[177Lu]Lu-AMTG / Stanford University, Technical University of Munich - LARVOL DELTA

Studies on the impact of modifications at the Gln-Trp site in RM2-based GRPR ligands. (PubMed, EJNMMI Res) - "Substitution of the Gln-Trp site in RM2 by artificial amino acids had a distinct impact on overall pharmacokinetics. While Hse (instead of Gln) and Bta (instead of Trp) led to a decreased, α-Me-Trp (instead of Trp) led to an increased in vivo stability, which resulted in improved pharmacokinetics over time in case of the latter. However, at 1 h post-injection both [68Ga]Ga-[Hse7]RM2 and [68Ga]Ga-[Bta8]RM2 displayed slightly higher tumor-to-pancreas and tumor-to-intestine ratios, rendering homoserine and β-(3-benzothienyl)alanine potential options for the modification of GRPR ligands with regard to imaging properties."

Journal • Oncology • Pancreatic Cancer • GRP-10

Comparison of the Treatment Efficacy of 161Tb- and 177Lu-Labeled GRPR Antagonists in PC3 Tumor-Bearing Mice (SNMMI 2025) - "161Tb- and 177Lu-labeling proceeded quantitatively, and labeled products were used without further purification. Animals were assigned to each of the four groups at the day of activity injection to obtain a similar average tumor volume (control group: 139 ± 36 mm3, [177Lu]Lu-RM2: 114 ± 28 mm3, [177Lu]Lu-AMTG: 127 ± 47 mm3, [161Tb]Tb-RM2: 120 ± 57 mm3, [161Tb]Tb-AMTG: 128 ± 26 mm3). Although aimed at similar amounts of activity injected per group, 161Tb-treated animals received a significantly higher activity due to a lower residual activity remaining in the syringe ([177Lu]Lu-RM2: 376 ± 34 µCi, [177Lu]Lu-AMTG: 346 ± 38 µCi, [161Tb]Tb-RM2: 510 ± 20 µCi, [161Tb]Tb-AMTG: 540 ± 20 µCi)."

Preclinical • Oncology • GRP-10

Identification and Optimization of a Lead Structure for B7H3-Targeted Peptides for Future use as Radiolabeled Compounds in Imaging and Treatment of Multiple Cancers (SNMMI 2025) - "161Tb- and 177Lu-labeling proceeded quantitatively, and labeled products were used without further purification. Animals were assigned to each of the four groups at the day of activity injection to obtain a similar average tumor volume (control group: 139 ± 36 mm3, [177Lu]Lu-RM2: 114 ± 28 mm3, [177Lu]Lu-AMTG: 127 ± 47 mm3, [161Tb]Tb-RM2: 120 ± 57 mm3, [161Tb]Tb-AMTG: 128 ± 26 mm3). Although aimed at similar amounts of activity injected per group, 161Tb-treated animals received a significantly higher activity due to a lower residual activity remaining in the syringe ([177Lu]Lu-RM2: 376 ± 34 µCi, [177Lu]Lu-AMTG: 346 ± 38 µCi, [161Tb]Tb-RM2: 510 ± 20 µCi, [161Tb]Tb-AMTG: 540 ± 20 µCi)."

Oncology • CD276 • GRP-10

Comparison of the Treatment Efficacy of 161Tb- and 177Lu-Labeled GRPR Antagonists in PC3 Tumor-Bearing Mice (SNMMI 2025) - "161Tb- and 177Lu-labeling proceeded quantitatively, and labeled products were used without further purification. Animals were assigned to each of the four groups at the day of activity injection to obtain a similar average tumor volume (control group: 139 ± 36 mm3, [177Lu]Lu-RM2: 114 ± 28 mm3, [177Lu]Lu-AMTG: 127 ± 47 mm3, [161Tb]Tb-RM2: 120 ± 57 mm3, [161Tb]Tb-AMTG: 128 ± 26 mm3). Although aimed at similar amounts of activity injected per group, 161Tb-treated animals received a significantly higher activity due to a lower residual activity remaining in the syringe ([177Lu]Lu-RM2: 376 ± 34 µCi, [177Lu]Lu-AMTG: 346 ± 38 µCi, [161Tb]Tb-RM2: 510 ± 20 µCi, [161Tb]Tb-AMTG: 540 ± 20 µCi)."

Preclinical • Oncology • GRP-10