HRP20211152T1 - Konjugati antitijela s lijekom koji ciljaju na uparap - Google Patents
Konjugati antitijela s lijekom koji ciljaju na uparap Download PDFInfo
- Publication number
- HRP20211152T1 HRP20211152T1 HRP20211152TT HRP20211152T HRP20211152T1 HR P20211152 T1 HRP20211152 T1 HR P20211152T1 HR P20211152T T HRP20211152T T HR P20211152TT HR P20211152 T HRP20211152 T HR P20211152T HR P20211152 T1 HRP20211152 T1 HR P20211152T1
- Authority
- HR
- Croatia
- Prior art keywords
- antibody
- drug conjugate
- fragment
- binds
- antigen
- Prior art date
Links
- 239000000611 antibody drug conjugate Substances 0.000 title claims 21
- 229940049595 antibody-drug conjugate Drugs 0.000 title claims 21
- 230000008685 targeting Effects 0.000 title 1
- 239000012634 fragment Substances 0.000 claims 14
- 125000003275 alpha amino acid group Chemical group 0.000 claims 13
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- 101001008321 Homo sapiens Immunoglobulin kappa variable 2D-26 Proteins 0.000 claims 6
- 101001047619 Homo sapiens Immunoglobulin kappa variable 3-20 Proteins 0.000 claims 6
- 101001008263 Homo sapiens Immunoglobulin kappa variable 3D-15 Proteins 0.000 claims 6
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- WOWDZACBATWTAU-FEFUEGSOSA-N (2s)-2-[[(2s)-2-(dimethylamino)-3-methylbutanoyl]amino]-n-[(3r,4s,5s)-1-[(2s)-2-[(1r,2r)-3-[[(1s,2r)-1-hydroxy-1-phenylpropan-2-yl]amino]-1-methoxy-2-methyl-3-oxopropyl]pyrrolidin-1-yl]-3-methoxy-5-methyl-1-oxoheptan-4-yl]-n,3-dimethylbutanamide Chemical class CC(C)[C@H](N(C)C)C(=O)N[C@@H](C(C)C)C(=O)N(C)[C@@H]([C@@H](C)CC)[C@H](OC)CC(=O)N1CCC[C@H]1[C@H](OC)[C@@H](C)C(=O)N[C@H](C)[C@@H](O)C1=CC=CC=C1 WOWDZACBATWTAU-FEFUEGSOSA-N 0.000 claims 1
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Classifications
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- 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
- A61K47/6817—Toxins
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Claims (20)
1. Konjugat antitijela s lijekom usmjeren protiv uPARAP, koji sadrži:
a) antitijelo koje se veže na aminokiselinski slijed SEQ ID NO: 32 ili 33 (fibronektinska domena tipa II (FN-II) u uPARAP),
b) aktivno sredstvo, gdje se aktivno sredstvo bira između terapijskog sredstva, citotoksičnog sredstva, radioizotopa i biljega kojeg se može detektirati, i
c) spojnicu koja spaja a) s b).
2. Konjugat antitijela s lijekom u skladu s patentnim zahtjevom 1, gdje se antitijelo bira iz skupine koju čine:
a) antitijelo, ili njegov fragment koji se veže na antigen, koje sadrži
i. varijabilno područje lakog lanca imunoglobulina koje sadrži ili se sastoji od aminokiselinskog slijeda SEQ ID NO: 11 ili slijed koji mu je istovjetan po slijedu najmanje 90 %, i
ii. varijabilno područje teškog lanca imunoglobulina koje sadrži ili se sastoji od aminokiselinskog slijeda SEQ ID NO: 15 ili slijed koji mu je istovjetan po slijedu najmanje 90 %,
gdje se bilo koja varijanca slijeda nalazi izvan područja određivanja komplementarnosti,
b) humanizirana verzija antitijela, ili njegovog fragmenta koji se veže na antigen, iz a),
c) kimerna verzija antitijela, ili njegovog fragmenta koji se veže na antigen, iz a),
d) antitijelo, ili njegov fragment koji se veže na antigen, koje sadrži
i. varijabilno područje lakog lanca imunoglobulina koje sadrži aminokiselinske sljedove SEQ ID NO: 12, 13 i 14, i
ii. varijabilno područje teškog lanca imunoglobulina koje sadrži aminokiselinske sljedove SEQ ID NO 16, 17 i 18,
e) antitijelo, ili njegov fragment koji se veže na antigen, koje sadrži
i. varijabilno područje lakog lanca imunoglobulina koje sadrži aminokiselinske sljedove SEQ ID NO: 48, 49 i 50, i
ii. varijabilno područje teškog lanca imunoglobulina koje sadrži aminokiselinske sljedove SEQ ID NO 51, 52 i 53,
f) humanizirana verzija antitijela, ili njegovog fragmenta koji se veže na antigen, iz d) ili e).
3. Konjugat antitijela s lijekom u skladu s patentnim zahtjevom 1, gdje se antitijelo bira iz skupine koju čine:
a) antitijelo, ili njegov fragment koji se veže na antigen, koje sadrži
i. varijabilno područje lakog lanca imunoglobulina koje sadrži ili se sastoji od aminokiselinskog slijeda SEQ ID NO: 19 ili 20 ili slijed koji mu je istovjetan po slijedu najmanje 90 %, i
ii. varijabilno područje teškog lanca imunoglobulina koje sadrži ili se sastoji od aminokiselinskog slijeda SEQ ID NO: 24 ili 25 ili slijed koji mu je istovjetan po slijedu najmanje 90 %,
gdje se bilo koja varijanca slijeda nalazi izvan područja određivanja komplementarnosti,
b) humanizirana verzija antitijela, ili njegovog fragmenta koji se veže na antigen, iz a),
c) kimerna verzija antitijela, ili njegovog fragmenta koji se veže na antigen, iz a),
d) antitijelo, ili njegov fragment koji se veže na antigen, koje sadrži
i. varijabilno područje lakog lanca imunoglobulina koje sadrži aminokiselinske sljedove SEQ ID NO: 21, 22 i 23, i
ii. varijabilno područje teškog lanca imunoglobulina koje sadrži aminokiselinske sljedove SEQ ID NO 26, 27 i 28,
e) antitijelo, ili njegov fragment koji se veže na antigen, koje sadrži
i. varijabilno područje lakog lanca imunoglobulina koje sadrži aminokiselinske sljedove SEQ ID NO: 54, 55 i 56, i
ii. varijabilno područje teškog lanca imunoglobulina koje sadrži aminokiselinske sljedove SEQ ID NO 57, 58 i 59,
f) humanizirana verzija antitijela, ili njegovog fragmenta koji se veže na antigen, iz d) ili e).
4. Konjugat antitijela s lijekom u skladu s bilo kojim od prethodnih patentnih zahtjeva, gdje se antitijelo bira između mišjeg antitijela, kimernog antitijela, ljudskog antitijela, humaniziranog antitijela, humanizirani fragment koji se veže na antigen, Fab fragmenta, Fab’ fragmenta, F(ab’)2 fragmenta, Fv, jednolančano antitijelo (SCA), poput scFv, varijabilnog dijela njegovih teških i/ili lakih lanaca, te Fab miniantitijela.
5. Konjugat antitijela s lijekom u skladu s bilo kojim od prethodnih patentnih zahtjeva, gdje je antitijelo monoklonsko antitijelo.
6. Konjugat antitijela s lijekom u skladu s bilo kojim od prethodnih patentnih zahtjeva, gdje je aktivno sredstvo kemoterapijsko sredstvo, poput kemoterapijskog sredstva kojeg se bira iz skupine koju čine alkilirajuća sredstva, antraciklini, antimetaboliti, sredstva protiv mikrotubula/protumitotska sredstva, inhibitori histonske deacetilaze, inhibitori kinaza, peptidni antibiotici, antineoplastična sredstva na bazi platine, inhibitori topoizomeraze i citotoksični antibiotici.
7. Konjugat antitijela s lijekom u skladu s bilo kojim od prethodnih patentnih zahtjeva, gdje je aktivno sredstvo protumitotsko sredstvo, kojeg se primjerice bira iz skupine koju čine monometilirani auristatin E (MMAE), monometilirani auristatin F (MMAF), taksan (primjerice paklitaksel ili docetaksel), vinka alkaloid (primjerice vinblastin, vinkristin, vindezin ili vinorelbin), kolhicin ili podofilotoksin.
8. Konjugat antitijela s lijekom u skladu s bilo kojim od prethodnih patentnih zahtjeva, gdje je aktivno sredstvo sredstvo za umrežavanje DNA, poput sredstva za umrežavanje DNA kojeg se bira između pirolobenzodiazepina ili dimernog derivata pirolobenzodiazepina.
9. Konjugat antitijela s lijekom u skladu s bilo kojim od prethodnih patentnih zahtjeva, gdje je aktivno sredstvo alkilirajuće sredstvo, poput duokarmicina SA.
10. Konjugat antitijela s lijekom u skladu s bilo kojim od prethodnih patentnih zahtjeva namijenjen upotrebi kao medikament.
11. Farmaceutski pripravak koji sadrži konjugat antitijela s lijekom u skladu s bilo kojim od patentnih zahtjeva 1 do 9, te farmaceutski prihvatljivi pufer, razrjeđivač, nosač, adjuvans ili pomoćno sredstvo.
12. Konjugat antitijela s lijekom u skladu s bilo kojim od patentnih zahtjeva 1 do 9 ili farmaceutski pripravak u skladu s patentnim zahtjevom 11, namijenjen upotrebi u postupku liječenja bolesti naznačene time što su prisutne stanice koje eksprimiraju uPARAP, primjerice gdje se bolest naznačena time što su prisutne stanice koje eksprimiraju uPARAP bira između raka, bolesti propadanja kostiju poput osteoporoze, fibroze, te bolesti ili poremećaji povezani s makrofazima poput ateroskleroze ili kronične upale.
13. Konjugat antitijela s lijekom ili farmaceutski pripravak namijenjeni upotrebi u skladu s patentnim zahtjevom 12, gdje je bolest rak.
14. Konjugat antitijela s lijekom ili farmaceutski pripravak namijenjeni upotrebi u skladu s patentnim zahtjevom 13, gdje je rak sarkom, poput osteosarkoma, liposarkoma, miksofibrosarkoma, protuberantnog dermatofibrosarkoma (DFSP) i/ili lejomiosarkoma (LMS).
15. Konjugat antitijela s lijekom ili farmaceutski pripravak namijenjeni upotrebi u skladu s patentnim zahtjevom 13, gdje je rak glioblastom.
16. Konjugat antitijela s lijekom ili farmaceutski pripravak namijenjeni upotrebi u skladu s patentnim zahtjevom 13, gdje je rak rak prostate ili metastaze na kostima iz raka prostate.
17. Konjugat antitijela s lijekom ili farmaceutski pripravak namijenjeni upotrebi u skladu s patentnim zahtjevom 13, gdje je rak rak dojke.
18. Konjugat antitijela s lijekom ili farmaceutski pripravak namijenjeni upotrebi u skladu s patentnim zahtjevom 13, gdje je rak rak glave i vrata.
19. Konjugat antitijela s lijekom ili farmaceutski pripravak namijenjeni upotrebi u skladu s patentnim zahtjevom 13, gdje je rak leukemija.
20. Komplet koji sadrži konjugat antitijela s lijekom u skladu s bilo kojim od patentnih zahtjeva 1 do 9 ili farmaceutski pripravak u skladu s patentnim zahtjevom 11, koji može dodatno sadržavati sredstvo za primjenu konjugata antitijela s lijekom na subjektu i/ili upute o upotrebi.
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DKPA201670063 | 2016-02-05 | ||
DKPA201670834 | 2016-10-24 | ||
PCT/DK2017/050024 WO2017133745A1 (en) | 2016-02-05 | 2017-02-03 | ANTIBODY-DRUG CONJUGATES TARGETING uPARAP |
EP17706673.5A EP3411076B1 (en) | 2016-02-05 | 2017-02-03 | Antibody-drug conjugates targeting uparap |
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