RU2013158037A - MOLECULE interferon-β-1a HUMAN pegylated, possess antiviral, immunomodulating and antiproliferative activity, with improved stability, reduced immunogenicity, improved pharmacokinetic and pharmacodynamic parameters suitable for medical applications, and immunobiological BEING ON ITS BASIS - Google Patents
MOLECULE interferon-β-1a HUMAN pegylated, possess antiviral, immunomodulating and antiproliferative activity, with improved stability, reduced immunogenicity, improved pharmacokinetic and pharmacodynamic parameters suitable for medical applications, and immunobiological BEING ON ITS BASIS Download PDFInfo
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- RU2013158037A RU2013158037A RU2013158037/10A RU2013158037A RU2013158037A RU 2013158037 A RU2013158037 A RU 2013158037A RU 2013158037/10 A RU2013158037/10 A RU 2013158037/10A RU 2013158037 A RU2013158037 A RU 2013158037A RU 2013158037 A RU2013158037 A RU 2013158037A
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- conjugate
- pharmaceutical composition
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- hepatitis
- antiviral
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- 108010005716 Interferon beta-1a Proteins 0.000 title claims abstract 9
- 229960004461 interferon beta-1a Drugs 0.000 title claims abstract 9
- 230000000840 anti-viral effect Effects 0.000 title claims abstract 8
- 230000001028 anti-proliverative effect Effects 0.000 title claims abstract 7
- 230000002519 immonomodulatory effect Effects 0.000 title claims abstract 7
- 230000001900 immune effect Effects 0.000 title 1
- 230000005847 immunogenicity Effects 0.000 title 1
- 230000003285 pharmacodynamic effect Effects 0.000 title 1
- 239000008194 pharmaceutical composition Substances 0.000 claims abstract 13
- 201000010099 disease Diseases 0.000 claims abstract 12
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims abstract 12
- 239000003814 drug Substances 0.000 claims abstract 11
- 230000003612 virological effect Effects 0.000 claims abstract 9
- 206010059313 Anogenital warts Diseases 0.000 claims abstract 4
- 208000023275 Autoimmune disease Diseases 0.000 claims abstract 4
- 208000000907 Condylomata Acuminata Diseases 0.000 claims abstract 4
- 208000005176 Hepatitis C Diseases 0.000 claims abstract 4
- 206010028980 Neoplasm Diseases 0.000 claims abstract 4
- 208000025009 anogenital human papillomavirus infection Diseases 0.000 claims abstract 4
- 201000004201 anogenital venereal wart Diseases 0.000 claims abstract 4
- 201000011510 cancer Diseases 0.000 claims abstract 4
- 208000002672 hepatitis B Diseases 0.000 claims abstract 4
- 201000001441 melanoma Diseases 0.000 claims abstract 4
- 125000001360 methionine group Chemical group N[C@@H](CCSC)C(=O)* 0.000 claims abstract 4
- 201000006417 multiple sclerosis Diseases 0.000 claims abstract 4
- 208000031951 Primary immunodeficiency Diseases 0.000 claims abstract 3
- 206010054979 Secondary immunodeficiency Diseases 0.000 claims abstract 3
- 230000001363 autoimmune Effects 0.000 claims abstract 2
- 230000000771 oncological effect Effects 0.000 claims abstract 2
- 125000003607 serino group Chemical group [H]N([H])[C@]([H])(C(=O)[*])C(O[H])([H])[H] 0.000 claims abstract 2
- 238000000034 method Methods 0.000 claims 9
- 238000004519 manufacturing process Methods 0.000 claims 5
- QTBSBXVTEAMEQO-UHFFFAOYSA-N Acetic acid Chemical compound CC(O)=O QTBSBXVTEAMEQO-UHFFFAOYSA-N 0.000 claims 3
- 230000002265 prevention Effects 0.000 claims 3
- 229940079593 drug Drugs 0.000 claims 2
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims 2
- BDKLKNJTMLIAFE-UHFFFAOYSA-N 2-(3-fluorophenyl)-1,3-oxazole-4-carbaldehyde Chemical compound FC1=CC=CC(C=2OC=C(C=O)N=2)=C1 BDKLKNJTMLIAFE-UHFFFAOYSA-N 0.000 claims 1
- FBPFZTCFMRRESA-KVTDHHQDSA-N D-Mannitol Chemical compound OC[C@@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-KVTDHHQDSA-N 0.000 claims 1
- KCXVZYZYPLLWCC-UHFFFAOYSA-N EDTA Chemical compound OC(=O)CN(CC(O)=O)CCN(CC(O)=O)CC(O)=O KCXVZYZYPLLWCC-UHFFFAOYSA-N 0.000 claims 1
- 229930195725 Mannitol Natural products 0.000 claims 1
- IWUCXVSUMQZMFG-AFCXAGJDSA-N Ribavirin Chemical compound N1=C(C(=O)N)N=CN1[C@H]1[C@H](O)[C@H](O)[C@@H](CO)O1 IWUCXVSUMQZMFG-AFCXAGJDSA-N 0.000 claims 1
- 229960000583 acetic acid Drugs 0.000 claims 1
- 235000011054 acetic acid Nutrition 0.000 claims 1
- 229940090047 auto-injector Drugs 0.000 claims 1
- 239000003795 chemical substances by application Substances 0.000 claims 1
- 239000000594 mannitol Substances 0.000 claims 1
- 235000010355 mannitol Nutrition 0.000 claims 1
- 229960001855 mannitol Drugs 0.000 claims 1
- 239000000244 polyoxyethylene sorbitan monooleate Substances 0.000 claims 1
- 235000010482 polyoxyethylene sorbitan monooleate Nutrition 0.000 claims 1
- 229920000053 polysorbate 80 Polymers 0.000 claims 1
- 229940068968 polysorbate 80 Drugs 0.000 claims 1
- 229940071643 prefilled syringe Drugs 0.000 claims 1
- 229960000329 ribavirin Drugs 0.000 claims 1
- HZCAHMRRMINHDJ-DBRKOABJSA-N ribavirin Natural products O[C@@H]1[C@H](O)[C@@H](CO)O[C@H]1N1N=CN=C1 HZCAHMRRMINHDJ-DBRKOABJSA-N 0.000 claims 1
- 235000017281 sodium acetate Nutrition 0.000 claims 1
- 229940087562 sodium acetate trihydrate Drugs 0.000 claims 1
- 239000003381 stabilizer Substances 0.000 claims 1
- 239000008215 water for injection Substances 0.000 claims 1
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- Medicinal Preparation (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Peptides Or Proteins (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
1. Стабильный конъюгат ПЭГилированного интерферон-β-1a человека формулы (I), представляющий собой один позиционный изомер:где n - целые значения от 454 до 909;m - целое число≥4;NH-IFN - интерферон-β-1a.2. Конъюгат по п.1, в котором m представляет собой целое число, равное 4.3. Конъюгат по п.1, в котором интерферон-β-1a представляет собой природный или рекомбинантный интерферон-β-1a человека.4. Конъюгат по п.1, в котором n имеет целые значения от 454 до 909.5. Конъюгат по п.1, в котором N-концевая группа представлена остатком метионина (Met).6. Конъюгат по п.1, в котором N-концевая группа представлена остатком серина (Ser).7. Фармацевтическая композиция, обладающая противовирусной, антипролиферативной и иммуномодулирующей активностью, содержащая конъюгат общей формулы (I) в эффективном количестве и фармацевтически приемлемые вспомогательные компоненты.8. Фармацевтическая композиция по п.7 для применения в качестве лекарственного средства для лечения аутоиммунных, вирусных и онкологических заболеваний, и заболеваний, сопровождающихся первичными или вторичными иммунодефицитными состояниями.9. Фармацевтическая композиция по п.8, где аутоиммунное заболевание представляет собой рассеянный склероз.10. Фармацевтическая композиция по п.8, где вирусное заболевание представляет собой гепатит C или гепатит B.11. Фармацевтическая композиция по п.8, где вирусное заболевание представляет собой остроконечные кондиломы.12. Фармацевтическая композиция по п.8, где онкологическое заболевание представляет собой меланому.13. Лекарственное средство, включающее конъюгат формулы (I), обладающее противовирусной, антипролиферативной и иммуномодулирующей активностью.14. Ле1. A stable conjugate of pegylated human interferon-β-1a of the formula (I), which is one positional isomer: where n is an integer from 454 to 909; m is an integer≥4; NH-IFN is interferon-β-1a.2 . The conjugate according to claim 1, in which m is an integer equal to 4.3. The conjugate according to claim 1, in which interferon-β-1a is a natural or recombinant human interferon-β-1a. The conjugate according to claim 1, in which n has integer values from 454 to 909.5. The conjugate according to claim 1, wherein the N-terminal group is represented by a methionine residue (Met). The conjugate according to claim 1, wherein the N-terminal group is represented by a serine residue (Ser). A pharmaceutical composition having antiviral, antiproliferative and immunomodulatory activity, containing an conjugate of the general formula (I) in an effective amount and pharmaceutically acceptable auxiliary components. The pharmaceutical composition according to claim 7 for use as a medicine for the treatment of autoimmune, viral and oncological diseases, and diseases accompanied by primary or secondary immunodeficiency conditions. The pharmaceutical composition of claim 8, wherein the autoimmune disease is multiple sclerosis. The pharmaceutical composition of claim 8, wherein the viral disease is hepatitis C or hepatitis B.11. The pharmaceutical composition of claim 8, wherein the viral disease is genital warts. The pharmaceutical composition of claim 8, wherein the cancer is melanoma. A medicament comprising a conjugate of formula (I) having antiviral, antiproliferative and immunomodulatory activity. 14. Le
Claims (32)
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| RU2013158037A RU2576372C3 (en) | 2013-12-26 | HUMAN INTERFERON-BETA-1A MOLECULE, MODIFIED WITH POLYETHYLENE GLYCOL, WITH ANTI-VIRAL, IMMUNOMODULATING AND ANTI-PROLIFERATIVE ACTIVITIES, WITH INCREASED STABILITY, REDUCED IMMUNOGENICITY, WITH REAL PHARMACOKINETIC AND PHARMACODYNAMIC PARAMETERS, SUITABLE FOR MEDICAL USE AND AN IMMUNOBIOLOGICAL DRUG BASED ON IT |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| RU2013158037A RU2576372C3 (en) | 2013-12-26 | HUMAN INTERFERON-BETA-1A MOLECULE, MODIFIED WITH POLYETHYLENE GLYCOL, WITH ANTI-VIRAL, IMMUNOMODULATING AND ANTI-PROLIFERATIVE ACTIVITIES, WITH INCREASED STABILITY, REDUCED IMMUNOGENICITY, WITH REAL PHARMACOKINETIC AND PHARMACODYNAMIC PARAMETERS, SUITABLE FOR MEDICAL USE AND AN IMMUNOBIOLOGICAL DRUG BASED ON IT |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| RU2013158037A true RU2013158037A (en) | 2015-07-10 |
| RU2576372C2 RU2576372C2 (en) | 2016-02-27 |
| RU2576372C3 RU2576372C3 (en) | 2024-04-12 |
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Also Published As
| Publication number | Publication date |
|---|---|
| RU2576372C2 (en) | 2016-02-27 |
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