HER3 peptides for imaging and radiotherapy

1. A composition of Formula Ia, Formula Ib, or Formula Ic:

wherein A is an imaging agent;

wherein A′ is a radioisotope;

wherein

refers to a disulfide bond between the cysteine groups;

X 2 is selected from the group consisting of L, L*, I, I*, P, P*, V, V*, G, and G*;

X 3 is selected from the group consisting of P, P*, L, L*, I, I*, V, V*, G, and G*;

X 4 is selected from the group consisting of T, T*, S, S*, C, C*, M, and M*;

X 5 is selected from the group consisting of any L-amino acid, any D-amino acid, and any non-natural amino acid;

X 6 is selected from the group consisting of any L-amino acid, any D-amino acid, and any non-natural amino acid;

X 7 is selected from the group consisting of R, R*, H, H*, K, K*, N, N*, Q, and Q*, and

X 8 is selected from the group consisting of S, S*, T, T*, C, C*, M, and M*,

wherein:

L* is a non-natural derivative of L;

I* is a non-natural derivative of I;

P* is a non-natural derivative of P;

V* is a non-natural derivative of V;

G* is a non-natural derivative of G;

T* is a non-natural derivative of T;

S* is a non-natural derivative of S;

C* is a non-natural derivative of C;

M* is a non-natural derivative of M;

R* is a non-natural derivative of R;

H* is a non-natural derivative of H;

K* is a non-natural derivative of K;

N* is a non-natural derivative of N; and

Q* is a non-natural derivative of Q.

2. The composition of claim 1 , wherein the imaging agent is selected from the group consisting of a paramagnetic ion, an x-ray imaging agent, a fluorophore, and a radioisotope.

3. The composition of claim 2 , wherein the radioisotope is suitable for PET imaging.

4. The composition of claim 2 , wherein the radioisotope is selected from the group consisting of 3 H, 11 C, 14 C, 18 F, 32 P, 35 S, 36 Cl, 51 Cr, 52 Fe, 57 Co, 58 Co, 59 Fe, 64 Cu, 67 Cu, 67 Ga, 68 Ga, 75 Se, 76 Br, 77 Br, 89 Zr, 90 Y, 99m Tc, 111 In, 123 I, 124 I, 125 I, 131 I, 152 Eu, 153 Sm, 166 Ho, 177 Lu, 186 Re, 188 Re, 201 Tl, 203 Pb, 210 At, 211 At, 212 Bi, 213 Bi, and 225 Ac.

5. The composition of claim 1 , wherein A further comprises a chelating agent selected from the group consisting of 1,4,7-triazacyclononanetriacetic acid (NOTA), 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid (DOTA), 1,4,7-triazacyclononane-1-glutaric acid-4,7-diacetic acid (NODAGA), ethylene diamine tetra-acetic acid (EDTA), diethylene triaminepentaacetic acid (DTPA), cyclohexyl-1,2-diaminetetraacetic acid (CDTA), ethyleneglycol-0,0′-bis(2-aminoethyl)-N,N,N′,N′-tetraacetic acid (EGTA), N,N-bis(hydroxybenzyl)-ethylenediamine-N,N′-diacetic acid (HBED), triethylene tetramine hexaacetic acid (TTHA), hydroxyethyidiamine triacetic acid (HEDTA), 1,4,8,11-tetraazacyclotetradecane-N,N′,N″,N′″-tetraacetic acid (TETA), 1,4,7,10-tetraaza-1,4,7,10-tetra-(2-carbamoyl methyl)-cyclododecane (TCMC), and 2,2′,2″-(2-(4-isothiocyanatobenzyl)-1,4,7-triazonane-1,4,7-triyl)triacetic acid (NOTA-NCS).

6. The composition of claim 1 , wherein:

X 2 is L or L*;

X 3 is P or P*;

X 4 is T or T*;

X 5 is K or K*;

X 6 is F or F*;

X 7 is R or R*; and

X 8 is S or S*.

7. The composition of claim 1 , wherein the composition of Formula I is:

wherein

refers to a disulfide bond between the cysteine groups.

8. A pharmaceutical composition comprising the composition of claim 1 , and a pharmaceutically acceptable carrier.