Abstract: A fluid, milky microcrystalline aqueous suspension of a peptide or peptidomimetic and a counter-ion of a strong proton donor in water, wherein the peptide or peptidomimetic and counter-ion are present in amounts and at a molar ratio sufficient to form the suspension upon mixing and without formation of a gel. Also, lyophilized compositions that include a dried suspension, methods of making the lyophilized composition, methods of preparing the suspension, and sustained release formulations prepared by the methods.

Abstract: The invention relates to a fluid, milky microcrystalline aqueous suspension of a peptide or peptidomimetic and a counter-ion of a strong proton donor in water, wherein the peptide or peptidomimetic and counter-ion are present in amounts and at a molar ratio sufficient to form the suspension upon mixing and without formation of a gel. The invention also relates to lyophilized compositions that include a dried suspension, methods of making the lyophilized composition, methods of preparing the suspension, and sustained release formulations prepared by the methods.

Abstract: The invention relates to a fluid, milky microcrystalline aqueous suspension of a peptide or peptidomimetic and a counter-ion of a strong proton donor in water, wherein the peptide or peptidomimetic and counter-ion are present in amounts and at a molar ratio sufficient to form the suspension upon mixing and without formation of a gel. The invention also relates to lyophilized compositions that include a dried suspension, methods of making the lyophilized composition, methods of preparing the suspension, and sustained release formulations prepared by the methods.

Abstract: The invention relates to a fluid, milky microcrystalline aqueous suspension of a peptide or peptidomimetic and a counter-ion of a strong proton donor in water, wherein the peptide or peptidomimetic and counter-ion are present in amounts and at a molar ratio sufficient to form the suspension upon mixing and without formation of a gel. The invention also relates to lyophilized compositions that include a dried suspension, methods of making the lyophilized composition, methods of preparing the suspension, and sustained release formulations prepared by the methods.

Abstract: The invention relates to a microcrystalline aqueous suspension of a peptide salt selected from the group consisting of Ac—D—Nal—D—Cpa—D—Pal—Ser—Tyr—D—Hci—Leu—Ilys—Pro—D—Ala—NH2trifluoroacetate and Ac—D—Nal—D—Cpa—D—Pal—Ser—Tyr—D—Hci—Leu—Ilys—Pro—D—Ala—NH2 sulfate. The invention also relates to methods of preparing the suspension, lyophilized compositions formed from the suspensions, and sustained release formulations that include the suspensions.

Abstract: The invention relates to a method of preventing gel formation of a hydrophobic peptides by contacting the hydrophobic peptide with a counter-ion in an amount and at a molar ratio with the peptide that are sufficient to provide a fluid, milky microcrystalline aqueous suspension of the peptide without formation of a gel. The invention also relates to a fluid, milky microcrystalline aqueous suspension of a hydrophobic peptide and a counter-ion in water, wherein the peptide and counter-ion are present in amounts and at a molar ratio sufficient to form, upon mixing, the suspension without formation of a gel.

Abstract: The present invention relates to novel growth hormone releasing pseudopeptides capable of stimulating the release of growth hormone from the pituitary and of promoting growth in mammals. The invention also provides pharmaceutical compositions comprising the pseudopeptides growth hormone secretagogues and a method for promoting the release of growth hormone in mammals. If continuously administered, the present pseudopeptides may also inhibit the release of growth hormone by down-regulating the growth response.

Abstract: There is provided a process for the preparation of an implantable or injectable pharmaceutical composition suitable for the extended release of an active ingredient, such as a peptide or a peptide analogue, to a patient following administration, by a process that includes: (a) wet granulation of a mixture of active ingredient and PLGA; (b) drying the granules so formed; (c) grinding the dried granules; and (d) extruding the ground product of step (c).

Abstract: The present invention relates to novel growth hormone releasing pseudopeptides capable of stimulating the release of growth hormone from the pituitary and of promoting growth in mammals. The invention also provides pharmaceutical compositions comprising the pseudopeptides growth hormone secretagogues and a method for promoting the release of growth hormone in mammals. If continuously administered, the present pseudopeptides may also inhibit the release of growth hormone by down-regulating the growth response.

Abstract: Implants are described for use in a novel therapy of hormone-insensitive tumors. The implants are inserted near, around or inside such tumors to provide a high local concentration and sustained release of a gonadotrophin-release hormone agonist or antagonist and a direct inhibitory action on the growth of such tumors. As the implants are not radioactive, the deleterious side-effects of radioactive treatments are avoided.

Abstract: The invention relates to a method of preventing gel formation of a hydrophobic peptides by contacting the hydrophobic peptide with a counter-ion in an amount and at a molar ratio with the peptide that are sufficient to provide a fluid, milky microcrystalline aqueous suspension of the peptide without formation of a gel. The invention also relates to a fluid, milky microcrystalline aqueous suspension of a hydrophobic peptide and a counter-ion in water, wherein the peptide and counter-ion are present in amounts and at a molar ratio sufficient to form, upon mixing, the suspension without formation of a gel.

Abstract: Novel peptides are disclosed having antagonistic properties to the Growth Hormone releasing peptide known as Ghrelin. The new peptides are useful in decreasing the circulating levels of Growth Hormone in a mammal and have therapeutic value.

Abstract: The present invention relates to small peptides that cause penile erections in male animals when injected into the paraventricular nucleus of the hypothalamus or when given systemically (intravenously or subcutaneously) to such animals. These peptides are useful in the treatment of erectile dysfunction.

Abstract: A pharmaceutical implant for the delivery of an effective amount of a bioactive peptide or peptide analog over a period of 1 to 12 months. This implant has a diameter of about 1 to 2 mm, a length of between about 10 and 25 mm and is obtainable from a process which includes the steps of grinding a copolymer of lactic acid and glycolic acid having a ratio of glycolide to lactide units of from about 0 to 5:1 to a particle size of between about 50 and 150 .mu.m; sterilizing the ground copolymer with a dose of between about 1 and 2.5 Mrads of ionizing .gamma.-radiation; wetting the ground and sterilized copolymer with a sterile aqueous slurry of a bioactive peptide or peptide analog; aseptically blending the copolymer and the slurry to obtain a homogeneous mixture of the copolymer and between about 10 and 50% of the bioactive peptide or peptide analog; drying the mixture at reduced pressure and at temperature not exceeding 25.degree. C.

Abstract: A method for treating a tumor in a mammal by administering a growth hormone releasing compound or an antagonist thereof in an amount effective to reduce or inhibit proliferation of tumorigenic cells in the mammal. In particular, the tumors to be treated include lung, mammary, thyroid or pancreas tumors. The preferred compounds are certain peptides that contain methyl tryptophan and lysine units.

Abstract: A pharmaceutical implant for the delivery of an effective amount of a bioactive peptide or peptide analog over a period of 1 to 12 months. This implant has a diameter of about 1 to 2 mm, a length of between about 10 and 25 mm and is obtainable from a process which includes the steps of grinding a copolymer of lactic acid and glycolic acid having a ratio of glycolide to lactide units of from about 0 to 5:1 to a particle size of between about 50 and 150 .mu.m; sterilizing the ground copolymer with a dose of between about 1 and 2.5 Mrads of ionizing .gamma.-radiation; wetting the ground and sterilized copolymer with a sterile aqueous slurry of a bioactive peptide or peptide analog; aseptically blending the copolymer and the slurry to obtain a homogeneous mixture of the copolymer and between about 10 and 50% of the bioactive peptide or peptide analog; drying the mixture at reduced pressure and at temperature not exceeding 25.degree. C.

Abstract: The present invention relates a number of novel peptide sequences which include a spirolactam, bicyclic or tricyclic peptidomimetic unit. The peptides disclosed herein exhibit binding to cardiac tissue and normalize cardiac pressure after administration, as well as diagnostic and therapeutic properties for certain neoplastic tissues. Importantly, these peptides do not release pituitary hormones such as corticotropin (ACTH) and growth hormone (GH), and are therefore devoid of certain unwanted side-effects. These peptides preferably have at least one lysine unit and at least one D-2-alkyl-trptophan unit.

Abstract: Cyclic peptides of general formula (I), wherein the groups are as described in the disclosure, having inhibitory activity on growth hormone. The peptides of formula (I) have also anticancer activity.

Abstract: Peptides containing in its amino acid chain a D-2-alkylTryptophan residue wherein the alkyl group has between one and three carbon atoms and having pharmacological activity equal to or greater than that of analogous peptides containing natural unsubstituted D-Tryptophan residues in place of the D-2-alkylTryptophan. These peptides are more resistant to oxidative degradation which usually takes place, for example, in the presence of reactive radicals or during high energy sterilization than unsubstituted Tryptophan containing peptides.

Abstract: A process for manufacturing a pharmaceutical composition for the delivery of an effective amount of a bioactive peptide or peptide analog over a period of 1 to 12 months. This process includes the steps of grinding a copolymer of lactic acid and glycolic acid having a ratio of glycolide to lactide units of from about 0 to 5:1 to a particle size of between about 50 and 150 .mu.m; sterilizing the ground copolymer with a dose of between about 1 and 2.5 Mrads of ionizing .gamma.-radiation; wetting the ground and sterilized copolymer with a sterile aqueous slurry of a bioactive peptide or peptide analog; aseptically blending the copolymer and the slurry to obtain a homogeneous mixture of the copolymer and between about 10 and 50% of the bioactive peptide or peptide analog; drying the mixture at reduced pressure and at temperature not exceeding 25.degree. C.; aseptically extruding the dried mixture at a temperature between about 70 and 110.degree. C.