Formulations of tegavivint
AssigneeIterion Therapeutics, Inc.
InventorsGowri Sukumar, Drazen Ostovic
Life of this patent
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Abstract
Formulations of tegavivint, methods of making such formulations, and methods of treatment of cancer by administering the formulations.
Claims21
A formulation comprising particles of Form I or Form IV polymorph of tegavivint or a pharmaceutically acceptable salt, ester, amide, stereoisomer or geometric isomer thereof;
- wherein the particles have an effective D90 of less than or equal to 0.2 micron when measured using laser diffraction, and wherein the formulation was prepared by high energy agitator milling at a temperature of between about 40° C. and about 60° C.
A formulation comprising particles of Form I or Form IV polymorph of tegavivint or a pharmaceutically acceptable salt, ester, amide, stereoisomer or geometric isomer thereof;
- wherein the formulation, when administered to rats via intravenous (IV) infusion at 15.5 mg/mL concentration, is capable of providing one or more of the following values:
- Cmax of at least about 50,000 ng/ml in plasma;
- at least about 200 ng/g in brain;
- at least about 2900 ng/g in heart;
- at least about 3700 ng/g in kidney;
- at least about 35000 ng/g in lungs;
- at least about 400 ng/g in pectoral thigh muscle;
- at least about 360000 ng/g in spleen;
- at least about 470 ng/g in visceral fat;
- and at least about 237,000 ng/g in liver.
A formulation comprising particles of Form I or Form IV polymorph of tegavivint or a pharmaceutically acceptable salt, ester, amide, stereoisomer or geometric isomer thereof;
- wherein the formulation, when administered to rats via intravenous (IV) infusion at 15.5 mg/mL concentration, is capable of providing one or more of the following values:
- AUClast of at least about 68,000 hr·ng/ml in plasma;
- at least about 1800 hr·ng/g in brain;
- at least about 45000 hr·ng/g in heart;
- at least about 58000 hr·ng/g in kidney;
- at least about 450000 hr·ng/g in lungs;
- at least about 5700 hr·ng/g in pectoral thigh muscle;
- at least about 4800000 hr·ng/g in spleen;
- at least about 4000 hr·ng/g in visceral fat;
- and at least about 3,600,000 hr·ng/g in liver.
A formulation comprising particles of Form I or Form IV polymorph of tegavivint or a pharmaceutically acceptable salt, ester, amide, stereoisomer or geometric isomer thereof;
- wherein the formulation, when administered to rats via intravenous (IV) infusion at 15.5 mg/mL concentration, is capable of providing one or more of the following values:
- Tmax of about 0.08 hr or less in plasma;
- about 0.5 hr or less in brain;
- about 1 hr or less in heart;
- about 0.5 hr or less in kidney;
- about 0.5 hr or less in lungs;
- about 0.5 hr or less in pectoral thigh muscle;
- about 0.5 hr or less in spleen;
- about 1 hr or less in visceral fat;
- and about 1 hr or less in liver.
Dependencies are inferred from the claim text.