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Drug intelligence / Profile preview
cantrixil
- Development stage
- Phase 1
- Lead developer
- Kazia Therapeutics
- Modality
- Small Molecules
- Administration
- Intraperitoneal
01
Overview
Cantrixil is a cyclodextrin-encapsulated, third-generation super-benzopyran (SBP) small molecule with potential antineoplastic activity. The active ingredient, TRXE-002-01 (also known as TRX-E-002–1), is designed to target a broad spectrum of cancer cells, including chemotherapy-resistant tumor stem cells believed to drive disease relapse. Cantrixil has demonstrated potent cytotoxicity against both chemoresistant ovarian cancer stem cells and chemosensitive ovarian cancer cell lines. Its mechanism involves activation of c-Jun (a component of the AP‑1 transcription factor), downregulation of phosphorylated ERK, and induction of caspase-dependent and -independent apoptosis in tumor cells. Preclinical studies suggest additional involvement of tumor-associated NADH oxidase (ENOX2) and disruption of transmembrane electron transport-mediated energy production. Cantrixil is administered intraperitoneally and has been evaluated in Phase I clinical trials for advanced ovarian cancer, showing promising anti-tumor activity both as monotherapy and in combination with standard intravenous chemotherapy[1][4][5][6][8]. Vivesto currently holds global development rights after acquiring them from Kazia Therapeutics.
- Brand names
- Cantrixil
- Other names
- cantrixil2135511-22-5UNII-5DVS457HEGUNII5DVS457HEGUNII 5DVS457HEG
02
Targets
CASP6 (Caspase-6)ENOX2 (Tumor-associated NADH oxidase)CASP3 (Caspase-3)CASP7 (Caspase-7)CASP9 (Caspase-9)MAPK3 (Mitogen-activated protein kinase 1)JUN (Transcription factor Jun)
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