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MBLI87 (also known as MBLI-87 or acridone 4b) is a novel, potent, and selective acridone derivative that acts as an inhibitor of the Breast Cancer Resistance Protein (BCRP/ABCG2) efflux transporter. Developed by researchers at the CNRS, Université Claude Bernard Lyon 1, and Université Grenoble Alpes, MBLI87 was specifically designed to overcome multidrug resistance (MDR) in cancer cells. By inhibiting ABCG2-mediated drug efflux, MBLI87 increases the intracellular accumulation and potency of chemotherapeutic substrates such as irinotecan, its active metabolite SN-38, and mitoxantrone. In preclinical xenograft models, co-administration of MBLI87 with irinotecan significantly sensitized ABCG2-expressing tumors to chemotherapy without altering systemic drug exposure or inducing significant toxicity.
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