# US 11,110,079 B2 · Mebendazole polymorph for treatment and prevention of tumors

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- Number: US 11,110,079 B2
- Document ID: US11110079B2
- Status: Granted
- Kind: B2
- Application number: 15/548,959
- Filed: 2016-02-08
- Published: 2018-01-25
- Granted: 2021-09-07
- Earliest claimed: 2015-02-06
- Assignees: The Johns Hopkins University
- Applicants: The Johns Hopkins University
- Inventors: Gregory Riggins; Renyuan Bai; Verena Staedtke; Avadhut D. Joshi; Tara Williamson
- Web page: https://patentgrep.com/patent/US11110079B2

## CPC

- A61K 31/4184: condensed with carbocyclic rings, e.g. benzimidazoles
- A23L 33/10: using additives (addition of substantially indigestible substances A23L33/21)
- A61K 9/0056: {Mouth soluble or dispersible forms; Suckable, eatable, chewable coherent forms; Forms rapidly disintegrating in the mouth; Lozenges; Lollipops; Bite capsules; Baked products; Baits or other oral forms for animals}
- A61K 9/1605: {Excipients; Inactive ingredients}
- A61K 9/50: Microcapsules {having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals (A61K9/2081 takes precedence; particles with a single coating comprising drug A61K9/167)}
- A61K 31/192: having aromatic groups, e.g. sulindac, 2-aryl-propionic acids, ethacrynic acid {(cannabinoids A61K31/658)}
- A61K 31/473: ortho- or peri-condensed with carbocyclic ring systems, e.g. acridines, phenanthridines
- A61K 45/06: Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
- A61P 1/04: for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
- A61P 11/00: Drugs for disorders of the respiratory system
- A61P 15/00: Drugs for genital or sexual disorders (for disorders of sex hormones A61P5/24); Contraceptives
- A61P 25/00: Drugs for disorders of the nervous system
- A23V 2002/00: Food compositions, function of food ingredients or processes for food or foodstuffs
- A61P 35/00: Antineoplastic agents
- C07B 2200/13: Crystalline forms, e.g. polymorphs
- G01N 21/35: using infrared light (G01N21/39 takes precedence)
- 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)
- A23L: FOODS, FOODSTUFFS OR NON-ALCOHOLIC BEVERAGES, NOT OTHERWISE PROVIDED FOR; PREPARATION OR TREATMENT THEREOF (preservation thereof A23B)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A23V: INDEXING SCHEME RELATING TO FOODS, FOODSTUFFS OR NON-ALCOHOLIC BEVERAGES AND LACTIC OR PROPIONIC ACID BACTERIA USED IN FOODSTUFFS OR FOOD PREPARATION
- C07B: GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR (preparation of carboxylic acid esters by telomerisation C07C67/47; telomerisation C08F)
- G01N: INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES (measuring or testing apparatus or processes other than immunoassay, involving enzymes or microorganisms C12M, C12Q)

## Abstract

Mebendazole is an antiparasitic drug with over 40 years of safe use. Recently mebendazole was repurposed for glioblastoma therapy. Three polymorphs of mebendazole exist, but the relative polymorph content for existing drugs varies, and the therapeutic anti-cancer relevance of the different polymorphs was unknown. As an oral drug mebendazole polymorph C is a superior form, and it reaches the brain and brain tumors in effective concentrations. Efficacy is further improved by combining mebendazole with a P-glycoprotein inhibitor. Mebendazole may also be used for therapy of other cancers, as well as a chemo-preventative agent.

## Claims

### Claim 1

A method of treating a brain tumor in a human subject comprising:
administering to the subject a sufficient amount of a pharmaceutical formulation comprising mebendazole wherein at least 90% of the mebendazole in the formulation is polymorph C and the pharmaceutical formulation is granulated.

### Claim 2 (depends on 1)

The method of claim 1 wherein the brain tumor is a medulloblastoma.

### Claim 3 (depends on 1)

The method of claim 1 wherein the brain tumor is a glioma.

### Claim 4 (depends on 1)

The method of claim 1 wherein the tumor has a multidrug resistant pump.

### Claim 5 (depends on 1)

The method of claim 1 wherein the subject is administered one or more non-steroidal anti-inflammatory drug or an inhibitor of P-glycoprotein.

### Claim 6 (depends on 1)

The method of claim 1 wherein the one or more non-steroidal drug or an inhibitor of P-glycoprotein and the pharmaceutical formulation comprising mebendazole are administered at the same time.

### Claim 7 (depends on 5, 6)

The method of claim 5 or 6 wherein the inhibitor of P-glycoprotein is elacridar.