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Ep 2326341 B1 (19) & (11) EP 2 326 341 B1 (12) EUROPEAN PATENT SPECIFICATION (45) Date of publication and mention (51) Int Cl.: of the grant of the patent: A61K 38/11 (2006.01) 04.07.2012 Bulletin 2012/27 (86) International application number: (21) Application number: 09788312.8 PCT/NL2009/050542 (22) Date of filing: 09.09.2009 (87) International publication number: WO 2010/030180 (18.03.2010 Gazette 2010/11) (54) Oxytocin formulations and uses thereof Oxytocin-Formulierungen und ihre Verwendungen Formulations d’oxytocine et leur utilisations (84) Designated Contracting States: • TRISSEL ET AL: INTERNATIONAL JOURNAL OF AT BE BG CH CY CZ DE DK EE ES FI FR GB GR PHARMACEUTICAL COMPOUNDING, vol. 10, HR HU IE IS IT LI LT LU LV MC MK MT NL NO PL 2006, pages 156-158, XP002513262 cited in the PT RO SE SI SK SM TR application • BOOTHBY ET AL: "Extended stability of oxytocin (30) Priority: 09.09.2008 EP 08163932 in Ringer’s lactate solution at 4° and 25°C" HOSPITAL PHARMACY, vol. 41, 2006, pages (43) Date of publication of application: 437-441, XP002513263 01.06.2011 Bulletin 2011/22 • DE GROOT ET AL: "Oxytocin and desamino- oxytocin tablets are not stable under simulated (73) Proprietor: Rijksuniversiteit Groningen tropical conditions" JOURNAL OF CLINICAL 9712 CP Groningen (NL) PHARMACY AND THERAPEUTICS, vol. 20, 1995, pages 115-119, XP002513264 cited in the (72) Inventors: application • AMORIJ, Jean-Pierre • WYTTENBACH ET AL: "Interactions of the NL-1544 PA Zaandijk (NL) hormone oxytocin with divalent metal ions" • AVANTI, Christina JOURNAL OF THE AMERICAN CHEMICAL NL-9725 AN Groningen (NL) SOCIETY, vol. 130, May 2008 (2008-05), pages • FRIJLINK, Henderik, Willem 5993-6000, XP002513366 NL-9761 KM Eelde (NL) • BAL ET AL: "Potentiometric and spectroscopic • HINRICHS, Wouter, Leonardus, Joseph studies of the Cu(II) complexes of Ala-Arg NL-9718 EG Groningen (NL) (8)-vasopressin and oxytocin: Two vasopressin- like peptides" JOURNAL OF INORGANIC (74) Representative: Jansen, Cornelis Marinus et al BIOCHEMISTRY, vol. 45, 1992, pages 193-202, VEREENIGDE XP002513265 Johan de Wittlaan 7 • ANANTHANARAYANAN ET AL: "Interaction of 2517 JR Den Haag (NL) oxytocin with Ca(2+): I. CD and fluorescence spectral characterization and comparison with (56) References cited: vasopressin" BIOPOLYMERS, vol. 40, 1996, MX-A- 9 707 899 pages 433-443, XP002513367 • SLANINOVÁ ET AL: "Oxytocin, divalent cations • KALIS ET AL: LATVIJAS PSR ZINATNU and mechanism of action" JOURNAL OF AKADEMIJAS VESTIS, KIMIJAS SERIJA, vol. 29, PEPTIDE SCIENCE, vol. 12, no. S1, 2006, page no. 1, 1970, pages 29-32, XP008101303 cited in 404, XP002590740 the application Note: Within nine months of the publication of the mention of the grant of the European patent in the European Patent Bulletin, any person may give notice to the European Patent Office of opposition to that patent, in accordance with the Implementing Regulations. Notice of opposition shall not be deemed to have been filed until the opposition fee has been paid. (Art. 99(1) European Patent Convention). EP 2 326 341 B1 Printed by Jouve, 75001 PARIS (FR) (Cont. next page) EP 2 326 341 B1 • LIU ET AL: "Oxytocin-receptor binding: Why • BRASUNET AL: "Histidine analoguesof oxytocin divalent metals are essential" JOURNAL OF THE andvasopressin as efficient ligands for Zn2+ ions AMERICAN CHEMICAL SOCIETY, vol. 127, 2005, - potentiometric and NMR studies" JOURNAL OF pages 2024-2025, XP002590741 INORGANIC BIOCHEMISTRY, vol. 103, 10 May 2009 (2009-05-10), pages 1033-1038, XP026218206 2 EP 2 326 341 B1 Description [0001] The present invention relates to the field of preventive and therapeutic medicine. In particular, it relates to therapeutic formulations comprising disulfide bridge-containing neurohypophysial nonapeptides, such oxytocin, vaso- 5 pressin or analogs thereof. Provided are heat-stable oxytocin formulations and uses thereof in indications such as induction of labor, augmentation of labor, post-partum haemorrhage or uterine atony. Also provides are heat-stable vasopressin formulations and uses thereof in indications such as diabetes insipidus and vasodilatory shock. [0002] Oxytocin (Cys-Tyr-Ile-Gln-Asn-Cys-Pro-Leu-Gly-NH2) and vasopressin (Cys-Tyr-Phe-Gln-Asn-Cys-Pro-Arg- Gly-NH2) are peptide hormones that are produced in the brain of most mammals, including humans, and that share a 10 high degree of homology. Both nonapeptides originate from the same evolutionary progenitor, vasotocin (Cys-Tyr-Ile- Gln-Asn-Cys-Pro-Arg-Gly-NH2). Their respective amino acid sequences differ only at position 3 (Ile versus Phe) and position 8 (Leu versus Arg). Both peptides contain a sulfur bridge that is formed by the cysteine residues at positions 1 and 6. [0003] Next to their structural resemblance, there is also an anatomical relationship between oxytocin and vasopressin 15 (also known as arginine vasopressine (AVP), argipressin and anti-diuretic hormone (ADH)). For example, in most species the genes for these peptides are located on the same chromosome and are separated by a relatively small distance of less than 15.000 bases. Also, the hypothalamic magnocellular neurons that synthesize oxytocin are located adjacent to those that synthesize vasopressin, and are similar in many respects. [0004] Furthermore, it is known that the structural similarity of these hormones causes some functional cross- reactions 20 in the body: whereas oxytocin has a slight antidiuretic function, high levels of vasopressin may cause uterine contractions. [0005] Oxytocin, vasopressin and analogues thereof are widely used in human and veterinarian medicine. Vasopressin is mainly applied for treatment of diabetes insipidus and vasodilatory shock, the latter occurring for example during sepsis, organ transplantation or after implantation of a cardiopulmonary bypass. It is commercially available as either generic vasopressin or synthetic analogues, such as desmopressin (1-desamino-8-D-arginine vasopressin or DDAVP; 25 trade names Stimate®, Minirin® and Octostim®) and terlipressin (trade name Glypressin®). Oxytocin is often used to induce labor and support labor in case of non- progression of parturition and to treat (post-partum) haemorrhage. Currently, oxytocin is considered to be the principal agent to treat post- partum haemorrhage. It is degraded in the gastrointestinal tract, therefore it is administered as aqueous formulation by injection or as nasal spray. Its half-life in the blood is typically about three minutes. Synthetic oxytocin is commercially available as ready- to-use aqueous formulations under the trade 30 names Pitocin® and Syntocinon® or as generic oxytocin. The oxytocin analogues desamino-oxytocin and carbetocin (trade name Duratocin®) are also commercially available. [0006] According to the World Health Report 2005 as issued by the World Health Organization, in Africa, Asia and Latin America each year half a million women die as a result of problems during pregnancy and childbirth. In Africa and Asia, at least 25% of those deaths can be attributed to haemorrhage, most commonly caused by failure of the uterus to 35 contract adequately after childbirth (atonicity). This makes haemorrhage the leading cause of maternal deaths in these continents (Khan et al., Lancet 367 (9516): 1066-1074, 2006). In third world countries, it is often practically and/or economically impossible to protect pharmaceutical preparations from the harmful effects of high temperatures during transportation, storage and use. Reports and stability studies of injectable oxytocins have shown serious instability on exposure to increased temperatures and exposure to light (see de Groot et al., World Health Organization, WHO/DAP/ 40 94.13, 1994 and de Groot et al., J Clin Pharm Ther 20 (2): 115-119, 2008, and references cited therein). The 1994 publication by de Groot et al. discloses that tablets of oral oxytoxin or analogs thereof (also referred to as oxytocics) such as ergometrine, methylergometrine, oxytocin and desamino-oxytocin, are not stable under simulated tropical con- ditions, and concludes that oral oxytocins are not suitable for use in the prevention of postpartum haemorrhage. Thus, despite the availability of various formulations of oxytocin and desamino-oxytocin for treatment of haemorrhage, the 45 (sub)tropical ambient temperatures and the absence of a so- called cold-chain in these parts of the world severely affect their stability and functionality. Proper prophylaxis and / or treatment of haemorrhage is therefore nearly impossible, resulting in this astonishingly high number of casualties each year. Vasopressin formulations known to date are similarly affected by exposure to high ambient temperature or light. [0007] Given the reduced stability of formulations comprising bioactive or therapeutic peptides such as oxytocin or 50 vasopressin at increased temperatures, their use in treatment methods in (sub)tropical countries, including many third world countries, is limited. Thus, there is a clear need for peptide formulations, preferably as a ready-to-use injectable aqueous solution, that have an improved thermal stability. [0008] One object of the invention to provide means and methods to increase the thermal stability of aqueous formu- lations comprising oxytocin, vasopressin or an analogue thereof. A further object is the provision of a therapeutic or 55 prophylactic oxytocin- or vasopressin- formulation, e.g. a ready-to- use medication that can be administered to a subject in need thereof, that has a stability that can withstand (sub)tropical ambient temperatures,
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