbonyl, substituted or non-substituted arylaminocarbonyl, substituted or non-substituted alkylsulfonyl, or substituted or non-substituted arylsulfonyl radical; Z represents hydrido, hydroxy, substituted or non-substituted alkyloxy, substituted or non-substituted aryloxy, substituted or non-substituted amino, substituted or non-substituted alkyl, or substituted or non-substituted aryl radical; B 1 , B 2 , ..., B n-1 , and B n are independently selected from natural nucleobases including adenine, thymine, guanine, cytosine and uracil, and unnatural nucleobases; and at least four of B 1 , B 2 , ..., B n-1 , and B n are independently selected from unnatural nucleobases with a substituted or non-substituted amino radical covalently linked to the nucleobase moiety. n is an integer between 11 and 21; the compound of Formula I possesses at least a 9-mer complementary overlap with a 17-mer RNA sequence of [(5' —> 3') CCUUGCCUGGUAAGGAA] within the human androgen receptor pre-mRNA; S 1 , S 2 , ..., S n-1 , S n , T 1 , T 2 , ..., T n-1 , and T n independently represent deuterido, hydrido, substituted or non-substituted alkyl, or substituted or non-substituted aryl radical; X and Y independently represent hydrido [H], formyl [H-C(=O)-], aminocarbonyl [NH 2 -C(=O)-], substituted or non-substituted alkyl, substituted or non-substituted aryl, substituted or non-substituted alkylacyl, substituted or non-substituted arylacyl, substituted or non-substituted alkyloxycarbonyl, substituted or non-substituted aryloxycarbonyl, substituted or non-substituted alkylaminocarbonyl, substituted or non-substituted arylaminocarbonyl, substituted or non-substituted alkylsulfonyl, or substituted or non-substituted arylsulfonyl radical; Z represents hydrido, hydroxy, substituted or non-substituted alkyloxy, substituted or non-substituted aryloxy, substituted or non-substituted amino, substituted or non-substituted alkyl, or substituted or non-substituted aryl radical; B 1 , B 2 , ..., B n-1 , and B n are independently selected from natural nucleobases including adenine, thymine, guanine, cytosine and uracil, and unnatural nucleobases; and at least four of B 1 , B 2 , ..., B n-1 , and B n are independently selected from unnatural nucleobases with a substituted or non-substituted amino radical covalently linked to the nucleobase moiety. <EOS>