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LL344 is a novel coumarin derivative developed as a dual inhibitor of the efflux transporters P-glycoprotein (P-gp/ABCB1) and breast cancer resistance protein (BCRP/ABCG2). Developed through a collaboration between Dongguk University and Ewha Womans University, LL344 is designed to overcome multidrug resistance (MDR) in cancer chemotherapy. By blocking these key ATP-binding cassette (ABC) transporters, LL344 increases the intracellular accumulation and cytotoxicity of chemotherapeutic substrates, such as topotecan and paclitaxel. In preclinical rodent models, oral co-administration of LL344 with topotecan significantly enhances the oral bioavailability of the chemotherapeutic agent and improves its antitumor efficacy in human colon cancer xenografts without causing notable systemic toxicity.
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