HRP20180945T1 - Konjugati protutijelo-pirolobenzodiazepin - Google Patents
Konjugati protutijelo-pirolobenzodiazepin Download PDFInfo
- Publication number
- HRP20180945T1 HRP20180945T1 HRP20180945TT HRP20180945T HRP20180945T1 HR P20180945 T1 HRP20180945 T1 HR P20180945T1 HR P20180945T T HRP20180945T T HR P20180945TT HR P20180945 T HRP20180945 T HR P20180945T HR P20180945 T1 HRP20180945 T1 HR P20180945T1
- Authority
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- Croatia
- Prior art keywords
- antibody
- conjugate according
- seq
- amino acid
- acid sequence
- Prior art date
Links
- 229940127121 immunoconjugate Drugs 0.000 title 1
- 239000000562 conjugate Substances 0.000 claims 14
- 125000003275 alpha amino acid group Chemical group 0.000 claims 6
- 229940079593 drug Drugs 0.000 claims 3
- 239000003814 drug Substances 0.000 claims 3
- 206010028980 Neoplasm Diseases 0.000 claims 2
- 239000000611 antibody drug conjugate Substances 0.000 claims 2
- 229940049595 antibody-drug conjugate Drugs 0.000 claims 2
- 201000011510 cancer Diseases 0.000 claims 2
- 150000001875 compounds Chemical class 0.000 claims 2
- 201000010099 disease Diseases 0.000 claims 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 2
- 239000000203 mixture Substances 0.000 claims 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 2
- 208000024893 Acute lymphoblastic leukemia Diseases 0.000 claims 1
- 208000014697 Acute lymphocytic leukaemia Diseases 0.000 claims 1
- 208000010839 B-cell chronic lymphocytic leukemia Diseases 0.000 claims 1
- 208000032791 BCR-ABL1 positive chronic myelogenous leukemia Diseases 0.000 claims 1
- 208000010833 Chronic myeloid leukaemia Diseases 0.000 claims 1
- 241000283086 Equidae Species 0.000 claims 1
- 101001057504 Homo sapiens Interferon-stimulated gene 20 kDa protein Proteins 0.000 claims 1
- 101001055144 Homo sapiens Interleukin-2 receptor subunit alpha Proteins 0.000 claims 1
- 102100026878 Interleukin-2 receptor subunit alpha Human genes 0.000 claims 1
- 208000031671 Large B-Cell Diffuse Lymphoma Diseases 0.000 claims 1
- 208000031422 Lymphocytic Chronic B-Cell Leukemia Diseases 0.000 claims 1
- 208000025205 Mantle-Cell Lymphoma Diseases 0.000 claims 1
- 208000033761 Myelogenous Chronic BCR-ABL Positive Leukemia Diseases 0.000 claims 1
- 208000015914 Non-Hodgkin lymphomas Diseases 0.000 claims 1
- 208000006664 Precursor Cell Lymphoblastic Leukemia-Lymphoma Diseases 0.000 claims 1
- 239000002246 antineoplastic agent Substances 0.000 claims 1
- 208000032852 chronic lymphocytic leukemia Diseases 0.000 claims 1
- 229940127089 cytotoxic agent Drugs 0.000 claims 1
- 206010012818 diffuse large B-cell lymphoma Diseases 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 201000003444 follicular lymphoma Diseases 0.000 claims 1
- 201000009277 hairy cell leukemia Diseases 0.000 claims 1
- 208000032839 leukemia Diseases 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 230000002062 proliferating effect Effects 0.000 claims 1
Classifications
-
- 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
- A61K47/6835—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 the modifying agent being an antibody or an immunoglobulin bearing at least one antigen-binding site
- A61K47/6849—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 the modifying agent being an antibody or an immunoglobulin bearing at least one antigen-binding site the antibody targeting a receptor, a cell surface antigen or a cell surface determinant
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
- A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
- A61K31/5513—1,4-Benzodiazepines, e.g. diazepam or clozapine
- A61K31/5517—1,4-Benzodiazepines, e.g. diazepam or clozapine condensed with five-membered rings having nitrogen as a ring hetero atom, e.g. imidazobenzodiazepines, triazolam
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P39/00—General protective or antinoxious agents
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K16/00—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies
- C07K16/18—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans
- C07K16/28—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
- C07K16/2866—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants against receptors for cytokines, lymphokines, interferons
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K39/00—Medicinal preparations containing antigens or antibodies
- A61K39/0005—Vertebrate antigens
- A61K39/0011—Cancer antigens
- A61K39/001102—Receptors, cell surface antigens or cell surface determinants
- A61K39/001116—Receptors for cytokines
- A61K39/001119—Receptors for interleukins [IL]
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K2317/00—Immunoglobulins specific features
- C07K2317/50—Immunoglobulins specific features characterized by immunoglobulin fragments
- C07K2317/56—Immunoglobulins specific features characterized by immunoglobulin fragments variable (Fv) region, i.e. VH and/or VL
- C07K2317/565—Complementarity determining region [CDR]
Claims (15)
1. Konjugat, naznačen time, da ima sljedeće formule:
KonjA:
KonjB:
KonjC:
KonjD:
KonjE:
gdje je Ab protutijelo koje se veže na CD25, pri čemu protutijelo obuhvaća sljedeće:
VH-domenu koja sadrži VH CDR1 s aminokiselinskom sekvencom od SEQ ID NO. 3, VH CDR2 s aminokiselinskom sekvencom od SEQ ID NO. 4, i VH CDR3 s aminokiselinskom sekvencom od SEQ ID NO. 5,
te pritom opterećenost lijekom (p) od lijekova (D) na protutijelu (Ab), iznosi cijeli broj od 1 do 8.
2. Konjugat prema zahtjevu 1, naznačen time, da protutijelo obuhvaća VH-domenu koja ima sekvencu u skladu sa SEQ ID NO. 1.
3. Konjugat prema zahtjevu 1 ili zahtjevu 2, naznačen time, da protutijelo obuhvaća sljedeće:
VL-domenu koja sadrži VL CDR1 s aminokiselinskom sekvencom od SEQ ID NO. 6, VL CDR2 s aminokiselinskom sekvencom od SEQ ID NO. 7, i VL CDR3 s aminokiselinskom sekvencom od SEQ ID NO. 8.
4. Konjugat prema bilo kojem od zahtjeva 1 do 3, naznačen time, da protutijelo obuhvaća VL-domenu koja ima sekvencu u skladu sa SEQ ID NO. 2.
5. Konjugat prema bilo kojem od zahtjeva 1 do 4, naznačen time, da se kod protutijela radi o intaktnom protutijelu.
6. Konjugat prema bilo kojem od zahtjeva 1 do 5, naznačen time, da je protutijelo humanizirano, deimunizirano ili je površinski promijenjeno.
7. Konjugat prema bilo kojem od zahtjeva 1 do 4, naznačen time, da se kod protutijela radi o punom ljudskom monoklonalnom protutijelu IgG1, poželjno je to IgG1,κ.
8. Konjugat prema bilo kojem od zahtjeva 1 do 7, naznačen time, da p je 1, 2, 3, ili 4.
9. Konjugat prema zahtjevu 1, naznačen time, da obuhvaća mješavinu spojeva konjugata protutijelo-lijek, pri čemu prosječno opterećenje lijekom po protutijelu u mješavini spojeva konjugata protutijelo-lijek, iznosi od oko 2 do oko 5.
10. Konjugat prema bilo kojem od zahtjeva 1 do 8, naznačen time, da se upotrebljava u liječenju.
11. Konjugat prema bilo kojem od zahtjeva 1 do 8, naznačen time, da se upotrebljava u liječenju proliferativne bolesti kod pojedinca.
12. Konjugat prema zahtjevu 11, naznačen time, da bolest je rak.
13. Konjugat prema zahtjevu 12, naznačen time, da je rak odabran iz skupine koju čine: non-Hodgkin-limfom, uključujući difuzni limfom velikih B-stanica, folikularni limfom, te limfom plaštenih stanica; i leukemija, uključujući akutnu limfoblastnu leukemiju, kroničnu limfocitnu leukemiju, kroničnu mijeloidnu leukemiju, te leukemiju kosmatih stanica.
14. Farmaceutski sastav, naznačen time, da obuhvaća konjugat u skladu s bilo kojim od zahtjeva 1 do 8, i farmaceutski prikladan razrjeđivač, nosač ili pomoćno sredstvo.
15. Farmaceutski sastav prema zahtjevu 14, naznačen time, da dodatno obuhvaća terapeutski učinkovitu količinu kemoterapeutskog sredstva.
Applications Claiming Priority (7)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US201261712928P | 2012-10-12 | 2012-10-12 | |
US201261712924P | 2012-10-12 | 2012-10-12 | |
US201361798072P | 2013-03-15 | 2013-03-15 | |
US201361798037P | 2013-03-15 | 2013-03-15 | |
US201361798106P | 2013-03-15 | 2013-03-15 | |
EP13785373.5A EP2906296B1 (en) | 2012-10-12 | 2013-10-11 | Pyrrolobenzodiazepine-antibody conjugates |
PCT/EP2013/071349 WO2014057119A1 (en) | 2012-10-12 | 2013-10-11 | Pyrrolobenzodiazepine-antibody conjugates |
Publications (1)
Publication Number | Publication Date |
---|---|
HRP20180945T1 true HRP20180945T1 (hr) | 2018-08-10 |
Family
ID=49515321
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
HRP20180945TT HRP20180945T1 (hr) | 2012-10-12 | 2018-06-18 | Konjugati protutijelo-pirolobenzodiazepin |
Country Status (23)
Country | Link |
---|---|
US (3) | US9931415B2 (hr) |
EP (1) | EP2906296B1 (hr) |
JP (1) | JP6392764B2 (hr) |
KR (1) | KR101995620B1 (hr) |
CN (1) | CN105102068B (hr) |
AU (1) | AU2013328625B2 (hr) |
BR (1) | BR112015008232A2 (hr) |
CA (1) | CA2887897C (hr) |
CY (1) | CY1120327T1 (hr) |
DK (1) | DK2906296T3 (hr) |
ES (1) | ES2670937T3 (hr) |
HR (1) | HRP20180945T1 (hr) |
HU (1) | HUE039329T2 (hr) |
LT (1) | LT2906296T (hr) |
MX (1) | MX364328B (hr) |
NZ (1) | NZ707543A (hr) |
PL (1) | PL2906296T3 (hr) |
PT (1) | PT2906296T (hr) |
RS (1) | RS57104B1 (hr) |
SI (1) | SI2906296T1 (hr) |
TR (1) | TR201808051T4 (hr) |
WO (1) | WO2014057119A1 (hr) |
ZA (1) | ZA201502523B (hr) |
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