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WO1995033475A1 - Utilisation de copolymere-1 dans la preparation d'un medicament destine au traitement de la nevrite optique - Google Patents

Utilisation de copolymere-1 dans la preparation d'un medicament destine au traitement de la nevrite optique Download PDF

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Publication number
WO1995033475A1
WO1995033475A1 PCT/EP1995/002125 EP9502125W WO9533475A1 WO 1995033475 A1 WO1995033475 A1 WO 1995033475A1 EP 9502125 W EP9502125 W EP 9502125W WO 9533475 A1 WO9533475 A1 WO 9533475A1
Authority
WO
WIPO (PCT)
Prior art keywords
copolymer
optic neuritis
medicament
treatment
manufacture
Prior art date
Application number
PCT/EP1995/002125
Other languages
English (en)
Inventor
Edna Kott
Anat Kesler
Original Assignee
Yeda Research & Development Company Limited
Orvet Bv
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Yeda Research & Development Company Limited, Orvet Bv filed Critical Yeda Research & Development Company Limited
Priority to AU27874/95A priority Critical patent/AU2787495A/en
Priority to EP95923229A priority patent/EP0767672A1/fr
Priority to JP8500007A priority patent/JPH10500695A/ja
Publication of WO1995033475A1 publication Critical patent/WO1995033475A1/fr

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Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • A61K38/16—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • A61K38/17—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • A61K38/1703—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans from vertebrates
    • A61K38/1709—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans from vertebrates from mammals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders

Definitions

  • the present invention relates to the use of copolymer-1 in 5 treating visual impairments associated with multiple sclerosis .
  • MS Multiple sclerosis
  • MS 15 characteri..ed by disseminated patches of demyelination in the brain and spinal cord, resulting in multiple and varied neurological symptoms and signs, usually with remissions and exacerbations (relapses) .
  • a common symptom prior to diagnosis of MS is some degree of visual impairment,frequently optic neuritis
  • these and other visual impairments may only develop after a diagnosis of MS has been confirmed. These symptoms may also develop during the progression of the disease alongside other associated visual problems.
  • Copolymer-1 is a synthetic polypeptide analog of yelin basic protein (MBP) , which is a natural component of the myelin sheath. It has been suggested as a potential therapeutic agent ⁇ " for '3.5 multiple sclerosis (E r. J. Immunol. [1971] 1:242; and J. Neurol. Sci. [1977] 31:433). Copolymer-1 was developed by Drs. Sela, Arnon, and their co- workers at the Weizmann Institute (Rehovot, Israel) . It has been shown to be beneficial for patients with the exacerbating- remitting form of multiple sclerosis (N. Engl. J. Med. [1987] 317: 408) .
  • MBP yelin basic protein
  • the present invention relates to the use of copolymer-1 in the manufacture of a medicament for the treatment of visual impairment associated with multiple sclerosis.
  • the invention relates to the use of copolymer-1 in the manufacture of a medicament for the treatment of optic neuritis.
  • the present invention includes a method of treating a patient suffering from visual impairment related to multiple sclerosis, comprising administering to said patient a therapeutically effective amount of copolymer-1.
  • the present invention further includes a method of treating a patient suffering from optic neuritis, comprising administering to said patient a therapeutically effective amount of copolymer- 1.
  • treatment with copolymer-1 may result in a prevention of any deterioration in visual impairment associated with MS, or in a reduction in the rate of such deterioration. Said treatment may also result in an improvement in vision.
  • Examples of the types of visual impairment associated with MS include deteriorations in visual acuity, state of the optic disc, pupil reaction, visual field and ocular motility.
  • Particular conditions that are associated with visual impairment in MS include optic neuritis, retrobulbar optic neuritis, diplopia, dimness of vision and scotomas.
  • treatment with copolymer- 1 may result in prevention of further episodes of optic neuritis, delaying of further episodes or return vision to an unimpaired state.
  • Copolymer-1 may be prepared by methods known in the art, for example, the process disclosed in US
  • Patent 3,849,550 wherein the N-carboxyanhydrides of tyrosine, alanine, -benzyl glutamate and E-N-trifluoro-acetyllysine are polymerised at ambient temperature in anhydrous dioxane with diethyiamine as initiator.
  • the deblocking of the y-carboxyl group of the glutamic acid is effected by hydrogen bromide in glacial acetic acid and is followed by the removal of the trifluoroacetyl groups from the lysine residues by 1 M piperidine.
  • ambient temperature and "room temperature” are used to indicate temperatures from about 20°C to about 26°C.
  • compositions of use in the present invention may be formulated by conventional methods known in the art.
  • the composition is lyophilized and formed into an aqueous solution suitable for sub ⁇ cutaneous injection, preferably copolymer-1 is formulated with mannitol.
  • copolymer- 1 may be formulated in any of the forms known in the art for preparing oral, nasal, buccal, or rectal formulations of peptide drugs.
  • copolymer- 1 is administered daily to patients at a dosage of 20mg.
  • Protected copolymer-1 is prepared as described by Teitelbau et al. Eur. J. Immun. Vol. 1 p. 242 (1971) from the N- carboxyanhydrides of tyrosine (18g) , alanine (50g) , 7-benzyl gluta ate (35g) and trifluoroacetyllysine (83g) dissolved in 3.5 liters of dioxane.
  • the polymerization process is initiated by the addition of 0.01 - 0.02% diethylamine.
  • the reaction mixture is stirred at room temperature for 24 hours and then poured into 10 liters water.
  • the product (protected copolymer-1) is filtered, washed with water and dried.
  • the removal of the gamma-benzyl blocking groups from the glutamate residue is carried-out by treating the protected copolymer-l with 33% hydrobromic acid in glacial acetic acid at room temperature for 6-12 hours with stirring.
  • the product is poured into excess water, filtered, washed and dried, yielding the trifluoroacetyl-copolymer-1.
  • Copolymer-l was administered sub-cutaneously at a daily dose of 20mg, formulated in 40mg of mannitol.

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Veterinary Medicine (AREA)
  • Chemical & Material Sciences (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Immunology (AREA)
  • Zoology (AREA)
  • Marine Sciences & Fisheries (AREA)
  • Ophthalmology & Optometry (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Epidemiology (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

Utilisation de copolymère-1 dans le traitement de déficiences de la vue associées à la sclérose en plaques.
PCT/EP1995/002125 1994-06-06 1995-06-05 Utilisation de copolymere-1 dans la preparation d'un medicament destine au traitement de la nevrite optique WO1995033475A1 (fr)

Priority Applications (3)

Application Number Priority Date Filing Date Title
AU27874/95A AU2787495A (en) 1994-06-06 1995-06-05 Use of copolymer-1 for the manufacture of a medicament for the treatment of optic neuritis
EP95923229A EP0767672A1 (fr) 1994-06-06 1995-06-05 Utilisation de copolymere-1 dans la preparation d'un medicament destine au traitement de la nevrite optique
JP8500007A JPH10500695A (ja) 1994-06-06 1995-06-05 視神経炎を処置する薬剤を調製するためのコポリマー−１の使用

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
GB9411292A GB9411292D0 (en) 1994-06-06 1994-06-06 Pharmaceuticals compositions
GB9411292.7 1994-06-06

Publications (1)

Publication Number Publication Date
WO1995033475A1 true WO1995033475A1 (fr) 1995-12-14

Family

ID=10756253

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/EP1995/002125 WO1995033475A1 (fr) 1994-06-06 1995-06-05 Utilisation de copolymere-1 dans la preparation d'un medicament destine au traitement de la nevrite optique

Country Status (8)

Country Link
EP (1) EP0767672A1 (fr)
JP (1) JPH10500695A (fr)
AU (1) AU2787495A (fr)
CA (1) CA2192218A1 (fr)
GB (1) GB9411292D0 (fr)
IL (1) IL113992A0 (fr)
WO (1) WO1995033475A1 (fr)
ZA (1) ZA954469B (fr)

Cited By (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6214791B1 (en) 1997-01-10 2001-04-10 Yeda Research And Development Co. Ltd. Treatment of multiple sclerosis through ingestion or inhalation of copolymer-1
WO2001093828A1 (fr) * 2000-06-05 2001-12-13 Teva Pharmaceuticals Industries, Ltd. Utilisation d'acetate de glatiramere (copolymere i) pour traiter des maladies du systeme nerveux central
WO2001097785A2 (fr) * 2000-06-20 2001-12-27 Caprion Pharmaceuticals Inc. Copolymeres et methodes de traitement des maladies a prions
US6800287B2 (en) 1998-09-25 2004-10-05 Yeda Research And Development Co., Ltd. Copolymer 1 related polypeptides for use as molecular weight markers and for therapeutic use
US6800285B2 (en) 2000-06-20 2004-10-05 Moses Rodriguez Treatment of central nervous system diseases by antibodies against glatiramer acetate
US7022663B2 (en) 2000-02-18 2006-04-04 Yeda Research And Development Co., Ltd. Oral, nasal and pulmonary dosage formulations of copolymer 1
US7033582B2 (en) 2000-06-05 2006-04-25 Teva Pharmaceutical Industries, Ltd. Use of glatiramer acetate (copolymer 1) in the treatment of central nervous system disorders
US7279172B2 (en) 1998-07-23 2007-10-09 Yeda Research And Development Co., Ltd. Treatment of autoimmune conditions with copolymer 1 and related copolymers
US7425332B2 (en) 1998-07-23 2008-09-16 Yeda Research And Development Co., Ltd. Treatment of autoimmune conditions with Copolymer 1 and related Copolymers
US7429374B2 (en) 2001-12-04 2008-09-30 Teva Pharmaceutical Industries, Ltd. Process for the measurement of the potency of glatiramer acetate
US8536305B2 (en) 2004-10-29 2013-09-17 Sandoz Ag Processes for preparing a polypeptide

Non-Patent Citations (5)

* Cited by examiner, † Cited by third party
Title
LOREN A. ROLAK: "Copolymer-I therapy for multiple sclerosis", CLINICAL NEUROPHARMACOLOGY, vol. 10, no. 5, pages 389 - 396 *
MARK J. RIEUMONT ET AL.: "Neuroimaging evaluation in multiple sclerosis", AM. FAM. PHYS., vol. 48, no. 2, pages 273 - 276 *
MASHA FRIDKIS-HARELI ET AL.: "Direct binding of myelin basic protein and synthetic copolymer 1 to class II major histocompatibility complex molecules on living antigen-presenting cells---specificity and promiscuity", PROC. NATL. ACAD. SCI. USA, vol. 91, no. 11, pages 4872 - 4876 *
ODED ABRAMSKI ET AL.: "Effect of a synthetic polypeptide (COP 1) on patients with multiple sclerosis and with acute disseminated encephalomyelitis", JOURNAL OF THE NEUROLOGICAL SCIENCES, vol. 31, no. 3, pages 433 - 438 *
ROBERT BERKOW ET AL.: "The Merck Manual of Diagnosis and Therapy", MERCK RESEARCH LABORATORIES, RAHWAY N.J. *

Cited By (18)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6214791B1 (en) 1997-01-10 2001-04-10 Yeda Research And Development Co. Ltd. Treatment of multiple sclerosis through ingestion or inhalation of copolymer-1
US7425332B2 (en) 1998-07-23 2008-09-16 Yeda Research And Development Co., Ltd. Treatment of autoimmune conditions with Copolymer 1 and related Copolymers
US7279172B2 (en) 1998-07-23 2007-10-09 Yeda Research And Development Co., Ltd. Treatment of autoimmune conditions with copolymer 1 and related copolymers
US7074580B2 (en) 1998-09-25 2006-07-11 Yeda Research And Development Co., Ltd. Copolymer 1 related polypeptides for use as molecular weight markers and for therapeutic use
US7163802B2 (en) 1998-09-25 2007-01-16 Yeda Research And Development Co., Ltd. Copolymer 1 related polypeptides for use as molecular weight markers and for therapeutic use
US8399211B2 (en) 1998-09-25 2013-03-19 Yeda Research And Development Co., Ltd. Copolymer 1 related polypeptides for use as molecular weight markers and for therapeutic use
US6800287B2 (en) 1998-09-25 2004-10-05 Yeda Research And Development Co., Ltd. Copolymer 1 related polypeptides for use as molecular weight markers and for therapeutic use
US7615359B2 (en) 1998-09-25 2009-11-10 Yeda Research And Development Co., Ltd. Copolymer 1 related polypeptides for use as molecular weight markers and for therapeutic use
US7022663B2 (en) 2000-02-18 2006-04-04 Yeda Research And Development Co., Ltd. Oral, nasal and pulmonary dosage formulations of copolymer 1
US7033582B2 (en) 2000-06-05 2006-04-25 Teva Pharmaceutical Industries, Ltd. Use of glatiramer acetate (copolymer 1) in the treatment of central nervous system disorders
WO2001093828A1 (fr) * 2000-06-05 2001-12-13 Teva Pharmaceuticals Industries, Ltd. Utilisation d'acetate de glatiramere (copolymere i) pour traiter des maladies du systeme nerveux central
WO2001097785A2 (fr) * 2000-06-20 2001-12-27 Caprion Pharmaceuticals Inc. Copolymeres et methodes de traitement des maladies a prions
WO2001097785A3 (fr) * 2000-06-20 2002-05-02 Caprion Pharmaceuticals Inc Copolymeres et methodes de traitement des maladies a prions
US6800285B2 (en) 2000-06-20 2004-10-05 Moses Rodriguez Treatment of central nervous system diseases by antibodies against glatiramer acetate
US7429374B2 (en) 2001-12-04 2008-09-30 Teva Pharmaceutical Industries, Ltd. Process for the measurement of the potency of glatiramer acetate
US7923215B2 (en) 2001-12-04 2011-04-12 Teva Pharmaceutical Industries, Ltd. Process for the measurement of the potency of glatiramer acetate
US8389228B2 (en) 2001-12-04 2013-03-05 Teva Pharmaceutical Industries, Ltd. Process for the measurement of the potency of glatiramer acetate
US8536305B2 (en) 2004-10-29 2013-09-17 Sandoz Ag Processes for preparing a polypeptide

Also Published As

Publication number Publication date
EP0767672A1 (fr) 1997-04-16
ZA954469B (en) 1996-01-24
JPH10500695A (ja) 1998-01-20
CA2192218A1 (fr) 1995-12-14
GB9411292D0 (en) 1994-07-27
IL113992A0 (en) 1995-10-31
AU2787495A (en) 1996-01-04

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