Improved sst-receptor binding peptidic ligands for diagnostic and therapeutic applications in nuclear medicine are provided. The improved ligands contain either natural or unnatural amino acids or peptidomimetic structures that are modified at either the N-terminal or the C-terminal end or at both termini a carbohydrate unit and a chelator or prosthetic group to provide a complexation of a radioisotope binding or holding the radioisotope. The sst- or SSTR-receptor binding peptidic ligands may al...

The present invention relates to a medical composition for treatment palliative care or prevention of cancer such as medullary thyroid carcinoma. Specifically the invention relates to a medical composition for treatment palliative care or prevention of medullary thyroid carcinoma which comprises liposomes modified with octreotide.

FIELD: chemistry.SUBSTANCE: disclosed is a method of producing octreotide or pharmaceutically acceptable salts thereof such as octreotide diacetate in which a linear peptide sequence is synthesised automatically on a Rink polymer modified with a N-Fmoc-threoninol-p-carboxybenzacetal linker Fmoc-amino acid is activated with hydroxybenzotriazole/O-(benzotriazole-NNNN-tetramethyluronium hexafluorophosphate)/diisopropyl-ethylamine (HOBt/HBTU/DIEA) in a dimethyl formamide medium splitting from the po...

The present invention is directed to the use of the peptide compound D-Phe-Cys-Phe-D-Trp-Lys-Thr-Cys-L-threoninol as a therapeutic agent for the prophylaxis and/or treatment of cancer autoimmune diseases fibrotic diseases inflammatory diseases neurodegenerative diseases infectious diseases lung diseases heart and vascular diseases and metabolic diseases. Moreover the present invention relates to pharmaceutical compositions preferably in form of a lyophilisate or liquid buffer solution or artific...

The present invention relates to a novel processes for commercial production of pharmaceutical grade octreotide using classical solution phase peptide synthesis in high yield and purity and using inexpensive amino acid derivatives. Thus the protected octapeptide alcohol Boc -D- Phe - Cys (Trt)-Phe -D - Trp - Lys (Boc) - Thr - Cys (Trt) - Thr - OL is prepared by condensation of hexapeptide acid Boc -D - Phe - Cys (Trt)-Phe -D - Trp - Lys (Boc) - Thr - OH with dipeptide alcohol H- Cys (Trt) - Thr ...

The present invention relates to sustained release formulations comprising as active ingredient octreotide or a pharmaceutically-acceptable salt thereof and two or more different polylactide-co-glycolide polymers (PLGAs).

A formulation of octreotide or pharmaceutically acceptable salts thereof which provides controlled release of a therapeutically effective amount of octreotide for a period of at least about two months. Methods of treating acromegaly decreasing growth hormone decreasing IGF-1 and treating conditions associated with carcinoid tumors and VIPomas by administering a controlled release formulation of octreotide are provided herein.