Targeted contrast agents for mri of amyloid deposition
AssigneeTexas Children's Hospital
InventorsEric A. Tanifum, Ketankumar B. Ghaghada, Ananth V. Annapragada
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Abstract
A liposomal composition (“ADx-001”) is provided, ADx-001 comprising a first phospholipid; a sterically bulky excipient that is capable of stabilizing the liposomal composition; a second phospholipid that is derivatized with a first polymer; a macrocyclic gadolinium-based imaging agent; and a third phospholipid that is derivatized with a second polymer, the second polymer being conjugated to a targeting ligand. The macrocyclic gadolinium-based imaging agent may be conjugated to a fourth phospholipid.
Claims20
A liposomal composition, comprising:
- a first phospholipid;
- a sterically bulky excipient that is capable of stabilizing the liposomal composition;
- a second phospholipid that is derivatized with a first polymer;
- a macrocyclic gadolinium-based imaging agent;
- and
- a third phospholipid that is derivatized with a second polymer, the second polymer being conjugated to a targeting ligand, the targeting ligand being represented by:
- wherein,
- Pyrimidine “P” may be substituted with zero, one, or more of —OH, O-alkyl, and —NH2;
- R2 is a linking group comprising C1-C6 alkyl or C1-C6 alkoxyalkyl;
- and
- R3 is hydrogen, C1-C6 alkyl, or C1-C6 alkoxyalkyl, and R3 other than hydrogen is substituted with zero, one, or more —OH.
A liposomal composition, comprising:
- a macrocyclic gadolinium-based imaging agent comprising:
- and
- a first phospholipid that is derivatized with a polymer, the polymer being conjugated to a targeting ligand, the targeting ligand being represented by:
- wherein,
- Pyrimidine “P” may be substituted with zero, one, or more of —OH, O-alkyl, and —NH2;
- R2 is a linking group comprising C1-C6 alkyl or C1-C6 alkoxyalkyl;
- and
- R3 is hydrogen, C1-C6 alkyl, or C1-C6 alkoxyalkyl, and R3 other than hydrogen is substituted with zero, one, or more —OH.
A liposomal composition, comprising:
- liposomes, the liposomes comprising;
- HSPC;
- Chol;
- DSPE-mPEG2000;
- Gd(III)-DOTA-DSPE;
- and
- ET3-73.
Dependencies are inferred from the claim text.