# US 10,369,119 B2 · Inhibition of multiple pathogenic agents using bithionol

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- Number: US 10,369,119 B2
- Document ID: US10369119B2
- Status: Granted
- Kind: B2
- Application number: 15/770,142
- Filed: 2016-10-21
- Published: 2018-10-25
- Granted: 2019-08-06
- Earliest claimed: 2015-10-21
- Assignees: Keck Graduate Institute of Applied Life Sciences
- Applicants: Keck Graduate Institute of Applied Life Sciences
- Inventors: Mikhail Martchenko; William Leonardi
- Web page: https://patentgrep.com/patent/US10369119B2

## CPC

- A61K 31/10: Sulfides; Sulfoxides; Sulfones
- A61K 31/4164: 1,3-Diazoles
- A61K 31/43: Compounds containing 4-thia-1-azabicyclo [3.2.0] heptane ring systems, i.e. compounds containing a ring system of the formula [IMAGE cpc-sch-A61K-0952.gif], e.g. penicillins, penems
- A61K 31/496: Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
- A61K 31/546: containing further heterocyclic rings, e.g. cephalothin
- A61K 31/65: Tetracyclines
- A61K 31/7048: having oxygen as a ring hetero atom, e.g. leucoglucosan, hesperidin, erythromycin, nystatin {, digitoxin or digoxin}
- A61K 31/7056: containing five-membered rings with nitrogen as a ring hetero atom
- A61K 38/14: Peptides containing saccharide radicals; Derivatives thereof {, e.g. bleomycin, phleomycin, muramylpeptides or vancomycin}
- A61K 45/06: Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
- A61P 31/04: Antibacterial agents
- A61P 31/14: for RNA viruses
- A61K 31/131: acyclic
- A61K 2300/00: Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
- Y02A 50/30: Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change
- 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
- Y02A: TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE

## Abstract

Compositions and methods including Bithionol are provided for treating, inhibiting, or preventing caspase-dependent pathogenic agents in a host cell or infected subject. Examples of caspase-dependent pathogenic agents include ricin, anthrax toxin, Botulinum neurotoxin A, diphtheria toxin, Pseudomonas aeruginosa exotoxin A, cholera toxin, Zika virus, and combinations thereof. Compositions and methods also include Bithionol in combination with an antibiotic for more effective clearance of the pathogen and/or toxins.

## Claims

### Claim 1

A method of inhibiting a pathogenic agent in a host cell or in a subject, the method comprising administering Bithionol to the host cell or the subject, the pathogenic agent being selected from the group consisting of ricin, anthrax toxin, Botulinum neurotoxin A, diphtheria toxin, Pseudomonas aeruginosa exotoxin A, cholera toxin, Zika virus, and combinations thereof.

### Claim 2 (depends on 1)

The method of claim 1, wherein the Bithionol is administered at a dose of about 1.5 mg/kg/day to about 50.0 mg/kg/day based on the weight of the subject.

### Claim 3 (depends on 1)

The method of claim 1, further comprising administering an antibiotic.

### Claim 4 (depends on 3)

The method of claim 3, wherein the antibiotic is selected from the group consisting of octodrine, vancomycin, clindamycin, cephaloridine, fidaxomicin, metronidazole, ciprofloxacin, doxycycline, erythromycin, penicillin, and tetracycline.

### Claim 5 (depends on 1)

The method of claim 1, wherein the pathogenic agent is Botulinum neurotoxin A.

### Claim 6 (depends on 1)

The method of claim 1, wherein the pathogenic agent is ricin.

### Claim 7 (depends on 1)

The method of claim 1, wherein the pathogenic agent is Zika virus.

### Claim 8 (depends on 5)

The method of claim 5, wherein the Bithionol is administered at a dose of about 1.5 mg/kg/day to about 50.0 mg/kg/day and the antibiotic comprises penicillin, the penicillin being administered at a dose of about 1.5 mg/kg/day to about 50 mg/kg/day based on the weight of the subject.

### Claim 9

A composition for inhibiting a pathogenic agent in a host cell or a subject, the pathogenic agent being selected from the group consisting of Botulinum neurotoxin A, Bacillus anthracis, Pseudomonas aeruginosa, cholera, diphtheria, Clostridium botulinum and combinations thereof, the composition comprising:
Bithionol; and
an antibiotic.

### Claim 10 (depends on 9)

The composition of claim 9, wherein the pathogenic agent is selected from Botulinum neurotoxin A.

### Claim 11 (depends on 9)

The composition of claim 9, wherein the antibiotic is selected from the group consisting of octodrine, vancomycin, clindamycin, cephaloridine, fidaxomicin, metronidazole, ciprofloxacin, doxycycline, erythromycin, penicillin, tetracycline, and combinations thereof.

### Claim 12 (depends on 9)

The composition of claim 9, wherein the antibiotic comprises penicillin.

### Claim 13 (depends on 9)

The composition of claim 9, wherein the antibiotic comprises penicillin, the Bithionol is at a dose of about 1.5 mg/kg/day to about 50.0 mg/kg/day, and the penicillin is at a dose of about 1.5 mg/kg/day to about 50 mg/kg/day based on the weight of the subject.

### Claim 14

A method of inhibiting a caspase-dependent pathogenic agent in a host cell or in a subject, the method comprising administering Bithionol to the host cell or the subject, wherein the caspase-dependent pathogenic agent is selected from the group consisting of ricin, anthrax toxin, Botulinum neurotoxin A, diphtheria toxin, Pseudomonas aeruginosa exotoxin A, cholera toxin, Zika virus, and combinations thereof.

### Claim 15 (depends on 14)

The method of claim 14, wherein the Bithionol is administered at a dose of about 1.5 mg/kg/day to about 50.0 mg/kg/day based on the weight of the subject.

### Claim 16 (depends on 14)

The method of claim 14, further comprising administering an antibiotic.

### Claim 17 (depends on 16)

The method of claim 16, wherein the antibiotic is selected from the group consisting of octodrine, vancomycin, clindamycin, cephaloridine, fidaxomicin, metronidazole, ciprofloxacin, doxycycline, erythromycin, penicillin, tetracycline, and combinations thereof.

### Claim 18

A composition for inhibiting a caspase-dependent pathogenic agent in a host cell or a subject, the composition comprising:
Bithionol; and
an antibiotic.

### Claim 19 (depends on 18)

The composition of claim 18, wherein the antibiotic is selected from the group consisting of octodrine, vancomycin, clindamycin, cephaloridine, fidaxomicin, metronidazole, ciprofloxacin, doxycycline, erythromycin, penicillin, tetracycline, and combinations thereof.