IP Library › Granted Patent US 12,384,855
Granted Patent B2
US 12,384,855 · App. 17/299,147 · Granted Aug 12, 2025

PCSK9 antagonists

Inventors: Allan Bradley (Cambridge, GB); Qi Liang (Cambridge, GB); E-Chiang Lee (Cambridge, GB); Li-Ying Liou (Xinyi District Taipei, TW); Yu-Hui Huang (Xinyi District Taipei, TW); Yen-Ju Chen (Xinyi District Taipei, TW); Li-Tzu Chen (Xinyi District Taipei, TW)
Assignee: KYMAB LIMITED
C07K16/40A61K45/06A61P3/06A61K2039/505C07K2317/56C07K2317/565
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Quick Facts
Patent No.
US 12,384,855
App. No.
17/299,147
Granted
Aug 12, 2025
Kind
B2
Abstract

The invention relates to Proprotein Convertase Subtilisin Kexin type 9 (PCSK9) antagonists, such as antibodies and fragments, as well as methods, uses and combinations.

Claims (30)

1. An antibody or a fragment thereof comprising a binding site which specifically binds to Proprotein Convertase Subtilisin Kexin type 9 (PCSK9), wherein the binding site of the antibody or the fragment thereof comprises:

(i) a VH domain comprising a CDRH1 comprising SEQ ID NO: 263 or 277, a CDRH2 comprising SEQ ID NO: 267 or 281, and a CDRH3 comprising SEQ ID NO: 271 or 285, respectively; and

a VL domain comprising a CDRL1 comprising SEQ ID NO: 293 or 307, a CDRL2 comprising SEQ ID NO: 297 or 311, and a CDRL3 comprising SEQ ID NO: 301 or 315, respectively; or

(ii) a VH domain comprising a CDRH1 comprising SEQ ID NO: 323 or 337, a CDRH2 comprising SEQ ID NO: 327 or 341, and a CDRH3 comprising SEQ ID NO: 331 or 345, respectively; and

a VL domain comprising a CDRL1 comprising SEQ ID NO: 353 or 367, a CDRL2 comprising SEQ ID NO: 357 or 371, and a CDRL3 comprising SEQ ID NO: 361 or 375, respectively; or

(iii) a VH domain comprising a CDRH1 comprising SEQ ID NO: 7 or 21, a CDRH2 comprising SEQ ID NO: 11 or 25, and a CDRH3 comprising SEQ ID NO: 15 or 29, respectively; and

a VL domain comprising a CDRL1 comprising SEQ ID NO: 39 or 53, a CDRL2 comprising SEQ ID NO: 43 or 57, and a CDRL3 comprising SEQ ID NO: 47 or 61, respectively; or

(iv) a VH domain comprising a CDRH1 comprising SEQ ID NO: 69 or 83, a CDRH2 comprising SEQ ID NO: 73 or 87, and a CDRH3 comprising SEQ ID NO: 77 or 91, respectively; and

a VL domain comprising a CDRL1 comprising SEQ ID NO: 99 or 113, a CDRL2 comprising SEQ ID NO: 103 or 117, and a CDRL3 comprising SEQ ID NO: 107 or 121, respectively, or

(v) a VH domain comprising a CDRH1 comprising SEQ ID NO: 203 or 217, a CDRH2 comprising SEQ ID NO: 207 or 221, and a CDRH3 comprising SEQ ID NO: 211 or 225, respectively; and

a VL domain comprising a CDRL1 comprising SEQ ID NO: 233 or 247, a CDRL2 comprising SEQ ID NO: 237 or 251, and a CDRL3 comprising SEQ ID NO: 241 or 255, respectively.

2. The antibody or the fragment thereof according to claim 1 , wherein the binding site comprises:

(i) a VH domain comprising SEQ ID NO: 259 or an amino acid sequence that is at least 70% identical thereto; and

a VL domain comprising SEQ ID NO: 289, or an amino acid sequence that is at least 70% identical thereto; or

(ii) a VH domain comprising SEQ ID NO: 319, or an amino acid sequence that is at least 70% identical thereto; and

a VL domain comprising SEQ ID NO: 349, or an amino acid sequence that is at least 70% identical thereto; or

(iii) a VH domain comprising SEQ ID NO: 1, or an amino acid sequence that is at least 70% identical thereto; and

a VL domain comprising SEQ ID NO: 33, or an amino acid sequence that is at least 70% identical thereto; or

(iv) a VH domain comprising SEQ ID NO: 65, or an amino acid sequence that is at least 70% identical thereto; and

a VL domain comprising SEQ ID NO: 95, or an amino acid sequence that is at least 70% identical thereto; or

(v) a VH domain comprising SEQ ID NO: 199, or an amino acid sequence that is at least 70% identical thereto; and

a VL domain comprising SEQ ID NO: 229, or an amino acid sequence that is at least 70% identical thereto.

3. The antibody or the fragment thereof according claim 1 , wherein the binding site comprises a VH domain comprising SEQ ID NO: 319 and a VL domain comprising SEQ ID NO: 349.

4. A method of treating hypercholesterolemia or hyperlipidemia in a subject, the method comprising:

administering a therapeutically effective amount of the antibody or the fragment thereof according to claim 1 to the subject.

5. A nucleic acid that encodes the antibody or the fragment thereof according to claim 1 .

6. A nucleic acid that encodes the antibody or the fragment thereof according to claim 3 .

7. A vector comprising the nucleic acid of claim 5 .

8. An isolated host cell comprising the nucleic acid of claim 5 .

9. The antibody or the fragment thereof according to claim 1 , wherein the binding site comprises a VH domain comprising SEQ ID NO: 259 and a VL domain comprising SEQ ID NO: 289.

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Oct 10, 2024
From: BRADLEY, ALLAN; LIANG, QI; HUANG, YU-HUI; CHEN, YEN-JU; CHEN, LI-TZU; LIOU, LI-YING; LEE, E-CHIANG
To: KYMAB LIMITED
Reel/Frame 068863/0975 →
Priority Claims (1)
GB 1820687 · Dec 19, 2018 · national
Continuity (1)
Related Publication 20220049017A1 · Feb 17, 2022
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