Asta Medica, Aktiengesellschaft

Zentaris Gmbh

Zentaris Ag

Aeterna Zentaris Gmbh

Æterna Zentaris Gmbh

Thomas Reissmann

Jurgen Engel

Dieter Sauerbier

Burkhard Wichert

Peter Romeis

Bernhard Kutscher

Thomas Beckers

J&uuml;rgen Engel

Jürgen Engel

Michael Bernd

Jurgen Rawert

Hilde Riethmuller-Winzen

Wolfgang Deger

Hilde Riethm&uuml;ller-Winzen

Gunter Losse

Wolfgang Naumann

Sandra Murgas

Peter Hilgard

Horst Bauer

Eckhard G&uuml;nther

Gudrun Sauerbier, Legal Representative

Berthold Roessler

J&uuml;rgen Rawert

The invention relates to pharmaceutical administration forms with sustained release comprising at least one pharmacologically active peptide. The invention also relates to a method for the production thereof, a kit comprising a lyophilised peptide and an aqueous solution of an inorganic salt or acetic acid salt and the use of an aqueous solution of an inorganic or acetic acid salt for producing a pharmaceutical administration form which releases peptides in a continuous manner over a long period of time.

Administration form for pharmaceutically active peptides with sustained release and method for the production thereof

The invention relates to peptides which contain N-methylated amino acid units and have improved water solubility. The invention also relates methods for treating a hormone-dependent tumor or a non-malignant indication that is treatable by LH-RH suppression, the method comprising administering to a patient in need of the treatment a therapeutically effective amount of a compound of the invention. Hormone-dependent cancers that can be treated with the methods of the invention include prostate cancer, breast cancer, ovarian cancer, endometrial cancer, and pancreatic cancer. Non-malignant indications which can be treated by the methods of the invention include benign prostate hyperplasia (BPH), endometriosis, acne, polycystic ovarian disease, dysmenorrhea, precocious puberty, and uterine fibroids and other leiomyomas.

Methods of treatment using novel LHRH antagonists having improved solubility properties

A novel lyophilizate and method of preparation as well as the use of the lyophilizate to treat female infertility and for gonad protection. Cetrorelix is dissolved in acetic acid 30% v/v, the solution is transferred to water and freeze dried.

Oligopeptide lyophilisate, their preparation and use

The invention relates to peptides which contain N-methylated amino acid units and have improved water solubility. Medicaments in which the peptides according to the invention are contained can be used for the treatment of hormone-dependent tumors and hormone-influenced non-malignant disorders.

LHRH antagonists having improved solubility properties

A lyophilizate, method of preparation, and use of the lyophilizate for gonad protection is described. The lyophilizate comprises cetrorelix dissolved in 30% (v/v) acetic acid, transferred to water, and freeze-dried.

Preparation and use of oligopeptide lyophilisate for gonad protection

The invention relates to peptides which contain N-methylated amino acid units and have improved water solubility. Medicaments in which the peptides according to the invention are contained can be used for the treatment of hormone-dependent tumours and hormone-influenced non-malignant disorders.

An improvement to the method of intrauterine insemination by the administration of luteinizing hormone-releasing hormone antagonists (LHRH antagonists).

Method for the treatment of fertility disorders

A regime for therapeutic management of a benign prostatic hyperplasia and prostatic cancer employs Cetrorelix alone or in combination with &agr;-reductase inhibitors or &agr;-receptor blocking agents. The regiment reduces the volume of the prostate and avoids the side effects associated with testosterone levels being in a castration range. Cetrorelix is administered at dosages between 0.5 mg/day and 20 mg/week or about 0.014 mg/kg body weight per day to 0.30 mg/kg body weight per week or at levels of about 25 to 120 mg of Cetrorelix per month or 0.376 mg/kg to 1.71 mg/kg per month. Cetrorelix can be administered with &agr;-reductase inhibitors or a &agr;-receptor blocking agents.

Means for treating prostate hypertrophy and prostate cancer

A regime for therapeutic management of a benign prostatic hyperplasia and prostatic cancer employs Cetrorelix alone or in combination with .alpha.-reductase inhibitors or .alpha.-receptor blocking agents. The regimen reduces the volume of the prostate and avoids the side effects associated with testosterone levels being in a castration range. Cetrorelix is administered at dosages between 0.5 mg/day and 20 mg/week or about 0.014 mg/kg body weight per day to 0.30 mg/kg body weight per week or at levels of about 25 to 120 mg of Cetrorelix per month or 0.376 mg/kg to 1.71 mg/kg per month. Cetrorelix can be administered with .alpha.-reductase inhibitors or .alpha.-receptor blocking agents.

A regime for therapeutic management of a benign prostatic hyperplasia and prostatic cancer employs Cetrorelix alone or in combination with .alpha.-reductase inhibitors or .alpha.-receptor blocking agents. The regimen reduces the volume of the prostate and avoids the side effects associated with testosterone levels being in a castration range Cetrorelix is administered at dosages between 0,5 mg/day and 20 mg/week or about 0.014 mg/kg body weight per day to 0,30 mg/kg body weight per week or at levels of about 25 to 120 mg of Cetrorelix per month or 0.376 mg kg to 1.71 mg/kg per month Cetrorelix can be administered with .alpha.-reductase inhibitors or .alpha.-receptor blocking agents.

In this invention, a release-delaying system is to be developed for LHRH antagonists, in particular for cetrorelix, which allows the active compound to be released in a controlled manner over several weeks by complexation with suitable biophilic carriers. The acidic polyamino acids polyglutamic acid and polyaspartic acid were selected for complexation with cetrorelix. The cetrorelix polyamino acid complexes are prepared from aqueous solutions by combination of the solutions and precipitation of the complexes, which are subsequently centrifuged off and dried over P.sub.2 O.sub.5 in vacuo. If complexes having a defined composition are to be obtained, lyophilization proves to be a suitable method. The cetrorelix-carboxylic acid complexes were also prepared from the aqueous solutions. In the random liberation system, the acidic polyamino acids poly-Glu and poly-Asp showed good release-delaying properties as a function of the hydrophobicity and the molecular mass of the polyamino acid. In animal experiments, it was possible to confirm the activity of the cetrorelix-polyamino acid complexes as a depot system in principle. It is thus possible by complexation of cetrorelix with polyamino acids to achieve testosterone suppression in male rats over 600 hours. The release of active compound here can be controlled by the nature and the molecular mass of the polymers.

Process for the preparation of immobilized and activity-stabilized

Immobilized and activity-stabilized complexes of LHRH antagonists and

A regime for therapeutic management of a benign prostatic hyperplasia and prostatic cancer employs Cetrorelix alone or in combination with .alpha.-reductase inhibitors or .alpha.-receptor blocking agents. The regimen reduces the volume of the prostate and avoids the side effects associated with testosterone levels being in a castration range. Cetrorelix is administered at dosages between 0,5 mg/day and 20 mg/week or about 0.014 mg/kg body weight per day to 0,30 mg/kg body weight per week or at levels of about 25 to 120 mg of Cetrorelix per month or 0.376 mg/kg to 1.71 mg/kg per month. Cetrorelix can be administered with .alpha.-reductase inhibitors or .alpha.-receptor blocking agents.

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Frankfurt am Main, Germany

Thomas Reissmann