The adenosine 5'‐triphosphate (ATP) binding cassette subfamily B member 1 (ABCB1) modulator zosuquidar disrupts PD‐L1 translocating from ER to Golgi apparatus, dramatically triggers autophagic degradation of PD‐L1, and exhibits significant anti‐tumor effect in vivo. The gene discussed is ABCB1; the disease is neoplasm.