CY1121573T1 - Συζευγμα αντισωματος anti-her2-φαρμακου - Google Patents
Συζευγμα αντισωματος anti-her2-φαρμακουInfo
- Publication number
- CY1121573T1 CY1121573T1 CY20191100406T CY191100406T CY1121573T1 CY 1121573 T1 CY1121573 T1 CY 1121573T1 CY 20191100406 T CY20191100406 T CY 20191100406T CY 191100406 T CY191100406 T CY 191100406T CY 1121573 T1 CY1121573 T1 CY 1121573T1
- Authority
- CY
- Cyprus
- Prior art keywords
- tumor
- her2
- binds
- conject
- drug antibody
- Prior art date
Links
- 229940043275 anti-HER2 drug Drugs 0.000 title 1
- 230000000259 anti-tumor effect Effects 0.000 abstract 4
- 150000001875 compounds Chemical class 0.000 abstract 3
- 239000000126 substance Substances 0.000 abstract 2
- 125000003277 amino group Chemical group 0.000 abstract 1
- 239000000611 antibody drug conjugate Substances 0.000 abstract 1
- 229940049595 antibody-drug conjugate Drugs 0.000 abstract 1
- 239000002246 antineoplastic agent Substances 0.000 abstract 1
- 229940041181 antineoplastic drug Drugs 0.000 abstract 1
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 abstract 1
- 239000003446 ligand Substances 0.000 abstract 1
- 229910052757 nitrogen Inorganic materials 0.000 abstract 1
- 125000004433 nitrogen atom Chemical group N* 0.000 abstract 1
- 230000001225 therapeutic effect Effects 0.000 abstract 1
Classifications
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- 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
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- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/47—Quinolines; Isoquinolines
- A61K31/4738—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems
- A61K31/4745—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having nitrogen as a ring hetero atom, e.g. phenantrolines
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- 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
- C07K16/30—Immunoglobulins [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
- C07K16/3069—Reproductive system, e.g. ovaria, uterus, testes, prostate
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- C07K16/32—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans against translation products of oncogenes
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- C07K2317/73—Inducing cell death, e.g. apoptosis, necrosis or inhibition of cell proliferation
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Abstract
Ως ένα φάρμακο κατά των όγκων που έχει μια εξαιρετική επίδραση κατά των όγκων και που έχει επίσης και μια εξαιρετική θεραπευτική επίδραση, ένα σύζευγμα αντισώματος-φαρμάκου παρέχεται, το οποίο χαρακτηρίζεται από το γεγονός ότι μια ένωση κατά των όγκων αναπαρίσταται από χημικό τύπο (1) συνδέεται σε ένα αντίσωμα αντι-ΗΕR2 μέσα από ένα συνδέτη έχοντας μια δομή που αναπαρίσταται από χημικό τύπο: -L1-L2-LP-NH-(CH2)n1-La-(CH2)n2-C(=O)- (όπου το αντίσωμα αντι-ΗΕR2 συνδέεται στο τερματικό του L1, και η ένωση κατά των όγκων συνδέεται σε μια ομάδα καρβονυλίου σε μια μερίδα -(CH2)n2-C(=O)- όπου ένα άτομο αζώτου σε μια αμινομάδα που εντοπίζεται στη θέση-1 στην ένωση κατά των όγκων χρησιμεύει ως ένα μέρος σύνδεσης).
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