Novel Chlorin with a HYNIC: Synthesis, 99mTc-Radiolabeling, and Initial Preclinical Evaluation

Mikhail A. Grin, Nikita Suvorov, Alexander Popov, M. S. Larkina, Evgenii Plotnikov, Ruslan Varvashenya, Vitalina Bodenko, Gleb Yanovich, Petr Ostroverkhov, Maxim Usachev, Е. В. Филоненко, М. В. Белоусов
2024-12-31

6-hydrazinylnicotinic acid (HYNIC)99mTc-radiolabelingchlorin-HYNIC conjugatepreclinical evaluationtetrapyrrole macrocycles
The use of radiopharmaceuticals for diagnostics in oncology allows for the detection of the disease at an early stage. Among diagnostic radionuclides, 99mTc is a promising isotope that has been used to create several drugs for clinical use. One of the most effective 99mTc chelators is 6-hydrazinylnicotinic acid (HYNIC), which, when combined with various vector molecules, can be used for targeted delivery of radionuclides to tumor tissues. At the same time, it is known that tetrapyrrole macrocycles are capable of selective accumulation in tumors, and thus can be used to target radiopharmaceuticals with 99mTc. In this work, the conjugate of natural chlorin and HYNIC was obtained, and preliminary preclinical studies were carried out on its radiocomplex with 99mTc.
1
A novel conjugate of natural chlorin and the 99mTc chelator HYNIC was synthesized.
2
Preliminary preclinical studies were performed on the 99mTc-chlorin-HYNIC radiocomplex to evaluate its potential for tumor-targeted diagnostics.
3
The approach leverages tetrapyrrole macrocycles' known selective tumor accumulation combined with HYNIC-mediated 99mTc delivery for targeted radiopharmaceutical development.
4
The chlorin-HYNIC conjugate was successfully radiolabeled with the diagnostic radionuclide 99mTc to form a radiocomplex.

Conjugate of natural chlorin and 6-hydrazinylnicotinic acid (HYNIC) and its 99mTc radiocomplex

Synthesis, 99mTc radiolabeling, and initial preclinical evaluation (biodistribution/targeting to tumor tissues) of the chlorin–HYNIC conjugate radiocomplex

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2024-12-31
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Authors
Mikhail A. Grin
Nikita Suvorov
Alexander Popov
M. S. Larkina
Evgenii Plotnikov
Ruslan Varvashenya
Vitalina Bodenko
Gleb Yanovich
Petr Ostroverkhov
Maxim Usachev
Е. В. Филоненко
М. В. Белоусов
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