Compositions comprising pemvidutide and an acylated amino acid
Inventors
Naessens, Ulysse • Noel, Romain
Assignees
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Publication Number
US-12544349-B1
Publication Date
2026-02-10
Expiration Date
Abstract
The invention relates to a pharmaceutical composition, in particular a solid composition, including a compound of (i), which is a permeation enhancer according to Formula I, said permeation enhancer being an acylated aminoacid substituted on the amine function, also called AC-aa-NS, and a compound of (ii) having at least 90% sequence identity to SEQ ID NOS: 1-23. Also disclosed are methods of preparing the pharmaceutical composition, formulations, and their use in medicine.
Core Innovation
The invention provides a pharmaceutical composition comprising a compound (i) having a structure wherein R1 is an alkyl comprising 5 to 15 carbon atoms and a carboxyl group, or an alkyl comprising 7 to 17 carbon atoms and a hydroxyl group, and R3 is hydrogen or a cation, together with a compound (ii) comprising a sequence having at least 90% sequence identity to pemvidutide. The composition includes a pharmaceutically acceptable carrier or excipient.
The described embodiments combine the acetylated amino-acid permeation enhancer scaffold AC-aa-NS with a pemvidutide-like second compound, including specific SEQ ID NO examples and sequence-identity tightening to 90% to 99%. The document additionally specifies concrete permeation enhancer embodiments, including NaGly(N-Bn)C8, and oral solid dosage forms.
The document characterizes the disclosed compositions using critical micellar concentration (CMC) in FaSSIF buffer and presents example results for oral pemvidutide exposure from a capsule formulation containing pemvidutide plus NaGly(N-Bn)C8 together with additional excipients including sodium carbonate and SBTI. The composition embodiments are presented together with protease inhibitor excipient options and multiple dosage and coating options, including enteric or controlled-release coating options.
Claims Coverage
The provided independent claim family covers a pharmaceutical composition defined by two core components: a permeation enhancer scaffold component with stated R1 and R3 definitions, and a pemvidutide-like sequence identity component, together with a pharmaceutically acceptable carrier or excipient. The main inventive features are the paired selection of the Formula I permeation enhancer and the specified high-identity peptide sequences within a single pharmaceutical composition claim.
Formula I acetylated amino-acid permeation enhancer selection
The composition comprises a compound (i) comprising a structure in which R1 is an alkyl comprising 5 to 15 carbon atoms, an alkyl comprising 7 to 17 carbon atoms and a carboxyl group, or an alkyl comprising 7 to 17 carbon atoms and a hydroxyl group; and R3 is hydrogen or a cation.
GLP-1/glucagon dual agonist peptide with at least 90% sequence identity
The composition comprises a compound (ii) comprising a sequence having at least 90% sequence identity to SEQ ID NO:1 to SEQ ID NO:23.
Pharmaceutical composition with pharmaceutically acceptable carrier or excipient
The composition further includes a pharmaceutically acceptable carrier or excipient in combination with compounds (i) and (ii).
Across the provided independent claim, the coverage is centered on the combination of a structured permeation enhancer component with the stated R1 and R3 definitions and a pemvidutide-like sequence component defined by at least 90% sequence identity to specified SEQ ID sequences, formulated as a pharmaceutical composition with a pharmaceutically acceptable carrier or excipient.
Stated Advantages
Improved bioavailability.
A short absorption window.
Reduced bioavailability variability.
Documented Applications
Treating obesity.
Treating type II diabetes.
Treating non-alcoholic steatohepatitis.
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