# US 10,765,682 B2 · Apilimod for use in the treatment of melanoma

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- Number: US 10,765,682 B2
- Document ID: US10765682B2
- Status: Granted
- Kind: B2
- Application number: 15/524,841
- Filed: 2015-11-06
- Published: 2017-11-23
- Granted: 2020-09-08
- Earliest claimed: 2014-11-07
- Assignees: AI Therapeutics, Inc.
- Applicants: LAM Therapeutics, Inc.
- Inventors: Neil Beeharry; Sophia Gayle; Sean Landrette; Paul Beckett; Chris Conrad; Tian Xu; Jonathan M. Rothberg; Henri Lichenstein
- Web page: https://patentgrep.com/patent/US10765682B2

## CPC

- A61K 31/5377: not condensed and containing further heterocyclic rings, e.g. timolol
- 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 31/282: Platinum compounds
- A61K 31/437: the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
- A61K 31/44: Non condensed pyridines; Hydrogenated derivatives thereof
- A61K 31/4745: condensed with ring systems having nitrogen as a ring hetero atom, e.g. phenantrolines (yohimbine derivatives, vinblastine A61K31/475; ergoline derivatives A61K31/48)
- A61K 31/513: having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
- A61K 45/06: Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
- A61P 35/04: specific for metastasis
- G01N 33/5751: of the skin, e.g. melanoma
- G01N 33/57535: of the large intestine, e.g. colon, rectum or anus
- G01N 2800/52: Predicting or monitoring the response to treatment, e.g. for selection of therapy based on assay results in personalised medicine; Prognosis
- 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
- 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

The present invention relates to methods for treating melanoma with apilimod and related compositions and methods.

## Claims

### Claim 1

A method for treating melanoma in a subject in need thereof, the method comprising administering to the subject a pharmaceutical composition comprising a therapeutically effective amount of apilimod, or a pharmaceutically acceptable salt thereof, and vemurafenib in a single dosage form with the apilimod, or in a separate dosage form.

### Claim 2 (depends on 1)

The method of claim 1, wherein the apilimod is apilimod dimesylate.

### Claim 3 (depends on 1)

The method of claim 1, wherein the composition is an oral dosage form or a dosage form suitable for intravenous administration.

### Claim 4 (depends on 1)

The method of claim 1, wherein the melanoma is a metastatic or malignant melanoma.

### Claim 5

A method for treating melanoma in a human subject in need thereof, the method comprising assaying a biological sample of the subject's cancer for one or more mutations in the BRAF protein selected from V600E BRAF and V600K BRAF, or the genetic equivalents thereof, identifying the subject having either of these mutations as a patient for treatment with a combination therapy comprising apilimod and vemurafenib, and administering a combination therapy comprising apilimod and vemurafenib to the subject.

### Claim 6 (depends on 1)

The method of claim 1, wherein the melanoma is refractory or non-responsive.

### Claim 7 (depends on 1)

The method of claim 1, wherein the vemurafenib is administered in a separate dosage form from the apilimod.

### Claim 8

A method for treating melanoma in a human subject in need thereof, the method comprising administering to the subject apilimod, or a pharmaceutically acceptable salt thereof, and vemurafenib.

### Claim 9 (depends on 8)

The method of claim 8, wherein the vemurafenib is administered in a separate dosage form from the apilimod.

### Claim 10 (depends on 8)

The method of claim 8, further comprising determining the presence of one or more of a V600E BRAF protein mutation and a V600K BRAF protein mutation in a biological sample of the subject's cancer.

### Claim 11 (depends on 8)

The method of claim 8, wherein the apilimod is apilimod dimesylate.