HANK & LIN'S GROUP

The past is prologue and the future is scintillating

177Lu-P17-087 (PSMA-087)

177Lu-P17-088 (PSMA-088)

  • 177Lu-P17-087: This radioligand demonstrates high tumor uptake with fast kinetics, enabling rapid internalization by tumor cells. Its metabolic clearance is relatively quick, allowing for prompt tumor cell destruction.
  • 177Lu-P17-088: Due to its binding to albumin, this compound has a longer circulation time and slower metabolism, maintaining elevated concentrations in the bloodstream for extended periods. This results in prolonged tumor uptake and slower clearance, enabling sustained radiation-induced damage to the tumor cells over a longer duration.
  • Li, Linlin, et al. "Comparison of novel PSMA-targeting [177Lu]Lu-P17-087 with its albumin binding derivative [177Lu]Lu-P17-088 in metastatic castration-resistant prostate cancer patients: a first-in-human study."European Journal of Nuclear Medicine and Molecular Imaging 51(2024):2794–2805.

    https://doi.org/10.1007/s00259-024-06721-x

  • 2024 PSMA CONFERENCE PSMA PET and RLT: Present and Future January 18-19, 2024  (UCSF)

Publication：


  1. Li, Linlin, et al."Comparison of novel PSMA-targeting [177Lu]Lu-P17-087 with its albumin binding derivative [177Lu]Lu-P17-088 in metastatic castration-resistant prostate cancer patients: a first-in-human study."European Journal of Nuclear Medicine and Molecular Imaging 51(2024):2794–2805. https://link.springer.com/article/10.1007/s00259-024-06721-x
  2. Zha Z, Choi SR, Li L, Zhao R, Ploessl K, Yao X, Alexoff D, Zhu L, Kung HF. New PSMA-Targeting Ligands: Transformation from Diagnosis (Ga-68) to Radionuclide Therapy (Lu-177). Journal of Medicinal Chemistry. 2022 Sep 14;65(19):13001-12.

    https://doi.org/10.1021/acs.jmedchem.2c00852

  3. Zha Z, Ploessl K, Choi SR, Zhao R, Jin W, Wang R, Alexoff D, Zhu L, Kung HF. Lu-177-Labeled Hetero-Bivalent Agents Targeting PSMA and Bone Metastases for Radionuclide Therapy. Journal of Medicinal Chemistry. 2023 Sep 5;66(17):12602-13.

    https://doi.org/10.1021/acs.jmedchem.3c01294

  4. Zhao R, Ploessl K, Zha Z, Choi S, Alexoff D, Zhu L, Kung HF. Synthesis and evaluation of 68Ga-and 177Lu-labeled (R)-vs (S)-DOTAGA prostate-specific membrane antigen-targeting derivatives. Molecular Pharmaceutics. 2020 Oct 27;17(12):4589-602.

    https://doi.org/10.1021/acs.molpharmaceut.0c00777

  5. Wang R, Jin W, Luo Y, Hong H, Zhao R, Li L, Yan L, Qiao J, Ploessl K, Zhu L, Kung HF. Novel [68Ga/177Lu]Ga/Lu-AZ-093 as PSMA-targeting agent for diagnosis and radiotherapy.Molecular Pharmaceutics. 2024, 21, 7, 3256–3267.

    https://doi.org/10.1021/acs.molpharmaceut.4c00020


 Meeting Abstracts：

  1. Li L, Wang J, Wang G, Wang R, Jin W, Zang J, Sui H, Jia C, Jiang Y, Hong H, Zhu L. Dosimetry and pilot therapy study of novel PSMA-targeting agents,[177Lu]Lu-P17-087 and [177Lu]Lu-P17-088, in metastatic castration-resistant prostate cancer patients. Journal of Nuclear MedicineJune 2024,65(supplement 2)241896;
  2. Lv J, Zhao R, Liang S, Li M, Gu D, Cai C, Liu Y, Zhong H, Yimin F, Yan Q, Zhu L. Feasibility, Biodistribution, and Preliminary Dosimetry in PSMA Targeted Radionuclide Therapy of Metastatic Castration-Resistant Prostate Cancer Using 177Lu-PSMA-087: First-in-Humans Results. Journal of Nuclear MedicineJune 2024,65(supplement 2)241661;
  3. Kung, Hank, et al. "[Ga-68]/[Lu-177] P17-087: A potential theranostic agent targeting PSMA expressing tumor."JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS. Vol. 62. 111 RIVER ST, HOBOKEN 07030-5774, NJ USA: WILEY, 2019.