Pharmaceutical formulations
Inventors
Sander, Tommy • Poulsen, Christian • Hansen, Rosa Rebecca Erritzoee
Assignees
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Publication Number
US-12527844-B2
Publication Date
2026-01-20
Expiration Date
Abstract
Disclosed herein are an aqueous pharmaceutical formulation comprising cagrilintide and an aqueous formulation comprising semaglutide. The compositions of these two pharmaceutical formulations allow for their presentation in, and administration using, the dual-chamber medical device disclosed herein. Individuals with diseases, such as diabetes and/or obesity and/or related co-morbidities, may benefit from the co-administration of semaglutide and cagrilintide, and/or of the two liquid pharmaceutical formulations disclosed herein, using the medical device disclosed herein.
Core Innovation
The invention provides aqueous pharmaceutical formulations containing cagrilintide with specified pH and defined buffer systems. The formulation comprises cagrilintide, a buffer selected from glutamic acid/glutamate, lactic acid/lactate, or acetic acid/acetate, and 90-99% w/w water, with a pH of 3.5-4.5, including about 4.0.
The invention addresses formulation stability of cagrilintide by using the specified buffer systems at defined concentrations. Reported stability improvements include reduced HMWP and reduced formation of amyloid fibrils when glutamate buffer is used, with emphasis around 5 mM glutamate concentration. The document also reports constraints for mixing and physical stability during ejection in a dual-chamber administration context, including a limitation for glutamate buffer concentration in the cagrilintide chamber.
The invention also provides aqueous semaglutide formulations defined by phosphate buffering at a defined millimolar range and a pH of 7.0-8.0. The document reports that phosphate buffer concentrations above 15 mM and up to 45 mM are used, with emphasis around 30 mM and pH around 7.4. In a dual-chamber medical device configured for single-needle co-administration, the formulations are designed to be stored separately in first and second chambers with distinct stability requirements, and the document reports altered semaglutide and cagrilintide pharmacokinetics after dual-chamber administration compared to separate injections.
Claims Coverage
The partial document provides three independent claim families covering aqueous cagrilintide and aqueous semaglutide formulations, with inventive features defined by buffer identity, buffer concentration ranges, pH ranges, and additional optional components. In total, three independent claims are identified in the provided claim list (cagrilintide: clm-00001 and clm-00002; semaglutide: clm-00005 and clm-00006).
Aqueous cagrilintide formulation with glutamate/lactate/acetate buffer at pH 3.5-4.5
An aqueous cagrilintide formulation comprising cagrilintide, a buffer selected from glutamic acid/glutamate (about 2-10 mM) or lactic acid/lactate (about 2-35 mM) or acetic acid/acetate (about 2-10 mM), 90-99% w/w water, and a pH of 3.5-4.5.
Aqueous cagrilintide formulation concentration with buffer at pH 3.5-4.5
An aqueous cagrilintide formulation comprising cagrilintide in a concentration of 0.1-20 mg/ml, a buffer selected from glutamic acid/glutamate (about 2-10 mM) or lactic acid/lactate (about 2-35 mM) or acetic acid/acetate (about 2-10 mM), and a pH of 3.5-4.5.
Aqueous semaglutide formulation with phosphate buffer at pH 7.0-8.0
An aqueous semaglutide formulation comprising semaglutide, phosphate at a concentration of more than 15 mM and less than or equal to 45 mM, 90-99% w/w water, and a pH of 7.0-8.0.
Aqueous semaglutide formulation concentration with phosphate buffer at pH 7-8
An aqueous semaglutide formulation comprising semaglutide in a concentration of 0.1-10 mg/ml, phosphate at a concentration of more than 15 mM and less than or equal to 45 mM, and a pH of 7-8.
Across the independent claims, the inventive coverage centers on aqueous peptide drug formulations in which buffering identity and concentration are explicitly defined (glutamic acid/glutamate, lactic acid/lactate, or acetic acid/acetate for cagrilintide at pH 3.5-4.5; phosphate for semaglutide at pH 7.0-8.0 or 7-8 with phosphate >15 mM and ≤45 mM), with specific additional components addressed in dependents (including optional tonicity agents and histidine).
Stated Advantages
Stability improvements for cagrilintide, including reduced HMWP and reduced formation of amyloid fibrils when glutamate buffer is used.
Altered pharmacokinetics of semaglutide and cagrilintide after dual-chamber administration versus separate injections.
Phase 1 combination trial reports weight loss and tolerability, with GI side effects comparable to GLP-1 monotherapy.
Documented Applications
Single-needle co-administration in a dual-chamber medical device for the combination of cagrilintide and semaglutide, with nonclinical/clinical reporting including pharmacokinetics and Phase 1 combination tolerability and weight loss.
Use in studies related to diabetes, obesity, and cardiovascular disease, as well as NAFLD/NASH, and Alzheimer’s disease are listed among relevant entities in the provided content.
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