Conjugates having a releasable linkage
View Patent ↗The present invention provides conjugates encompassed by the following structure, wherein: D is a residue of an active agent bearing at least one amino group; and PEG-m is a methoxy end-capped poly(ethylene glycol), and further wherein the active agent is a coagulation factor having a molecular weight of greater than 100 kDa. Methods of making conjugates, and methods for administering conjugates, are also provided.
1. A compound having the following structure:
wherein:
D is a residue of an active agent bearing at least one amino group; and;
PEG-m is a methoxy end-capped poly(ethylene glycol), and further wherein the active agent is a coagulation factor having a molecular weight of greater than 100 kDa.
2. The compound of claim 1 , wherein the coagulation factor is Factor VIII.
3. The compound of claim 2 , wherein the coagulation factor is a recombinantly synthesized coagulation factor of human origin.
4. The compound of claim 1 , wherein the poly(ethylene glycol) has a weight-average molecular weight of between 10,000 Daltons to 85,000 Daltons.
5. The compound of claim 4 , wherein the poly(ethylene glycol) has a weight-average molecular weight of between 20,000 and 50,000 Daltons.
6. The compound of claim 1 , wherein the poly(ethylene glycol) has between about 20 to 2000 monomeric repeats.
7. The compound of claim 6 , wherein the poly(ethylene glycol) has between about 100 to 1000 monomeric repeats.
8. A composition comprising a compound of claim 1 , and a pharmaceutically acceptable excipient.
9. A method of treatment comprising administering a composition of claim 8 to a subject in need thereof.