# US 2026/0096992 A1 · Formulations of tegavivint

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- Number: US 2026/0096992 A1
- Document ID: US20260096992A1
- Status: Published application
- Kind: A1
- Application number: 19/405,894
- Filed: 2025-12-02
- Published: 2026-04-09
- Earliest claimed: 2020-11-24
- Assignees: Iterion Therapeutics, Inc.
- Applicants: Iterion Therapeutics Inc.
- Inventors: Gowri Sukumar; Drazen Ostovic
- Web page: https://patentgrep.com/patent/US20260096992A1

## CPC

- A61K 9/19: lyophilised {, i.e. freeze-dried, solutions or dispersions (lyophilised products with subsequent particle size reduction A61K9/14; granules or pellets made by lyphilisation A61K9/1682; solid oral dosage forms made by lyophilisation A61K9/2095; lyophilisation additives A61K47/00)}
- A61K 9/0019: {Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner (non-active ingredients are additionally classified in A61K47/00)}
- A61K 9/0053: {Mouth and digestive tract, i.e. intraoral and peroral administration}
- A61K 9/0095: {Drinks; Beverages; Syrups; Compositions for reconstitution thereof, e.g. powders or tablets to be dispersed in a glass of water; Veterinary drenches (A61K9/0007 takes precedence; eatable gels or foams A61K9/0056; oral mucosa adhesive forms A61K9/006)}
- A61K 9/10: Dispersions; Emulsions
- A61K 9/1623: {Sugars or sugar alcohols, e.g. lactose; Derivatives thereof; Homeopathic globules}
- A61K 9/1641: {obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyethylene glycol, poloxamers}
- A61K 9/1694: {resulting in granules or microspheres of the matrix type containing more than 5% of excipient}
- A61K 31/4545: containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
- A61K 47/10: Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
- A61K 47/26: Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
- A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D)

## Abstract

Formulations of tegavivint, methods of making such formulations, and methods of treatment of cancer by administering the formulations.

## Claims

### Claim 1

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.

### Claim 2 (depends on 1)

The formulation of claim 1, wherein the particles have an effective D50 of less than or equal to 0.12 micron when measured using laser diffraction.

### Claim 3 (depends on 1)

The formulation of claim 1, wherein the particles have an effective D10 of less than or equal to 0.1 micron when measured using laser diffraction.

### Claim 4

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.

### Claim 5

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.

### Claim 6

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.

### Claim 7 (depends on 1)

The formulation of claim 1, wherein the formulation is anhydrous.

### Claim 8 (depends on 1)

The formulation of claim 1, wherein the formulation is stable for three months at storage at a temperature of between 5° C. and about 25° C.

### Claim 9 (depends on 1)

The formulation of claim 1, wherein the formulation is stable for six months at storage at a temperature of between 5° C. and about 25° C.

### Claim 10 (depends on 1)

The formulation of claim 1, wherein the formulation is stable for twelve months at storage at a temperature of between 5° C. and about 25° C.

### Claim 11 (depends on 1)

The formulation of claim 1, wherein the formulation is stable for eighteen months at storage at a temperature of between 5° C. and about 25° C.

### Claim 12 (depends on 1)

The formulation of claim 1, wherein the formulation comprises a poloxamer, and one or more stabilizer selected from the group consisting of sucrose, trehalose and sorbitol.

### Claim 13 (depends on 11)

The formulation of claim 11, wherein tegavivint concentration is between about 25 mg/mL and about 50 mg/mL.

### Claim 14 (depends on 12)

The formulation of claim 12, wherein the poloxamer is Poloxamer 188.

### Claim 15 (depends on 12)

The formulation of claim 12, wherein the poloxamer concentration is between about 6 mg/mL and about 12 mg/mL.

### Claim 16 (depends on 12)

The formulation of claim 12, wherein the poloxamer concentration is about 6 mg/mL.

### Claim 17 (depends on 12)

The formulation of claim 12, wherein the poloxamer concentration is about 12.5 mg/mL.

### Claim 18 (depends on 12)

The formulation of claim 12, wherein the sorbitol concentration is about 50 mg/mL.

### Claim 19 (depends on 1)

The formulation of claim 1, wherein the tegavivint is Form I polymorph.

### Claim 20 (depends on 1)

The formulation of claim 1, wherein the tegavivint is Form IV polymorph.

### Claim 21 (depends on 1)

A method for treating cancer or tumor metastasis in a mammal in need thereof comprising administering to said mammal an effective amount of the formulation according to claim 1.