The systemic use of pharmaceutical drugs for cancer patients is a compromise between desirable therapy and side effects because of the intrinsic shortage of organâspecific pharmaceutical drug. Design and construction of pharmaceutical drug to achieve the organâspecific delivery is thus desperately desirable. We herein regulate perylene skeleton to effect organâspecificity and present an example of lungâspecific distribution on the basis of bayâtwisted PDICâNC. We further demonstrate that PDICâNC can target into mitochondria to act as cellular respiration inhibitor, inducing insufficient production of adenosine triphosphate, promoting endogenous H2O2 and .OH burst, elevating calcium overload, efficiently triggering the synergistic apoptosis, autophagy and endoplasmic reticulum stress of lung cancer cells. The antitumor performance of PDICâNC is verified on in vivo xenografted, metastasis and orthotopic lung cancer, presenting overwhelming evidences for potentially clinical application. This study contributes a proofâofâconcept demonstration of twisted perylene to well attain lungâspecific distribution, and meanwhile achieves intensive lung cancer chemotherapy.