Drug intelligence / Profile preview

Peptide-drug conjugate

Development stage
Preclinical
Lead developer
MolGenie
Modality
Peptide-Drug Conjugates → Peptide Conjugates → Peptides
01

Overview

Peptide-drug conjugate (PDC) is a preclinical-stage, NPY1R-targeted peptide-drug conjugate being developed by MolGenie, in collaboration with TUBE Pharmaceuticals, for the treatment of high-risk breast cancer (metastasis prevention), sarcoma, and Ewing sarcoma. Originally derived from a platform acquired from OntoChem, the conjugate consists of a neuropeptide Y (NPY)-inspired targeting peptide conjugated to a cytotoxic tubulysin payload (such as tubugi-1) via a cleavable disulfide linker. The peptide moiety selectively binds to the Neuropeptide Y receptor type 1 (NPY1R), which is overexpressed in various tumor tissues, facilitating receptor-mediated endocytosis and intracellular delivery of the payload. Once internalized, the linker is cleaved to release the tubulysin payload, which disrupts the microtubule network and induces cell death. The asset has demonstrated efficacy in patient-derived xenograft (PDX) models of breast cancer and sarcoma and is undergoing preparation for formal preclinical GLP studies.

Other names
First PDCNPY1R peptide-tubulysin conjugateNPY-1R peptide-tubulysin conjugateNPY 1R peptide-tubulysin conjugatetubugi-1-SS-NPYtubugi1-SS-NPYtubugi 1-SS-NPY
02

Targets

NPY1R (Neuropeptide Y receptor Y1)NPY2R (Neuropeptide Y receptor subtype 2)NPY4R (Neuropeptide Y receptor Y4)NPY5R (Neuropeptide Y receptor type 5)TUBB (Tubulin (alpha and beta subunits))

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