Mebendazole polymorph for treatment and prevention of tumors

Patent metadata

Field	Value
Publication number	US-11110079-B2
Application number	US-201615548959-A
Country	US
Kind code	B2
Filing date	Feb 8, 2016
Priority date	Feb 6, 2015
Publication date	Sep 7, 2021
Grant date	Sep 7, 2021

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.

First claim

We 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.

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

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

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

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

6. 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.

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

Assignees

• Univ Johns Hopkins

Inventors

• Riggins Gregory
• Bai Renyuan
• Staedtke Verena
• Joshi Avadhut D
• Williamson Tara

Classifications

• A61K31/192

  having aromatic groups, e.g. sulindac, 2-aryl-propionic acids, ethacrynic acid  {(cannabinoids A61K31/658)} · CPC title

• A61P15/00

  Drugs for genital or sexual disorders (for disorders of sex hormones A61P5/24); Contraceptives · CPC title

• A61K45/06

  Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca · CPC title

• A61K31/4184 Primary

  condensed with carbocyclic rings, e.g. benzimidazoles · CPC title

• G01N21/35

  using infrared light (G01N21/39 takes precedence) · CPC title