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Table 1 PSMA affinities, internalization, and lipophilicity of In-, Ga-, and Lu-PSMA-I&T

From: [111In]PSMA-I&T: expanding the spectrum of PSMA-I&T applications towards SPECT and radioguided surgery

Ligand IC50 [nM] Internalization [% of reference] Lipophilicity [log POW]
In-PSMA-I&T 7.5 ± 1.5 104 ± 7 −4.5
Ga-PSMA-I&T 9.4 ± 2.9 59 ± 2 −4.3
Lu-PSMA-I&T 7.9 ± 2.4 76 ± 2 −4.1
  1. PSMA affinities were determined in a competitive binding assay using LNCaP prostate cancer cells and (125I-BA)KuE as radioligand [2]. Data represent means ± SD of n ≥ 3 separate determinations
  2. PSMA-specific ligand internalization was determined by incubation of LNCaP cells (37 °C, 60 min) with the respective radioligands (0.2 nM) in the absence (total internalization) and presence (non-specific internalization) of 10 μM PMPA. Data were corrected for non-specific internalization and normalized to the specific internalization observed for the reference compound (125I-BA)KuE in a parallel experiment [2]. Data are means ± SD (n = 3)
  3. Lipophilicities (from n-octanol/PBS partition coefficients POW) were determined using a shake-flask method; values are means from n = 6 determinations