30-08-2018 дата публикации
Номер: US20180243437A1
Принадлежит:
A conjugate comprising an anti-VEGFR-2 antibody moiety conjugated to a urease moiety is described. 1. A conjugate comprising an anti-VEGFR-2 antibody moiety conjugated to a urease moiety.2. The conjugate of claim 1 , wherein the antibody moiety is conjugate to the urease moiety via a cross-linker claim 1 , optionally wherein the cross-linker is relatively long and flexible.3. The conjugate of claim 2 , wherein the cross-linker is a (PEG)class cross-linker selected from SM(PEG)or BM(PEG).4. The conjugate of claim 1 , wherein the conjugate has a conjugation ratio selected from about 1 claim 1 , about 2 claim 1 , about 3 claim 1 , about 4 claim 1 , about 5 claim 1 , about 6 claim 1 , about 7 claim 1 , about 8 claim 1 , about 9 claim 1 , about 10 claim 1 , about 11 claim 1 , or about 12 antibody moieties per urease moiety.5. The conjugate of claim 4 , wherein the conjugation ratio is up to about 3.3.6. The conjugate of claim 4 , wherein the conjugation ratio is about 3.3.7. The conjugate of claim 1 , wherein the urease moiety is a Jack bean urease.8. The conjugate of claim 1 , wherein the antibody moiety is a single domain antibody or fragment thereof or variant thereof.9. The conjugate of claim 8 , wherein the antibody comprises at least one CDR having a sequence selected from the group consisting of SYAMG claim 8 , AISWSDDSTYYANSVKG claim 8 , HKSLQRPDEYTY and a sequence at least 70% identical thereto which binds VEGFR2.10. The conjugate of claim 8 , wherein the single domain antibody or fragment thereof comprises or consists of a sequence selected from the group consisting of SEQ ID NO:2-30 claim 8 , fragments thereof claim 8 , and variants thereof.11. The conjugate of claim 10 , wherein the variants have at least 70% claim 10 , 75% claim 10 , 80% claim 10 , 85% claim 10 , 86% claim 10 , 87% claim 10 , 88% claim 10 , 89% claim 10 , 90% claim 10 , 910% claim 10 , 92% claim 10 , 93% claim 10 , 94% claim 10 , 95% claim 10 , 97% claim 10 , 98% claim 10 , or 99% sequence ...
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