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US 2023/0404922 A1Published application
Microsphere formulations comprising btk inhibitors and methods for making and using the same
OwnerMichaela Giltner, Rachel Galaska +2inventors
InventorsMichaela Giltner, Rachel Galaska, Tracy Richey, Mark Smith
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Abstract
Extended-release microsphere formulations comprising a BTK inhibitor are provided. In one aspect, the microsphere formulations are characterized in that the BTK inhibitor is ibrutinib, and the ibrutinib is released in vivo in humans over a period of from about 7 to about 28 days. Methods for making and using the formulations are also provided.
Claims17
A microsphere formulation, comprising:
- polymer microspheres, each polymer microsphere comprising:
- (i) ibrutinib;
- and
- (ii) a biodegradable polymer,
- wherein each polymer microsphere comprises a drug load of the ibrutinib of greater than 30% by weight of the polymer microsphere, and
- wherein the polymer microspheres have a particle size of less than 110 μm (D50).
3 more elements
A microsphere formulation, comprising:
- polymer microspheres, each polymer microsphere comprising:
- (i) ibrutinib;
- and
- (ii) a biodegradable polymer comprising an ester-terminated poly(D,L-lactide-co-glycolide) having a lactide:glycolide ratio selected from 50:50, 55:45, and 75:25, or a combination thereof;
- wherein each polymer microsphere comprises a drug load of the ibrutinib of between about 30% and about 55% by weight of the polymer microsphere, and
- wherein the polymer microspheres have a particle size of between about 25 μm (D50) and 40 μm (D50), and
- wherein the microsphere formulation is characterized in that about 75% to 100% of the ibrutinib is released over a period of between about 12 to about 16 days of injection into a human subject, but not more than about 20% of the ibrutinib has been released within 24 hours of injection into the human subject.
4 more elements
A microsphere formulation, comprising:
- polymer microspheres, each polymer microsphere comprising:
- (i) ibrutinib;
- and
- (ii) a biodegradable polymer comprising an acid-terminated poly(D,L-lactide-co-glycolide) having a lactide:glycolide ratio of 85:15;
- wherein each polymer microsphere comprises a drug load of the ibrutinib of between about 45% and about 55% by weight of the polymer microsphere, and
- wherein the polymer microspheres have a particle size of between about 30 μm (D50) and 40 μm (D50), and
- wherein the microsphere formulation is characterized in that about 75% to 100% of the ibrutinib is released over a period of between about 25 to about 31 days of injection into a human subject, but not more than about 20% of the ibrutinib has been released within 24 hours of injection into the human subject.
4 more elements
Dependencies are inferred from the claim text.