Conjugates of an anti-TNF-alpha antibody

摘要

Conjugates of an anti-TNF antibody and one or more nonpeptidic water soluble polymers are provided. Typically, the nonpeptidic water soluble polymer is poly(ethylene glycol) or a derivative thereof. Also provided, among other things, are compositions comprising conjugates, methods of making conjugates, and methods of administering compositions to a patient.

主权项

1. A method for delivering a conjugate to a patient in need thereof, the method comprising subcutaneously administering a pharmaceutical composition, the pharmaceutical composition comprising a conjugate and a pharmaceutically acceptable excipient, the conjugate comprising a single water-soluble polymer covalently attached, either directly or through a spacer moiety of one to twenty atoms, to an amino group of an amino acid side chain or an N-terminal amine of a residue of a full length anti-TNFα antibody, wherein: (i) the one to twenty atoms within the spacer moiety, when present, correspond to the covalent attachment to the amino group of the full length anti-TNFα antibody and atoms derived from a water-soluble polymeric reagent used to attach the water-soluble polymer; (ii) the anti-TNFα antibody is neither galactosylated nor glycosylated; (iii) the water-soluble polymer is a polyethylene glycol terminally capped with a methoxy; and (iv) the water-soluble polymer has a weight-average molecular weight in the range of from about 10,000 Daltons to about 100,000 Daltons.