Preclinical Evaluation of a Novel BOC-Modified Triazoloacridinone (TRA-01AR) in Combination with 5-Fluorouracil in Colorectal Cancer

In HT-29 colorectal cancer xenografts, adding TRA-01AR to 5-fluorouracil did not significantly reduce tumor weight versus 5-fluorouracil alone, despite improved systemic profile and higher intratumoral blood flow.

• Why it matters: 5-fluorouracil efficacy in colorectal cancer is constrained by resistance, toxicity, and pharmacokinetic limitations, motivating combination strategies that sensitize tumors without worsening tolerability.
• What they did: The study tested 5-fluorouracil with triazoloacridinones C-1305 and TRA-01AR using integrated cellular assays, transcriptomics, bioenergetic profiling, and in vivo HT-29 xenografts.
• The result: TRA-01AR showed delayed cytotoxicity and distinct transcriptional and metabolic effects, and in vivo it increased intratumoral blood flow and improved systemic tolerability, but its combination benefit on tumor weight was not statistically significant.

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