Efficacy and safety of 188Re-HEDP in lung cancer patients with bone metastases: a randomized, multicenter, multiple-dose phase IIa study

Chen, Ping; Li, Jun; Gui, Jicong; Liu, Congjin; Wang, Yuan-Kai; Zhang, Guangming; Dayu, Kuai; Wu, Yiwei; Liu, Zengli; Zuo, Changjing; Lv, Zhongwei; ZhangLi, Yingjian Biao; Liu, Xingdang

doi:10.1007/s10147-021-01906-y

Cited by 5 publications

(5 citation statements)

References 20 publications

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“…On the other hand, this short half-life requires rapid targeting and treatment protocols. 188 Re has been used in many clinical trials to label various compounds such as liposomes or hydroxyethylidine diphosphonate [50,51].…”

Section: Commonly Used Radioactive Isotopes In Radioimmunotherapymentioning

confidence: 99%

Radioimmunotheragnosis in Cancer Research

Garaulet,

Baez,

Medrano

et al. 2024

Preprint

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The combination of immunoPET—where an antibody (Ab) is labeled with an isotope for PET imaging—and radioimmunotherapy (RIT), using the same antibody with a therapeutic isotope, offers significant advantages in cancer management. ImmunoPET allows non-invasive imaging of antigen expression, which aids in patient selection for a subsequent radioimmunotherapy. It also facilitates the assessment of tumor response to therapy, allowing for treatment adjustments if necessary. In addition, immunoPET provides critical pharmacokinetic data, including antibody biodistribution and clearance rates, which are essential for dosimetry calculations and treatment protocol optimization. There are still challenges to overcome. Identifying appropriate target antigens that are selectively expressed on cancer cells while minimally expressed on normal tissues remains a major hurdle to reduce off-target toxicity. In addition, it is critical to optimize the pharmacokinetics of radio-labeled antibodies to maximize tumor uptake and minimize normal tissue uptake, particularly in vital organs such as the liver and kidney. This approach offers the potential for targeted and personalized cancer therapy with reduced systemic toxicity by exploiting the specificity of monoclonal antibodies and the cytotoxic effects of radiation. However, further research is needed to address remaining challenges and to optimize these technologies for clinical use.

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Section: Commonly Used Radioactive Isotopes In Radioimmunotherapymentioning

confidence: 99%

Radioimmunotheragnosis in Cancer Research

Garaulet,

Baez,

Medrano

et al. 2024

Preprint

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“…In addition to the mentioned therapeutic strategies, there are interesting works focusing on pain alleviation. Recently, Chen et al [65] published the results of effectiveness in pain alleviation and improvement of global quality of life in 54 LC patients with painful bone metastases using [ 188 Re]Re-hydroxyethylidine diphosphonate. According to the authors' results, the radiopharmaceutical was safe and well tolerated at doses of 40-50 MBq/kg.…”

Section: Therapy For Lung Cancermentioning

confidence: 99%

Diagnosis and treatment of lung cancer using nuclear medicine techniques — current state of the art

et al. 2023

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Lung cancer is the leading cause of cancer-related death worldwide. Planar radiography and computed tomography are the most common imaging modalities used in diagnosis, staging, and therapy response assessment. However, the role of nuclear methods in assessing the severity of the disease and the effectiveness of treatment has increased in recent years. Introducing these diagnostic modalities into standard practice in lung cancer may contribute to the personalization of treatment. In this review, we summarize the current knowledge of nuclear medicine techniques in the diagnosis and treatment of lung cancer.

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“…In this context, the most appropriate molecules for bone matrix targeting tend to be bisphosphonates; as a matter of fact, the simplest 99m Tc-labeled derivatives of this chemical family, i.e., medronate and oxidronate, have been extensively used as bone single-photon emission computed tomography (SPECT) imaging agents for over 40 years [8]. Therapeutic counterparts to these SPECT tracers have been designed and studied in humans, such as [ 188 Re]Re-etidronate, which showed some potential in terms of efficacy [9][10][11][12][13][14][15][16][17][18][19][20][21] and improvement of patients' quality of life [22]. However, 2 of 26 rhenium's complex redox chemistry hampered the expansion of this therapeutic option, as it is challenging to implement in a conventional radiopharmaceutical environment [23].…”

Section: Introductionmentioning

confidence: 99%

“…imaging agents for over 40 years [8]. Therapeutic counterparts to these SPECT tracers have been designed and studied in humans, such as [ 188 Re]Re-etidronate, which showed some potential in terms of efficacy [9][10][11][12][13][14][15][16][17][18][19][20][21] and improvement of patients' quality of life [22]. However, rhenium's complex redox chemistry hampered the expansion of this therapeutic option, as it is challenging to implement in a conventional radiopharmaceutical environment [23].…”

Section: Introductionmentioning

confidence: 99%

“…Concerning therapy, a bisphosphonate-related derivative with an ethylenediamine tetraphosphonate structure (EDTMP, also named lexidronam) radiolabeled with 153 Sm (t 1/2 = 1.9 days; E β-max = 0.81 MeV) has also been used since the late 1980s [120,121] for the relief of pain resulting from bone metastases; two clinical trials demonstrated its efficacy in this indication versus the placebo and its improved toxicity profile compared to 89 Sr and 32 P [122,123]. Notably, etidronate was also selected for radionuclide therapy applications after radiolabeling with beta minus-emitting rhenium isotopes, either 186 Re or 188 Re [9][10][11][12][13][14][15][16][17][18][19][20][21], but with rather limited clinical use.…”

mentioning

confidence: 99%

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Bisphosphonates as Radiopharmaceuticals: Spotlight on the Development and Clinical Use of DOTAZOL in Diagnostics and Palliative Radionuclide Therapy

Souche,

Fouillet,

Rubira

et al. 2023

IJMS

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Bisphosphonates are therapeutic agents that have been used for almost five decades in the treatment of various bone diseases, such as osteoporosis, Paget disease and prevention of osseous complications in cancer patients. In nuclear medicine, simple bisphosphonates such as 99mTc-radiolabelled oxidronate and medronate remain first-line bone scintigraphic imaging agents for both oncology and non-oncology indications. In line with the growing interest in theranostic molecules, bifunctional bisphosphonates bearing a chelating moiety capable of complexing a variety of radiometals were designed. Among them, DOTA-conjugated zoledronate (DOTAZOL) emerged as an ideal derivative for both PET imaging (when radiolabeled with 68Ga) and management of bone metastases from various types of cancer (when radiolabeled with 177Lu). In this context, this report provides an overview of the main medicinal chemistry aspects concerning bisphosphonates, discussing their roles in molecular oncology imaging and targeted radionuclide therapy with a particular focus on bifunctional bisphosphonates. Particular attention is also paid to the development of DOTAZOL, with emphasis on the radiochemistry and quality control aspects of its preparation, before outlining the preclinical and clinical data obtained so far with this radiopharmaceutical candidate.

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Efficacy and safety of 188Re-HEDP in lung cancer patients with bone metastases: a randomized, multicenter, multiple-dose phase IIa study

Cited by 5 publications

References 20 publications

Radioimmunotheragnosis in Cancer Research

Radioimmunotheragnosis in Cancer Research

Diagnosis and treatment of lung cancer using nuclear medicine techniques — current state of the art

Bisphosphonates as Radiopharmaceuticals: Spotlight on the Development and Clinical Use of DOTAZOL in Diagnostics and Palliative Radionuclide Therapy

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