Patent classifications
C07K14/655
CORTISTATIN OR AN ANALOGUE THEREOF AS A PHARMACEUTICALLY ACTIVE AGENT IN LATENT FORM
The blood half-life of endogenous peptides such as somatostatin and cortistatin is extremely short, barely reaching a few In minutes [Skamene et al., Clin. Endocrinol. 1984, 20, 555-564]. Thus, there is a need to find new systems or compositions that comprise cortistatinor an analogue thereof for the treatment of those pathologies in which specific cortistatin receptors and those receptors shared with other molecules like somatostatin (sstr1, sstr2, sstr3, sstr4 and/or sstr5) and/or ghrelin (GHSR) are expressed, being, furthermore, more stable in blood than cortistatin. The present invention providesan improved means for providing cortistatinor an analogue thereof as a pharmaceutically active agent in latent form, more stable in blood than cortistatin that liberates cortistatin in a controlled-release manner.
CORTISTATIN OR AN ANALOGUE THEREOF AS A PHARMACEUTICALLY ACTIVE AGENT IN LATENT FORM
The blood half-life of endogenous peptides such as somatostatin and cortistatin is extremely short, barely reaching a few In minutes [Skamene et al., Clin. Endocrinol. 1984, 20, 555-564]. Thus, there is a need to find new systems or compositions that comprise cortistatinor an analogue thereof for the treatment of those pathologies in which specific cortistatin receptors and those receptors shared with other molecules like somatostatin (sstr1, sstr2, sstr3, sstr4 and/or sstr5) and/or ghrelin (GHSR) are expressed, being, furthermore, more stable in blood than cortistatin. The present invention providesan improved means for providing cortistatinor an analogue thereof as a pharmaceutically active agent in latent form, more stable in blood than cortistatin that liberates cortistatin in a controlled-release manner.
HUMANIZED ANTIBODIES WITH ULTRALONG COMPLEMENTARY DETERMINING REGIONS
The present disclosure provides humanized antibodies, including antibodies comprising an ultralong CDR3 and uses thereof.
HUMANIZED ANTIBODIES WITH ULTRALONG COMPLEMENTARY DETERMINING REGIONS
The present disclosure provides humanized antibodies, including antibodies comprising an ultralong CDR3 and uses thereof.
Synthetic somatostatin receptor ligands
Disclosed are Somatostatin receptor ligands comprising a peptide moiety, pharmaceutical compositions and uses thereof. Disclosed are also synthetic Somatostatin receptor ligands comprising a cyclic peptide moiety and an active agent moiety covalently bonded to the cyclic peptide moiety through a nitrogen atom of a side chain functional group of an internal residue of the cyclic peptide moiety, pharmaceutical compositions and uses thereof. Disclosed are also synthetic Somatostatin receptor ligands comprising a cyclic peptide moiety and a nanoparticle active agent moiety covalently bonded to the cyclic peptide moiety, pharmaceutical compositions and uses thereof.
Synthetic somatostatin receptor ligands
Disclosed are Somatostatin receptor ligands comprising a peptide moiety, pharmaceutical compositions and uses thereof. Disclosed are also synthetic Somatostatin receptor ligands comprising a cyclic peptide moiety and an active agent moiety covalently bonded to the cyclic peptide moiety through a nitrogen atom of a side chain functional group of an internal residue of the cyclic peptide moiety, pharmaceutical compositions and uses thereof. Disclosed are also synthetic Somatostatin receptor ligands comprising a cyclic peptide moiety and a nanoparticle active agent moiety covalently bonded to the cyclic peptide moiety, pharmaceutical compositions and uses thereof.
PEPTIDE ANALOGS
Analogs for CLR/RAMP receptor ligands are provided that have agonist, superagonist, antagonist, super-antagonist, or multiple receptor modulatng activity. The analogs can be selective for one or more CLR/RAMP receptors, or can be pan-specific for multiple G protein-coupled receptors.
PEPTIDE ANALOGS
Analogs for CLR/RAMP receptor ligands are provided that have agonist, superagonist, antagonist, super-antagonist, or multiple receptor modulatng activity. The analogs can be selective for one or more CLR/RAMP receptors, or can be pan-specific for multiple G protein-coupled receptors.
Controlled release peptide formulations
The present invention relates to compositions forming a low viscosity mixture of: a) 20-80 wt. % of at least one diacyl glycerol and/or a tocopherol; b) 20-80 wt. % of at least one phosphatidyl choline (PC); c) 5-20 wt. % of at least one biocompatible, organic mono-alcoholic solvent; d) up to 20 wt. % polar solvent e) at least one peptide active agent; f) optionally at least one antioxidant; wherein the ratio of components a:b is in the range 40:60 to 54:46; wherein the pre-formulation forms, or is capable of forming, at least one liquid crystalline phase structure upon contact with excess aqueous fluid. The invention further relates to methods of treatment comprising administration of such compositions, and to pre-filled administration devices and kits containing the formulations.
Controlled release peptide formulations
The present invention relates to compositions forming a low viscosity mixture of: a) 20-80 wt. % of at least one diacyl glycerol and/or a tocopherol; b) 20-80 wt. % of at least one phosphatidyl choline (PC); c) 5-20 wt. % of at least one biocompatible, organic mono-alcoholic solvent; d) up to 20 wt. % polar solvent e) at least one peptide active agent; f) optionally at least one antioxidant; wherein the ratio of components a:b is in the range 40:60 to 54:46; wherein the pre-formulation forms, or is capable of forming, at least one liquid crystalline phase structure upon contact with excess aqueous fluid. The invention further relates to methods of treatment comprising administration of such compositions, and to pre-filled administration devices and kits containing the formulations.