3-iodobenzylguanidine profile

3-iodobenzylguanidine (MIBG) is a synthetic guanethidine analog that has been studied for its use in treating neuroblastoma, a type of cancer that affects the nervous system. MIBG is an effective radiopharmaceutical agent, meaning it concentrates in tissues and can be visualized with imaging. This is possible due to its ability to target the norepinephrine transporter (NET) in neuroblastoma cells, which results in the compound being accumulated within the tumor. This characteristic allows for the use of MIBG in both diagnostic imaging and therapeutic applications. When labeled with radioactive iodine-131 (I-131), MIBG serves as a therapeutic agent. The therapeutic effects are due to the localized radiation emitted by the I-131 within the tumor cells. In terms of synthesis, MIBG is typically synthesized through a series of reactions involving the coupling of 3-iodobenzyl bromide with guanidine. MIBG is actively studied for its potential in cancer therapy, particularly neuroblastoma, and for its applications in nuclear medicine imaging. The accumulation of MIBG in neuroblastoma cells, its ability to be labeled with radioactive isotopes, and its relatively low toxicity make it a promising tool for both diagnosis and treatment. However, further research is still needed to better understand its mechanisms of action and to optimize its use in clinical settings.'

3-Iodobenzylguanidine: A guanidine analog with specific affinity for tissues of the sympathetic nervous system and related tumors. The radiolabeled forms are used as antineoplastic agents and radioactive imaging agents. (Merck Index, 12th ed) MIBG serves as a neuron-blocking agent which has a strong affinity for, and retention in, the adrenal medulla and also inhibits ADP-ribosyltransferase. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

ID Source	ID
PubMed CID	60860
CHEMBL ID	818
CHEBI ID	92769
SCHEMBL ID	140591
MeSH ID	M0029373
PubMed CID	11957572
CHEMBL ID	1374843
MeSH ID	M0029373

Synonym
BRD-K43860855-065-03-6
BPBIO1_000395
PRESTWICK2_000490
lopac-i-9890
NCGC00015572-02
prestwick-07a11
NCGC00015572-01
2-[(3-iodophenyl)methyl]guanidine
LOPAC0_000644
PRESTWICK3_000490
BSPBIO_000359
m-iodobenzylguanidine
3-iodobenzylguanidine
meta-iodobenzylguanidine
SPBIO_002280
PRESTWICK0_000490
PRESTWICK1_000490
NCGC00162211-01
iobenguane (127-i)
CHEMBL818
iobenguane
80663-95-2
CCG-204731
metaiodobenzylguanidine
guanidine, ((3-iodophenyl)methyl)-
35mrw7b4ad ,
(3-iodobenzyl)guanidine
unii-35mrw7b4ad
NCGC00015572-03
guanidine,n-[(3-iodophenyl)methyl]-
iobenguane [mi]
iobenguane [vandf]
DB06704
((3-iodophenyl)methyl)guanidine
SCHEMBL140591
DTXSID4048438
2-m-iodo-benzyl guanidine
1-(3-iodobenzyl)guanidine
SR-01000075167-1
CHEBI:92769
PDWUPXJEEYOOTR-UHFFFAOYSA-N
meta-iodobenzyl guanidine
Q3154058
SDCCGSBI-0050624.P002
NCGC00015572-09
NCGC00015572-06
2-(3-iodobenzyl)guanidine
STARBLD0001019
SY340573
mfcd00133520
EN300-37158608
n''-[(3-iodophenyl)methyl]guanidine
EU-0100644 ,
m-iodobenzylguanidine hemisulfate salt, >=98% (hplc and tlc)
mibg
m-iodobenzylguanidine hemisulfate
NCGC00094011-01
I 9890
NCGC00015572-04
2-[(3-iodanylphenyl)methyl]guanidine; sulfuric acid
A839961
HMS3262A09
tox21_113518
3-iodobenzyl-guanidine hemisulfate
3-iodobenzyl-guanidine hemisulfate 103346-16-3 80663-96-3
3-iodobenzylguanidine hemisulphate
m-iodobenzylguanidine hemisulfate salt
87862-25-7
3-iodobenzylguanidine hemisulfate
cas-87862-25-7
dtxcid6025773
tox21_111237
dtxsid8045773 ,
AKOS015996512
guanidine, [(3-iodophenyl)methyl]-, sulfate (2:1)
s8i0922465 ,
m-iodobenzyl guanidine sulfate
unii-s8i0922465
guanidine, n-((3-iodophenyl)methyl)-, sulfate (2:1)
m-idobenzyl guanidine sulfate [vandf]
m-iodobenzyl guanidine sulphate
3-iodobenzyl-guanidine sulfate
3-iodobenzyl-guanidine sulphate
iobenguane sulphate
LP00644
CCG-221948
meta-iodobenzylguanidine sulfate
tox21_500644
NCGC00261329-01
CHEMBL1374843
iobenguane sulfate, european pharmacopoeia (ep) reference standard
1-(3-iodobenzyl)guanidine hcl
80663-96-3
E74924
iobenguane (sulfate)
1-(3-iodobenzyl)guanidine hemisulfate
mibg (sulfate)
BS-45793
Q27289056
1-(3-iodobenzyl)guanidinehemisulfate

Excerpt	Reference	Relevance
" This study shows that treatment with 131I-MIBG is safe and can be effective in refractory neuroblastoma, particularly in patients who do not have extensive bone and bone marrow involvement."	( Efficacy and safety of [131I]metaiodobenzylguanidine therapy for patients with refractory neuroblastoma. Ablin, AR; Engelstad, BL; Hasegawa, BH; Hattner, RS; Huberty, JP; Matthay, KK; Price, D; Zoger, S, )	0.13
" The only side effect we witnessed was a reversible bone marrow depression."	( Treatment of neuroblastoma with metaiodobenzylguanidine: results and side effects. Bruchelt, G; Feine, U; Klingebiel, T; Niethammer, D; Treuner, J, 1987)	0.27
" We think that this reversible left ventricular dysfunction was due to the synergistic toxic effect of mildly increased catecholamine and transiently damaged sympathetic nerve endings in the myocardium, presumably due to Guillain-Barré syndrome."	( Reversible left ventricular dysfunction associated with Guillain-Barré syndrome--an expression of catecholamine cardiotoxicity? Gen, H; Himura, Y; Iga, K; Izumi, C; Kijima, K; Konishi, T; Miyamoto, T, 1995)	0.29
" The Auger electron-emitting conjugates ([123I]MIBG and [125I]MIBG) and the alpha-emitting conjugate ([211At]MABG) were highly toxic to monolayers and small spheroids, whereas the beta-emitting conjugate [131I]MIBG was relatively ineffective."	( Toxicity to neuroblastoma cells and spheroids of benzylguanidine conjugated to radionuclides with short-range emissions. Cunningham, SH; Mairs, RJ; Vaidyanathan, G; Welsh, PC; Wheldon, TE; Zalutsky, MR, 1998)	0.3
"1-131 MIBG therapy is a safe and cost-effective therapeutic option to successfully control symptoms in patients with carcinoid syndrome."	( (131)I-MIBG radionuclide therapy is safe and cost-effective in the control of symptoms of the carcinoid syndrome. Byrne, C; Ghaneh, P; Pathirana, AA; Poston, GJ; Vinjamuri, S; Vora, J, 2001)	0.31
" In addition to serious side effects and increased long-lasting morbidity and mortality, dose limitation and suboptimal usage is an important adverse effect."	( Monitoring chemotherapy-induced cardiotoxicity: role of cardiac nuclear imaging. Jain, D; Panjrath, GS, )	0.13
" Patients were followed for adverse events for 2 weeks."	( Radiation dosimetry, pharmacokinetics, and safety of ultratrace Iobenguane I-131 in patients with malignant pheochromocytoma/paraganglioma or metastatic carcinoid. Babich, JW; Barrett, JA; Coleman, RE; de la Guardia, M; Lafrance, N; Stubbs, JB, 2009)	0.35
" I-131-labeled MIBG has been thought to be safe and effective in the evaluation of neuroendocrine tumors, mainly in neuroblastoma and pheochromocytoma."	( Acute intravenous injection toxicity study of MIBG in mice. Chiang, TC; Shen, LH; Yang, AS, 2010)	0.36
" The majority of treatments led to grade 3 or 4 hematologic toxicities (graded according to the National Cancer Institute Common Terminology Criteria for Adverse Events [version 3]) that were similar in frequency among age strata."	( Response, survival, and toxicity after iodine-131-metaiodobenzylguanidine therapy for neuroblastoma in preadolescents, adolescents, and adults. Dubois, SG; Haas-Kogan, D; Hawkins, R; Matthay, KK; Polishchuk, AL, 2011)	0.37
"Targeted radiotherapy with (131) I-Metaiodobenzylguanidine ((131) I-MIBG) is safe and effective therapy for patients with relapsed neuroblastoma, but anti-tumor activity is sometimes transient."	( Safety and efficacy of tandem 131I-metaiodobenzylguanidine infusions in relapsed/refractory neuroblastoma. Baniewicz, D; Johnson, K; Maris, JM; McGlynn, B; Mosse, YP; Saggio, J; Zhuang, H, 2011)	0.37
" We consider (131)I-MIBG therapy to be a safe treatment modality."	( Toxicity of upfront ¹³¹I-metaiodobenzylguanidine (¹³¹I-MIBG) therapy in newly diagnosed neuroblastoma patients: a retrospective analysis. Bleeker, G; Caron, HN; de Kraker, J; Hoefnagel, CA; Schoot, RA; Tytgat, GA; van Eck, BL, 2013)	0.39
"6% (thrombocytopenia) of applied cycles and a suspected late adverse event (3% of patients), myelodysplastic syndrome, after a cumulative administered activity of 66."	( Long-term outcome and toxicity after dose-intensified treatment with 131I-MIBG for advanced metastatic carcinoid tumors. Ahmadzadehfar, H; Alkawaldeh, K; Biersack, HJ; Ezziddin, S; Grünwald, F; Logvinski, T; Sabet, A; Yong-Hing, CJ, 2013)	0.39
"1 GBq (300 mCi) per cycle is safe and offers effective palliation of symptoms and disease stabilization in patients with advanced carcinoid tumors."	( Long-term outcome and toxicity after dose-intensified treatment with 131I-MIBG for advanced metastatic carcinoid tumors. Ahmadzadehfar, H; Alkawaldeh, K; Biersack, HJ; Ezziddin, S; Grünwald, F; Logvinski, T; Sabet, A; Yong-Hing, CJ, 2013)	0.39
" We also evaluated the data for any adverse effects."	( Effects and safety of ¹³¹I-metaiodobenzylguanidine (MIBG) radiotherapy in malignant neuroendocrine tumors: results from a multicenter observational registry. Fukuoka, M; Higuchi, T; Inaki, A; Ito, YM; Jinguji, M; Kayano, D; Kinuya, S; Nakajo, M; Okamoto, S; Oriuchi, N; Shiga, T; Tomiyama, Y; Toratani, A; Wakabayashi, H; Yoshinaga, K, 2014)	0.4
"Image-guided biopsy for relapsed or refractory neuroblastoma was safe and likely to provide NGS data to guide therapy decisions."	( Image-Guided Biopsy for Relapsed Neuroblastoma: Focus on Safety, Adequacy for Genetic Sequencing, and Correlation of Tumor Cell Percent With Quantitative Lesion MIBG Uptake. Acord, M; Alai, E; Cahill, AM; Edgar, JC; Escobar, F; Maris, JM; Mosse, YP; Pawel, B; Pogoriler, J; Samoyedny, A; Shellikeri, S; Srinivasan, A; States, L; Vatsky, S, 2021)	0.62

Excerpt	Reference	Relevance
" In initial experiments we characterized some pharmacokinetic aspects of the disposition of these amines."	( Disposition of radioiodinated benzylguanidines in perfused rabbit lung: pharmacokinetics and effect of an organo-gold complexed antineoplastic agent. Gillis, CN; Lazo, JS; Pitt, BR; Weng, WL, 1990)	0.28
"A pharmacokinetic study was done to elucidate the body distribution, elimination, and metabolism of m-[131I]iodobenzylguanidine (m-[131I]IBG)."	( Stability and pharmacokinetics of m-[131I]iodobenzylguanidine in patients. Ehninger, G; Feine, U; Klingebiel, T; Kumbier, I; Schuler, U; Treuner, J; Waller, HD, 1987)	0.27
" Percent whole-body retention rates of I-MIBG at 24, 48, and 72 hours after administration were 48% ± 7%, 23% ± 7%, and 12% ± 6%, with a whole-body I-MIBG effective half-life of 23 ± 5 hours for all patients."	( Pediatric 131I-MIBG Therapy for Neuroblastoma: Whole-Body 131I-MIBG Clearance, Radiation Doses to Patients, Family Caregivers, Medical Staff, and Radiation Safety Measures. Buchpiguel, CA; Coura-Filho, GB; Crema, KP; Oliveira, NC; Pelissoni, RA; Sapienza, MT; Willegaignon, J, 2018)	0.48

Excerpt	Reference	Relevance
"131I-meta-iodobenzylguanidine treatment combined with hyperbaric oxygen therapy becomes a well-tolerated therapy for high-risk neuroblastoma patients non-responding to the conventional treatment."	( [131I meta-iodobenzylguanidine in combination with hyperbaric oxygen therapy in the treatment of prognostically high-risk forms of neuroblastoma]. Dosel, P; Hermanská, E; Kavan, P; Krízová, H; Sázel, M; Stanková, J, 2001)	0.31
" This study was aimed at assessing the effects of losartan or its combination with quinapril on the cardiac nervous system and neurohormonal status in essential hypertension."	( Effects of losartan and its combination with quinapril on the cardiac sympathetic nervous system and neurohormonal status in essential hypertension. Doi, O; Ishikawa, J; Nawada, R; Obayashi, K; Sakata, K; Tamekiyo, H; Yoshida, H, 2002)	0.31
"Treatment with (131)I-MIBG in combination with myeloablative chemotherapy and hematopoietic stem-cell rescue is feasible with acceptable toxicity."	( Pilot study of iodine-131-metaiodobenzylguanidine in combination with myeloablative chemotherapy and autologous stem-cell support for the treatment of neuroblastoma. Braun, T; Ferrara, JL; Hubers, D; Hutchinson, RJ; Levine, JE; Matthay, KK; Shapiro, B; Shulkin, BL; Sisson, JC; Spalding, S; Yanik, GA, 2002)	0.31
" To enable the evaluation of targeted radiotherapy combined with gene transfer in vivo, we have developed a transfectant mosaic xenograft (TMX) model."	( A transfectant mosaic xenograft model for evaluation of targeted radiotherapy in combination with gene therapy in vivo. Boyd, M; Mairs, RJ; McCluskey, AG; Ross, SC, 2007)	0.34
" We evaluated the toxicity of, and response to, a novel induction regimen that included ¹³¹I-MIBG combined with cisplatin, cyclophosphamide, etoposide, vincristine, and doxorubicin."	( Treatment of advanced neuroblastoma in children over 1 year of age: the critical role of ¹³¹I-metaiodobenzylguanidine combined with chemotherapy in a rapid induction regimen. Di Giannatale, A; Mastrangelo, S; Riccardi, R; Rufini, V; Ruggiero, A, 2011)	0.37
"The results of this pilot study show that ¹³¹I-MIBG, in combination with chemotherapy, appears to play an important role in a new and effective induction regimen for advanced NB."	( Treatment of advanced neuroblastoma in children over 1 year of age: the critical role of ¹³¹I-metaiodobenzylguanidine combined with chemotherapy in a rapid induction regimen. Di Giannatale, A; Mastrangelo, S; Riccardi, R; Rufini, V; Ruggiero, A, 2011)	0.37
" These results suggest that the inhibition of MATEs, but not OCT2, is a likely mechanism underlying the drug-drug interactions with cimetidine in renal elimination."	( Competitive inhibition of the luminal efflux by multidrug and toxin extrusions, but not basolateral uptake by organic cation transporter 2, is the likely mechanism underlying the pharmacokinetic drug-drug interactions caused by cimetidine in the kidney. Inoue, K; Ito, S; Kusuhara, H; Sugiyama, Y; Toyoshima, J; Yokochi, M; Yuasa, H, 2012)	0.38
" Patients with disseminated disease, who also have a few index bulky or symptomatic lesions, may benefit from the addition of targeted external beam radiotherapy alone or in combination with systemic 131I-MIBG."	( External beam radiation therapy (EBRT) for patients with malignant pheochromocytoma and non-head and -neck paraganglioma: combination with 131I-MIBG. Bonner, L; Cengel, KA; Cohen, DL; Fishbein, L; Nathanson, KL; Pryma, D; Torigian, DA, 2012)	0.38
" The present study investigated the utility of [(123)I]-Ioflupane single photon emission computed tomography (SPECT) combined with MIBG myocardial scintigraphy for the diagnosis of PD."	( [(123)I]-Ioflupane SPECT in combination with MIBG myocardial scintigraphy in Parkinson's disease: a case series study. Iikuni, Y; Ito, H; Kang, Y; Morimatsu, A; Murakami, T; Shirata, A; Ugawa, Y; Yamada, A; Yamane, K, 2016)	0.43
"In our case, who had refractory metastatic neuroblastoma, we use histone deacetylase inhibitor (panobinostat) in combination with chemotherapy agents and iodine-131-meta-iodobenzylguanidine (MIBG) therapy."	( Successful treatment of refractory metastatic neuroblastoma with panobinostat in combination with chemotherapy agents and iodine-131-meta-iodobenzylguanidine therapy. Bordbar, M; Shahriari, M; Shakibazad, N; Zareifar, S; Zekavat, OR, 2020)	0.56
"Panobinostat can cause apoptosis induction in refractory metastatic neuroblastoma in combination with MIBG therapy and chemotherapy."	( Successful treatment of refractory metastatic neuroblastoma with panobinostat in combination with chemotherapy agents and iodine-131-meta-iodobenzylguanidine therapy. Bordbar, M; Shahriari, M; Shakibazad, N; Zareifar, S; Zekavat, OR, 2020)	0.56

Excerpt	Reference	Relevance
" Orally administered MIBG demonstrated a bioavailability of 59%, with a maximal tolerated dose of 60 mg kg(-1)."	( Bioavailability and toxicity after oral administration of m-iodobenzylguanidine (MIBG). Beijnen, JH; Kuin, A; Rutgers, M; Smets, LA; van der Valk, MA, 1999)	0.3
" Low bioavailability may have limited fenretinide activity."	( Phase II study of oral capsular 4-hydroxyphenylretinamide (4-HPR/fenretinide) in pediatric patients with refractory or recurrent neuroblastoma: a report from the Children's Oncology Group. Ames, MM; Buhrow, SA; Cohn, SL; Jackson, H; Kitchen, BJ; London, WB; McGovern, RM; McGrady, P; Naranjo, A; Parisi, MT; Reid, JM; Reynolds, CP; Shulkin, B; Sondel, PM; Stranzinger, E; Villablanca, JG; Yanik, GA, 2011)	0.37
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."	( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019)	0.51

Excerpt	Relevance	Reference
" To evaluate dose escalation, alternative dosage schedules, and alternative MIBG-radioconjugates, additional trials of radiolabeled MIBG are indicated."	( 131-I-metaiodobenzylguanidine treatment in patients with refractory advanced neuroblastoma. Carey, JE; Francis, IR; Hutchinson, RJ; Johnson, JW; Miser, JS; Normole, D; Shapiro, B; Shulkin, BL; Sisson, JC; Zasadny, K, 1992)	0.28
"Treatment of resistant neuroblastoma with high dosage [131I]metaiodobenzylguanidine (131I-MIBG) appears effective since encouraging results have been obtained so far even in patients with very advanced, intensively pre-treated disease."	( [131I]metaiodobenzylguanidine in neuroblastoma patients at diagnosis. Iavarone, A; Lasorella, A; Mastrangelo, R; Riccardi, R; Rufini, V; Troncone, L, )	0.13
" We observed the complete disappearance of a large abdominal tumor mass after a relatively low dosage of 131I-MIBG, with minimal hematologic toxicity."	( 131I-metaiodobenzylguanidine in the treatment of neuroblastoma at diagnosis. Lasorella, A; Mastrangelo, R; Montemaggi, P; Riccardi, R; Rufini, V; Troncone, L, 1989)	0.28
" The children were each administered from 1 to 5 courses with a dosage per course of between 1,295 and 9,065 MBq."	( Treatment of neuroblastoma with metaiodobenzylguanidine: results and side effects. Bruchelt, G; Feine, U; Klingebiel, T; Niethammer, D; Treuner, J, 1987)	0.27
" The single patient treated at diagnosis showed a dramatic response to a relatively low dosage of MIBG, with histologically proved disappearance of the tumor mass."	( Treatment of neuroblastoma with 131I-metaiodobenzylguanidine. Lasorella, A; Mastrangelo, R; Montemaggi, P; Riccardi, R; Rufini, V; Troncone, L, 1987)	0.27
" In summary, MIBG myocardial SPECT could be a useful test for determining a dosage regimen of ADR therapy of individual patients."	( [Clinical usefulness of 123I-MIBG myocardial SPECT in patients with adriamycin-induced cardiomyopathy]. Igarashi, M; Morishita, T; Niitsu, N; Umeda, M; Yamazaki, J, 1994)	0.29
" Furthermore, a single course of 131-I-MIBG at the dosage employed does not appear to jeopardize the subsequent use of chemotherapy."	( Critical observations on neuroblastoma treatment with 131-I-metaiodobenzylguanidine at diagnosis. Danza, F; Iavarone, A; Lasorella, A; Mastrangelo, R; Riccardi, R; Rufini, V; Troncone, L, 1993)	0.29
" Findings also suggested that (123)I-MIBG was useful for examining the severity of DCM, determining the applicability of beta-blocker therapy, estimating the maintenance dosage of beta-blocker, and evaluating prognosis."	( Evaluation of beta-blocker therapy in patients with dilated cardiomyopathy--Clinical meaning of iodine 123-metaiodobenzylguanidine myocardial single-photon emission computed tomography. Inoue, A; Kabano, T; Muto, H; Nanjo, S; Yamashina, S; Yamazaki, J, 2001)	0.31
" The first blood sample was irradiated in vitro with 60Co gamma-rays to determine the dose-response curve."	( Patient dosimetry after 131I-MIBG therapy for neuroblastoma and carcinoid tumours. Brans, B; De Ridder, L; Dierckx, RA; Monsieurs, MA; Thierens, HM; Vral, A, 2001)	0.31
" Patients who could not be dosed with up to 40 mg daily of metoprolol or 20 mg daily of carvedilol were defined as intolerant."	( Comparative left ventricular functional and neurohumoral effects of chronic treatment with carvedilol versus metoprolol in patients with dilated cardiomyopathy. Hanatani, A; Hirooka, K; Hori, M; Ishida, Y; Komamura, K; Miyatake, K; Nakatani, S; Yamagishi, M; Yasumura, Y, 2001)	0.31
" A dose-response relationship needs confirmation on a larger cohort of patients to reach statistical value."	( Thyroidal uptake and radiation dose after repetitive I-131-MIBG treatments: influence of potassium iodide for thyroid blocking. Brans, B; Dierckx, RA; Kaufman, JM; Laureys, G; Monsieurs, M; Thierens, H, 2002)	0.31
" Therapy was considered beneficial if clinical status improved, laboratory tests for secreting tumors improved by >20%, tumor progression was halted, the size of the most significant localization had decreased by >25%, and the dosage of analgesic and cold somatostatin therapy could be lowered."	( Long-term efficacy of radionuclide therapy in patients with disseminated neuroendocrine tumors uncontrolled by conventional therapy. Aparicio, T; Askienazy, S; de Labriolle-Vaylet, C; Faraggi, M; Giraudet, AL; Mignon, M; Nguyen, C; Rouzet, F; Sobhani, I, 2004)	0.32
" Cell kill of monolayers and disaggregated spheroids, dosed with [131I]MIBG, was assessed by clonogenic assay."	( Application of targeted radiotherapy/gene therapy to bladder cancer cell lines. Boyd, M; Brown, M; Carruthers, R; Fullerton, NE; Keith, WN; Kirk, D; Mairs, RJ; McCluskey, AG; Wilson, L, 2005)	0.33
" In phase I and II trials, dosimetry may be considered an inherent part of therapy to establish the maximum tolerated dose and dose-response relationship."	( Clinical radionuclide therapy dosimetry: the quest for the "Holy Gray". Bodei, L; Brans, B; Giammarile, F; Linden, O; Luster, M; Oyen, WJG; Tennvall, J, 2007)	0.34
" Further main alterations are related to the recommended (123)I activities with respect to the new EANM Paediatric Dosage Card and the explicit recommendation of SPECT."	( [Procedure guidelines for MIBG-scintigraphy in children]. Franzius, C; Hahn, K; Hero, B; Pfluger, T; Schmidt, M, 2008)	0.35
" Dosimetry using combined anatomical and functional imaging is being developed for patient-specific dosing of targeted radiotherapy and as an extremely sensitive monitor of response to therapy."	( Combining anatomic and molecularly targeted imaging in the diagnosis and surveillance of embryonal tumors of the nervous and endocrine systems in children. Bushnell, D; Khanna, G; O'Dorisio, MS, 2008)	0.35
" Cells exposed to media from [131I]MIBG- or [131I]IUdR-treated cells demonstrated a dose-response relationship with respect to clonogenic cell death."	( Radiation quality-dependent bystander effects elicited by targeted radionuclides. Boyd, M; Mairs, RJ; McCluskey, AG; Sorensen, A, 2008)	0.35
" It was designed to maximize cytoreduction via high dosing of synergistically interacting agents, while minimizing morbidity in patients with resistant neuroblastoma (NB) and ineligible for clinical trials due to myelosuppression from previous therapy."	( 5-day/5-drug myeloablative outpatient regimen for resistant neuroblastoma. Basu, EM; Cheung, NK; Kramer, K; Kushner, BH; Modak, S; Roberts, SS, 2013)	0.39
" Subsequently, the doses received by the technologists were analyzed with respect to specific process steps performed during 131I-metaiodobenzylguanidine therapy including package receipt, dosage preparation, and dosage administration."	( Minimizing nuclear medicine technologist radiation exposure during 131I-MIBG therapy. Gelfand, MJ; Lemen, L; Morris, VR; Turpin, BK; Weiss, BD, 2013)	0.39
"Escalating the disulfiram dosage caused a biphasic reduction in the surviving fraction of clonogens."	( The role of copper in disulfiram-induced toxicity and radiosensitization of cancer cells. Babich, JW; Boyd, M; Mairs, RJ; Rae, C; Sorensen, A; Tesson, M, 2013)	0.39
"Reported experience with systemic (131)I-metaiodobenzylguanidine ((131)I-MIBG) therapy of neuroendocrine tumors comprises different dosing schemes."	( Long-term outcome and toxicity after dose-intensified treatment with 131I-MIBG for advanced metastatic carcinoid tumors. Ahmadzadehfar, H; Alkawaldeh, K; Biersack, HJ; Ezziddin, S; Grünwald, F; Logvinski, T; Sabet, A; Yong-Hing, CJ, 2013)	0.39
" (131)I-MIBG dosing was determined by pre-therapy glomerular filtration rate (GFR), with 8 mCi/kg given if GFR was 60 to 99 mL/minute/1."	( 131I-metaiodobenzylguanidine with intensive chemotherapy and autologous stem cell transplantation for high-risk neuroblastoma. A new approaches to neuroblastoma therapy (NANT) phase II study. Courtier, J; Czarnecki, S; Goodarzian, F; Groshen, S; Haas-Koga, D; Hasenauer, CB; Hawkins, R; Hutchinson, R; Jackson, H; Katzenstein, HM; Marachelian, A; Maris, JM; Matthay, KK; Park, JR; Shimada, H; Shulkin, BL; Tsao-Wei, D; Villablanca, JG; Weiss, B; Yanik, GA, 2015)	0.42
"71) or potassium iodate blockade despite variations in iodate dosage and duration (χ(2) = 0."	( A comparison of thyroid blockade strategies in paediatric 123I-meta-iodobenzylguanidine scanning: a dual centre study. Biassoni, L; Easty, M; King, S; Melhuish, T; Michopoulou, S; Morris, E; Price, L; Thurlow, B, 2020)	0.56
"8 mCi/kg) single dose and fractionated dosing 16."	( Preclinical Development of [211At]meta- astatobenzylguanidine ([211At]MABG) as an Alpha Particle Radiopharmaceutical Therapy for Neuroblastoma. Batra, V; Carlin, S; Elias, J; Groff, D; Hou, C; Li, Y; Makvandi, M; Maris, JM; Martinez, D; Martorano, P; Pawel, B; Pryma, DA; Ranieri, P; Samanta, M; Tsang, M; Vaidyanathan, G, 2022)	0.72

Class	Description
organoiodine compound	An organoiodine compound is a compound containing at least one carbon-iodine bond.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein	Taxonomy	Measurement	Average (µ)	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
dopamine D1 receptor	Homo sapiens (human)	Potency	18.3564	0.0052	1.3022	8.1995	AID624455
thioredoxin reductase	Rattus norvegicus (Norway rat)	Potency	8.9125	0.1000	20.8793	79.4328	AID588453
GLS protein	Homo sapiens (human)	Potency	5.6234	0.3548	7.9355	39.8107	AID624146
Thrombopoietin	Homo sapiens (human)	Potency	1.5849	0.0251	7.3048	31.6228	AID917; AID918
hypoxia-inducible factor 1, alpha subunit (basic helix-loop-helix transcription factor)	Homo sapiens (human)	Potency	12.5893	0.0013	7.7625	44.6684	AID914; AID915
cytochrome P450 2D6 isoform 1	Homo sapiens (human)	Potency	15.8489	0.0020	7.5337	39.8107	AID891
cytochrome P450 2C19 precursor	Homo sapiens (human)	Potency	39.8107	0.0025	5.8400	31.6228	AID899
ras-related protein Rab-9A	Homo sapiens (human)	Potency	79.4328	0.0002	2.6215	31.4954	AID485297
histone acetyltransferase KAT2A isoform 1	Homo sapiens (human)	Potency	39.8107	0.2512	15.8432	39.8107	AID504327
lethal factor (plasmid)	Bacillus anthracis str. A2012	Potency	12.5893	0.0200	10.7869	31.6228	AID912
Spike glycoprotein	Severe acute respiratory syndrome-related coronavirus	Potency	39.8107	0.0096	10.5250	35.4813	AID1479145
ATP-dependent phosphofructokinase	Trypanosoma brucei brucei TREU927	Potency	4.7755	0.0601	10.7453	37.9330	AID485368
endonuclease IV	Escherichia coli	Potency	5.0119	0.7079	12.4324	31.6228	AID1708
TDP1 protein	Homo sapiens (human)	Potency	11.8215	0.0008	11.3822	44.6684	AID686978; AID686979
AR protein	Homo sapiens (human)	Potency	26.0655	0.0002	21.2231	8,912.5098	AID743036; AID743042; AID743054
estrogen-related nuclear receptor alpha	Homo sapiens (human)	Potency	9.7756	0.0015	30.6073	15,848.9004	AID1224819; AID1224820; AID1224821
estrogen nuclear receptor alpha	Homo sapiens (human)	Potency	16.4371	0.0002	29.3054	16,493.5996	AID743069; AID743075; AID743079; AID743080; AID743091
arylsulfatase A	Homo sapiens (human)	Potency	30.1313	1.0691	13.9551	37.9330	AID720538
nuclear receptor subfamily 1, group I, member 2	Rattus norvegicus (Norway rat)	Potency	17.7828	0.1000	9.1916	31.6228	AID1346983
peripheral myelin protein 22 isoform 1	Homo sapiens (human)	Potency	30.1313	23.9341	23.9341	23.9341	AID1967
thyroid hormone receptor beta isoform 2	Rattus norvegicus (Norway rat)	Potency	20.3583	0.0003	23.4451	159.6830	AID743065; AID743067
survival motor neuron protein isoform d	Homo sapiens (human)	Potency	35.4813	0.1259	12.2344	35.4813	AID1458
lamin isoform A-delta10	Homo sapiens (human)	Potency	35.4813	0.8913	12.0676	28.1838	AID1459
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Protein	Taxonomy	Measurement	Average	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
POU domain, class 2, transcription factor 1	Homo sapiens (human)	Km	15.9000	2.1000	5.3900	8.6000	AID1769498
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Process	via Protein(s)	Taxonomy
negative regulation of DNA-templated transcription	POU domain, class 2, transcription factor 1	Homo sapiens (human)
negative regulation of DNA-templated transcription	POU domain, class 2, transcription factor 1	Homo sapiens (human)
positive regulation of transcription by RNA polymerase II	POU domain, class 2, transcription factor 1	Homo sapiens (human)
positive regulation of miRNA transcription	POU domain, class 2, transcription factor 1	Homo sapiens (human)
regulation of transcription by RNA polymerase II	POU domain, class 2, transcription factor 1	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Process	via Protein(s)	Taxonomy
RNA polymerase II cis-regulatory region sequence-specific DNA binding	POU domain, class 2, transcription factor 1	Homo sapiens (human)
RNA polymerase II core promoter sequence-specific DNA binding	POU domain, class 2, transcription factor 1	Homo sapiens (human)
DNA-binding transcription factor activity, RNA polymerase II-specific	POU domain, class 2, transcription factor 1	Homo sapiens (human)
DNA-binding transcription activator activity, RNA polymerase II-specific	POU domain, class 2, transcription factor 1	Homo sapiens (human)
DNA binding	POU domain, class 2, transcription factor 1	Homo sapiens (human)
protein binding	POU domain, class 2, transcription factor 1	Homo sapiens (human)
sequence-specific DNA binding	POU domain, class 2, transcription factor 1	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Process	via Protein(s)	Taxonomy
nucleus	POU domain, class 2, transcription factor 1	Homo sapiens (human)
nucleoplasm	POU domain, class 2, transcription factor 1	Homo sapiens (human)
endoplasmic reticulum	POU domain, class 2, transcription factor 1	Homo sapiens (human)
intracellular membrane-bounded organelle	POU domain, class 2, transcription factor 1	Homo sapiens (human)
chromatin	POU domain, class 2, transcription factor 1	Homo sapiens (human)
RNA polymerase II transcription regulator complex	POU domain, class 2, transcription factor 1	Homo sapiens (human)
virion membrane	Spike glycoprotein	Severe acute respiratory syndrome-related coronavirus
[Information is prepared from geneontology information from the June-17-2024 release]

Assay ID	Title	Year	Journal	Article
AID15750	Distribution in female dog urine 24 hours after administration.	1984	Journal of medicinal chemistry, Feb, Volume: 27, Issue:2	Adrenal medulla imaging agents: a structure-distribution relationship study of radiolabeled aralkylguanidines.
AID15737	Distribution in female dog lung 72 hours after administration.	1984	Journal of medicinal chemistry, Feb, Volume: 27, Issue:2	Adrenal medulla imaging agents: a structure-distribution relationship study of radiolabeled aralkylguanidines.
AID15738	Distribution in female dog muscle 24 hours after administration.	1984	Journal of medicinal chemistry, Feb, Volume: 27, Issue:2	Adrenal medulla imaging agents: a structure-distribution relationship study of radiolabeled aralkylguanidines.
AID1769498	Substrate activity at human OCT1 expressed in HEK293 cells assessed as increase in compound uptake by measuring Km incubated for 2 mins by LC-MS/MS analysis	2021	Journal of medicinal chemistry, 03-11, Volume: 64, Issue:5	Identification of Novel High-Affinity Substrates of OCT1 Using Machine Learning-Guided Virtual Screening and Experimental Validation.
AID15741	Distribution in female dog pancreas 72 hours after administration.	1984	Journal of medicinal chemistry, Feb, Volume: 27, Issue:2	Adrenal medulla imaging agents: a structure-distribution relationship study of radiolabeled aralkylguanidines.
AID230956	Ratio of the concentration levels determined for the adrenal medulla to the liver after 72 hr; [Adrenal Medulla] / [liver]	1984	Journal of medicinal chemistry, Feb, Volume: 27, Issue:2	Adrenal medulla imaging agents: a structure-distribution relationship study of radiolabeled aralkylguanidines.
AID1152956	Antiproliferative activity against human SK-N-SH cells at 10 to 100 uM after 72 hrs by MTT assay	2014	Bioorganic & medicinal chemistry letters, Jun-15, Volume: 24, Issue:12	Synthesis and biological effects of new hybrid compounds composed of benzylguanidines and the alkylating group of busulfan on neuroblastoma cells.
AID15725	Distribution in female dog bile 72 hr after administration.	1984	Journal of medicinal chemistry, Feb, Volume: 27, Issue:2	Adrenal medulla imaging agents: a structure-distribution relationship study of radiolabeled aralkylguanidines.
AID15739	Distribution in female dog muscle 72 hours after administration.	1984	Journal of medicinal chemistry, Feb, Volume: 27, Issue:2	Adrenal medulla imaging agents: a structure-distribution relationship study of radiolabeled aralkylguanidines.
AID1603708	Dissociation constant, pKa of compound	2020	Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5	Norepinephrine-Transporter-Targeted and DNA-Co-Targeted Theranostic Guanidines.
AID15729	Distribution in female dog heart 72 hours after administration.	1984	Journal of medicinal chemistry, Feb, Volume: 27, Issue:2	Adrenal medulla imaging agents: a structure-distribution relationship study of radiolabeled aralkylguanidines.
AID15572	Distribution in female dog adrenal cortex 72 hours after administration.	1984	Journal of medicinal chemistry, Feb, Volume: 27, Issue:2	Adrenal medulla imaging agents: a structure-distribution relationship study of radiolabeled aralkylguanidines.
AID15727	Distribution in female dog blood 72 hours after administration.	1984	Journal of medicinal chemistry, Feb, Volume: 27, Issue:2	Adrenal medulla imaging agents: a structure-distribution relationship study of radiolabeled aralkylguanidines.
AID1769499	Substrate activity at human OCT1 expressed in HEK293 cells assessed as increase in compound uptake by measuring Vmax incubated for 2 mins by LC-MS/MS analysis	2021	Journal of medicinal chemistry, 03-11, Volume: 64, Issue:5	Identification of Novel High-Affinity Substrates of OCT1 Using Machine Learning-Guided Virtual Screening and Experimental Validation.
AID15566	Distribution in dog adrenal medulla 72 hours after administration.	1984	Journal of medicinal chemistry, Feb, Volume: 27, Issue:2	Adrenal medulla imaging agents: a structure-distribution relationship study of radiolabeled aralkylguanidines.
AID15724	Distribution in female dog bile 24 hours after administration.	1984	Journal of medicinal chemistry, Feb, Volume: 27, Issue:2	Adrenal medulla imaging agents: a structure-distribution relationship study of radiolabeled aralkylguanidines.
AID1754854	Drug uptake in human SK-N-F1 cells at 10 uM measured upto 60 mins by LC-MS/MS analysis	2021	Bioorganic & medicinal chemistry, 07-15, Volume: 42	Design, synthesis, and biological evaluation of novel bifunctional thyrointegrin antagonists for neuroblastoma.
AID1152959	Increase in glycolysis in human Kelly cells assessed as conversion of glucose to lactate at 100 uM after 12 hrs relative to untreated control	2014	Bioorganic & medicinal chemistry letters, Jun-15, Volume: 24, Issue:12	Synthesis and biological effects of new hybrid compounds composed of benzylguanidines and the alkylating group of busulfan on neuroblastoma cells.
AID15731	Distribution in female dog kidney 72 hours after administration.	1984	Journal of medicinal chemistry, Feb, Volume: 27, Issue:2	Adrenal medulla imaging agents: a structure-distribution relationship study of radiolabeled aralkylguanidines.
AID1769501	Ratio of drug uptake in human OCT1 expressing HEK293 cells at 2.5 uM to drug uptake in empty vector transfected human HEK293 cells at 2.5 uM	2021	Journal of medicinal chemistry, 03-11, Volume: 64, Issue:5	Identification of Novel High-Affinity Substrates of OCT1 Using Machine Learning-Guided Virtual Screening and Experimental Validation.
AID15730	Distribution in female dog kidney 24 hours after administration.	1984	Journal of medicinal chemistry, Feb, Volume: 27, Issue:2	Adrenal medulla imaging agents: a structure-distribution relationship study of radiolabeled aralkylguanidines.
AID15567	Distribution in female dog Ovary 24 hours after administration.	1984	Journal of medicinal chemistry, Feb, Volume: 27, Issue:2	Adrenal medulla imaging agents: a structure-distribution relationship study of radiolabeled aralkylguanidines.
AID15744	Distribution in female dog spleen 24 hours after administration.	1984	Journal of medicinal chemistry, Feb, Volume: 27, Issue:2	Adrenal medulla imaging agents: a structure-distribution relationship study of radiolabeled aralkylguanidines.
AID15732	Distribution in female dog large intestine 24 hours after administration.	1984	Journal of medicinal chemistry, Feb, Volume: 27, Issue:2	Adrenal medulla imaging agents: a structure-distribution relationship study of radiolabeled aralkylguanidines.
AID15747	Distribution in female dog stomach 72 hours after administration.	1984	Journal of medicinal chemistry, Feb, Volume: 27, Issue:2	Adrenal medulla imaging agents: a structure-distribution relationship study of radiolabeled aralkylguanidines.
AID1152954	Antiproliferative activity against human Kelly cells at 10 to 100 uM after 72 hrs by MTT assay	2014	Bioorganic & medicinal chemistry letters, Jun-15, Volume: 24, Issue:12	Synthesis and biological effects of new hybrid compounds composed of benzylguanidines and the alkylating group of busulfan on neuroblastoma cells.
AID15569	Distribution in female dog adipose 24 hours after administration.	1984	Journal of medicinal chemistry, Feb, Volume: 27, Issue:2	Adrenal medulla imaging agents: a structure-distribution relationship study of radiolabeled aralkylguanidines.
AID1152953	Antiproliferative activity against human LS cells at 10 to 100 uM after 72 hrs by MTT assay	2014	Bioorganic & medicinal chemistry letters, Jun-15, Volume: 24, Issue:12	Synthesis and biological effects of new hybrid compounds composed of benzylguanidines and the alkylating group of busulfan on neuroblastoma cells.
AID15740	Distribution in female dog pancreas 24 hours after administration.	1984	Journal of medicinal chemistry, Feb, Volume: 27, Issue:2	Adrenal medulla imaging agents: a structure-distribution relationship study of radiolabeled aralkylguanidines.
AID15726	Distribution in female dog blood 24 hours after administration.	1984	Journal of medicinal chemistry, Feb, Volume: 27, Issue:2	Adrenal medulla imaging agents: a structure-distribution relationship study of radiolabeled aralkylguanidines.
AID15742	Distribution in female dog small intestine 24 hours after administration.	1984	Journal of medicinal chemistry, Feb, Volume: 27, Issue:2	Adrenal medulla imaging agents: a structure-distribution relationship study of radiolabeled aralkylguanidines.
AID15565	Distribution in dog adrenal medulla 30 min after administration.	1984	Journal of medicinal chemistry, Feb, Volume: 27, Issue:2	Adrenal medulla imaging agents: a structure-distribution relationship study of radiolabeled aralkylguanidines.
AID15736	Distribution in female dog lung 24 hours after administration.	1984	Journal of medicinal chemistry, Feb, Volume: 27, Issue:2	Adrenal medulla imaging agents: a structure-distribution relationship study of radiolabeled aralkylguanidines.
AID15733	Distribution in female dog large intestine 72 hours after administration.	1984	Journal of medicinal chemistry, Feb, Volume: 27, Issue:2	Adrenal medulla imaging agents: a structure-distribution relationship study of radiolabeled aralkylguanidines.
AID15735	Distribution in female dog liver 72 hours after administration.	1984	Journal of medicinal chemistry, Feb, Volume: 27, Issue:2	Adrenal medulla imaging agents: a structure-distribution relationship study of radiolabeled aralkylguanidines.
AID15746	Distribution in female dog stomach 24 hours after administration.	1984	Journal of medicinal chemistry, Feb, Volume: 27, Issue:2	Adrenal medulla imaging agents: a structure-distribution relationship study of radiolabeled aralkylguanidines.
AID1152957	Increase in glycolysis in human LS cells assessed as conversion of glucose to lactate at 100 uM after 12 hrs relative to untreated control	2014	Bioorganic & medicinal chemistry letters, Jun-15, Volume: 24, Issue:12	Synthesis and biological effects of new hybrid compounds composed of benzylguanidines and the alkylating group of busulfan on neuroblastoma cells.
AID15751	Distribution in female dog urine 72 hr after administration.	1984	Journal of medicinal chemistry, Feb, Volume: 27, Issue:2	Adrenal medulla imaging agents: a structure-distribution relationship study of radiolabeled aralkylguanidines.
AID679501	TP_TRANSPORTER: decrease in liver concentration in Oct1 -/- mouse	2001	Molecular and cellular biology, Aug, Volume: 21, Issue:16	Reduced hepatic uptake and intestinal excretion of organic cations in mice with a targeted disruption of the organic cation transporter 1 (Oct1 [Slc22a1]) gene.
AID15570	Distribution in female dog adipose 72 hours after administration.	1984	Journal of medicinal chemistry, Feb, Volume: 27, Issue:2	Adrenal medulla imaging agents: a structure-distribution relationship study of radiolabeled aralkylguanidines.
AID15568	Distribution in female dog Ovary 72 hours after administration.	1984	Journal of medicinal chemistry, Feb, Volume: 27, Issue:2	Adrenal medulla imaging agents: a structure-distribution relationship study of radiolabeled aralkylguanidines.
AID15734	Distribution in female dog liver 24 hours after administration.	1984	Journal of medicinal chemistry, Feb, Volume: 27, Issue:2	Adrenal medulla imaging agents: a structure-distribution relationship study of radiolabeled aralkylguanidines.
AID15571	Distribution in female dog adrenal cortex 72 hours after administration.	1984	Journal of medicinal chemistry, Feb, Volume: 27, Issue:2	Adrenal medulla imaging agents: a structure-distribution relationship study of radiolabeled aralkylguanidines.
AID15745	Distribution in female dog spleen 72 hours after administration.	1984	Journal of medicinal chemistry, Feb, Volume: 27, Issue:2	Adrenal medulla imaging agents: a structure-distribution relationship study of radiolabeled aralkylguanidines.
AID1152948	Cellular uptake in human SK-N-SH cells assessed as noradrenaline transporter-mediated uptake at 1 x 10'-4 M after 15 mins by [3H]-noradrenaline uptake assay	2014	Bioorganic & medicinal chemistry letters, Jun-15, Volume: 24, Issue:12	Synthesis and biological effects of new hybrid compounds composed of benzylguanidines and the alkylating group of busulfan on neuroblastoma cells.
AID1603709	Partition coefficient, logP of compound	2020	Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5	Norepinephrine-Transporter-Targeted and DNA-Co-Targeted Theranostic Guanidines.
AID1152955	Antiproliferative activity against human SiMa cells at 10 to 100 uM after 72 hrs by MTT assay	2014	Bioorganic & medicinal chemistry letters, Jun-15, Volume: 24, Issue:12	Synthesis and biological effects of new hybrid compounds composed of benzylguanidines and the alkylating group of busulfan on neuroblastoma cells.
AID15723	Distribution in female dog adrenal medulla 72 hours after administration.	1984	Journal of medicinal chemistry, Feb, Volume: 27, Issue:2	Adrenal medulla imaging agents: a structure-distribution relationship study of radiolabeled aralkylguanidines.
AID15748	Distribution in female dog thyroid 24 hours after administration.	1984	Journal of medicinal chemistry, Feb, Volume: 27, Issue:2	Adrenal medulla imaging agents: a structure-distribution relationship study of radiolabeled aralkylguanidines.
AID15743	Distribution in female dog small intestine 72 hours after administration.	1984	Journal of medicinal chemistry, Feb, Volume: 27, Issue:2	Adrenal medulla imaging agents: a structure-distribution relationship study of radiolabeled aralkylguanidines.
AID15728	Distribution in female dog heart 24 hours after administration.	1984	Journal of medicinal chemistry, Feb, Volume: 27, Issue:2	Adrenal medulla imaging agents: a structure-distribution relationship study of radiolabeled aralkylguanidines.
AID1152958	Increase in glycolysis in human SiMa cells assessed as conversion of glucose to lactate at 100 uM after 12 hrs relative to untreated control	2014	Bioorganic & medicinal chemistry letters, Jun-15, Volume: 24, Issue:12	Synthesis and biological effects of new hybrid compounds composed of benzylguanidines and the alkylating group of busulfan on neuroblastoma cells.
AID15722	Distribution in female dog adrenal medulla 24 hours after administration.	1984	Journal of medicinal chemistry, Feb, Volume: 27, Issue:2	Adrenal medulla imaging agents: a structure-distribution relationship study of radiolabeled aralkylguanidines.
AID15749	Distribution in female dog thyroid 72 hours after administration.	1984	Journal of medicinal chemistry, Feb, Volume: 27, Issue:2	Adrenal medulla imaging agents: a structure-distribution relationship study of radiolabeled aralkylguanidines.
AID1769500	Substrate activity at human OCT1 expressed in HEK293 cells assessed as increase in compound uptake by measuring intrinsic clearance incubated for 2 mins by LC-MS/MS analysis	2021	Journal of medicinal chemistry, 03-11, Volume: 64, Issue:5	Identification of Novel High-Affinity Substrates of OCT1 Using Machine Learning-Guided Virtual Screening and Experimental Validation.
AID504836	Inducers of the Endoplasmic Reticulum Stress Response (ERSR) in human glioma: Validation	2002	The Journal of biological chemistry, Apr-19, Volume: 277, Issue:16	Sustained ER Ca2+ depletion suppresses protein synthesis and induces activation-enhanced cell death in mast cells.
AID504810	Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign	2010	Endocrinology, Jul, Volume: 151, Issue:7	A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID504812	Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign	2010	Endocrinology, Jul, Volume: 151, Issue:7	A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID588349	qHTS for Inhibitors of ATXN expression: Validation of Cytotoxic Assay
AID588378	qHTS for Inhibitors of ATXN expression: Validation
AID1159607	Screen for inhibitors of RMI FANCM (MM2) intereaction	2016	Journal of biomolecular screening, Jul, Volume: 21, Issue:6	A High-Throughput Screening Strategy to Identify Protein-Protein Interaction Inhibitors That Block the Fanconi Anemia DNA Repair Pathway.
AID1346986	P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen	2019	Molecular pharmacology, 11, Volume: 96, Issue:5	A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1346987	P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen	2019	Molecular pharmacology, 11, Volume: 96, Issue:5	A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1347082	qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal	2020	Antiviral research, 01, Volume: 173	A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID651635	Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID1296008	Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening	2020	SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1	Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1347050	Natriuretic polypeptide receptor (hNpr2) antagonism - Pilot subtype selectivity assay	2019	Science translational medicine, 07-10, Volume: 11, Issue:500	Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID1508630	Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay	2021	Cell reports, 04-27, Volume: 35, Issue:4	A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1347083	qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen	2020	Antiviral research, 01, Volume: 173	A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347045	Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot counterscreen GloSensor control cell line	2019	Science translational medicine, 07-10, Volume: 11, Issue:500	Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID1347049	Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot screen	2019	Science translational medicine, 07-10, Volume: 11, Issue:500	Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID1347086	qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal	2020	Antiviral research, 01, Volume: 173	A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID504749	qHTS profiling for inhibitors of Plasmodium falciparum proliferation	2011	Science (New York, N.Y.), Aug-05, Volume: 333, Issue:6043	Chemical genomic profiling for antimalarial therapies, response signatures, and molecular targets.
AID1347410	qHTS for inhibitors of adenylyl cyclases using a fission yeast platform: a pilot screen against the NCATS LOPAC library	2019	Cellular signalling, 08, Volume: 60	A fission yeast platform for heterologous expression of mammalian adenylyl cyclases and high throughput screening.
AID1347405	qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS LOPAC collection	2020	ACS chemical biology, 07-17, Volume: 15, Issue:7	High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1347151	Optimization of GU AMC qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay	2020	Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49	Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347059	CD47-SIRPalpha protein protein interaction - Alpha assay qHTS validation	2019	PloS one, , Volume: 14, Issue:7	Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID1347058	CD47-SIRPalpha protein protein interaction - HTRF assay qHTS validation	2019	PloS one, , Volume: 14, Issue:7	Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID1347057	CD47-SIRPalpha protein protein interaction - LANCE assay qHTS validation	2019	PloS one, , Volume: 14, Issue:7	Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID1794808	Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL).	2014	Journal of biomolecular screening, Jul, Volume: 19, Issue:6	A High-Throughput Assay to Identify Inhibitors of the Apicoplast DNA Polymerase from Plasmodium falciparum.
AID1794808	Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL).
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Timeframe	Studies, This Drug (%)	All Drugs %
pre-1990	399 (12.00)	18.7374
1990's	883 (26.56)	18.2507
2000's	863 (25.95)	29.6817
2010's	940 (28.27)	24.3611
2020's	240 (7.22)	2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Publication Type	This drug (%)	All Drugs (%)
Trials	260 (7.30%)	5.53%
Trials	0 (0.00%)	5.53%
Reviews	396 (11.11%)	6.00%
Reviews	0 (0.00%)	6.00%
Case Studies	821 (23.04%)	4.05%
Case Studies	0 (0.00%)	4.05%
Observational	15 (0.42%)	0.25%
Observational	0 (0.00%)	0.25%
Other	2,071 (58.13%)	84.16%
Other	13 (100.00%)	84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (58)

Trial Overview

Trial	Phase	Enrollment	Study Type	Start Date	Status
I-Metaiodobenzylguanidine (131 I-MIBG) Therapy for Refractory Neuroblastoma, Expanded Access Protocol [NCT01163383]		0 participants	Expanded Access		Available
Compassionate Use of 131I-MIBG for Patients With Malignant Pheochromocytoma [NCT01377532]		0 participants	Expanded Access		Approved for marketing
[NCT01373736]	Phase 3	0 participants	Interventional		Not yet recruiting
A Compassionate Use/Expanded Access Protocol Using 131I-MIBG Therapy for Patients With Refractory Neuroblastoma and Metastatic Pheochromocytoma [NCT03015844]		0 participants	Expanded Access		Available
An Open-Label, Multicenter, Phase 3 Study Evaluating the Prognostic Usefulness of I-123 mIBG Scintigraphy for Identifying Subjects With Heart Failure Who Will Experience an Adverse Cardiac Event [NCT00126438]	Phase 3	515 participants (Actual)	Interventional	2005-07-31	Completed
A COG Pilot Study of Intensive Induction Chemotherapy and 131I-MIBG Followed by Myeloablative Busulfan/Melphalan (Bu/Mel) for Newly Diagnosed High-Risk Neuroblastoma [NCT01175356]	Phase 1	99 participants (Actual)	Interventional	2010-10-04	Active, not recruiting
Cardiac Mapping of Autonomic Atrial Innervation and Its Relation to MIBG Nuclear Imaging in Patients With Atrial Fibrillation [NCT02071680]	Phase 3	5 participants (Actual)	Interventional	2015-03-31	Completed
Activation of Brown Adipose Tissue in Lean and Obese Men [NCT02173834]		20 participants (Actual)	Interventional	2013-03-31	Completed
A Pilot Study of Dinutuximab, Sargramostim (GM-CSF), and Isotretinoin in Combination With Irinotecan and Temozolomide in the Post-Consolidation Setting for High-Risk Neuroblastoma [NCT04385277]	Phase 2	34 participants (Actual)	Interventional	2020-12-31	Active, not recruiting
A Phase 3 Study of 131I-Metaiodobenzylguanidine (131I-MIBG) or ALK Inhibitor Therapy Added to Intensive Therapy for Children With Newly Diagnosed High-Risk Neuroblastoma (NBL) [NCT03126916]	Phase 3	724 participants (Anticipated)	Interventional	2018-05-14	Active, not recruiting
131I-Metaiodobenzylguanidine (131I-MIBG) Therapy for Refractory Neuroblastoma and Pheochromocytoma [NCT01850888]		100 participants (Anticipated)	Interventional	2013-12-31	Suspended(stopped due to Drugs unavailable. Seeking new supplier.)
Three Dimension Neuron Imaging Using 123I-metaiodobenzylguanidine Single Photon Emission Computed Tomography to Guide Ventricular Tachycardia Ablations [NCT01250912]		20 participants (Actual)	Interventional	2010-03-31	Completed
A Phase I Study of 131I-MIBG With Dinutuximab +/- Vorinostat for Relapsed/Refractory Neuroblastoma [NCT03332667]	Phase 1	45 participants (Actual)	Interventional	2018-09-12	Active, not recruiting
Molecular Characterization Trial for the Harvard/UCSF ROBIN Center: Radiation Oncology at the Interface of Pediatric Cancer Biology and Data Science [NCT06000787]		47 participants (Anticipated)	Interventional	2023-09-19	Recruiting
Myocardial 123I-MIBG Scintigraphy in Aging and Neurodegenerative Disease [NCT05514106]	Phase 4	50 participants (Anticipated)	Interventional	2023-05-08	Enrolling by invitation
An Open-Label, Multicenter, Phase 3 Study Evaluating the Prognostic Usefulness of I-123 mIBG Scintigraphy for Identifying Subjects With Heart Failure Who Will Experience an Adverse Cardiac Event [NCT00126425]	Phase 3	587 participants (Actual)	Interventional	2005-07-31	Completed
Combination Targeted Radiotherapy in Neuroendocrine Tumors [NCT01099228]		2 participants (Actual)	Interventional	2006-09-30	Completed
Open Access Protocol of Targeted Radiotherapy With I-metaiodobenzylguanidine (I-MIBG) in Patients With Resistant Neuroblastoma or Malignant Chromaffin Cell Tumors [NCT00107289]	Phase 2	200 participants (Anticipated)	Interventional	2006-05-31	Recruiting
Phase II Study of the Association of Iodobenzylguanidine Meta-I131 (I131 MIBG) and Topotecan in the Treatment of Refractory or Relapsed Metastatic Neuroblastoma [NCT00960739]	Phase 2	30 participants (Actual)	Interventional	2008-11-30	Completed
High-dose MIBG With Subsequent Transplantation of Haploidentical Stem Cells in Children With Therapy Resistant Neuroblastoma [NCT00790413]	Early Phase 1	15 participants (Anticipated)	Interventional	2005-08-31	Active, not recruiting
Evaluating Myocardial Ischemia in Chest Pain Using Cardiovascular Magnetic Resonance (CMR) Imaging Exercise Bike [NCT03217227]		300 participants (Anticipated)	Observational	2017-05-01	Recruiting
131I-Metaiodobenzylguanidine (131I-MIBG) Therapy for Relapsed/Refractory Neuroblastoma [NCT03649438]		0 participants	Expanded Access		No longer available
A Phase 2a Study of Ultratrace™ Iobenguane I 131 in Patients With Relapsed/Refractory High-Risk Neuroblastoma [NCT00659984]	Phase 2	15 participants (Actual)	Interventional	2008-06-30	Completed
Dose Escalation Study of 131 I-Metaiodobenzylguanidine (MIBG) With Intensive Chemotherapy and Autologous Stem Cell Rescue for High-Risk Neuroblastoma - A Phase I Study [NCT00005978]	Phase 1	0 participants	Interventional	2000-05-31	Completed
124I-Metaiodobenzylguanidine (MIBG) PET/CT Diagnostic Imaging and Dosimetry for Patients With Neuroblastoma: A Pilot Study [NCT01583842]	Early Phase 1	10 participants (Actual)	Interventional	2013-04-09	Terminated(stopped due to Funding)
The Leiden Nonischemic Cardiomyopathy Study [NCT01940081]		148 participants (Actual)	Observational	2011-10-31	Completed
A Phase 2b Study Evaluating the Efficacy and Safety of Ultratrace™ Iobenguane I 131 Among Patients With Relapsed/Refractory High-Risk Neuroblastoma [NCT00992173]	Phase 2	0 participants (Actual)	Interventional	2010-01-31	Withdrawn
Expanded Access Protocol for [123I]mIBG for Patients With Known or Suspected Neuroblastoma [NCT00730444]		0 participants	Expanded Access		Approved for marketing
International Phase II Studies of I-mIBG in Combination With Topotecan and Peripheral Blood Stem Cell Rescue for (A) Primary Resistant High Risk Neuroblastoma and (B) Relapsed Stage 4 Neuroblastoma [NCT00389766]	Phase 2	0 participants (Actual)	Interventional	2008-07-31	Withdrawn(stopped due to Withdrawn because protocol has been discontinued. It was never opened.)
NB2004 Trial Protocol for Risk Adapted Treatment of Children With Neuroblastoma [NCT00410631]	Phase 3	642 participants (Anticipated)	Interventional	2004-10-31	Recruiting
An Exploratory Study of 3-[18F]Fluoro-para-hydroxyphenethylguanidine ([18F]3F-PHPG) in Patients With Neuroendocrine Tumors [NCT04510311]	Early Phase 1	30 participants (Anticipated)	Interventional	2020-10-19	Recruiting
I-MIBG Escalating Dose Rapid Sequence Double Infusion Followed By Autologous Stem Cell Infusion For Refractory Neuroblastoma [NCT00083135]	Phase 1	18 participants (Anticipated)	Interventional	2004-03-31	Completed
An Open Label, Expanded Access Protocol Using 131I-METAIODOBENZYLGUANIDINE (131I-MIBG) Therapy +/- Vorinostat in Patients With Refractory Neuroblastoma, Pheochromocytoma, or Paraganglioma [NCT01838187]		0 participants	Expanded Access		No longer available
A Phase I Study Evaluating the Maximum Tolerated Dose, Dosimetry, Safety, and Efficacy of Ultratrace Iobenguane I 131 in Patients With Malignant Pheochromocytoma/Paraganglioma [NCT00458952]	Phase 1/Phase 2	24 participants (Actual)	Interventional	2007-04-30	Completed
A Phase II Study Evaluating the Efficacy and Safety of Ultratrace Iobenguane I 131 in Patients With Malignant Relapsed/Refractory Pheochromocytoma/Paraganglioma [NCT00874614]	Phase 2	74 participants (Actual)	Interventional	2009-06-04	Active, not recruiting
Trial Protocol for the Treatment of Children With High Risk Neuroblastoma (NB2004-HR) [NCT00526318]		360 participants (Anticipated)	Interventional	2007-01-31	Recruiting
Phase 1 Study Evaluating the Safety, Distribution, Metabolism, and Radiation Dosimetry of ULTRATRACE Iobenguane I 131 in Patients With Malignant Pheochromocytoma/Paraganglioma or Metastatic Carcinoid [NCT00339131]	Phase 1	24 participants (Anticipated)	Interventional	2006-06-30	Completed
Cardiac Resynchronization and MIBG Imaging [NCT01522378]	Phase 1	14 participants (Actual)	Interventional	2012-02-29	Terminated(stopped due to The study was terminated because the funding was withdrawn.)
High Dose I-131 Metaiodobenzylguanidine (MIBG) Therapy for Metastatic Neuroendocrine Tumors [NCT00037869]	Phase 3	15 participants (Actual)	Interventional	2001-11-30	Completed
(131)I-Metaiodobenzylguanidine Treatment of Malignant Pheochromocytoma [NCT00028106]	Phase 2	32 participants	Interventional	2001-12-05	Completed
An Open-Label, Multicentre, Phase 3 Scintigraphy Study Assessing 123I-mIBG Uptake in Subjects Being Evaluated for Phaeochromocytoma or Neuroblastoma [NCT00126412]	Phase 3	251 participants (Actual)	Interventional	2005-08-02	Completed
Expanded Access Program of AZEDRA (Ultratrace Iobenguane I131) in Subjects With Malignant Relapsed/Refractory Pheochromocytoma/Paraganglioma: A Sub-study of Protocol MIP-IB12B [NCT02961491]		0 participants	Expanded Access		Approved for marketing
I-Metaiodobenzylguanidine (I-MIBG) Therapy for Refractory Neuroblastoma, A Phase II Study [NCT00293319]	Phase 2	164 participants (Actual)	Interventional	2005-04-30	Completed
A Cancer Research UK Phase I/II Study to Compare [124I]Meta-Iodobenzylguanidine (mIBG) Positron Emission Tomography/Computerised Tomography (PET/CT) to [123I]mIBG Imaging in Patients With Metastatic Neuroblastoma [NCT02043899]	Phase 1/Phase 2	36 participants (Actual)	Interventional	2014-02-28	Completed
Phase I Study of the Safety, Distribution, and Radiation Dosimetry of Ultratrace Iobenguane 123I-mIBG-Nanodosing: the Path to Higher Sensitivity and Lower Toxicity Radiopharmaceuticals [NCT01730417]	Phase 1	12 participants (Actual)	Interventional	2009-11-30	Completed
[NCT01822431]		100 participants (Anticipated)	Observational	2011-06-30	Enrolling by invitation
Pilot Study of High-Dose 131I-MIBG Therapy Combined With Vincristine and Five Days of Irinotecan for Resistant/Relapsed High-Risk Neuroblastoma [NCT01313936]	Phase 1	32 participants (Actual)	Interventional	2011-03-31	Completed
An Open Label, Expanded Access Protocol Using 131I-metaiodobenzylguanidine (131I-MIBG) Therapy in Patients With Refractory Neuroblastoma, Pheochromocytoma, or Paraganglioma (Not Eligible for Approved Treatment) [NCT01590680]		0 participants	Expanded Access		Available
Vorinostat With 131-I MIBG Therapy for Resistant/Relapsed Neuroblastoma: A Phase I Study IND# 105,744 [NCT01019850]	Phase 1	27 participants (Actual)	Interventional	2010-03-31	Completed
A Phase II, Open Label, Two-Arm Study of Therapeutic Iobenguane (131I) as Single Agent or in Combination With Vorinostat for Recurrent or Progressive High- Risk Neuroblastoma Subjects (OPTIMUM TRIAL) [NCT03561259]	Phase 2	60 participants (Anticipated)	Interventional	2019-10-21	Recruiting
131I-Labeled MIBG for Refractory Neuroblastoma: A Compassionate Use Protocol [NCT01370330]		0 participants	Expanded Access		Available
A Phase II Study of 131I-labeled Metaiodobenzylguanidine (MIBG) for Treatment of Patients With Metastatic or Unresectable Pheochromocytoma and Related Tumors [NCT01413503]	Phase 2	50 participants (Actual)	Interventional	1991-05-31	Completed
A Phase 4, Open-label Test-retest Study to Assess the Reproducibility of Quantitative Measurements of Myocardial Uptake of AdreView (Iobenguane I 123 Injection) [NCT01936649]	Phase 4	63 participants (Actual)	Interventional	2013-08-31	Completed
Irinotecan and Vincristine With 131I-MIBG Therapy for Resistant/Relapsed High-Risk Neuroblastoma, A Phase I Study [NCT00509353]	Phase 1	26 participants (Actual)	Interventional	2007-01-31	Completed
A Phase II Study of <131>I-Metaiodobenzyguanidine (<131>I-MIBG) Therapy for Patients With MIBG Avid Tumors [NCT02378428]	Phase 2	65 participants (Anticipated)	Interventional	2014-03-31	Active, not recruiting
The Evaluation of the Pathogenesis of Stress-Induced Cardiomyopathy by I-123 MIBG Imaging [NCT01432626]		10 participants (Actual)	Interventional	2011-09-30	Completed
NANT 2011- 01: Randomized Phase II Pick the Winner Study of 131I-MIBG, 131I-MIBG With Vincristine and Irinotecan, or 131I-MIBG With Vorinostat for Resistant/Relapsed Neuroblastoma [NCT02035137]	Phase 2	114 participants (Actual)	Interventional	2014-07-31	Completed
AdreView™ Myocardial Imaging for Risk Evaluation - A Multicentre Trial to Guide ICD Implantation in NYHA Class II & III Heart Failure Patients With 25%≤LVEF≤35% [NCT02656329]	Phase 3	395 participants (Actual)	Interventional	2015-12-30	Terminated(stopped due to Sponsor discretion (low recruitment rate))
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Trial Outcomes

Trial	Outcome
NCT00126425 (1) [back to overview]	Relationship Between the Occurrence of Adverse Cardiac Event and 123I-mIBG Uptake on Planar Scintigraphy Categorized as High or Low Heart to Mediastinum (H/M) Ratio
NCT00126438 (1) [back to overview]	Relationship Between the Occurrence of Adverse Cardiac Event and 123I-mIBG Uptake on Planar Scintigraphy Categorized as High or Low Heart to Mediastinum (H/M) Ratio
NCT00458952 (1) [back to overview]	MTD of Ultratrace Iobenguane I 131
NCT00659984 (6) [back to overview]	Dose Limiting Toxicities
NCT00659984 (6) [back to overview]	Maximum Tolerated Dose
NCT00659984 (6) [back to overview]	Overall Objective Tumor Response Post Therapeutic Treatment
NCT00659984 (6) [back to overview]	Quality of Life
NCT00659984 (6) [back to overview]	Tumor Response in CT/MRI Lesions Post Therapeutic Treatment
NCT00659984 (6) [back to overview]	Dosimetric Estimation of Radiation Absorbed Doses to Measurable Lesions
NCT00874614 (4) [back to overview]	Best Confirmed Overall Tumor Response of Complete Response (CR) or Partial Response (PR) by RECIST 1.0.
NCT00874614 (4) [back to overview]	Changes From Baseline in Overall Quality of Life (QoL) - Best Response Within 12 Months After First Therapeutic Dose of AZEDRA®.
NCT00874614 (4) [back to overview]	Overall Survival
NCT00874614 (4) [back to overview]	Percentage of Patients Who Experienced a 50% or Greater Reduction (Including Discontinuation) of All Antihypertensive Medication(s) Lasting for at Least Six Months.
NCT01175356 (3) [back to overview]	Incidence of Unacceptable Toxicity and Sinusoidal Obstruction Syndrome (SOS), Assessed by Common Terminology Criteria (CTV)v.4.0 for Toxicity Assessment and Grading for I-MIBG
NCT01175356 (3) [back to overview]	Percentage of MIBG Avid Patients Treated With Meta-iodobenxylguanide (MIBG) Labeled With Iodine-131
NCT01175356 (3) [back to overview]	Percentage of MIBG Avid Patients Treated With MIBG Labeled With Iodine-131 and Bu/Mel Chemotherapy
NCT01250912 (3) [back to overview]	Median Segmental MIBG Uptake at 6 Months After Ablation
NCT01250912 (3) [back to overview]	Median Segmental MIBG Uptake at Baseline
NCT01250912 (3) [back to overview]	Comparison of the Percentage of Patients With Scar in Each Segment as Determined by MIBG SPECT Versus Electroanatomic at Baseline
NCT01313936 (3) [back to overview]	Number of Participants With Dose-limiting Toxicity as a Measure of Tolerability
NCT01313936 (3) [back to overview]	Therapeutic Response Rate
NCT01313936 (3) [back to overview]	Changes in Diarrhea
NCT01413503 (1) [back to overview]	Number of Patients With Complete (CR), Partial (PR), or Minor (MR) Response and Without Progressive Disease
NCT01432626 (1) [back to overview]	Number of Participants Who Had an Abnormal Regional Uptake of I-123 mIBG at Baseline (Acute Phase) and the Number of Participants Who Had an Abnormal I-123 mIBG Uptake on Follow up (Recovery Phase)
NCT01936649 (2) [back to overview]	To Assess Test-retest Reproducibility of Iobenguane I 123 Injection Myocardial Uptake in Heart Failure (HF) Participants on Planar Imaging at 3 Hours 50 Minutes Following I.V. Injection of AdreView (Iobenguane I 123 Injection)
NCT01936649 (2) [back to overview]	To Assess the Test-retest Reproducibility of Iobenguane I 123 Injection Myocardial Uptake on Planar Imaging at 15 Minutes Following Administration of AdreView (Iobenguane I 123 Injection)
NCT02035137 (2) [back to overview]	Number of Participants With Grade 3 or Greater Non-hematologic Toxicities
NCT02035137 (2) [back to overview]	Objective Tumor Response After One Course of Therapy
NCT02043899 (3) [back to overview]	Comparison of the Number of Lesions Detected as Positive by [123I]mIBG Planar Scintigraphy Which Are Also Considered Positive With [124I]mIBG PET/CT.
NCT02043899 (3) [back to overview]	Comparison of the Number of Lesions Detected as Positive by [123I]mIBG SPECT Which Are Also Considered Positive With [124I]mIBG PET/CT.
NCT02043899 (3) [back to overview]	Determining the Causality of Each Adverse Event to [124I]mIBG and Grading Severity According to National Cancer Institute Common Toxicity Criteria for Adverse Events (NCI CTCAE) Version 4.02.
NCT02656329 (9) [back to overview]	All-cause Mortality
NCT02656329 (9) [back to overview]	Percentage of Participants With All-Cause Hospitalization
NCT02656329 (9) [back to overview]	Percentage of Participants With Cardiac Death
NCT02656329 (9) [back to overview]	Percentage of Participants With Events (Composite of the Occurrence of Resuscitated Life-Threatening Ventricular Tachycardia, Unstable Ventricular Tachyarrhythmias, Sudden Cardiac Death [SCD] and Resuscitated Cardiac Arrest)
NCT02656329 (9) [back to overview]	Percentage of Participants With Hospitalization for Cardiovascular Cause
NCT02656329 (9) [back to overview]	Percentage of Participants With Implantable Cardioverter Defibrillator (ICD) Implantation
NCT02656329 (9) [back to overview]	Percentage of Participants With Syncope
NCT02656329 (9) [back to overview]	Percentage of Participants With Events of Complications of Device
NCT02656329 (9) [back to overview]	Percentage of Participants With Events of Complications of Device: H/M >=1.6 in Full Analysis Set

Relationship Between the Occurrence of Adverse Cardiac Event and 123I-mIBG Uptake on Planar Scintigraphy Categorized as High or Low Heart to Mediastinum (H/M) Ratio

H/M ratio for 123I-mIBG uptake at 3 hours 50 minutes post administration was calculated by dividing the counts/pixel in the total myocardium region of interest (ROI) by the counts/pixel in the 7x7 pixel mediastinal ROI. Assessments were done by 3 independent readers. H/M ratios were categorized as 'Low' and 'High' based on being <1.6 or ≥1.6 respectively. The efficacy of 123I-mIBG was based on the prognostic value of the imaging data collected relative to time to adverse cardiac events. (NCT00126425)
Timeframe: Approximately 24 months from the date of administration of 123I-mIBG

Intervention	number of adverse cardiac events (Number)
	Reader A (n=115, 401)	Reader B (n=115, 403)	Reader C (n=116, 402)
AdreView-Heart Failure Group With High H/M Ratio	14	14	14
AdreView-Heart Failure Group With Low H/M Ratio	100	100	100

Intervention	number of adverse cardiac events (Number)
	Reader A (n=86, 355)	Reader B (n=86, 358)	Reader C (n=86, 352)
AdreView-Heart Failure Group With High H/M Ratio	11	11	11
AdreView-Heart Failure Group With Low H/M Ratio	111	113	112

Intervention	months (Median)
At Least One Therapeutic Dose of AZEDRA®	37
Two Therapeutic Doses of AZEDRA®	44

Intervention	Participants (Count of Participants)
	Basal Anterior	basal Anteroseptal	Basal Inferoseptal	Basal Inferior	Basal Anterolateral	Mid Anterior	Mid Anteroseptal	Mid Inferoseptal	Mid Inferior	Mid Inferolateral	Mid Anterolateral	Apical Anterior	Apical Septal	Apical Inferior	Apical Lateral	Apex
Electroanatomic Imaging Assessment	4	4	9	10	13	6	6	11	13	10	4	4	9	11	8	8
MIBG/SPECT	2	1	11	18	16	2	3	14	15	13	3	2	12	14	11	11

Intervention	Participants (Count of Participants)
	Diarrhoea (any grade)	Diarrhoea (> grade 2)
Heterozygous UGT1A1*28 Genotype	5	0
Homozygous UGT1A1*28 Genotype	4	0
Homozygous Wildtype	8	2

Intervention	participants (Number)
	Abnormal at baseline (acute phase)	Abnormal at follow up (recovery phase)
Stress Induced Cardiomyopathy Patients	3	1

Intervention	Ratio (Mean)
	Technologist A (post dosing-1) (n=46)	Technologist A (post dosing-2) (n=47)	Technologist A(Dosings:absolute difference) (n=46)	Technologist B (post dosing-1) (n=47)	Technologist B (post dosing-2) (n=47)	Technologist B(Dosings:absolute difference) (n=47)	Technologist C (post dosing-1) (n=47)	Technologist C (post dosing-2) (n=47)	Technologist C(Dosings:absolute difference) (n=47)	Average (post dosing-1) (n=47)	Average (post dosing-2) (n=47)	Average (Dosings:absolute difference) (n=47)
AdreView (Iobenguane I 123 Injection)	1.435	1.422	0.070	1.430	1.436	0.060	1.427	1.441	0.067	1.429	1.433	0.065

Intervention	Ratio (Mean)
	Technologist A (post dosing-1) (n=47)	Technologist A (post dosing-2) (n=47)	Technologist A(Dosings:absolute difference) (n=47)	Technologist B (post dosing-1) (n=47)	Technologist B (post dosing-2) (n=47)	Technologist B(Dosings:absolute difference) (n=47)	Technologist C (post dosing-1) (n=47)	Technologist C (post dosing-2) (n=47)	Technologist C(Dosing:absolute difference) (n=47)	Average (post dosing-1) (n=47)	Average (post dosing-2) (n=47)	Average (Dosings:absolute difference) (n=47)
AdreView (Iobenguane I 123 Injection)	1.584	1.567	0.081	1.568	1.553	0.062	1.593	1.571	0.071	1.581	1.564	0.072

Intervention	Participants (Count of Participants)
Single-Agent 131I-MIBG	7
131I-MIBG With Vincristine/Irinotecan	17
131I-MIBG With Vorinostat	12

Intervention	Lesions (Number)
	Number of positive lesions observed using [124I]mIBG PET/CT	Number of positive lesions observed using [123I]mIBG planar scintigraphy
Single Arm Trial	714	405

Intervention	Lesions (Number)
	Number of positive skeletal lesions observed using [124I]mIBG PET/CT	Number of positive skeletal lesions observed using [123I]mIBG SPECT/CT	Number of positive soft tissue lesions observed using [124I]mIBG PET/CT	Number of positive soft tissue lesions observed using [123I]mIBG SPECT/CT
Single Arm Trial	421	249	132	64

Intervention	number of DLTs (Number)
11.2 mCi Group	0
15.5 mCi Group	0
18.2 mCi Group	0

Intervention	Gy (Mean)
	Kidney	Liver	Lungs
Ultratrace™ Iobenguane I 131	16.7	12.7	11.1

Intervention	Events (Number)
	All AEs	Pretreatment AEs (occurring before [123I]mIBG administration)	Treatment Emergent AEs (occurring following [123I]mIBG administration)	SAEs	[123I]mIBG Related AEs	[124I]mIBG Related AEs
Single Arm Trial	25	16	9	3	0	0

Intervention	percentage of participants (Number)
	Hospitalization/death	Complications of long-term device therapy	Complications of device
AdreView™	4.9	4.3	5.5
Standard of Care	3.8	6.4	6.4

3-iodobenzylguanidine

Description

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Clinical Trials (58)

Trial Overview

Trial Outcomes

Relationship Between the Occurrence of Adverse Cardiac Event and 123I-mIBG Uptake on Planar Scintigraphy Categorized as High or Low Heart to Mediastinum (H/M) Ratio

Relationship Between the Occurrence of Adverse Cardiac Event and 123I-mIBG Uptake on Planar Scintigraphy Categorized as High or Low Heart to Mediastinum (H/M) Ratio

MTD of Ultratrace Iobenguane I 131

Dose Limiting Toxicities

Maximum Tolerated Dose

Overall Objective Tumor Response Post Therapeutic Treatment

Quality of Life

Tumor Response in CT/MRI Lesions Post Therapeutic Treatment

Dosimetric Estimation of Radiation Absorbed Doses to Measurable Lesions

Best Confirmed Overall Tumor Response of Complete Response (CR) or Partial Response (PR) by RECIST 1.0.

Changes From Baseline in Overall Quality of Life (QoL) - Best Response Within 12 Months After First Therapeutic Dose of AZEDRA®.

Overall Survival

Percentage of Patients Who Experienced a 50% or Greater Reduction (Including Discontinuation) of All Antihypertensive Medication(s) Lasting for at Least Six Months.

Incidence of Unacceptable Toxicity and Sinusoidal Obstruction Syndrome (SOS), Assessed by Common Terminology Criteria (CTV)v.4.0 for Toxicity Assessment and Grading for I-MIBG

Percentage of MIBG Avid Patients Treated With Meta-iodobenxylguanide (MIBG) Labeled With Iodine-131

Percentage of MIBG Avid Patients Treated With MIBG Labeled With Iodine-131 and Bu/Mel Chemotherapy

Median Segmental MIBG Uptake at 6 Months After Ablation

Median Segmental MIBG Uptake at Baseline

Comparison of the Percentage of Patients With Scar in Each Segment as Determined by MIBG SPECT Versus Electroanatomic at Baseline

Number of Participants With Dose-limiting Toxicity as a Measure of Tolerability

Therapeutic Response Rate

Changes in Diarrhea

Number of Patients With Complete (CR), Partial (PR), or Minor (MR) Response and Without Progressive Disease

Number of Participants Who Had an Abnormal Regional Uptake of I-123 mIBG at Baseline (Acute Phase) and the Number of Participants Who Had an Abnormal I-123 mIBG Uptake on Follow up (Recovery Phase)

To Assess Test-retest Reproducibility of Iobenguane I 123 Injection Myocardial Uptake in Heart Failure (HF) Participants on Planar Imaging at 3 Hours 50 Minutes Following I.V. Injection of AdreView (Iobenguane I 123 Injection)

To Assess the Test-retest Reproducibility of Iobenguane I 123 Injection Myocardial Uptake on Planar Imaging at 15 Minutes Following Administration of AdreView (Iobenguane I 123 Injection)

Number of Participants With Grade 3 or Greater Non-hematologic Toxicities

Objective Tumor Response After One Course of Therapy

Comparison of the Number of Lesions Detected as Positive by [123I]mIBG Planar Scintigraphy Which Are Also Considered Positive With [124I]mIBG PET/CT.

Comparison of the Number of Lesions Detected as Positive by [123I]mIBG SPECT Which Are Also Considered Positive With [124I]mIBG PET/CT.

Determining the Causality of Each Adverse Event to [124I]mIBG and Grading Severity According to National Cancer Institute Common Toxicity Criteria for Adverse Events (NCI CTCAE) Version 4.02.

All-cause Mortality

Percentage of Participants With All-Cause Hospitalization

Percentage of Participants With Cardiac Death

Percentage of Participants With Events (Composite of the Occurrence of Resuscitated Life-Threatening Ventricular Tachycardia, Unstable Ventricular Tachyarrhythmias, Sudden Cardiac Death [SCD] and Resuscitated Cardiac Arrest)

Percentage of Participants With Hospitalization for Cardiovascular Cause

Percentage of Participants With Implantable Cardioverter Defibrillator (ICD) Implantation

Percentage of Participants With Syncope

Percentage of Participants With Events of Complications of Device

Percentage of Participants With Events of Complications of Device: H/M >=1.6 in Full Analysis Set

Related Drugs (402)

Related Conditions (1,022)