Inhibitors of prostate-specific membrane antigen in the diagnosis and therapy of metastatic prostate cancer - a review of patent literature.
Hyunsoo HaHongmok KwonTaehyeong LimJaebong JangSong-Kyu ParkYoungjoo ByunPublished in: Expert opinion on therapeutic patents (2021)
: PSMA-targeted imaging agents labeled with radionuclides such as fluorine-18, copper-64, gallium-68, and technetium-99m have been successfully translated into clinical phase for the early diagnosis of metastatic prostate cancer. Recently, PSMA-targeted therapeutic agents labeled with iodine-131, lutetium-177, astatine-211, and lead-212 have also been developed with notable progress. Most PSMA-targeted agents are based on the Lys-urea-Glu or Glu-urea-Glu structure, demonstrate strong PSMA-binding affinity in nanomolar range, and achieve diverse structural modifications in the non-pharmacophore pocket. By exploiting the S1 accessory pocket or the tunnel region of the PSMA active site, the in vivo efficacy and pharmacokinetic profiles of the PMSA-targeted agents can be effectively modulated.
Keyphrases
- pet imaging
- prostate cancer
- pet ct
- cancer therapy
- positron emission tomography
- radical prostatectomy
- squamous cell carcinoma
- systematic review
- high resolution
- magnetic resonance imaging
- magnetic resonance
- drug delivery
- molecular docking
- benign prostatic hyperplasia
- cell therapy
- mass spectrometry
- smoking cessation
- contrast enhanced