CY1121246T1 - Συζευγμα αντισωματος αντι-trop2-φαρμακου - Google Patents
Συζευγμα αντισωματος αντι-trop2-φαρμακουInfo
- Publication number
- CY1121246T1 CY1121246T1 CY20191100002T CY191100002T CY1121246T1 CY 1121246 T1 CY1121246 T1 CY 1121246T1 CY 20191100002 T CY20191100002 T CY 20191100002T CY 191100002 T CY191100002 T CY 191100002T CY 1121246 T1 CY1121246 T1 CY 1121246T1
- Authority
- CY
- Cyprus
- Prior art keywords
- trop2
- tumor
- conject
- antibody
- drug antibody
- Prior art date
Links
- 229940079593 drug Drugs 0.000 title abstract 2
- 239000003814 drug Substances 0.000 title abstract 2
- 230000000259 anti-tumor effect Effects 0.000 abstract 3
- 150000001875 compounds Chemical class 0.000 abstract 2
- 125000003277 amino group Chemical group 0.000 abstract 1
- 239000002246 antineoplastic agent Substances 0.000 abstract 1
- 229940041181 antineoplastic drug Drugs 0.000 abstract 1
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 abstract 1
- 229940127121 immunoconjugate Drugs 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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- A61K47/6801—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
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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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- C07K2317/24—Immunoglobulins specific features characterized by taxonomic origin containing regions, domains or residues from different species, e.g. chimeric, humanized or veneered
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- C07K2317/00—Immunoglobulins specific features
- C07K2317/70—Immunoglobulins specific features characterized by effect upon binding to a cell or to an antigen
- C07K2317/77—Internalization into the cell
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K2317/00—Immunoglobulins specific features
- C07K2317/90—Immunoglobulins specific features characterized by (pharmaco)kinetic aspects or by stability of the immunoglobulin
- C07K2317/92—Affinity (KD), association rate (Ka), dissociation rate (Kd) or EC50 value
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Abstract
Ο σκοπός της παρούσας εφεύρεσης είναι να παρασχεθεί ένα φάρμακο κατά των όγκων που να υπερέχει σε επίδραση κατά των όγκων και ασφάλεια, και που να έχει εξαιρετική θεραπευτική επίδραση. Παρέχεται ένα σύζευγμα αντισώματος φαρμάκου που χαρακτηρίζεται από το γεγονός ότι μία ένωση κατά των όγκων που αναπαρίσταται από έναν χημικό τύπο και αντίσωμα αντι-ΤROP2 συνδέονται μέσω ενός συνδέτη που έχει μια δομή που αναπαρίσταται από τον χημικό τύπο -L1-L2-LP-NH-(CH2)n1-La-(CH2)n2-C(=O)- (όπου το αντίσωμα αντι-ΤRΟΡ2 δεσμεύεται με το L1 τερματικό και η ένωση κατά των όγκων δεσμεύεται με την ομάδα καρβοξυλίου της οντότητας (CH2)n2-C(=O)-χρησιμοποιώντας το άτομο αζώτου της αμινομάδας στη θέση 1 ως το σημείο δέσμευσης).
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PCT/JP2014/006421 WO2015098099A1 (ja) | 2013-12-25 | 2014-12-24 | 抗trop2抗体-薬物コンジュゲート |
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