RAPTA-C

RAPTA-C is an **organoruthenium(II) arene anticancer compound** with the formula [Ru(η6-p-cymene)Cl2(pta)], where pta stands for 1,3,5-triaza-7-phosphaadamantane[1][2][4]. It is a half-sandwich metal complex designed for increased water solubility and low toxicity compared to platinum chemotherapeutics[2][4]. It exhibits **anti-tumor, anti-metastatic, and anti-angiogenic activity**, shown in various preclinical models, including ovarian and colorectal cancer xenografts with significant reduction in tumor growth and microvessel density[1][2][5]. RAPTA-C primarily inhibits metastasis and tumor angiogenesis rather than directly killing tumor cells, with evidence that its mechanism involves adduct formation with chromatin histone proteins and significant interaction with proteins (such as cathepsin B and thioredoxin reductase), differentiating it from DNA-targeting drugs like cisplatin[1][2][4]. It has shown synergistic effects in combination with erlotinib, an EGFR inhibitor, enhancing anti-tumor efficacy in preclinical models[1][5]. The compound also displays broad in vitro antimicrobial activity[2]. RAPTA-C is an experimental compound under academic-led development, not yet in clinical use[1][2][4].

Other names

Ru(η6-p-cymene)Cl2(pta)]