<18/19>F-labeled PSMA targeted diagnosis and treatment integrated small-molecular drug conjugate, preparation method and application of <18/19>F-labeled PSMA targeted diagnosis and treatment integrated small-molecular drug conjugate

Abstract

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.

Description

technical field [0001] The present invention relates to an integrated drug compound for tumor targeting diagnosis and treatment, in particular to a 18 / 19 F-labeled PSMA-positive tumor targeted diagnosis and treatment integrated specific small molecule drug conjugate, preparation method and application thereof. Background technique [0002] Prostate cancer is a common malignant tumor in the male genitourinary system, and it is the second most common male tumor in the world. In recent years, the incidence and detection rate of prostate cancer have increased year by year, and the mortality rate has also increased year by year. A serious fact is that most newly diagnosed patients have locally advanced or distantly metastasized, and have lost the opportunity for radical treatment. Treatment of advanced patients is one of the key issues in the field of prostate cancer treatment research. [0003] Castration therapy is currently one of the most commonly used treatments for advanc...

AI Technical Summary

Problems solved by technology

However, the former is expensive and not widely accepted by patients

Docetaxel chemotherapy is currently recognized as an effective chemotherapy regimen, but as a traditional tumor chemotherapy method, its application is systemic therapy, which does not have tumor target specificity, and it will kill normal cells in the body while killing cancer cells , cause systemic toxic adverse reactions, such as nausea and vomiting, dry mouth, loss of appetite, numb hands and feet, hair loss, blood cell reduction, etc., resulting in a general decline in the quality of life of patients, and even being forced to stop treatment due to intolerance

In addition, because the efficiency of chemotherapeutic drugs finally delivered into the tumor tissue is often not high, its tumor suppressive efficacy is also limited; at the same time, there are cases of hypersensitivity or ineffectiveness due to factors such as individual differences in patients, which lead to treatment failure.

Images