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paclitaxel-octreotide conjugate
- Development stage
- Preclinical
- Lead developer
- Southeast University
- Modality
- Peptides, Small Molecules
- Administration
- Intravenous
01
Overview
Paclitaxel-octreotide conjugate (POC) is a peptide-drug conjugate (PDC) designed for the targeted treatment of somatostatin receptor (SSTR)-expressing malignancies, particularly paclitaxel-resistant ovarian cancer. The molecule consists of the cytotoxic microtubule-stabilizing agent paclitaxel chemically linked via a succinyl linker to octreotide, a synthetic octapeptide analog of somatostatin. POC leverages the high expression of SSTR2 and SSTR5 on tumor cells to achieve selective delivery and internalization of paclitaxel through receptor-mediated endocytosis. Preclinical studies conducted by researchers at Southeast University have demonstrated that POC significantly inhibits tumor growth in xenograft models while exhibiting reduced systemic toxicity compared to free paclitaxel. Furthermore, the conjugate appears to reverse multidrug resistance by downregulating MDR1, VEGF, and MMP-9, and by modulating the expression of tubulin isoforms.
- Other names
- paclitaxel + octreotidepaclitaxel-octreotide conjugatePTX-OCT conjugateFITC-POC
02
Targets
TUBB (Tubulin (alpha and beta subunits))SSTR5 (Somatostatin receptor 5)SSTR2 (Somatostatin receptor type 2)
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