132307-50-7Relevant articles and documents
An Eighteen-Membered Macrocyclic Ligand for Actinium-225 Targeted Alpha Therapy
Thiele, Nikki A.,Brown, Victoria,Kelly, James M.,Amor-Coarasa, Alejandro,Jermilova, Una,MacMillan, Samantha N.,Nikolopoulou, Anastasia,Ponnala, Shashikanth,Ramogida, Caterina F.,Robertson, Andrew K. H.,Rodríguez-Rodríguez, Cristina,Schaffer, Paul,Williams, Clarence,Babich, John W.,Radchenko, Valery,Wilson, Justin J.
, p. 14712 - 14717 (2017)
The 18-membered macrocycle H2macropa was investigated for 225Ac chelation in targeted alpha therapy (TAT). Radiolabeling studies showed that macropa, at submicromolar concentration, complexed all 225Ac (26 kBq) in 5 min at RT. [225Ac(macropa)]+ remained intact over 7 to 8 days when challenged with either excess La3+ ions or human serum, and did not accumulate in any organ after 5 h in healthy mice. A bifunctional analogue, macropa-NCS, was conjugated to trastuzumab as well as to the prostate-specific membrane antigen-targeting compound RPS-070. Both constructs rapidly radiolabeled 225Ac in just minutes at RT, and macropa-Tmab retained >99 % of its 225Ac in human serum after 7 days. In LNCaP xenograft mice, 225Ac-macropa-RPS-070 was selectively targeted to tumors and did not release free 225Ac over 96 h. These findings establish macropa to be a highly promising ligand for 225Ac chelation that will facilitate the clinical development of 225Ac TAT for the treatment of soft-tissue metastases.
MACROCYCLIC COMPLEXES OF ALPHA-EMITTING RADIONUCLIDES AND THEIR USE IN TARGETED RADIOTHERAPY OF CANCER
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Paragraph 0286-0287, (2020/06/08)
The present technology provides compounds as well as compositions including such compounds useful in targeted radiotherapy of cancer and/or mammalian tissue overexpressing prostate specific membrane antigen (“PSMA”) where the compounds are represented by
Modified hydrophobic auxiliary material as well as preparation method and application thereof
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Paragraph 0073; 0077; 0081; 0087, (2020/12/31)
The invention relates to preparation of novel pharmaceutic auxiliary materials and drug-loaded fat emulsions, and provides a hydrophobic auxiliary material, the molecular formula of which is as follows: R is a hydrophobic natural compound or synthetic compound with one to three hydroxyl groups (n= 1-3); R1 is an alpha-amino protecting group, R2 is an amino acid side chain, m is equal to 0, and atthe moment, R reacts with the amino acid derivative with the protecting group through esterification to form a hydrophobic auxiliary material carrying the amino acid derivative with the protecting group; or m is equal to 1, at the moment, an amino acid connecting arm (l being equal to 1, 2, 4, and 6) with different chain lengths is introduced into R through an ester group, then an amino acid derivative with a protective group is introduced, and the hydrophobic auxiliary material carrying the amino acid derivative polypeptide with the protective group is formed. According to the method, the amino acid derivative with the aromatic or alkoxycarbonyl or acyl amino protecting group is introduced to the hydrophobic auxiliary material, so that the solubility of the drug in the hydrophobic auxiliary material is increased, and the stability of the drug-loaded fat emulsion is improved.