# US 10,864,190 B2 · Combination of an antiandrogen with a vitamin K antagonist or with a gamma-glutamyl carboxylase inhibitor for the therapy of androgen receptor positive cancer

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- Number: US 10,864,190 B2
- Document ID: US10864190B2
- Status: Granted
- Kind: B2
- Application number: 15/568,330
- Filed: 2016-04-22
- Published: 2018-06-28
- Granted: 2020-12-15
- Earliest claimed: 2015-04-22
- Assignees: CeMM - Forschungszentrum für Molekulare Medizin GmbH
- Applicants: CeMM—Forschungszentrum für Molekulare Medizin GmbH
- Inventors: Stefan Kubicek; Marco Licciardello
- Web page: https://patentgrep.com/patent/US10864190B2

## CPC

- A61K 31/37: Coumarins, e.g. psoralen
- A61K 31/167: having the nitrogen of a carboxamide group directly attached to the aromatic ring, e.g. lidocaine, paracetamol
- A61K 31/4166: having oxo groups directly attached to the heterocyclic ring, e.g. phenytoin
- A61P 35/00: Antineoplastic agents
- 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)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS

## Abstract

The present invention relates to the combination of an antiandrogen with a vitamin K antagonist or with a γ-glutamyl carboxylase inhibitor for use in the treatment or prevention of an androgen receptor positive cancer, such as prostate cancer, or a hyperactive androgen receptor signaling disease/disorder. The invention also relates to a vitamin K antagonist or a γ-glutamyl carboxylase inhibitor for use in resensitizing an antiandrogen-resistant prostate cancer to the treatment with an antiandrogen. The invention further provides a pharmaceutical composition comprising an antiandrogen, a vitamin K antagonist or a γ-glutamyl carboxylase inhibitor, and a pharmaceutically acceptable excipient.

## Claims

### Claim 1

A pharmaceutical composition comprising: an antiandrogen, wherein the antiandrogen is flutamide, nilutamide, bicalutamide, enzalutamide, or a pharmaceutically acceptable salt or solvate of any of these agents; a vitamin K antagonist, wherein the vitamin K antagonist is phenprocoumon or warfarin; and a pharmaceutically acceptable excipient.

### Claim 2 (depends on 1)

The pharmaceutical composition of claim 1, wherein the antiandrogen is flutamide or a pharmaceutically acceptable salt or solvate thereof.

### Claim 3 (depends on 1)

The pharmaceutical composition of claim 1, wherein the vitamin K antagonist is phenprocoumon.

### Claim 4 (depends on 1)

The pharmaceutical composition of claim 1, wherein the vitamin K antagonist is warfarin.

### Claim 5 (depends on 1)

The pharmaceutical composition of claim 1, wherein the antiandrogen is flutamide or a pharmaceutically acceptable salt or solvate thereof, and wherein the vitamin K antagonist is phenprocoumon.