Multivalent aptamer therapeutics with improved pharmacodynamic properties and methods of making and using the same
First Claim
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1. A high molecular weight aptamer composition comprising:
- (a) an aptamer, and (b) two or more polyalkylene glycol (PAG) moieties, wherein said high molecular weight aptamer composition comprises the structure;
5′
-polyalkylene glycol moiety—
aptamer—
polyalkylene moiety-3′
.
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Abstract
Materials and methods are provided for producing aptamer therapeutics having improved pharmacokinetic and pharmacodymanic properties, as well as increased target valency. The aptamers produced by the methods of the invention are useful as therapeutics for treating disease.
53 Citations
20 Claims
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1. A high molecular weight aptamer composition comprising:
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(a) an aptamer, and (b) two or more polyalkylene glycol (PAG) moieties, wherein said high molecular weight aptamer composition comprises the structure;
5′
-polyalkylene glycol moiety—
aptamer—
polyalkylene moiety-3′
. - View Dependent Claims (2, 3, 4, 5, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20)
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6. A method of improving the pharmacokinetic or pharmacodynamic properties of an aptamer therapeutic composition comprising the steps of:
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(a) introducing a 5′
reactive group at the 5′
end of a nucleic acid aptamer and a 3′
reactive group at the 3′
end of the aptamer;
(b) reacting the 5′ and
3′
reactive groups on the aptamer with reactive groups on two or more polyalkylene glycol (PAG) stabilizing moieties,thereby forming a stabilized high molecular weight therapeutic aptamer comprising the structure;
5′
-polyalkylene glycol moiety—
aptamer—
polyalkylene moiety-3′
. - View Dependent Claims (7, 8, 9, 10)
-
Specification