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JF-10-81

Development stage
Preclinical
Lead developer
Tulane University
Modality
Peptide-Drug Conjugates → Peptide Conjugates → Peptides, Small Molecules
Administration
Subcutaneous
01

Overview

JF-10-81 is a peptide-drug conjugate (PDC) designed for targeted chemotherapy. It comprises the cytotoxic quinoline alkaloid camptothecin (CPT) covalently linked to the N-terminus of a somatostatin (SST) analog, JF-07-69, through an activated carbamate linker. The conjugate is engineered to selectively target cells expressing the somatostatin receptor subtype 2 (SSTR2), which is frequently overexpressed in neuroendocrine tumors, pancreatic cancer, and other malignancies. By utilizing the SST analog as a delivery vector, JF-10-81 facilitates the receptor-mediated internalization of the cytotoxic payload, thereby increasing local drug concentration within the tumor while minimizing systemic toxicity. Preclinical studies have shown significant efficacy in inhibiting the growth of SSTR2-positive tumors, including neuroblastoma, leukemia, and prostate cancer, as well as reducing tumor metastasis.

Other names
camptothecin-somatostatin conjugateCPT-SST conjugate
02

Targets

TOP1 (DNA Topoisomerase I)SSTR2 (Somatostatin receptor type 2)

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