IP Library › Patent Application 15749288
Patent Application
App. No. 15/749,288

EXTRACELLULAR DRUG CONJUGATES TARGETING CD20

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Quick Facts
Patent No.
US None
App. No.
15/749,288
Abstract

Extracellular drug conjugates targeting nucleotide-metabolizing (ecto)-enzymes and the Na,K-ATPase and their use as therapeutics.

Claims (18)

1 . An extracellular drug conjugate (EDC) comprising a targeting moiety portion that binds CD20, a drug portion that binds to a target on the surface of a cell, and a linker portion that covalently joins the targeting moiety portion to the drug portion.

2 . The EDC of claim 1 where the targeting moiety portion is an antibody that binds CD20.

3 . The EDC of claim 1 , wherein the drug portion comprises scillarenin or a scillarenin derivative.

4 . The EDC of claim 1 , wherein the drug portion comprises bufalin or a bufalin derivative.

5 . The EDC of claim 1 , wherein the linker portion comprises a functional group, and a polyethylene glycol spacer of 12 to 36 units.

6 . The EDC of claim 1 , wherein the linker portion comprises a nitrogen heteroatom within 10 atomic bonds of the drug portion.

7 . The EDC of claim 1 , wherein the target on the surface of the cell is an extracellular portion of an Na,K-ATPase.

8 . The EDC of claim 2 , wherein the antibody comprises rituximab.

9 . The EDC of claim 2 , wherein the antibody comprises a rituximab biosimilar.

10 . The EDC of claim 1 , wherein the targeting moiety comprises rituximab, the drug portion comprises scillarenin and an aminoglycoside covalently bound to the C3 oxygen substituent of scillarenin, and the linker portion comprises a polyethylene glycol spacer including 36 PEG units.

11 . The EDC of claim 1 , wherein the targeting moiety comprises rituximab, the drug portion comprises bufalin and a piperazine-carbamate moiety covalently bound to the C3 oxygen substituent of bufalin, and the linker portion comprises a polyethylene glycol spacer including 24 PEG units.

12 . An EDC of claim 1 , wherein the EDC is Rituximab-CEN10-131.

13 . An EDC of claim 1 , wherein the EDC is Rituximab-CEN-375.

14 . The EDC of claim 12 having an antibody loading of about 1 to about 10.

15 . The EDC of claim 14 , where in the antibody loading is about 4 to about 8.

16 . The EDC of claim 14 , wherein the antibody loading is about 4 to about 6.

17 .- 45 . (canceled)

46 . An extracellular drug conjugate (EDC) comprising a CD20-specific antibody covalently attached to an agent that modulates or inhibits Na,K-ATPase.

Assignments (2)
SECURITY INTEREST Recorded Sep 20, 2019
From: CENTROSE, LLC
To: GOBLET FUNDS, LLC
Reel/Frame 050445/0314 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jan 31, 2018
From: PRUDENT, JAMES R.
To: CENTROSE, LLC
Reel/Frame 044788/0463 →