Formulation of immunopotentiators

a technology of immunopotentiators and forms, which is applied in the field of formulating immunopotentiators, can solve the problems of smips typically lacking suitable functional groups, and achieve the effects of improving the immunopotentiator's pharmacological properties, reducing the general activation of b cells, and improving immunostimulating activity

Inactive Publication Date: 2012-07-12
GLAXOSMITHKLINE BIOLOGICALS SA
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Benefits of technology

[0008]It is an object of the invention to provide new formulations of immunopotentiators, and in particular of SMIPs, which can modify or improve the immunopotentiators' pharmacological properties, such as

Problems solved by technology

Stable adsorption of the compounds ideally takes place by ligand e

Method used

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  • Formulation of immunopotentiators
  • Formulation of immunopotentiators
  • Formulation of immunopotentiators

Examples

Experimental program
Comparison scheme
Effect test

example compound 102

[0526 includes a phosphate group attached to compound O's phenyl ring. The phosphate provides a group which could undergo ligand exchange with an aluminium salt. Compound 102 is synthesised as disclosed in reference 10.

Adsorption Studies—Aluminium Hydroxide

[0527]Adsorption of compounds to aluminium hydroxide (Al—H) is studied at various pH.

[0528]Compound 13 (0.5 mg / mL) is dissolved in 10 mM NaOH (pH 6.5 or pH 9) and added to aluminium hydroxide adjuvant (2 mg / mL) resulting in a 100 μg / dose formulation. The supernatant is evaluated with HPLC using a ballistic gradient (from 10% CH3CN-0.1% TFA to 100% CH3CN-0.1% TFA in 2.5 minutes) on a C18 (50 cm×4.6 mm) ACE column at 45° C. To evaluate the effect of supernatant temperature and incubation time on binding, the supernatant is evaluated at room temperature and at 37° C. after 1 hour, 5 hours and 24 hours. A control without aluminium hydroxide is also evaluated. HPLC chromatograms for compound 1 formulations with and without aluminium hy...

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Abstract

Immunopotentiators can be adsorbed to insoluble metal salts, such as aluminium salts, to modify their pharmacokinetics, pharmacodynamics, intramuscular retention time, and/or immunostimulatory effect. Immunopotentiators are modified to introduce a moiety, such as a phosphonate group, which can mediate adsorption. These modified compounds can retain or improve their in vivo immunological activity even when delivered in an adsorbed form.

Description

[0001]This application claims the benefit of U.S. Provisional Application No. 61 / 379,126 (filed Sep. 1, 2010), U.S. Provisional Application No. 61 / 448,394 (filed Mar. 2, 2011) and U.S. Provisional Application No. 61 / 466,887 (filed Mar. 23, 2011), the complete contents of all of which are hereby incorporated herein by reference for all purposes.TECHNICAL FIELD[0002]The invention is in the field of formulating immunopotentiating compounds for in vivo use. More particularly, the invention relates to the design of immunopotentiating agents for formulation by association with insoluble metal salts e.g. by adsorption.BACKGROUND ART[0003]Early detection of specific classes of pathogens is accomplished by the innate immune system with help of pattern recognition receptors (PRRs). The detected pathogens include viruses, bacteria, protozoa and fungi, and each constitutively expresses a set of class-specific, mutation-resistant molecules called pathogen-associated molecular patterns (PAMPs).[0...

Claims

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Application Information

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IPC IPC(8): A61K39/39C07F9/6512A61K31/675A61P31/12C07F9/553C07F9/645A61P37/04A61P31/04C07F9/6561C07F9/38
CPCA61K39/39A61K45/06A61K2039/55505A61K2039/55511A61K31/661A61K31/6615A61K31/662A61K39/095C07D471/04C07D487/04C07F9/6512A61P31/04A61P31/12A61P37/04A61P43/00Y02A50/30C07F9/645C07F9/65583C07F9/6561C07F9/65616A61K39/02A61K39/05A61K39/08A61K39/092A61K39/13A61K39/145A61K39/292
Inventor SINGH, MANMOHANSKIBINSKI, DAVID A.G.WU, TOM YAO-HSIANGLI, YONGKAICORTEZ, ALEXZHANG, XIAOYUEZOU, YEFENHOFFMAN, TIMOTHY Z.PAN, JIANFENGYUE, KATHY
Owner GLAXOSMITHKLINE BIOLOGICALS SA
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