In vitro and in vivo studies on the development of the α-emitting radionuclide bismuth 212 for intraperitoneal use against microscopic ovarian carcinoma

Rotmensch, Jacob; Whitlock, Jenny L.; Schwartz, Jeffrey L.; Hines, John J.; Reba, Richard C.; Harper, Paul V.

doi:10.1016/s0002-9378(97)70608-2

Cited by 18 publications

(17 citation statements)

References 7 publications

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“…A concerted effort to identify more stable chelates identified the CHXA-DTPA ( trans -cyclohexyldiethylenetriaminepentaacetic acid) chelate as the most stable antibody–radiometal conjugate in vivo (51, 52). This chelate conjugation method has been used in several preclinical studies focused primarily on targeting leukemia (53, 54), ovarian cancer (55), and bone metastases (56)—scenarios in which targeting is rapid and compatible with the short, 1-h half-life of 212 Bi. Human studies using 212 Bi-conjugated agents have not been performed.…”

Section: Brief Review Of the Physics Radiobiology And Dosimetry mentioning

confidence: 99%

Targeted and Nontargeted α-Particle Therapies

McDevitt

Sgouros

Sofou

2018

Annu. Rev. Biomed. Eng.

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α-Particle irradiation of cancerous tissue is increasingly recognized as a potent therapeutic option. We briefly review the physics, radiobiology, and dosimetry of α-particle emitters, as well as the distinguishing features that make them unique for radiopharmaceutical therapy. We also review the emerging clinical role of α-particle therapy in managing cancer and recent studies on in vitro and preclinical α-particle therapy delivered by antibodies, other small molecules, and nanometer-sized particles. In addition to their unique radiopharmaceutical characteristics, the increased availability and improved radiochemistry of α-particle radionuclides have contributed to the growing recent interest in α-particle radiotherapy. Targeted therapy strategies have presented novel possibilities for the use of α-particles in the treatment of cancer. Clinical experience has already demonstrated the safe and effective use of α-particle emitters as potent tumor-selective drugs for the treatment of leukemia and metastatic disease.

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Section: Brief Review Of the Physics Radiobiology And Dosimetry mentioning

confidence: 99%

Targeted and Nontargeted α-Particle Therapies

McDevitt

Sgouros

Sofou

2018

Annu. Rev. Biomed. Eng.

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“…[133][134][135] Bi was compared with 32 P, 250 keV X-ray, and cisplatinum, RBE's of 2-8 were reported for survival of human ovarian cancer cells, either in single cell suspensions or with cells grown as 0.1-and 0.8-mm spheroids. Autoradiography demonstrated that radioactivity was distributed throughout the crosssection of the spheroid.…”

Section: Nontargeted Radiotherapy With 212 Bimentioning

confidence: 99%

The Development of the α-Particle Emitting Radionuclides ²¹²Bi and ²¹³Bi, and Their Decay Chain Related Radionuclides, for Therapeutic Applications

2001

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“…Other considerations in selecting an appropriate α-emitter include physical half life of the radionuclide, which ideally should match the biological half life of the radiotracer or its catabolites, ease of chemical synthesis and availability at a reasonable cost. Bismuth-212 [7], 213 Bi [8], 223 Ra [9], 225 Ac [10, 11], and 211 At [12] are some of the most commonly investigated α-particle emitting radionuclides. A strong case can be made that 211 At is the most promising among these for the α-particle therapy.…”

Section: Introductionmentioning

confidence: 99%

Astatine Radiopharmaceuticals: Prospects and Problems

Vaidyanathan¹,

Zalutsky²

2008

CRP

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For the treatment of minimum residual diseases such micrometastases and residual tumor margins that remain after debulking of the primary tumor, targeted radiotherapy using radiopharmaceuticals tagged with α-particle-emitting radionuclides is very attractive. In addition to the their short range in tissue, which helps minimize harmful effects on adjacent normal tissues, α-particles, being high LET radiation, have several radiobiological advantages. The heavy halogen, astatine-211 is one of the prominent α-particle-emitting radionuclides in practice. Being a halogen, it can often be incorporated into biomolecules of interest by adapting radioiodination chemistry. A wide spectrum of compounds from the simple [ 211 At]astatide ion to small organic molecules, peptides, and large proteins labeled with 211 At have been investigated with at least two reaching the stage of clinical evaluation. The chemistry, cytotoxic advantages, biodistribution studies, and microdosimetry/ pharmacokinetic modeling of some of these agents will be reviewed. In addition, potential problems such as the harmful effect of radiolysis on the synthesis, lack of sufficient in vivo stability of astatinated compounds, and possible adverse effects when they are systemically administered will be discussed.

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In vitro and in vivo studies on the development of the α-emitting radionuclide bismuth 212 for intraperitoneal use against microscopic ovarian carcinoma

Cited by 18 publications

References 7 publications

Targeted and Nontargeted α-Particle Therapies

Targeted and Nontargeted α-Particle Therapies

The Development of the α-Particle Emitting Radionuclides ²¹²Bi and ²¹³Bi, and Their Decay Chain Related Radionuclides, for Therapeutic Applications

Astatine Radiopharmaceuticals: Prospects and Problems

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In vitro and in vivo studies on the development of the α-emitting radionuclide bismuth 212 for intraperitoneal use against microscopic ovarian carcinoma

Cited by 18 publications

References 7 publications

Targeted and Nontargeted α-Particle Therapies

Targeted and Nontargeted α-Particle Therapies

The Development of the α-Particle Emitting Radionuclides 212Bi and 213Bi, and Their Decay Chain Related Radionuclides, for Therapeutic Applications

Astatine Radiopharmaceuticals: Prospects and Problems

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Product

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The Development of the α-Particle Emitting Radionuclides ²¹²Bi and ²¹³Bi, and Their Decay Chain Related Radionuclides, for Therapeutic Applications