Method and composition for treating obesity

Patent metadata

Field	Value
Publication number	US-12370137-B2
Application number	US-201917077754-A
Country	US
Kind code	B2
Filing date	Apr 25, 2019
Priority date	Apr 27, 2018
Publication date	Jul 29, 2025
Grant date	Jul 29, 2025

Abstract

A method for treating obesity associated to Prader Willi Syndrome and/or binge eating is disclosed. The method utilizes a rapid drug delivery system which delivers small molecules and peptides to the lungs by oral inhalation.

First claim

What is claimed is:

1. An inhalable dry powder pharmaceutical composition comprising a crystalline, amorphous, or crystalline composite form of fumaryl diketopiperazine having the formula:

leucine; and pramlintide, wherein said inhalable dry powder pharmaceutical composition in the form of microparticles, and about 35% to about 75% of the microparticles have an aerodynamic diameter of less than 5.8 μm, wherein the composition is effective in the treatment of obesity associated with Prader Willi Syndrome.

2. The dry powder pharmaceutical composition of claim 1 , wherein the leucine is about 0.5% to about 30% by weight of the composition.

3. The dry powder pharmaceutical composition of claim 1 , wherein the composition is used in combination therapy with a rapid acting insulin, fluoxetidine, duloxetine, or combinations thereof.

4. The dry powder pharmaceutical composition of claim 1 , wherein the pramlintide is present up to 10 mg (wt %) of the pharmaceutical composition.

5. The dry powder pharmaceutical composition of claim 1 , wherein the pramlintide is present up to 3 mg of dry powder for a single dose.

6. The dry powder pharmaceutical composition of claim 1 , wherein the leucine is L-leucine.

7. An inhalable dry powder pharmaceutical composition comprising a crystalline, amorphous, or crystalline composite form of fumaryl diketopiperazine having the formula:

an aliphatic amino acid selected from the group consisting of: alanine, glycine, leucine, isoleucine, norleucine and serine; optionally a pharmaceutically acceptable excipient; and two active agents, said active agents are present consisting of pramlintide and insulin, wherein the insulin is present and comprises up to about 30% (wt %) of the pharmaceutical composition, wherein said inhalable dry powder pharmaceutical composition comprises microparticles, and about 35% to about 75% of the microparticles have an aerodynamic diameter of less than 5.8 μm, and wherein the composition is effective in the treatment of obesity associated with Prader Willi Syndrome.

8. An inhalable dry powder pharmaceutical composition for comprising a crystalline, amorphous, or crystalline composite form of fumaryl diketopiperazine having the formula:

an aliphatic amino acid selected from the group consisting of: alanine, glycine, leucine, isoleucine, norleucine and serine; optionally a pharmaceutically acceptable excipient; and three active agents, said active agents are present consisting of a serotonin receptor agonist, pramlintide, and insulin, wherein the insulin comprises up to about 30% (wt %) of the pharmaceutical composition, wherein said inhalable dry powder pharmaceutical composition comprises microparticles, and about 35% to about 75% of the microparticles have an aerodynamic diameter of less than 5.8 μm, and wherein the composition is effective in the treatment of obesity associated with Prader Willi Syndrome.

9. The dry powder pharmaceutical composition of claim 7 or 8 , wherein the insulin is a rapid acting insulin.

10. The dry powder pharmaceutical composition of claim 8 , wherein the serotonin receptor agonist is a triptan.

11. The dry powder pharmaceutical composition of claim 10 , wherein the triptan is sumatriptan, zolmitriptan, rizatriptan, naratriptan, almotriptan, eletriptan, or frovatriptan.

12. An inhalable dry powder pharmaceutical composition comprising a crystalline, amorphous, or crystalline composite form of fumaryl diketopiperazine having the formula:

an aliphatic amino acid selected from the group consisting of: alanine, glycine, leucine, isoleucine norleucine and serine; optionally, a pharmaceutically acceptable excipient; and an active agent, said active agent is present consisting of pramlintide, effective in the treatment of obesity associated with Prader Willi Syndrome, wherein said inhalable dry powder pharmaceutical composition comprises microparticles, and about 35% to about 75% of the microparticles have an aerodynamic diameter of less than 5.8 μm.

Assignees

• Mannkind Corp

Inventors

• Castagna Michael
• Kendall David
• Kraft Kelly
• Smutney Chad C
• Grant Marshall

Classifications

• A61K45/06

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

• A61K38/28

  Insulins · CPC title

• A61K31/495 Primary

  having six-membered rings with two {or more} nitrogen atoms as the only ring heteroatoms, e.g. piperazine {or tetrazines}(A61K31/48 takes precedence {; with three nitrogen atoms A61K31/53}) · CPC title

• A61K31/198

  Alpha-amino acids, e.g. alanine or edetic acid [EDTA] (betaine A61K31/205; proline A61K31/401; tryptophan A61K31/405; histidine A61K31/4172; peptides not degraded to individual amino acids A61K38/00) · CPC title

• A61K38/22

  Hormones (derived from pro-opiomelanocortin, pro-enkephalin or pro-dynorphin A61K38/33, e.g. corticotropin A61K38/35) · CPC title