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10‐Hydroxycamptothecin is a drug to cure various cancers. However, the 10‐hydroxycamptothecin cannot be widely applied in clinics due to fast elimination and resistance of various cancers to the drug. Nevertheless, co‐treatment with tetrandine is known to reverse the resistance of multi‐drug resistant cancers, and may present an effective strategy to improve the efficacy of 10‐hydroxycamptothecin...