IP Library Granted Patent US 9,597,531
Granted Patent B2
US 9,597,531 · App. 13/303,045 · Granted Mar 21, 2017

Selective, lipophilic, and long-acting beta agonist monotherapeutic formulations and methods for the cosmetic treatment of adiposity and contour bulging

Inventors: John Daniel Dobak (La Jolla, CA); Kenneth Walter Locke (Carlsbad, CA)
Assignee: NEOTHETICS, INC.
A61Q19/06A61K8/41A61K9/0019A61K9/19A61K31/137A61K31/138A61K47/10A61K47/34A61K2800/91
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Quick Facts
Patent No.
US 9,597,531
App. No.
13/303,045
Granted
Mar 21, 2017
Kind
B2
Abstract

Provided herein are pharmaceutical and cosmetic formulations and methods for regional adiposity reduction and treatment of body contour defects such as abdominal bulging; comprising an injectable formulation, said formulation comprising: an active ingredient that consists essentially of an adipose tissue-reducing amount of one or more lipophilic long-acting selective beta-2 adrenergic receptor agonists, or salts, solvates, or polymorphs thereof; and one or more subcutaneously acceptable inactive ingredients.

Claims (15)

1. A method for treating a body contour defect by a monotherapy treatment regimen of at least about 4 weeks in duration, comprising subcutaneously administering a monotherapeutic formulation, wherein each administration during the monotherapy treatment regimen comprises the single active agent salmeterol, or a salt, solvate, or polymorph thereof that is present in an effective amount that is equal to or less than about 1 microgram per week, and wherein the formulation further consists of one or more subcutaneously acceptable inactive ingredients.

2. A cosmetic method for treating a body contour defect by a monotherapy treatment regimen of at least about 4 weeks in duration, comprising subcutaneously administering a monotherapeutic formulation, wherein each administration during the monotherapy treatment regimen comprises the single active agent salmeterol, or a salt, solvate, or polymorph thereof that is present in an effective amount that is equal to or less than about 1 microgram per week, and wherein the formulation further consists of one or more subcutaneously acceptable inactive ingredients.

3. A method for the aesthetic treatment of contour defects comprising abdominal bulging in a human patient by a monotherapy treatment regimen of at least about 4 weeks in duration, said method comprising subcutaneously administering a monotherapeutic formulation suitable for subcutaneous injection wherein the single active agent is salmeterol, or a salt, solvate, or polymorph thereof that is present in an effective amount that is equal to or less than about 1 microgram per week, and wherein the formulation further consists of one or more subcutaneously acceptable inactive ingredients.

4. The method of claim 1 wherein the lipophilic long-acting selective beta-2 adrenergic receptor agonist is salmeterol xinafoate.

5. The method of claim 4 wherein the formulation is formulated into a weekly dose of salmeterol xinafoate in an amount that is between about 12 nanograms to about 1 microgram.

6. The method of claim 1 wherein the salmeterol, or a salt, solvate, or polymorph thereof selectively partitions into adipose tissue relative to blood plasma when administered to a patient.

7. The method of claim 1 that provides a partition ratio of between about 0.01 to about 0.4 when salmeterol, or a salt, solvate, or polymorph thereof is administered subcutaneously.

8. The method of claim 1 wherein the injectable formulation is substantially free of glucocorticosteroids.

9. The method of claim 2 wherein the formulation is formulated to be administered to a patient once per week at a single session dose of salmeterol xinafoate that is equal to or less than about 1 microgram.

10. The method of claim 9 wherein the session dose is divided into at least two sub-doses of salmeterol xinafoate wherein each sub-dose is in an amount that is between about 12 nanograms to about 1 microgram.

11. The method of claim 2 wherein the formulation is administered to a patient once per week at a session dose of salmeterol xinafoate that is equal to or less than about 650 nanograms.

12. The method of claim 2 wherein the administration comprises at least one injection into a submental region of the patient, an abdominal region of the patient, a hip region of the patient, a thigh region of the patient, a buttocks region of the patient, a back region of the patient, an upper arms region of the patient, or a chest region of the patient.

13. The method of claim 3 wherein the lipophilic long-acting selective beta-2 adrenergic receptor agonist is salmeterol xinafoate.

14. The method of claim 13 wherein the formulation is formulated to be administered to a patient once per week at a single session dose of salmeterol xinafoate that is equal to or less than about 1 microgram.

15. The method of claim 14 wherein the session dose is divided into at least two sub-doses of salmeterol xinafoate wherein each sub-dose is in an amount that is between about 12 nanograms to about 1 microgram.

Assignments (3)
CHANGE OF NAME Recorded Sep 5, 2014
From: LITHERA, INC.
To: NEOTHETICS, INC.
Reel/Frame 033694/0006 →
SECURITY AGREEMENT Recorded Aug 20, 2012
From: LITHERA, INC.
To: SILICON VALLEY BANK
Reel/Frame 028816/0351 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Dec 7, 2011
From: DOBAK, JOHN DANIEL; LOCKE, KENNETH WALTER
To: LITHERA, INC.
Reel/Frame 027343/0629 →
Continuity (2)
Provisional Application 61417098 · Nov 24, 2010
Related Publication 20120178819A1 · Jul 12, 2012