Pegylated growth hormone antagonists
AssigneeBurr Oak Therapeutics LLC
InventorRichard S. Brody
Life of this patent
Estimating the term…
Abstract
A composition that is a human growth hormone receptor antagonist comprising human growth hormone receptor antagonist G120K, wherein one or two amino acids of human growth hormone receptor antagonist G120K have been mutated to cysteine; and a polyethylene glycol molecule conjugated to each substituted cysteine in the human growth hormone receptor antagonist G120K mutant.
Claims20
A human growth hormone receptor antagonist, comprising:
- (a) human growth hormone receptor antagonist G120K, wherein one amino acid of human growth hormone receptor antagonist G120K has been mutated to cysteine or wherein two amino acids of human growth hormone receptor antagonist G120K have been mutated to cysteine, and wherein the one amino acid mutated to cysteine is selected from the group consisting of N99, T142, and H151, and wherein the two amino acids mutated to cysteine are selected from the group consisting of N99/T142, N99/H151, and T142/H151;
- and
- (b) a polyethylene glycol molecule conjugated to each substituted cysteine in the human growth hormone receptor antagonist G120K mutant.
A human growth hormone receptor antagonist, comprising:
- (a) human growth hormone receptor antagonist G120K, wherein one amino acid of human growth hormone receptor antagonist G120K has been mutated to cysteine or wherein two amino acids of human growth hormone receptor antagonist G120K have been mutated to cysteine, and wherein the one amino acid mutated to cysteine is selected from the group consisting of N99, T142, and H151, and wherein the two amino acids mutated to cysteine are selected from the group consisting of N99/T142, N99/H151, and T142/H151;
- and
- (b) a polyethylene glycol molecule conjugated to each substituted cysteine in the human growth hormone receptor antagonist G120K mutant,
- (i) wherein the polyethylene glycol molecule conjugated to the one amino acid mutated to cysteine is a polydispersed 40 kDa branched polyethylene glycol molecule;
- and
- (ii) wherein the polyethylene glycol molecules conjugated to the two amino acids mutated to cysteine are either two 40 kDa branched polyethylene glycol molecules or two 4.5 kDa branched polyethylene glycols each containing three carboxylate anions.
The composition of claim 11, wherein the polyethylene glycol molecule is prepared by polymerization and is polydispersed or wherein the polyethylene glycol molecule is prepared by step-wise organic chemistry and is a substantially pure single compound.
A human growth hormone receptor antagonist, comprising:
- (a) human growth hormone receptor antagonist G120K, wherein two amino acids of human growth hormone receptor antagonist G120K have been mutated to cysteine, and wherein the two amino acids mutated to cysteine are selected from the group consisting of N99/T142, N99/H151, and T142/H151;
- and
- (b) a polyethylene glycol molecule conjugated to each substituted cysteine in the human growth hormone receptor antagonist G120K mutant.
Dependencies are inferred from the claim text.