IP Library Granted Patent US 11,007,219
Granted Patent B2
US 11,007,219 · App. 16/898,201 · Granted May 18, 2021

Gut-selective sequestering agents for the treatment and prevention of autism and related disorders

Inventors: Anthony Stewart Campbell (Framingham, MA); David H. Donabedian (Providence, RI)
Assignee: Axial Therapeutics, Inc.
A61K33/44A61K9/14A61K31/717A61K33/06A61P25/22
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Quick Facts
Patent No.
US 11,007,219
App. No.
16/898,201
Granted
May 18, 2021
Kind
B2
Abstract

The present disclosure describes methods and compositions for the treatment of neurological disorders and related symptoms by the in vivo sequestration and excretion of microbial metabolites. These metabolites are related to neurological disorders such as autism and Parkinson's disease, as well as intestinal hyperpermeability (leaky gut) and gastrointestinal comorbidities associated with such disorders.

Claims (28)

1. A method of treating a subject having a behavioral symptom of a neurological disorder associated with autism spectrum disorder, comprising:

administering to the subject a therapeutically effective amount of an activated carbon sequestrant composition which binds to at least a fraction of at least one intestinal metabolite present in the digestive tract of the subject to form a sequestrant-metabolite complex, such that the sequestrant-metabolite complex is eliminated from the digestive tract;

wherein the at least one intestinal metabolite is 4-ethylphenol and the behavioral symptom is clinical irritability;

wherein the sequestrant composition comprises a multiplicity of biocompatible particles which are non-absorbable by the digestive tract of the subject;

wherein the therapeutically effective amount is 35 mg to 35 g per day;

and wherein the therapeutically effective amount alleviates the clinical irritability.

2. The method of claim 1 , wherein the subject is identified as having autism spectrum disorder.

3. The method of any one of claim 1 or 2 , wherein the subject does not have chronic kidney disease.

4. The method of any one of claim 1 or 2 , or wherein the subject does not have clinical anxiety or an anxiety disorder.

5. The method of any one of claim 1 or 2 , wherein the sequestrant composition binds to at least a portion of an additional intestinal metabolite present in the digestive tract of the subject to form a sequestrant-metabolite complex, such that the sequestrant-metabolite complex is eliminated from the digestive tract, and wherein the additional metabolite is selected from the group consisting of: 4-ethylphenylsulfate (4-EPS), p-cresol (PC), p-cresyl sulfate (PCS), 3-hydroxy indole, and 3-indoxyl sulfate.

6. The method of any one of claim 1 or 2 , wherein: the sequestrant composition comprises an AB-2004 preparation comprising spherical activated carbon particles having a minimum average specific surface area determined by the Brunauer-Emmett-Teller (BET) method of at least 500 m 2 /g and a maximum average specific surface area determined by the Brunauer-Emmett-Teller (BET) method less than 4000 m 2 /g.

7. The method of claim 5 , wherein the sequestrant composition comprises an AB-2004 preparation comprising spherical activated carbon particles having a minimum average particle diameter of at least 0.005 mm and a maximum average particle diameter of less than 1.5 mm.

8. The method of any one of claim 1 or 2 , further comprising monitoring intestinal metabolite levels of the subject during a course of treatment.

9. The method of any one of claim 1 or 2 , further comprising monitoring changes in the behavioral symptom of the subject.

10. The method of any one of claim 1 or 2 , wherein the sequestrant composition is administered following appearance of the behavioral symptom of the neurological disorder.

11. The method of any one of claim 1 or 2 , wherein the method is repeated as necessary to maintain reduced levels of intestinal metabolites relative to levels identified prior to first administration of the sequestrant composition.

12. The method of claim 1 wherein, the therapeutically effective amount is 5 mg/kg to 500 mg/kg of body weight per day.

13. The method of claim 2 wherein, the therapeutically effective amount is 5 mg/kg to 500 mg/kg of body weight per day.

14. The method of claim 3 wherein, the therapeutically effective amount is 5 mg/kg to 500 mg/kg of body weight per day.

15. The method of claim 4 wherein, the therapeutically effective amount is 5 mg/kg to 500 mg/kg of body weight per day.

16. The method of claim 5 wherein, the therapeutically effective amount is 5 mg/kg to 500 mg/kg of body weight per day.

17. The method of claim 6 wherein, the therapeutically effective amount is 5 mg/kg to 500 mg/kg of body weight per day.

18. The method of claim 7 wherein,

the therapeutically effective amount is 5 mg/kg to 500 mg/kg of body weight per day.

19. The method of claim 8 wherein, the therapeutically effective amount is 5 mg/kg to 500 mg/kg of body weight per day.

20. The method of claim 9 wherein, the therapeutically effective amount is 5 mg/kg to 500 mg/kg of body weight per day.

21. The method of claim 10 wherein, the therapeutically effective amount is 5 mg/kg to 500 mg/kg of body weight per day.

22. The method of claim 12 wherein, the therapeutically effective amount is 5 mg/kg to 500 mg/kg of body weight per day.

Assignments (2)
CHANGE OF NAME Recorded Feb 22, 2021
From: AXIAL BIOTHERAPEUTICS, INC.
To: AXIAL THERAPEUTICS, INC.
Reel/Frame 055349/0844 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Feb 17, 2021
From: CAMPBELL, ANTHONY STEWART; DONABEDIAN, DAVID H.
To: AXIAL THERAPEUTICS
Reel/Frame 055291/0447 →
Continuity (5)
Continuation 16827629 · Mar 23, 2020
Continuation 15994571 · May 31, 2018
Continuation PCTUS2018025607 · Mar 31, 2018
Provisional Application 62480039 · Mar 31, 2017
Related Publication 20200368276A1 · Nov 26, 2020