Search results for "177Lu"
showing 8 items of 8 documents
Bone targeting compounds for radiotherapy and imaging: *Me(III)-DOTA conjugates of bisphosphonic acid, pamidronic acid and zoledronic acid
2016
Background Bisphosphonates have a high adsorption on calcified tissues and are commonly used in the treatment of bone disorder diseases. Conjugates of bisphosphonates with macrocyclic chelators open new possibilities in bone targeted radionuclide imaging and therapy. Subsequent to positron emission tomography (PET) examinations utilizing 68Ga-labelled analogues, endoradiotheraphy with 177Lu-labelled macrocyclic bisphosphonates may have a great potential in the treatment of painful skeletal metastases. Methods Based on the established pharmaceuticals pamidronate and zoledronate two new DOTA-α-OH-bisphosphonates, DOTAPAM and DOTAZOL(MM1.MZ) were successfully synthesized. The ligands were labe…
Sterilu jaunu radioaktīvu peptīdu sintēze un to pretvēža aktivitāte in vitro sistēmās
2020
NET audzēji ir visbiežāk diagnosticētā onkoloģiskā saslimšana no visiem vēža veidiem. Krūts vēzis, kas pieskaitāms NET audzējiem, ir biežākā onkoloģiskā saslimšana sievietēm ar vairākiem simtiem tūkstošu jaunu gadījumu katru gadu. Kopš pagājušā gadsimta beigām klīniskajā praksē tiek izmantota audzēju un to metastāžu diagnostika ar radiofarmaceitiskajiem preparātiem. Pēdējos gados onkoloģijā tiek ieviesta teranostika – diagnostika un terapija ar audzējam specifisku peptīdu, kas piesaistīts pie radionuklīda. Ar HA-DOTA-TATE, kas ir somatostatīna analogs, saistīti radionuklīdi paver iespējas pacientiem pieejamai teranostikai. Taču trūkst pētījumu par HA-DOTA-TATE spēju saistīties pie SSTR. Tāp…
Amide-to-triazole switch vs. in vivo NEP-inhibition approaches to promote radiopeptide targeting of GRPR-positive tumors
2017
Abstract Introduction Radiolabeled bombesin (BBN)-analogs have been proposed for diagnosis and therapy of gastrin-releasing peptide receptor (GRPR)-expressing tumors, such as prostate, breast and lung cancer. Metabolic stability represents a crucial factor for the success of this approach by ensuring sufficient delivery of circulating radioligand to tumor sites. The amide-to-triazole switch on the backbone of DOTA-PEG 4 -[Nle 14 ]BBN(7–14) ( 1 ) was reported to improve the in vitro stability of resulting 177 Lu-radioligands. On the other hand, in-situ inhibition of neutral endopeptidase (NEP) by coinjection of phosphoramidon (PA) was shown to significantly improve the in vivo stability and …
In vitro vēža šūnu modeļsistēmas izstrāde molekulāri mērķētu radionuklīdu testēšanai
2019
Prostatas vēzis ir ceturtais biežāk diagnosticētais vēzis Eiropā, 2018. gadā un tas ir kļuvis par visbiežāk sastopamo vēzi vīriešu vidū. Nozīmīgi klīnisko pētījumu rezultāti prostatas vēža diagnostikā un terapijā ir sasniegti ar radioaktīvi iezīmētu PSMA ligandu 68Ga-PSMA – diagnostikai un 177Lu-PSMA – terapijai. Neiroendokrīnie audzēji ir neviendabīga agresīvu audzēju grupa, kam raksturīgi dažādi un bieži nespecifiski simptomi, kas apgrūtina precīzu audzēja primāro diagnostiku un saslimšanas stadijas precizēšanu. Pašlaik šo audzēju diagnostikā un ārstēšanā izmanto ar SSTR2 ligandiem (somatostatīna analogiem) konjugētus radionuklīdus. Šī darba mērķis bija izveidot uz dažādām šūnu līnijām ba…
Biodistribution and post-therapy dosimetric analysis of [177Lu]Lu-DOTAZOL in patients with osteoblastic metastases: first results
2019
Abstract Background Preclinical biodistribution and dosimetric analysis of [177Lu]Lu-DOTAZOL suggest the bisphosphonate zoledronate as a promising new radiopharmaceutical for therapy of bone metastases. We evaluated biodistribution and normal organ absorbed doses resulting from therapeutic doses of [177Lu]Lu-DOTAZOL in patients with metastatic skeletal disease. Method Four patients with metastatic skeletal disease (age range, 64–83 years) secondary to metastatic castration-resistant prostate carcinoma or bronchial carcinoma were treated with a mean dose of 5968 ± 64 MBq (161.3 mCi) of [177Lu]Lu-DOTAZOL. Biodistribution was assessed with serial planar whole body scintigraphy at 20 min and 3,…
Prevention and Management of Hormonal Crisis during Theragnosis with LU-DOTA-TATE in Neuroendocrine Tumors. A Systematic Review and Approach Proposal.
2020
Neuroendocrine tumors (NETs) frequently overexpress somatostatin receptors (SSTR) on their cell surface. The first-line pharmacological treatment for inoperable metastatic functioning well-differentiated NETs are somatostatin analogs. On second line, Lu-DOTA-TATE (177Lu-DOTA0 Tyr 3 octreotate) has shown stabilization of the disease and an increase in progression free survival, as well as effectiveness in controlling symptoms and increasing quality of life. The management of functional NETs before and during LU-DOTA-TATE treatment is specially challenging, as several complications such as severe carcinoid and catecholamine crisis have been described. The aim of this review is to establish pr…
Novel Radiolabeled Bisphosphonates for PET Diagnosis and Endoradiotherapy of Bone Metastases.
2017
Bone metastases, often a consequence of breast, prostate, and lung carcinomas, are characterized by an increased bone turnover, which can be visualized by positron emission tomography (PET), as well as single-photon emission computed tomography (SPECT). Bisphosphonate complexes of 99mTc are predominantly used as SPECT tracers. In contrast to SPECT, PET offers a higher spatial resolution and, owing to the 68Ge/68Ga generator, an analog to the established 99mTc generator exists. Complexation of Ga(III) requires the use of chelators. Therefore, DOTA (1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid), NOTA (1,4,7-triazacyclododecane-1,4,7-triacetic acid), and their derivatives, are ofte…
(177)Lu-labelled macrocyclic bisphosphonates for targeting bone metastasis in cancer treatment.
2015
Background Metastatic bone lesion is a common syndrome of many cancer diseases in an advanced state. The major symptom is severe pain, spinal cord compression, and pathological fracture, associated with an obvious morbidity. Common treatments including systemic application of bisphosphonate drugs aim on pain reduction and on improving the quality of life of the patient. Particularly, patients with multiple metastatic lesions benefit from bone-targeting therapeutic radiopharmaceuticals. Agents utilizing beta-emitting radionuclides in routine clinical praxis are, for example, [89Sr]SrCl2 and [153Sm]Sm-EDTMP. No-carrier-added (n.c.a.) 177Lu is remarkably suitable for an application in this sco…