zoptarelin doxorubicin

Zoptarelin doxorubicin is an investigational **peptide-drug conjugate** developed by Aeterna Zentaris for LHRH receptor-positive malignancies. It covalently couples the GnRH agonist peptide D-Lys6-LHRH to doxorubicin, enabling receptor-mediated uptake by tumor cells expressing gonadotropin-releasing hormone receptor; the released doxorubicin moiety intercalates DNA and inhibits topoisomerase II, producing cytotoxic antineoplastic activity. The lead program was a Phase 3 second-line study in locally advanced, recurrent, or metastatic endometrial cancer, but the trial did not improve overall survival and development was discontinued in 2017. ([cdn.clinicaltrials.gov](https://cdn.clinicaltrials.gov/large-docs/55/NCT01767155/Prot_001.pdf))

Brand names

Zoptrex

Other names

Lys6-LHRH-doxorubicinLys-6-LHRH-doxorubicinLys 6-LHRH-doxorubicin