Aptamers and use thereof
The present disclosure provides an anti-Ang2 aptamer, a bispecific molecule or a composition comprising the anti-Ang2 aptamer, as well as uses thereof.
1 . An anti-Angiopoietin-2 (Ang2) aptamer, which specifically binds to Ang2 with a Ko value of about 100 picomolar (pM) or less, and does not bind to human Angiopoietin-1 (Ang1), wherein the anti-Ang2 aptamer is shown in SEQ ID NO: 68.
2 . A bispecific aptamer, which is of the formula A1-(L) n-A2, wherein
(1) A1 is an anti-vascular endothelial growth factor (VEGF) aptamer as set forth in SEQ ID NO: 48, and A2 is an anti-Ang2 aptamer as set forth in SEQ ID NO: 68, and L is a hexaethylene glycol linker, and n is 0 to 10; or,
(2) A1 is an anti-Ang2 aptamer as set forth in SEQ ID NO: 68, and A2 is an anti-VEGF aptamer as set forth in SEQ ID NO: 48, and L is a hexaethylene glycol linker, and n is 0 to 10.
3 . The bispecific aptamer of claim 2 , which is set forth in any of SEQ ID NO: 75-78 and 152-157.
4 . A method for treating and/or ameliorating a neovascular disease, disorder or condition, comprising administering to a subject in need thereof an effective amount of the anti-Ang2 aptamer of claim 1 .
5 . The method of claim 4 , wherein said neovascular disease, disorder or condition is selected from wet age-related macular degeneration, choroidal neovascularization, diabetic macular edema, retinal vein occlusion, and diabetic retinopathy.
6 . A method for treating and/or ameliorating a neovascular disease, disorder or condition, comprising administering to a subject in need thereof an effective amount of the bispecific aptamer of claim 2 .
7 . The method of claim 6 , wherein said neovascular disease, disorder or condition is selected from wet age-related macular degeneration, choroidal neovascularization, diabetic macular edema, retinal vein occlusion, and diabetic retinopathy.