KR900005995A - 변형 인터류킨-2 및 그의 제조방법 - Google Patents

변형 인터류킨-2 및 그의 제조방법 Download PDF

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KR900005995A
KR900005995A KR1019890015545A KR890015545A KR900005995A KR 900005995 A KR900005995 A KR 900005995A KR 1019890015545 A KR1019890015545 A KR 1019890015545A KR 890015545 A KR890015545 A KR 890015545A KR 900005995 A KR900005995 A KR 900005995A
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modified
fragment
amino group
immunoglobulin
antibody activity
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KR1019890015545A
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English (en)
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야스따까 이가리
가즈히로 도껜
준 사또
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우메모또 요시마사
다께다야꾸힝 고오교 가부시끼가이샤
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Publication of KR900005995A publication Critical patent/KR900005995A/ko

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K14/00—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • C07K14/435—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • C07K14/52—Cytokines; Lymphokines; Interferons
    • C07K14/54—Interleukins [IL]
    • C07K14/55—IL-2
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/68—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
    • A61K47/6801—Drug-antibody or immunoglobulin conjugates defined by the pharmacologically or therapeutically active agent
    • A61K47/6803—Drugs conjugated to an antibody or immunoglobulin, e.g. cisplatin-antibody conjugates
    • A61K47/6811—Drugs conjugated to an antibody or immunoglobulin, e.g. cisplatin-antibody conjugates the drug being a protein or peptide, e.g. transferrin or bleomycin
    • A61K47/6813—Drugs conjugated to an antibody or immunoglobulin, e.g. cisplatin-antibody conjugates the drug being a protein or peptide, e.g. transferrin or bleomycin the drug being a peptidic cytokine, e.g. an interleukin or interferon
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/68—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
    • A61K47/6889—Conjugates wherein the antibody being the modifying agent and wherein the linker, binder or spacer confers particular properties to the conjugates, e.g. peptidic enzyme-labile linkers or acid-labile linkers, providing for an acid-labile immuno conjugate wherein the drug may be released from its antibody conjugated part in an acidic, e.g. tumoural or environment
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides

Abstract

내용 없음

Description

변형 인터류킨-2 및 그의 제조방법
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음
제1도는 아미노말단이 H-Ala-인 인간 IL-2의 아미노산 서열을 나타낸다.
제2도는 실시예 1(1)에서 수득된 접합체의 겔 여과 형태를 나타낸다.
제3도는 실시예 1(1)에서 수득되고, 실시예 1(2)에서 수득된 접합체의 혈액 농도의 EIA 결정법의 결과를 나타낸다.

Claims (16)

  1. IL-2 및 면역 글로불린(Ig) 또는 항체 활성을 갖는 그의 단편을 서로 화학적으로 결합시킨 변형 인터류킨-2(IL-2)
  2. 제1항에 있어서, IL-2의 아미노기 및 면역 글로불린 또는 항체 활성을 갖는 그의 단편의 환원에 의해 얻은 메르캅토기를 교차 결합제를 통해 결합시킨 변형 IL-2.
  3. 제1항에 있어서, IL-2의 아미노기 및 면역 글로불린 또는 항체 활성을 갖는 그의 단편의 아미노기에 도입된 티올기를 교차 결합제를 통해 결합시킨 변형 IL-2.
  4. 제1항에 있어서, IL-2가 제조합 인간 IL-2인 변형 IL-2.
  5. 제1항에 있어서, Ig가 IgG인 변형 IL-2.
  6. 제1항에 있어서, 항체 활성을 갖는 Ig 단편을 사용한 변형 IL-2.
  7. 제6항에 있어서, Ig 단편이 Fab,Fab´또는 F(ab´)2인 변형 IL-2.
  8. 제6항에 있어서, Ig 단편이 Fab´인 변형 IL-2.
  9. 제6항에 있어서, Ig 단편이 F(ab´)2인 변형 IL-2.
  10. IL-2의 아미노기 및 면역 글로불린 또는 항체 활성을 갖는 그의 단편의 환원에 의해 얻은 메르캅토기를 교차 결합제를 통해 결합 시킴을 특징으로 하는 변형 인터류킨 -2(IL-2)의 제조방법.
  11. 제10항에 있어서, 교차 결합제가 N-(ε-말레이미도카프로일옥시)숙신이미 드(EMCS)인 방법.
  12. IL-2의 아미노기 및 면역 글로불린 또는 항체 활성을 갖는 그의 단편의 아미노기에 도입된 티올기를 교차 결합제를 통해 결합 시킴을 특징으로 하는 변형 인터류킨 -2(IL-2)의 제조방법.
  13. 제12항에 있어서, 교차 결합제가 N-(ε-말레이미도카프로일옥시)숙신이미드 (EMCS)인 방법.
  14. 제12항에 있어서, 교차 결합제가 N-(ε-말레이미도카프로일옥시)숙신이미드 (EMCS)이고, 티올기-도입제가 N-숙신이미딜-s-아세틸티오아세테이트(SATA)인 방법.
  15. IL-2의 아미노기 및 면역 글로불린 또는 항체 활성을 갖는 그의 단편의 환원에 의해 얻은 메르캅토기를 교차 결합제를 통해 결합 시킴으로서 제조된 변형 인터류킨 -2(IL-2).
  16. IL-2의 아미노기 및 면역 글로불린 또는 항체 활성을 갖는 그의 단편의 아미노기에 도입된 티올기를 교차 결합제를 통해 결합 시킴으로서 제조된 변형 인터류킨 -2(IL-2).
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019890015545A 1988-10-31 1989-10-27 변형 인터류킨-2 및 그의 제조방법 KR900005995A (ko)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
JP27691788 1988-10-31
JP63-276917 1988-10-31

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KR900005995A true KR900005995A (ko) 1990-05-07

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EP (1) EP0367166A1 (ko)
KR (1) KR900005995A (ko)
AU (1) AU622724B2 (ko)
CA (1) CA2001787A1 (ko)
DK (1) DK540289A (ko)

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