Drug intelligence / Profile preview

PSMA I&T

Development stage
Unknown
Lead developer
Curium
Modality
Small Molecules, Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics
Administration
Intravenous
01

Overview

PSMA I&T is a small-molecule radioligand designed for theranostic use in prostate cancer, specifically *prostate-specific membrane antigen* (PSMA) targeting[1][6][7]. Structurally, it is a urea-based inhibitor of PSMA, chemically modified by conjugation with DOTAGA for stable chelation of radioisotopes such as Lutetium-177 (^177Lu) for therapy or Indium-111 (^111In) for imaging[1]. The primary **mechanism of action** involves binding with high affinity to PSMA, which is highly expressed on the surface of prostate cancer cells. When labeled with a radionuclide (e.g., ^177Lu), PSMA I&T delivers targeted radiation to tumor sites for radioligand therapy (RLT), promoting tumor cell death while sparing healthy tissues. For imaging, the radiolabeled compound allows precise tumor localization through SPECT or PET.

Brand names
PSMA I&T
Other names
DOTAGA-PSMADOTAGA-(I-y)fk(Sub-KuE)
02

Targets

PSMA (Prostate-specific membrane antigen)

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