DK2714740T3 - Neutraliserende prolactinreceptor-antistof mat3 og terapeutisk anvendelse deraf - Google Patents

Neutraliserende prolactinreceptor-antistof mat3 og terapeutisk anvendelse deraf Download PDF

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DK2714740T3
DK2714740T3 DK12729030.2T DK12729030T DK2714740T3 DK 2714740 T3 DK2714740 T3 DK 2714740T3 DK 12729030 T DK12729030 T DK 12729030T DK 2714740 T3 DK2714740 T3 DK 2714740T3
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antibody
antigen
host cell
acid sequence
binding fragment
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Lars Linden
Axel Harrenga
Simone Greven
Andreas Wilmen
Christoph Freiberg
Christiane Otto
Mark Trautwein
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Bayer Ip Gmbh
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    • C07K16/00Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies
    • C07K16/18Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans
    • C07K16/28Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
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    • C07K16/00Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies
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    • C07K16/28Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
    • AHUMAN NECESSITIES
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    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/06Drugs for disorders of the endocrine system of the anterior pituitary hormones, e.g. TSH, ACTH, FSH, LH, PRL, GH
    • A61P5/08Drugs for disorders of the endocrine system of the anterior pituitary hormones, e.g. TSH, ACTH, FSH, LH, PRL, GH for decreasing, blocking or antagonising the activity of the anterior pituitary hormones
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    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K16/00Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies
    • C07K16/18Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans
    • C07K16/28Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
    • C07K16/30Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants from tumour cells
    • C07K16/3015Breast
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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    • C07K2317/00Immunoglobulins specific features
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    • C07K2317/76Antagonist effect on antigen, e.g. neutralization or inhibition of binding
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    • C07K2317/90Immunoglobulins specific features characterized by (pharmaco)kinetic aspects or by stability of the immunoglobulin
    • C07K2317/92Affinity (KD), association rate (Ka), dissociation rate (Kd) or EC50 value

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Claims (22)

1. Antistof Mat3 eller antigenbindende fragmenter deraf, som antagoniserer prolactinreceptor-medieret signallering, hvor antistoffet eller de antigenbindende fragmenter deraf omfatter a. en variabel tung region med en aminosyresekvens ifølge SEQ ID NO: 1 og b. en variabel let region med en aminosyresekvens ifølge SEQ ID NO: 2.
2. Antistof eller antigenbindende fragmenter deraf ifølge krav 1, hvor antistoffet eller de antigenbindende fragmenter deraf består af en antigenbindende region, der binder specifikt til en eller flere regioner af det ekstracellulære domæne af prolactinreceptor (PRLR) fra menneske, abe og mus, og hvor aminosyresekvensen for den humane PRLR er vist ved aminosyresekvensen fra position 1 til 210 af SEQ ID NO: 12 og humane polymorfe varianter af SEQ ID NO: 12, ved aminosyresekvensen fra position 1 til 210 af abe-PRLR'en ifølge SEQ ID NO: 11 og af muse-PRLR'en ifølge SEQ ID NO: 13.
3. Antistof eller antigenbindende fragmenter deraf ifølge krav 2, hvor affiniteten til det ekstracellulære domæne af PRLR fra menneske, abe og mus er 100 nM, mindre end 30 nM, eller en affinitet på 10 nM, og hvor affiniteten er blevet målt ved hjælp af overflade-plasmonresonans, for eksempel Biacore.
4. Antistof eller antigenbindende fragmenter deraf ifølge krav 1, hvor antistoffet består af en antigenbindende region, der binder specifikt til en eller flere regioner af det ekstracellulære domæne af human PRLR, og hvor affiniteten er 10 nM eller 1 nM, og hvor affiniteten er blevet målt ved hjælp af overflade-plasmonresonans, for eksempel Biacore.
5. Antistof eller antigenbindende fragmenter deraf ifølge et hvilket som helst af kravene 1 til 4, hvor de konstante domæner af tung kæde er modificeret eller umodificeret IgGl, IgG2, IgG3 eller IgG4.
6. Isoleret nukleinsyresekvens, der koder for et antistof eller et antigenbindende fragment ifølge et hvilket som helst af kravene 1 til 5.
7. Isoleret nukleinsyresekvens ifølge krav 6, hvor den isolerede nukleinsyresekvenser er ifølge SEQ ID NO: 3 og 4.
8. Ekspressionvektor, der omfatter en nukleinsyresekvens ifølge krav 6 eller 7.
9. Værtscelle, der omfatter vektoren ifølge krav 8 eller et nukleinsyremolekyle ifølge krav 6 eller 7, hvor værtscellen er en højere eukaryot værtscelle, en lavere eukaryot værtscelle eller en prokaryot celle.
10. Værtscelle ifølge krav 9, hvor den højere eukaryote værtscelle er en mammaliacelle.
11. Værtscelle ifølge krav 9, hvor den lavere eukaryote værtscelle er en gærcelle.
12. Værtscelle ifølge krav 9, hvor den prokaryote celle er en bakteriecelle.
13. Fremgangsmåde til anvendelse af værtscellen ifølge et hvilket som helst af kravene 9 til 12 til frembringelse af et antistof eller et antigenbindende fragment, som omfatter dyrkning af værtscellen ifølge krav 9 under egnede betingelser og indvinding af antistoffet.
14. Antistof eller antigenbindende fragment, der er frembragt ved hjælp af fremgangsmåden ifølge krav 13.
15. Antistof eller antigenbindende fragment ifølge et hvilket som helst af kravene 1 til 5, der er oprenset til mindst 95 vægt-% homogenitet.
16. Antistof eller antigenbindende fragment ifølge et hvilket som helst af kravene 1 til 5 til anvendelse som et medikament.
17. Farmaceutisk sammensætning, der omfatter antistoffet eller det antigenbindende fragment ifølge et hvilket som helst af kravene 1 til 5 og et farmaceutisk acceptabelt bæremateriale, der omfatter excipienser og hjælpestoffer.
18. Kit, der omfatter et antistof ifølge krav 1 til 5, der omfatter en terapeutisk effektiv mængde af antistof Mat3, der er pakket i en beholder, hvilket kit eventuelt indeholder et andet terapeutisk middel, og yderligere omfatter en etiket, der er fastgjort til eller pakket med beholderen, hvilken etiket beskriver indholdet i beholderen og tilvejebringer indikationer og/eller anvisninger med hensyn til anvendelsen af indholdet i beholderen til behandling af endometriose, adenomyose, benign brystsygdom og mastalgi, laktationshæmning, hårtab som følge af hyper- og normoprolaktinemi, benign prostatahyperplasi, fibroider eller til anvendelse som ikke-hormonelt præventionsmiddel til kvinder eller til behandling af kvinder, der er i kombineret hormonterapi, østrogen plus progestin-terapi, til hæmning af brystepitelcelleproliferation eller til behandling og forebyggelse af antiøstrogenresistent brystcancer.
19. Antistof eller antigenbindende fragment ifølge et hvilket som helst af kravene 1 til 5 til anvendelse i et medikament til behandling og/eller forebyggelse af endometriose og adenomyose, endometriosis interna.
20. Antistof eller antigenbindende fragment ifølge et hvilket som helst af kravene 1 til 5 til anvendelse i et medikament til behandling of benign brystsygdom og mastalgi.
21. Antistof eller antigenbindende fragment ifølge et hvilket som helst af kravene 1 til 5 til anvendelse i et medikament til behandling eller forebyggelse af antiøstrogenresistent brystcancer .
22. Farmaceutisk sammensætning ifølge krav 17, der omfatter et PRLR-antistoffer eller antigenbindende fragmenter ifølge et hvilket som helst af kravene 1 til 5 i kombination med mindst ét andet middel.
DK12729030.2T 2011-06-03 2012-05-31 Neutraliserende prolactinreceptor-antistof mat3 og terapeutisk anvendelse deraf DK2714740T3 (da)

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EP11168644A EP2530089A1 (en) 2011-06-03 2011-06-03 Neutralising prolactin receptor antibody Mat3 and its therapeutical use
PCT/EP2012/060078 WO2012163932A1 (en) 2011-06-03 2012-05-31 Neutralizing prolactin receptor antibody mat3 and its therapeutic use

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US (2) US9353186B2 (da)
EP (2) EP2530089A1 (da)
JP (1) JP5859641B2 (da)
KR (1) KR101920521B1 (da)
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RS54727B1 (sr) 2016-10-31
CR20130632A (es) 2014-02-04
CN103764679A (zh) 2014-04-30
EP2714740A1 (en) 2014-04-09
ES2572215T3 (es) 2016-05-30
AU2012264765B2 (en) 2016-07-28
SI2714740T1 (sl) 2016-06-30
NZ618316A (en) 2016-01-29
BR112013030995A2 (pt) 2016-11-22
US9777063B2 (en) 2017-10-03
HK1195081A1 (zh) 2014-10-31
JP2014522239A (ja) 2014-09-04
MX2013014174A (es) 2014-11-13
KR20140036275A (ko) 2014-03-25
MX343683B (es) 2016-11-17
US20140141003A1 (en) 2014-05-22
PE20141158A1 (es) 2014-09-26
EP2530089A1 (en) 2012-12-05
US9353186B2 (en) 2016-05-31
ZA201309683B (en) 2016-08-31
CY1117660T1 (el) 2017-05-17
HUE028775T2 (en) 2017-01-30
EA201301356A1 (ru) 2014-09-30
IL229504B (en) 2018-10-31
ECSP13013063A (es) 2014-01-31
IL229504A0 (en) 2014-01-30
PL2714740T3 (pl) 2016-08-31
CO6852025A2 (es) 2014-01-30
SG195060A1 (en) 2013-12-30
CA2837736C (en) 2018-11-20
AU2012264765A1 (en) 2013-12-19
ME02659B (me) 2017-06-20
KR101920521B1 (ko) 2018-11-21
AP2013007266A0 (en) 2013-11-30
HRP20160506T1 (hr) 2016-06-17
CN103764679B (zh) 2016-05-04
EA029316B1 (ru) 2018-03-30
EP2714740B1 (en) 2016-03-30
UY34116A (es) 2013-01-03
CU20130163A7 (es) 2014-04-24
AR086631A1 (es) 2014-01-08
CL2013003459A1 (es) 2014-08-08
CA2837736A1 (en) 2012-12-06
MA35237B1 (fr) 2014-07-03
DOP2013000285A (es) 2014-03-16
TN2013000501A1 (en) 2015-03-30
TWI548649B (zh) 2016-09-11
WO2012163932A1 (en) 2012-12-06
JP5859641B2 (ja) 2016-02-10
BR112013030995B1 (pt) 2021-11-09
TW201302798A (zh) 2013-01-16

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