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US 2024/0408247 A1Published application
Non-peptide targeted therapeutics and uses thereof
AssigneeCrinetics Pharmaceuticals, Inc.
InventorsR. Scott STRUTHERS, Jian ZHAO, Yunfei ZHU
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Abstract
Described herein are non-peptide drug conjugates (NPDCs) that target tumor cells expressing cell surface peptide and protein G protein-coupled receptors and their use in the treatment and/or diagnosis of cancer.
Claims32
A compound of Formula (I), or a pharmaceutically acceptable salt thereof:
- NP-L-Q Formula (I)
- wherein:
- NP is a non-peptide ligand that binds to G protein-coupled receptor (GPCR) expressed in tumor cells;
- Q is a payload moiety comprising a chelating moiety or a radionuclide (Z) complex thereof;
- and
- L is a linker that covalently connects the non-peptide ligand NP and the payload moiety Q;
- wherein the linker L is attached to NP at a position that permits binding of NP to the GPCR;
- wherein upon administration to a mammal, the compound of Formula (I), or a pharmaceutically acceptable salt thereof, is targeted to tumor cells expressing the GPCR;
- wherein the GPCR is gonadotropin-releasing hormone receptor or somatostatin receptor;
- wherein the chelating moiety is:
- 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid (DOTA) or 1,4,7,10-tetraazacyclododecane-1,4,7-triacetic acid (DO3A);
- and
- wherein Z is an Auger electron-emitting radionuclide, α-emitting radionuclide, β-emitting radionuclide, or γ-emitting radionuclide.
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A method for identifying tissues or organs in a mammal with tumor cells expressing a G protein-coupled receptor (GPCR) comprising:
- (i) administering to the mammal a compound of Formula (I), or a pharmaceutically acceptable salt thereof:
- NP-L-Q Formula (I)
- wherein:
- NP is a non-peptide ligand that binds to a G protein-coupled receptor (GPCR) expressed in tumor cells;
- Q is a payload moiety comprising a chelating moiety or a radionuclide (Z) complex thereof;
- L is a linker that covalently connects the non-peptide ligand NP and the payload moiety Q;
- wherein the linker L is attached to NP at a position that permits binding of NP to the GPCR;
- (ii) performing positron emission tomography (PET) analysis, single-photon emission computerized tomography (SPECT), or magnetic resonance imaging (MRI);
- wherein:
- Z is a diagnostic radionuclide;
- wherein the GPCR is gonadotropin-releasing hormone receptor or somatostatin receptor;
- wherein the chelating moiety is:
- 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid (DOTA) or 1,4,7,10-tetraazacyclododecane-1,4,7-triacetic acid (DO3A);
- and
- wherein:
- step (ii) is imitated after an amount of time following step (i) sufficient for interaction between the compound of Formula (I) and GPCR expressed in tumor cells in the mammal.
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Dependencies are inferred from the claim text.