The invention relates to a 
tumor targeted diagnosis and treatment integrated 
drug compound, in particular to an <18 / 19>F-labeled PSMA targeted diagnosis and treatment integrated small molecular 
drug conjugate, a preparation method and an application of the <18 / 19>F-labeled PSMA targeted diagnosis and treatment integrated small molecular 
drug conjugate. By utilizing a PSMA targeted small molecular ligand, a DM1 drug with a high 
toxicity killing effect is delivered to PSMA positive 
prostate cancer cells in a targeted manner, the effect of effectively killing 
castration-resistant 
prostate CRPC cells with relative 
drug resistance is expected to be achieved, besides, the toxic and side effects of the DM1 on the 
whole body are effectively controlled and reduced, and the tolerance of a patient is improved; and besides, on the basis, a tumor diagnosis and treatment integrated mode is introduced, 
molecular imaging diagnosis is used for assisting in visualizing the in-vivo transfer process of drugs, predicting the 
curative effect of the patient, knowing the in-vivo distribution of the drugs, achieving real-time monitoring and individualized administration of the tumor 
treatment effect and achieving diagnosis and treatment integration.