Drug intelligence / Profile preview

Ibu-DAB-PSMA

Development stage: Unknown
Lead developer: ITM Isotope Technologies Munich
Modality: Small Molecules, Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics, Peptides
Administration: Intravenous

Overview

Ibu-DAB-PSMA is a small-molecule radioligand developed by ITM Oncologics GmbH for the treatment of prostate-specific membrane antigen (PSMA)-positive metastatic castration-resistant prostate cancer (mCRPC). The compound is designed with a glutamine-urea-lysine motif for high-affinity binding to PSMA, which is highly overexpressed in prostate cancer cells. It features a unique linker containing diaminobutyric acid (DAB) and an ibuprofen moiety; the latter serves as a moderate albumin binder to prolong the drug's blood half-life, thereby increasing tumor accumulation and improving the therapeutic index. Ibu-DAB-PSMA is typically radiolabeled with the alpha-emitter actinium-225 ($^{225}$Ac) for clinical use, though preclinical studies have also utilized lutetium-177 ($^{177}$Lu). It is currently undergoing Phase I clinical evaluation to assess safety, pharmacokinetics, and preliminary efficacy in patients with progressive mCRPC.

Other names: [225Ac]Ac-Ibu-DAB-PSMA[177Lu]Lu-Ibu-DAB-PSMA

Targets

PSMA (Prostate-specific membrane antigen)

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