IP Library › Granted Patent US 12,285,502
Granted Patent B2
US 12,285,502 · App. 17/562,861 · Granted Apr 29, 2025

HER3 peptides for imaging and radiotherapy

Inventors: Umar Mahmood (Winchester, MA); Benjamin Larimer (Woburn, MA)
Assignee: The General Hospital Corporation
A61K51/088A61K38/10A61P31/00C07K7/08
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Quick Facts
Patent No.
US 12,285,502
App. No.
17/562,861
Granted
Apr 29, 2025
Kind
B2
Abstract

Provided herein are compositions of Formula I useful for imaging HER3. The structure of Formula I is A-B-C, where A is an imaging agent, B is a linking group or a covalent bond, and C is a polypeptide comprising from about 9 to about 75 amino acids and contains a disulfide bond between two cysteine groups. An exemplary composition provided herein is useful as a radiotracer for position emission tomography (PET) imaging. Methods of imaging HER3 and combination therapies comprising the HER3 imaging agents are also provided.

Claims (57)

1. A composition of Formula II:

B-C,

wherein:

B comprises a sequence:

and

C comprises a sequence:

wherein:

is a disulfide bond between the cysteine groups, and wherein the polypeptide comprises from about 9 to about 75 amino acids;

is a bond between B and C;

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*;

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

X 9 is selected from the group consisting of beta A, 6-aminohexanoic acid, 8-aminooctanoic acid, and 2-(2-(2-aminoethoxy) ethoxy) acetic acid;

X 10 is selected from the group consisting of G, G*, A, A, S, S*, P, P*, W, W*, Y, Y*, H, H*, T, T*, M, M*, N, N*, Q, and Q*;

X 11 is selected from the group consisting of G, G*, A, A, S, S*, P, P*, W, W*, Y, Y*, H, H*, T, T*, M, M*, N, N*, Q, and Q*;

X 12 is selected from the group consisting of G, G*, A, A, S, S*, P, P*, W, W*, Y, Y*, H, H*, T, T*, M, M*, N, N*, Q, and Q*;

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;

Q* is a non-natural derivative of Q;

A* is a non-natural derivative of A;

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

Y* is a non-natural derivative of Y.

2. The composition of claim 1 , wherein B is:

wherein refers to the bond between B and C.

3. The composition of claim 1 , wherein X 2 is L or L*.

4. The composition of claim 1 , wherein X 3 is P or P*.

5. The composition of claim 1 , wherein X 4 is T or T*.

6. The composition of claim 1 , wherein X 5 is K or K*.

7. The composition of claim 1 , wherein X 6 is F or F*.

8. The composition of claim 1 , wherein X 7 is R or R*.

9. The composition of claim 1 , wherein X 8 is S or S*.

10. 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*.

11. The composition of claim 1 , wherein Formula II is:

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

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded May 9, 2022
From: MAHMOOD, UMAR; LARIMER, BENJAMIN
To: THE GENERAL HOSPITAL CORPORATION
Reel/Frame 059872/0193 →
Continuity (3)
Division 16475020
Provisional Application 62440052 · Dec 29, 2016
Related Publication 20220175975A1 · Jun 9, 2022
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