IP Library › Granted Patent US 12,428,644
Granted Patent B2
US 12,428,644 · App. 17/642,753 · Granted Sep 30, 2025

CA-IX aptamers and diagnostic and therapeutic uses thereof

Inventors: Vittorio De Franciscis (Naples, IT); Carla Lucia Esposito (Naples, IT); Silvia Catuogno (Naples, IT); Silvia Nuzzo (Salerno, IT); Alessandro Maiocchi (Monza, IT); Margherita Iaboni (Qualiano, IT); Aldo Di Vito (Naples, IT); Erika Reitano (Banchette, IT); Luisa Poggi (Banchette d'Ivrea, IT)
Assignee: BRACCO IMAGING S.P.A.
C12N15/115A61K45/06C12Q1/6886C12N2310/16C12N2310/3517
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Quick Facts
Patent No.
US 12,428,644
App. No.
17/642,753
Granted
Sep 30, 2025
Kind
B2
Abstract

The present invention provides nucleic acid aptamers binding to the Carbonic Anhydrase IX (CA-IX) enzyme, derivatives and conjugates thereof and their use as diagnostic tools, particularly for the imaging of organs and tissues expressing CA-IX, or as therapeutic agents for prevention or treatment of CA-IX related diseases.

Claims (17)

1. A RNA aptamer that specifically binds to Carbonic Anhydrase IX enzyme (CA-IX), containing SEQ ID NO: 1 or SEQ ID NO: 2.

2. The aptamer according to claim 1 , characterized in that it has a length of up to 100 nucleotides.

3. The aptamer according to claim 1 , consisting of SEQ ID NO: 1.

4. The aptamer according to claim 1 , consisting of SEQ ID NO: 2.

5. The aptamer according to claim 1 , wherein all the pyrimidine residues are modified to 2′-fluoropyrimidines.

6. The aptamer according to claim 5 which is further modified to comprise at least one chemical modification, wherein said modification is a chemical substitution at a position selected from a sugar position, a phosphate position and a base position of the nucleic acid.

7. The aptamer according to claim 6 , wherein said modification is selected from the group consisting of incorporation of a modified nucleotide, conjugation to a compound and labelling with a reporter moiety.

8. The aptamer according to claim 7 , wherein the reporter moiety is selected from the group consisting of a fluorophore moiety, a magnetic or paramagnetic moiety, a radiolabel moiety, an affinity label, an X-ray moiety, an ultrasound imaging moiety, a photoacoustic imaging moiety and a nanoparticle-based moiety.

9. The aptamer according to claim 8 , wherein the affinity label is biotin.

10. The aptamer according to claim 2 , wherein all the pyrimidine residues are modified to 2′-fluoropyrimidines.

11. The aptamer according to claim 3 , wherein all the pyrimidine residues are modified to 2′-fluoropyrimidines.

12. The aptamer according to claim 4 , wherein all the pyrimidine residues are modified to 2′-fluoropyrimidines.

13. A diagnostic, therapeutic or imaging composition comprising an aptamer as defined in claim 1 with pharmaceutically acceptable carriers and excipients.

14. A composition according to claim 13 , which is suitable for the imaging of organs and tissues expressing CA-IX.

15. A composition according to claim 14 , wherein said imaging is based on magnetic resonance imaging, positron-emission tomography (PET), computed tomography (CT), ultrasound, photoacoustic imaging (PAI), near-infrared fluorescence (NIRF) or single photon emission computed tomography (SPECT).

16. A diagnostic, therapeutic or imaging composition comprising an aptamer as defined in claim 3 with pharmaceutically acceptable carriers and excipients.

17. A diagnostic, therapeutic or imaging composition comprising an aptamer as defined in claim 4 with pharmaceutically acceptable carriers and excipients.

Assignments (3)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Mar 14, 2022
From: MAIOCCHI, ALESSANDRO; IABONI, MARGHERITA; DI VITO, ALDO; REITANO, ERIKA; POGGI, LUISA
To: BRACCO IMAGING SPA
Reel/Frame 059253/0550 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Mar 14, 2022
From: DE FRANCISCIS, VITTORIO; CATUOGNO, SILVIA; ESPOSITO, CARLA LUCIA; NUZZO, SILVIA
To: CONSIGLIO NAZIONALE DELLE RICERCHE
Reel/Frame 059253/0669 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Mar 14, 2022
From: CONSIGLIO NAZIONALE DELLE RICERCHE
To: BRACCO IMAGING SPA
Reel/Frame 059253/0729 →
Priority Claims (1)
EP 19197506 · Sep 16, 2019 · regional
Continuity (1)
Related Publication 20220348923A1 · Nov 3, 2022
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