213Bi production and complexation with new picolinate containing ligands

Sinenko, Irina; Калмыкова, Т. П.; Likhosherstova, Daria V.; Egorova, Bayirta V.; Zubenko, Anastasia D.; Vasiliev, A. N.; Ermolaev, S. V.; Lapshina, E.V.; Ostapenko, V.S.; Федорова, О. А.; Kalmykov, Stepan N.

doi:10.1007/s10967-019-06610-w

Cited by 17 publications

(23 citation statements)

References 38 publications

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“…[5] Previously, we have developed rigid pyridine-bisamide azacrown ethers of varied size and pendant groups, and studied their copper(II) complexation properties. [13][14][15][16] We found that they readily form thermodynamically stable complexes. Structural factors, such as ligand rigidity, cavity size, soft and hard nature, and the number of donor atoms, have been shown to play an important role in the binding features of ligands towards metal cations.…”

Section: Introductionmentioning

confidence: 89%

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Comparative Study of Macrocyclic and Acyclic Picolinate Derivatives for Chelation of Copper Cations

et al. 2021

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In this work we presented a synthesis and investigation of relative acyclic and macrocyclic polyamines with picolinate pendant arms as potential chelators for copper radiopharmaceuticals. It has been shown that linear chelators lacking bisamide moiety are much more basic and form complexes with higher stability constants compared to macrocyclic ones. Both types of ligands possess many donor sites due to picolinate groups enabling formation of polynuclear complexes in the solution and solid state. According to crystal structures metal cations coordinates with studied ligands through the binding with aminogroups and picolinates donor atoms, while terminal aminogroups of acyclic ligands do not take part in the complex formation. Tripicolinate azacrown ligand coordinates cations outside the macrocyclic cavity in non-equivalent positions. However this out-cage location as well as a moderate logK value do not induce fast release of cation from this complex in the challenging medium of serum proteins.

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Section: Introductionmentioning

confidence: 89%

“…This is in line with earlier published data for Bismuth complexes of L2 and L4 only 1 : 1 stoichiometry was detected. [15] The presence of many strong basic sites in L1-L4 defines the binding of cations even by protonated forms of ligands.…”

Section: Complexationmentioning

confidence: 99%

Comparative Study of Macrocyclic and Acyclic Picolinate Derivatives for Chelation of Copper Cations

et al. 2021

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“…225 Ac can be loaded on 225 Ac/ 213 Bi generators to deliver 213 Bi on site, but it can also be used directly as a therapeutic radionuclide. 225 Ac/ 213 Bi generators are well explored and discussed [37][38][39]. The most established strategy is based on the direct generator method in which the parent 225 Ac in acidic solution (e.g.…”

Section: Ac/ 213 Bi Radionuclide Generatorsmentioning

confidence: 99%

Bismuth-213 for Targeted Radionuclide Therapy: From Atom to Bedside

Ahenkorah¹,

Cassells²,

Deroose³

et al. 2021

Preprint

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Besides external high-energy photon or proton beam therapy, targeted radionuclide therapy (TRNT) is an alternative approach to deliver radiation to cancer cells. TRNT is distributed within the body by the vascular system and allows targeted irradiation of a primary tumor and all its metastases, resulting in substantially less collateral damage to normal tissues as compared to ex-ternal beam radiotherapy (EBRT). It is a systemic cancer therapy, tackling systemic spread of the disease, which is the cause of death in most cancer patients. The α-emitting radionuclide bis-muth-213 (213Bi) has interesting properties and can be considered as a magic bullet for TRNT. The benefits and drawbacks of targeted alpha therapy with 213Bi are discussed in this review, covering the entire chain from radionuclide production to bedside. First, the radionuclide properties and production of 225Ac and its daughter 213Bi are discussed, followed by the fundamental chemical properties of bismuth. Next, an overview of available acyclic and macrocyclic bifunctional chelators for bismuth, and general considerations for designing a 213Bi-radiopharmaceutical are provided. Finally, we will provide an overview of preclinical and clinical studies involving 213Bi-radiopharmaceuticals, as well as the future perspectives of this promising cancer treatment option.

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“…225 Ac can be loaded on 225 Ac/ 213 Bi generators to deliver 213 Bi on site, but it can also be used directly as a therapeutic radionuclide. 225 Ac/ 213 Bi generators are well explored and discussed [ 29 , 30 , 31 ]. The most established strategy is based on the direct generator method, in which the parent 225 Ac in acidic solution (e.g., 0.05M HNO 3 ) is strongly retained by the sorbent (e.g., AG MP-50 cation exchange resin) and 213 Bi is eluted.…”

Section: Radionuclide Properties and Production Of 225 Ac And Its Daughter 213 Bimentioning

confidence: 99%

Bismuth-213 for Targeted Radionuclide Therapy: From Atom to Bedside

et al. 2021

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In contrast to external high energy photon or proton therapy, targeted radionuclide therapy (TRNT) is a systemic cancer treatment allowing targeted irradiation of a primary tumor and all its metastases, resulting in less collateral damage to normal tissues. The α-emitting radionuclide bismuth-213 (213Bi) has interesting properties and can be considered as a magic bullet for TRNT. The benefits and drawbacks of targeted alpha therapy with 213Bi are discussed in this review, covering the entire chain from radionuclide production to bedside. First, the radionuclide properties and production of 225Ac and its daughter 213Bi are discussed, followed by the fundamental chemical properties of bismuth. Next, an overview of available acyclic and macrocyclic bifunctional chelators for bismuth and general considerations for designing a 213Bi-radiopharmaceutical are provided. Finally, we provide an overview of preclinical and clinical studies involving 213Bi-radiopharmaceuticals, as well as the future perspectives of this promising cancer treatment option.

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213Bi production and complexation with new picolinate containing ligands

Cited by 17 publications

References 38 publications

Comparative Study of Macrocyclic and Acyclic Picolinate Derivatives for Chelation of Copper Cations

Comparative Study of Macrocyclic and Acyclic Picolinate Derivatives for Chelation of Copper Cations

Bismuth-213 for Targeted Radionuclide Therapy: From Atom to Bedside

Bismuth-213 for Targeted Radionuclide Therapy: From Atom to Bedside

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