Antibody-drug conjugates
AssigneeSpirea Limited
InventorsMyriam Ouberai, Théophile Baïssas
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Abstract
The present invention relates to antibody-drug conjugates comprising (i) an antibody or antigen-binding fragment thereof, (ii) a polymer comprising a particular repeat unit, which is covalently bound to one or more biologically active moieties, such as small molecule drugs, optionally via a linker, and (iii) a polymer-antibody linker moiety which is covalently bound to both the polymer and the antibody or antigen-binding fragment thereof. Additionally, the present invention relates to pharmaceutical compositions comprising the antibody-drug conjugates and to use of the antibody-drug conjugates in medicine.
Claims22
An antibody-drug conjugate comprising:
- (i) an antibody or antigen-binding fragment thereof,
- (ii) a polymer comprising a repeat unit of Formula (I′):
- wherein:
- each n and each p is independently 0 or an integer between 1 and 6;
- each m is independently 0 or an integer between 1 and 4, and preferably at least one m is 1;
- V is
- ------- is a bond which may be absent or present;
- each D1 is independently O or L1-B1;
- each D2 is independently O or L2-B2;
- each D3 is independently O or L3-B3;
- wherein L1 is a linker group or a bond, L2 is a linker group or a bond, L3 is a linker group or a bond, and each B1, B2 and B3 is a biologically active moiety;
- provided that at least one D1, D2 or D3 group within the polymer is not O, and further provided that when D1, D2 or D3 is O, there is a double bond between the O atom and the carbon atom to which it is attached;
- each q is an integer between 1 and 8;
- X and Y are independently selected from O, NH, NR′ and S;
- R′ is C1-20 hydrocarbyl;
- Q is selected from —CH2(NMe(C═O)CH2)o—, -T1O(CH2CH2O)sT2- and -T1O(CH2CH2CH2O)sT2-, wherein T1 is selected from a divalent methylene, ethylene, propylene or butylene radical, and T2 is selected from a divalent methylene, ethylene, propylene or butylene radical;
- o is an integer from 0 to 100;
- and
- s is an integer from 0 to 150;
- and
- (iii) a polymer-antibody linker which is covalently bonded to both the antibody and the polymer.
6-8. (canceled)
19-20. (canceled)
(canceled)
A targeting agent-drug conjugate comprising:
- (i) a targeting agent;
- (ii) a polymer comprising a repeat unit of Formula (I′):
- wherein:
- each n and each p is independently 0 or an integer between 1 and 6;
- each m is independently 0 or an integer between 1 and 4, and preferably at least one m is 1;
- V is
- ------- is a bond which may be absent or present;
- each D1 is independently O or L1-B1;
- each D2 is independently O or L2-B2;
- each D3 is independently O or L3-B3;
- L1 is a linker group or a bond, L2 is a linker group or a bond, L3 is a linker group or a bond, and each B1, B2 and B3 is a biologically active moiety;
- provided that at least one D1, D2 or D3 group within the polymer is not O, and further provided that when D1, D2 or D3 is O, there is a double bond between the O atom and the carbon atom to which it is attached;
- each q is an integer between 1 and 8;
- X and Y are independently selected from O, NH, NR′ and S;
- R′ is C1-20 hydrocarbyl;
- Q is selected from —CH2(NMe(C═O)CH2)o—, -T1O(CH2CH2O)sT2- and -T1O(CH2CH2CH2O)sT2-, wherein T1 is selected from a divalent methylene, ethylene, propylene or butylene radical, and T2 is selected from a divalent methylene, ethylene, propylene or butylene radical;
- o is an integer from 0 to 100;
- and
- s is an integer from 0 to 150;
- and
- (iii) a polymer-targeting agent linker which is covalently bonded to both the targeting agent and the polymer.
Dependencies are inferred from the claim text.