HEINSWORD
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TARGETED RADIONUCLIDE THERAPY
– NEW HORIZONS FOR SYSTEMIC CANCER THERAPY
Radionuclide Therapy Experience
- Radionuclide Therapy has been widely used in nuclear medicine worldwide ever since the middle of the previous century. Before the 21st century, it was used mainly for thyroid disorders treatment – thyrotoxicosis and cancer.
- Radionuclide Therapy has also been long used for treatment of bone metastases based on the uptake of calcium or phosphorus compounds by osteoblasts. Aiming at target cells with diagnostically proved high uptake of specific agents.
- Radionuclide Therapy represents a unique and systemic treatment method. Radionuclide Therapy can be effectively combined with other treatment methods – surgery, radiotherapy, chemotherapy and etc. as it significantly improves overall efficiency of therapy without increasing its toxicity. Used for more than 75 years, Radionuclide Therapy, in particular Radioiodine Therapy, has not only confirmed its efficiency and safety but has been significantly improved, both generally and specifically. This is what predetermined its tremendous development in this era of personalized medicine.
Theranostics – New Development Direction for Nuclear Medicine
- In the 21th century, the development of nuclear medicine and radiopharmacy has given rise to new means for targeted delivery of radioactive isotopes to target cells which are mostly tumor cells.
- The most rapidly developed approach called THERANOSTICS represents the independent succession between THERApy and diagNOSTICS as the main paradigm of modern personalized medicine.
- This succession is expressed by firstly using molecular imaging (PET/CT) to detect the accumulation of target molecule (ligand) in tumor cells, labeled with a diagnostic radioisotope which acts as a ‘spy’. If the ligand is found to be highly accumulated, Radioligand Therapy is to be used, and diagnostic radioisotope is replaced by therapeutic activity (charge) to completely impact all the tumor cells.
- To make Radionuclide Therapy more efficient and safer, personal dosimetry is used (SPECT/CT) which is to be performed at the diagnostic stage and monitored at the stage of treatment. This comprises the theranostic approach in modern nuclear medicine, based on the use of theranostic pair – diagnostic and complementary therapeutic radiopharmaceutical.
- More than 300 different theranostic pairs for cancer treatment are currently under various phases of clinical trials. The vast evidence-based experience helped to define indications and contraindications (inclusion and exclusion criteria) for the use of Radionuclide Therapy.
Peptide Receptor Radionuclide Therapy for Neuroendocrine Tumors
- The first Targeted Radionuclide Therapy to be developed was Peptide Receptor Radionuclide Therapy (PRRT) with 177Lu (Lutetium-177)-DOTA (LutatheraTM).
- Its efficiency and safety for treatment of neuroendocrine tumors of gastrointestinal tract was confirmed in 2017 and it was approved by FDA after completion of three phases of clinical trials. In Phase III of the clinical trials (NETTER-1), the efficiency of treatment with 177Lu-DOTA was compared not to a placebo but to the best of the known options of systemic therapy (analogs of Somatostatin with prolonged action), which truly demonstrated a higher survival in patients, both relapse-free and overall survival, without an increase in toxicity.
- All foreign clinical guidelines recommend PRRT for a wide clinical use. Clinical trials of 177Lu-DOTA-TOC and a number of other therapeutic radiopharmaceuticals are currently under way. Their theranostic pairs are the same ligands labeled with 68Ga (Gallium-68): 68Ga-DOTA-TATE, 68Ga-DOTA-TOC and etc.
- For diagnosis of neuroendocrine tumors, staging and patient recruitment for PRRT, SPECT/CT with Tectrotide can be used, for example, which is more accessible and less expensive than PET/CT with 68Ga-DOTA-TOC.
Radioligand Therapy for Prostate Cancer
- The membranes of prostate cancer cells often have prostate-specific antigen receptors (PSMA). The more aggressive the carcinoma, the higher the concentration of PSMA receptors to PSMA of its cells.
- This is determined by using PET/CT molecular imaging (diagnosis, tumor stage) with PSMA-receptor ligands labeled with 68Ga or 18F. PET/CT with68Ga-PSMA-11 demonstrates the highest accuracy (sensitivity and specificity).
- Apart from this, it is a theranostic pair for 177Lu-PSMA-617 (PluvictoTM), which is approved by FDA upon completion of Phase III of clinical trials (VISION) in 2022 and is currently recommended worldwide for systemic radioligand therapy in patients with prostate cancer.
- Other Lu-177- and Ac-225-based radioligand therapy options are currently under clinical trials, for example, 177Lu-PSMA-I&T and 225Ac-PSMA-617, which broaden the range of efficient treatment options.
STABLE ISOTOPES SUPPLY
Heinsword is a provider of stable enriched isotopes for the worldwide markets.
Stable isotopes are non-radioactive chemical isotopes. Of the 118 elements currently known, 80 have one or more stable isotopes.
We are able to provide the following stable isotopes and custom-made products based upon request:
Ca
Calcium
Ca
Calcium
Cu
Copper
Cu
Copper
Ga
Gallium
Ga
Gallium
Gd
Gadolinium
Gd
Gadolinium
Lu
Lutetium
Lu
Lutetium
Ni
Nickel
Ni
Nickel
Rb
Rubidium
Rb
Rubidium
Yb
Ytterbium
Yb
Ytterbium
Zn
Zinc
Zn
Zinc
Element
Calcium
Isotope
40 Ca
42 Ca
43 Ca
44 Ca
46 Ca
48 Ca
42 Ca
43 Ca
44 Ca
46 Ca
48 Ca
Natural abundance atom (%)
96,941
0,647
0,135
2,086
0,004
0,187
0,647
0,135
2,086
0,004
0,187
Enrichment atom (%)
99,92 ÷ 99,98
92,45 ÷ 97,80
72,54 ÷ 90,00
98,66 ÷ 99,04
10,60 ÷ 25,60
91,58 ÷ 98,00
92,45 ÷ 97,80
72,54 ÷ 90,00
98,66 ÷ 99,04
10,60 ÷ 25,60
91,58 ÷ 98,00
Chemical purity (%)
> 99,96
Chemical form
carbonate, oxide
Element
Copper
Isotope
63 Cu
65 Cu
65 Cu
Natural abundance atom (%)
69,17
30,83
30,83
Enrichment atom (%)
99,70 ÷ 99,80
99,50 ÷ 99,70
99,50 ÷ 99,70
Chemical purity (%)
> 99,98
Chemical form
metal, oxide, chloride, sulphate
Element
Gallium
Isotope
69 Ga
71 Ga
71 Ga
Natural abundance atom (%)
60,108
39,892
39,892
Enrichment atom (%)
99,80 ÷ 99,90
99,80 ÷ 99,90
99,80 ÷ 99,90
Chemical purity (%)
> 99,7
Chemical form
metal, oxide
Element
Gadolinium
Isotope
152 Gd
154 Gd
155 Gd
156 Gd
157 Gd
158 Gd
160 Gd
154 Gd
155 Gd
156 Gd
157 Gd
158 Gd
160 Gd
Natural abundance atom (%)
0,20
2,18
14,80
20,47
15,65
24,84
21,86
2,18
14,80
20,47
15,65
24,84
21,86
Enrichment atom (%)
34,20 ÷ 34,80
61,00 ÷ 64,20
90,80 ÷ 92,80
93,10 ÷ 96,00
87,30 ÷ 90,90
97,20 ÷ 97,60
98,10 ÷ 98,40
61,00 ÷ 64,20
90,80 ÷ 92,80
93,10 ÷ 96,00
87,30 ÷ 90,90
97,20 ÷ 97,60
98,10 ÷ 98,40
Chemical purity (%)
> 99,50
Chemical form
oxide
Gado-linium
Element
Lutetium
Isotope
175 Lu
176 Lu
176 Lu
Natural abundance atom (%)
97,41
2,59
2,59
Enrichment atom (%)
99,80 ÷ 99,88
74,00 ÷ 88,40
74,00 ÷ 88,40
Chemical purity (%)
> 99,90
Chemical form
oxide
Element
Nickel
Isotope
58 Ni
60 Ni
61 Ni
62 Ni
64 Ni
60 Ni
61 Ni
62 Ni
64 Ni
Natural abundance atom (%)
68,08
26,21
1,14
3,64
0,93
26,21
1,14
3,64
0,93
Enrichment atom (%)
99,84 ÷ 99,87
99,50 ÷ 99,65
88,60 ÷ 92,40
98,60 ÷ 98,80
94,20 ÷ 96,10
99,50 ÷ 99,65
88,60 ÷ 92,40
98,60 ÷ 98,80
94,20 ÷ 96,10
Chemical purity (%)
> 99,95
Chemical form
metal, oxide
Element
Rubidium
Isotope
85 Rb
87 Rb
87 Rb
Natural abundance atom (%)
72,17
27,83
27,83
Enrichment atom (%)
99,40 ÷ 99,84
98,60 ÷ 99,00
98,60 ÷ 99,00
Chemical purity (%)
> 99,87
Chemical form
chloride, metal, carbonate, bichromate
Element
Ytterbium
Isotope
168 Yb
170 Yb
171 Yb
172 Yb
173 Yb
174 Yb
176 Yb
170 Yb
171 Yb
172 Yb
173 Yb
174 Yb
176 Yb
Natural abundance atom (%)
0,13
3,04
14,28
21,83
16,13
31,83
12,76
3,04
14,28
21,83
16,13
31,83
12,76
Enrichment atom (%)
21,00 ÷ 42,00
70,10 ÷ 83,20
90,20 ÷ 95,60
92,60 ÷ 97,10
85,80 ÷ 92,70
97,80 ÷ 99,30
95,30 ÷ 99,80
70,10 ÷ 83,20
90,20 ÷ 95,60
92,60 ÷ 97,10
85,80 ÷ 92,70
97,80 ÷ 99,30
95,30 ÷ 99,80
Chemical purity (%)
> 99,98
Chemical form
oxide
Element
Zinc
Isotope
64 Zn
66 Zn
67 Zn
68 Zn
70 Zn
66 Zn
67 Zn
68 Zn
70 Zn
Natural abundance atom (%)
48,63
27,90
4,10
18,75
0,62
27,90
4,10
18,75
0,62
Enrichment atom (%)
99,10 ÷ 99,40
98,40 ÷ 98,90
89,60 ÷ 94,20
98,40 ÷ 99,00
70,70 ÷ 74,40
98,40 ÷ 98,90
89,60 ÷ 94,20
98,40 ÷ 99,00
70,70 ÷ 74,40
Chemical purity (%)
> 99,96
Chemical form
oxide, metal, sulphate
RADIOCHEMISTRY CONSULTING
Chemistry of radioactive elements: radium, actinium, thorium, uranium, neptunium, plutonium, americium, curium, cesium, strontium, rare-earth metals and etc;
Heinsword provides basic and applied radiochemistry consulting in the following areas:
Methods for recovery of radioactive elements from natural sources and irradiated nuclear fuel reprocessing products;
State of radioactive elements in aqueous solutions, natural waters and liquid radioactive waste;
Distribution of radioactive elements between different phases during precipitation, sorption and extraction.
