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AssigneeChildren's Medical Center Corporation
InventorsOfra Benny-Ratsaby, Robert D'Amato, Judah Folkman
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Described herein are MetAP-2 inhibitors and compositions and formulations thereof, and more particularly compositions and formulations of MetAP-2 inhibitors wherein the MetAP-2 inhibitor is associated with a block copolymer comprising a hydrophilic polymer moiety and a hydrophobic polymer moiety. The present invention also relates to compositions and formulations comprising MetAP-2 inhibitors for oral administration or administration via routes such as topical or ocular administration. The present invention also provides methods to treat conditions associated with or related to the over-expression or over-activity of MetAP-2 by administering the compositions and formulations comprising MetAP-2 inhibitors as disclosed herein.
A composition comprising a fumagillol derivative formulation having anti-proliferative activity, wherein said formulation comprises a fumagillol derivative that is covalently linked to a block copolymer comprising a hydrophilic polymer moiety and a hydrophobic polymer moiety, wherein the fumagillol derivative is covalently linked with the hydrophobic moiety of said block copolymer, and wherein the hydrophilic polymer moiety is a poly(ethylene glycol) (PEG) polymer and the hydrophobic polymer moiety of said block copolymer is selected from the group consisting of poly(L-lysine), poly(aspartic acid), polyglycolic acid (PGA), poly(D,L-lactic-co-glycolic acid) (PLGA), poly(valerolactone), poly(hydroxybutyrate), poly(hydroxyvalerate), poly(caprolactone) (PCL), and poly(propylene oxide).
A method of treating a condition involving or relying upon MetAP-2 activity for its pathology, the method comprising administering a fumagillol derivative formulation comprising a fumagillol derivative having anti-proliferative activity and is covalently linked to a block copolymer comprising a hydrophilic polymer moiety and a hydrophobic polymer moiety, wherein the hydrophilic polymer moiety is a poly(ethylene glycol) (PEG) polymer and the hydrophobic polymer moiety of said block copolymer is selected from the group consisting of poly(L-lysine), poly(aspartic acid), polyglycolic acid (PGA), poly(D,L-lactic-co-glycolic acid) (PLGA), poly(valerolactone), poly(hydroxybutyrate), poly(hydroxyvalerate), poly(caprolactone) (PCL), and poly(propylene oxide).
A method of making a diblock copolymer composition comprising a fumagillol derivative that has anti-proliferative activity, the method comprising conjugating said fumagillol derivative to a diblock copolymer comprising a hydrophilic polymer moiety and a hydrophobic polymer moiety, wherein the hydrophilic polymer moiety is a poly(ethylene glycol) (PEG) polymer and the hydrophobic polymer moiety of said block copolymer is selected from the group consisting of poly(L-lysine), poly(aspartic acid), polyglycolic acid (PGA), poly(D,L-lactic-co-glycolic acid) (PLGA), poly(valerolactone), poly(hydroxybutyrate), poly(hydroxyvalerate), poly(caprolactone) (PCL), and poly(propylene oxide).
Dependencies are inferred from the claim text.