Claims for Patent: 10,357,472

Summary for Patent: 10,357,472

Title:	Homogenous antibody drug conjugates via enzymatic methods
Abstract:	The present application in one aspect provide Fc-containing polypeptide conjugates comprising an Fc-containing polypeptide conjugated to a conjugate moiety, wherein the Fc-containing polypeptide comprises an N-glycosylated Fc region comprising an acceptor glutamine residue flanked by an N-glycosylation site and wherein the conjugate moiety is conjugated to the Fc-containing polypeptide via the acceptor glutamine residue. Also provided are methods of making such Fc-containing polypeptide conjugates by using a wildtype or engineered transglutaminases. Further provided are engineered transglutaminases specifically designed for carrying out such reactions.
Inventor(s):	Hu; Sean (West Sacramento, CA), Allen; Lisha (Sacramento, CA)
Assignee:	CSPC Dophen Corporation (Sacramento, CA)
Application Number:	15/317,907
Patent Claims:	1. An antibody drug conjugate comprising an antibody conjugated to a conjugation moiety via an endogenous acceptor glutamine residue on the antibody, wherein the antibody drug conjugate is glycosylated in the Fc region, wherein the conjugation moiety comprises a cleavable linker, and wherein the conjugation moiety is: ##STR00001## 2. The antibody drug conjugate of claim 1, wherein the antibody drug conjugate is N-glycosylated in the Fc region. 3. The antibody drug conjugate of claim 1, wherein the antibody is a human antibody. 4. The antibody drug conjugate of claim 1, wherein the antibody is a humanized antibody. 5. The antibody drug conjugate of claim 1, wherein both heavy chains of the antibody are conjugated to the conjugation moiety. 6. The antibody drug conjugate of claim 1, wherein the antibody is an anti-Her2 antibody. 7. The antibody drug conjugate of claim 6, wherein the antibody is trastuzumab. 8. The antibody drug conjugate of claim 6, wherein the anti-Her2 antibody is N-glycosylated in the Fc region. 9. The antibody drug conjugate of claim 8, wherein the anti-Her2 antibody is N-glycosylated at position 297, and wherein the anti-Her2 antibody is conjugated to a conjugation moiety via an endogenous acceptor glutamine residue at position 295. 10. A composition comprising the antibody drug conjugate of claim 1, wherein at least about 50% of antibody drug conjugates in the composition are glycosylated in the Fc region. 11. The composition of claim 10, wherein at least 50% of the antibody drug conjugates in the composition has a molar ratio between the antibody and the conjugation moiety of 1:1 or 1:2. 12. A composition comprising the antibody drug conjugate of claim 9, wherein at least about 50% of antibody drug conjugates in the composition are glycosylated in the Fc region. 13. The composition of claim 12, wherein at least 50% of the antibody drug conjugates in the composition has a molar ratio between the antibody and the conjugation moiety of about 1:2. 14. A pharmaceutical composition comprising the antibody drug conjugate of claim 1. 15. A pharmaceutical composition comprising the antibody drug conjugate of claim 9.

Details for Patent 10,357,472

Applicant	Tradename	Biologic Ingredient	Dosage Form	BLA	Approval Date	Patent No.	Expiredate
Genentech, Inc.	HERCEPTIN	trastuzumab	For Injection	103792	09/25/1998		2034-06-12
Genentech, Inc.	HERCEPTIN	trastuzumab	For Injection	103792	02/10/2017		2034-06-12
Genentech, Inc.	HERCEPTIN HYLECTA	trastuzumab and hyaluronidase-oysk	Injection	761106	02/28/2019		2034-06-12