ライフサイエンスコーパス: DOTA

1 DOTA-alendronate was synthesized, radiolabeled with (64)

2 DOTA-tetrazine was labeled with (111)In and (177)Lu.

3 Gln-Trp-Ala-Val-Gly-His-Sta-Leu-NH2 (RM2, 1; DOTA:1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic

4 Ga (FBP14, 68Ga-NODAGA), 111In (FBP15, 111In-DOTA-MA), or 99mTc (FBP16, 99mTc(CO)3-DETA-PA), respecti

5 e-response study with the beta-emitter 177Lu-DOTA-daratumumab, the lowest tested dose, 1.85 MBq, exte

6 u-Ala-Tyr-Gly-Trp-(N-Me)Nle-Asp-1-Nal-NH(2) (DOTA-MGS5) radiolabeled with (111)In, (68)Ga, and (177)L

7 In contrast, the alpha-emitter 225Ac-DOTA-daratumumab had a dose-dependent effect, in which 0

8 Parallel studies with untargeted 225Ac-DOTA-trastuzumab conferred no improvement over untreated

9 properties of a series of Eu(3+) and Dy(3+) DOTA-tetraamide complexes with four appended primary ami

10 CP1 has three distinct components: a DOTA-Gd(III) chelate that provides the MR signal enhance

11 odium acetate-buffered solution containing a DOTA (1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraaceti

12 c conjugation to a maleimido derivative of a DOTA chelator, enabling radionuclide labeling, (1)(1)(1)

13 a PET imaging surrogate for (225)Ac using a DOTA-based, tumor-targeting alkylphosphocholine (NM600).

14 tial for the clinical translation of (225)Ac-DOTA-MC1RL as a novel therapy for metastatic uveal melan

15 Methods: The (225)Ac-DOTA-MC1RL conjugate was synthesized in high radiochemic

16 den after a single administration of (225)Ac-DOTA-MC1RL in treated mice relative to controls.

17 d to tetraazacyclododecane tetraacetic acid (DOTA) and labeled with copper 64 ((64)Cu) or fluorescent

18 aazacyclododecane-1,4,7,10-tetraacetic acid (DOTA) tetra(glycinate) has a higher reduction potential

19 aazacyclododecane-1,4,7,10-tetraacetic acid (DOTA), and evaluated in the following ways: (a) the affi

20 aazacyclododecane-1,4,7,10-tetraacetic acid (DOTA)-conjugated CCK2R ligands with proline substitution

21 [Ahx]-DOTA)]GIP(1-30)NH2 (EG1), [Lys(16)(Ahx-DOTA)]GIP(1-30)NH2 (EG2), and [Nle(14), Lys(30)(Ahx-DOTA

22 IP(1-30)NH2 (EG2), and [Nle(14), Lys(30)(Ahx-DOTA)]GIP(1-30)NH2 (EG4) were conjugated with Ahx-DOTA v

23 The reference agonist [Nle(14),Lys(40)(Ahx-DOTA)NH2]Ex-4 demonstrated the highest affinity (IC50 =

24 Biodistribution of [Nle(14),Lys(40)(Ahx-DOTA-(68)Ga)NH2]Ex-4 at 1 h after injection demonstrated

25 GLP-1 receptor agonist [Nle(14),Lys(40)(Ahx-DOTA-(68)Ga)NH2]Ex-4.

26 vel PET/CT imaging with [Nle(14),Lys(40)(Ahx-DOTA-(68)Ga)NH2]exendin-4 ((68)Ga-DOTA-exendin-4) is fea

27 ]GIP(1-30)NH2 (EG4) were conjugated with Ahx-DOTA via the Lys(16) and Lys(30) side chains.

28 d peptides [Lys(30)(aminohexanoic acid [Ahx]-DOTA)]GIP(1-30)NH2 (EG1), [Lys(16)(Ahx-DOTA)]GIP(1-30)NH

29 We designed and synthesized an IRDye 650 and DOTA-conjugated GRPr antagonist, HZ220 (DOTA-Lys(IRDye 6

30 -Phe(6), Sta(13)]-BN(6-14)NH2 (DOTA-AR), and DOTA-(4-amino-1-carboxymethyl-piperidine)-[D-Phe(6), Sta

31 ln-Trp-Ala-Val-betaAla-His-Phe-Nle-NH2), and DOTA-MG11 (DOTA-dGlu-Ala-Tyr-Gly-Trp-Met-Asp-Phe-NH2) we

32 8.5 MBq of the (90)Y-labeled GRPr antagonist DOTA-AR and underwent in vivo and ex vivo CLI at 1-48 h

33 stablished statine-based receptor antagonist DOTA-4-amino-1-carboxymethylpiperidine-d-Phe-Gln-Trp-Ala

34 Additionally, imaging of [(213)Bi-DOTA,Tyr(3)]octreotate and (213)Bi-diethylene triamine p

35 earing mouse injected with 3 MBq of [(213)Bi-DOTA,Tyr(3)]octreotate, tumor uptake could be visualized

36 alphaCD11b was conjugated with p-SCN-Bn-DOTA followed by labeling with (64)Cu.

37 The chelator DOTA was used in all cases.

38 The peptide conjugates [DOTA-Ala(1)]SS14 (DOTA-Ala-Gly-c[Cys-Lys-Asn-Phe-Phe-Trp

39 cer, a tailor-made novel naphthyl-containing DOTA-conjugated PSMA inhibitor has been developed.

40 -DOTA may be unstable in vivo whereas (64)Cu-DOTA appears suitable for quantitative imaging.

41 2)=21.3h), whereas surface-conjugated (64)Cu-DOTA cleared only slightly faster and non-significantly,

42 purpose of this study was to evaluate (64)Cu-DOTA-alendronate as a mammary microcalcification-targeti

43 Our long-term goal is to develop (64)Cu-DOTA-alendronate for the detection and noninvasive diffe

44 eeder rats showed specific binding of (64)Cu-DOTA-alendronate in mammary glands and mammary tumors.

45 Conclusion:(64)Cu-DOTA-alendronate is a promising PET imaging agent for th

46 The highest uptake of (64)Cu-DOTA-alendronate was in malignant tumors and the lowest

47 Results:(64)Cu-DOTA-alendronate was radiolabeled with a 98% yield.

48 o evaluate the efficacy and safety of (64)Cu-DOTA-alendronate.

49 We generated a (64)Cu-DOTA-anti-periostin-F(ab')2 with a dissociation constant

50 e the extent of the antibody fragment (64)Cu-DOTA-B-Fab binding specificity.

51 (64)Cu-DOTA-B-Fab is a stable and effective immuno-PET tracer f

52 The antibody fragment (64)Cu-DOTA-B-Fab was more than 95% stable after 24 hours in hu

53 u-DOTA-DAPTA-comb in C57BL/6 mice and (64)Cu-DOTA-comb in ApoE(-/-) mice verified low nonspecific nan

54 The assessment of (64)Cu-DOTA-DAPTA-comb in C57BL/6 mice and (64)Cu-DOTA-comb in

55 e; P = .002), which was detected with (64)Cu-DOTA-ECL1i by using autoradiography.

56 Conclusion (64)Cu-DOTA-ECL1i is a promising tool for PET-based detection o

57 Results: (64)Cu-DOTA-ECL1i showed sensitive and specific detection of CC

58 aphy demonstrated specific binding of (64)Cu-DOTA-ECL1i to CCR2 in both rat and human aortic tissues.

59 This work establishes the utility of (64)Cu-DOTA-ECL1i to image CCR2+ monocytes and macrophages in m

60 tron emission tomography radiotracer ((64)Cu-DOTA-ECL1i).

61 nd autoradiography (n = 6, COPD) with (64)Cu-DOTA-ECL1i.

62 formed after intravenous injection of (64)Cu-DOTA-ECL1i.

63 at 1 hour post tail vein injection of (64)Cu-DOTA-ECL1i.

64 Methods: (64)Cu-DOTA-extracellular loop 1 inverso (ECL1i) PET was used t

65 Recently, we showed that (64)Cu-DOTA-labeled PET probes based on fibrin-specific peptide

66 relationship between tumor uptake of (64)Cu-DOTA-trastuzumab as measured by PET/CT and standard, imm

67 By 1 d after injection, uptake of (64)Cu-DOTA-trastuzumab in MBC is strongly associated with pati

68 Eighteen patients underwent (64)Cu-DOTA-trastuzumab injection, preceded in 16 cases by tras

69 -25 (day 1) and 47-49 (day 2) h after (64)Cu-DOTA-trastuzumab injection.

70 and HER2- groups, suggests a role for (64)Cu-DOTA-trastuzumab PET/CT in optimizing treatments that in

71 magnetic resonance imaging (MRI) and (64)Cu-DOTA-trastuzumab positron emission tomography (PET) are

72 here of the chelates (52)Mn-DOTA and (64)Cu-DOTA.

73 [(64)Cu]PCTA, [(64)Cu]Oxo-DO3A, and [(64)Cu]DOTA chelates in vivo.

74 mAb-based newly developed PET tracer [(64)Cu]DOTA-JF5 distinguished IPA from bacterial lung infection

75 Administration of a [(64)Cu]DOTA-labeled A. fumigatus-specific monoclonal antibody (

76 of two MRI contrast agents (Gd-BOPTA and Dy-DOTA-azide) in a mouse glioma model.

77 2)-(CH2)2-CH3 (RM7, 2), and the methyl ester DOTA-4-amino-1-carboxymethylpiperidine-d-Phe-Gln-Trp-Ala

78 longated with respective chelators (NODA-GA, DOTA) for (68)Ga-labeling or propargylglycine for (18)F-

79 tron emission tomography radiotracer ((68)Ga-DOTA [1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraaceti

80 range, 43-81 y) who underwent hybrid (68)Ga-DOTA PET/MRI at 3 T between January 2017 and July 2019 m

81 (68)Ga-DOTATOC, (68)Ga-DOTATATE, and [(68)Ga-DOTA,1-Nal(3)]octreotide ((68)Ga-DOTANOC), plays an impo

82 in vivo tumor accumulation similar to (68)Ga-DOTA-AR (4.63 +/- 0.31 vs. 4.07 +/- 0.29 percentage inje

83 ayed a higher kidney uptake than both (68)Ga-DOTA-AR and (68)Ga-DOTA-RM2 (16.9 +/- 6.5 vs. 4.48 +/- 1

84 ed selective uptake of (68)Ga-P03034 ((68)Ga-DOTA-dPEG2-Lys-Arg-Pro-Hyp-Gly-Cha-Ser-Pro-Leu) in B1R-p

85 yp-Gly-Igl-Ser-D-Igl-Oic) and Z02090 ((68)Ga-DOTA-dPEG2-Lys-Lys-Arg-Pro-Hyp-Gly-Cpg-Ser-D-Tic-Cpg) de

86 Ga-P03034 with (68)Ga-labeled P04158 ((68)Ga-DOTA-dPEG2-Lys-Lys-Arg-Pro-Hyp-Gly-Igl-Ser-D-Igl-Oic) an

87 line lung tumor volume addressed with (68)Ga-DOTA-E-[c(RGDfK)](2) PET/CT correlated with serum vascul

88 Conclusion:(68)Ga-DOTA-E-[c(RGDfK)](2) PET/CT is a potentially useful tool

89 All patients underwent PET/CT with (68)Ga-DOTA-E-[c(RGDfK)](2) radiotracer and blood-sample tests

90 New radiotracers, such as (68)Ga-DOTA-E-[c(RGDfK)](2), that target alphavbeta3 integrin m

91 Therefore, (68)Ga-DOTA-E-[c(RGDfK)]2 can safely be used for imaging integr

92 and estimate the radiation dose from (68)Ga-DOTA-E-[c(RGDfK)]2 using whole-body PET scans in humans.

93 measurements with cyclic-RGD peptide (68)Ga-DOTA-E[c(RGDfK)](2) After the last (68)Ga-DOTA-E[c(RGDfK

94 Results: The ex vivo uptake of (68)Ga-DOTA-E[c(RGDfK)](2) in the mouse skin and tumor was sign

95 PET imaging with (68)Ga-DOTA-E[c(RGDfK)](2) peptide at day 10 after inoculation

96 Ga-DOTA-E[c(RGDfK)](2) After the last (68)Ga-DOTA-E[c(RGDfK)](2) peptide PET/CT, tumors were cut into

97 (3)-selective cyclic, dimeric peptide (68)Ga-DOTA-E[c(RGDfK)](2), where E[c(RGDfk)](2) = glutamic aci

98 te the sensitivity and specificity of (68)Ga-DOTA-ECL1i in the mouse heart and highlight the translat

99 (68)Ga-DOTA-ECL1i signal localized to sites of tissue injury an

100 Autoradiography demonstrated that (68)Ga-DOTA-ECL1i specifically binds human heart failure specim

101 (68)Ga-DOTA-ECL1i uptake was associated with CCR2+ monocyte and

102 (64)Cu- and (68)Ga-DOTA-ECL1i were compared in an ischemia-reperfusion inju

103 , with efficacy comparable to that of (68)Ga-DOTA-ECL1i.

104 (68)Ga-DOTA-exendin-4 PET/CT and (111)In-DOTA-exendin-4 SPECT/C

105 (68)Ga-DOTA-exendin-4 PET/CT correctly identified the insulinom

106 liminary data suggest that the use of (68)Ga-DOTA-exendin-4 PET/CT in detecting hidden insulinomas is

107 nt refused surgery despite a positive (68)Ga-DOTA-exendin-4 PET/CT scan.

108 ys(40)(Ahx-DOTA-(68)Ga)NH2]exendin-4 ((68)Ga-DOTA-exendin-4) is feasible and sensitive in detecting b

109 r injection, (68)Ga-NOTA-HACA-PD1 and (68)Ga-DOTA-HACA-PD1 exhibited promising target-to-background r

110 Similar results were observed for (68)Ga-DOTA-MGS5 incubated up to 4 h.

111 neoplasia and positive for uptake on (68)Ga-DOTA-octreotate ((68)Ga-DOTATATE) PET/CT underwent seria

112 eceptor (GRPR) antagonist (68)Ga-SB3 ((68)Ga-DOTA-p-aminomethylaniline-diglycolic acid-DPhe-Gln-Trp-A

113 ge, 43-81 years), who received hybrid (68)Ga-DOTA-PET/MRI examinations at 3T between January 2017 and

114 ter injection) but lower than that of (68)Ga-DOTA-RM2 (10.4 +/- 0.4 %IA/mL).

115 y uptake than both (68)Ga-DOTA-AR and (68)Ga-DOTA-RM2 (16.9 +/- 6.5 vs. 4.48 +/- 1.63 vs. 5.01 +/- 2.

116 atoid arthritis was studied with both (68)Ga-DOTA-Siglec-9 and (18)F-FDG PET/CT to determine the abil

117 Most importantly, however, (68)Ga-DOTA-Siglec-9 was comparable to (18)F-FDG in detecting a

118 (68)Ga-DOTA-Siglec-9 was rapidly cleared from the blood circula

119 Conclusion: Intravenous injection of (68)Ga-DOTA-Siglec-9 was safe and biodistribution was favorable

120 Results: (68)Ga-DOTA-Siglec-9 was well tolerated by all subjects.

121 The effective radiation dose of (68)Ga-DOTA-Siglec-9 was within the same range as the effective

122 Injection of 150 MBq of (68)Ga-DOTA-Siglec-9 would expose a subject to 3.3 mSv.

123 A (68)Ga-labeled peptide of Siglec-9, (68)Ga-DOTA-Siglec-9, holds promise as a novel PET tracer for i

124 the possible repeated clinical use of (68)Ga-DOTA-Siglec-9, such as in trials to elucidate the treatm

125 avenous injection of 162 +/- 4 MBq of (68)Ga-DOTA-Siglec-9.

126 PET/CT with (68)Ga-DOTA-somatostatin analogs has been tested for therapy mo

127 my or biopsy), EUS, CT or MRI, and/or (68)Ga-DOTA-TATE PET/CT.

128 zation, and tumor cytopenia on repeat (68)Ga-DOTA-TATE positron emission tomography (PET) within 6 mo

129 of pre-therapeutic and early interim (68)Ga-DOTA-Tyr3-octreotide ((68)Ga-DOTATOC) positron emission

130 e fully engineered molecule (111)In/(6)(8)Ga-DOTA-(HE)3-ADAPT6 was specifically bound and taken up by

131 tion of 50% [IC50], 21.4 +/- 7.4 nM) than Ga-DOTA-AR (IC50, 0.48 +/- 0.18 nM) or Ga-HZ219 (IC50, 0.69

132 hesized a new liposome containing gadolinium-DOTA lipid bilayer, as a targeting multimodal molecular

133 RI) contrast agent, CREKA-Tris(Gd-DOTA)3 (Gd-DOTA (4,7,10-tris(carboxymethyl)-1,4,7,10-tetraazacyclod

134 magnetic contrast such as gadoteric acid (Gd-DOTA) administration into cerebrospinal fluid (CSF) requ

135 lurane and infused paramagnetic contrast (Gd-DOTA) into the cisterna magna during dynamic contrast-en

136 revealed impeded glymphatic transport of Gd-DOTA in SHR compared with WKY rats in both age groups, i

137 We observed ventricular reflux of Gd-DOTA in SHR rats only, indicating abnormal CSF flow dyna

138 ice, glymphatic transport and drainage of Gd-DOTA to submandibular and deep cervical lymph nodes was

139 1 mapping which also captures drainage of Gd-DOTA to the cervical lymph nodes.

140 erified increased glymphatic transport of Gd-DOTA transport in mice anesthetized with KX in compariso

141 The Gd-DOTA injection into CSF was performed on the bench after

142 imaging (MRI) contrast agent, CREKA-Tris(Gd-DOTA)3 (Gd-DOTA (4,7,10-tris(carboxymethyl)-1,4,7,10-tet

143 strate that molecular MRI with CREKA-Tris(Gd-DOTA)3 may facilitate early detection of high-risk breas

144 We find that CREKA-Tris(Gd-DOTA)3 provides robust contrast enhancement in the metas

145 re we assess the capability of CREKA-Tris(Gd-DOTA)3 to detect micrometastasis with MRI in co-registra

146 rafts with a fractionated 3-cycle anti-GPA33 DOTA-PRIT regimen (total administered (177)Lu-DOTA-Bn ac

147 ur hypothesis that a fractionated anti-GPA33 DOTA-PRIT regimen calibrated to deliver a radiation abso

148 ese studies support the view that anti-GPA33 DOTA-PRIT will be a potent radioimmunotherapy regimen fo

149 amine-succinyl-glycine [HSG]) and the di-HSG-DOTA peptide IMP288.

150 re compared with the GRPr antagonists HZ219, DOTA-PEG4-[D-Phe(6), Sta(13)]-BN(6-14)NH2 (DOTA-AR), and

151 and DOTA-conjugated GRPr antagonist, HZ220 (DOTA-Lys(IRDye 650)-PEG4-[D-Phe(6), Sta(13)]-BN(6-14)NH2

152 140-fold lower renal uptake than the (111)In-DOTA label at 4 after injection.

153 and site-specifically labeled using (111)In-DOTA or (125)I-iodo-((4-hydroxyphenyl)ethyl) maleimide (

154 We characterized (111)In-DOTA-5D3 by SPECT/CT imaging, tissue biodistribution stu

155 Significant clearance of (111)In-DOTA-5D3 from all organs occurred at 192 h.

156 Distribution of (111)In-DOTA-5D3 in PSMA(+) PC3 PIP tumor peaked at 24 h after i

157 Conclusion: (111)In-DOTA-5D3 is a new radiolabeled antibody for imaging and

158 Results: (111)In-DOTA-5D3 was synthesized with specific activity of appro

159 cell uptake, and internalization of (111)In-DOTA-5D3 were performed by established techniques.

160 Coinjection of (111)In-DOTA-5D3 with a 10- and 50-fold excess of nonradiolabele

161 We reviewed (111)In-DOTA-anti-CD45 antibody (BC8) imaging and bone marrow bi

162 were obtained after infusion of the (111)In-DOTA-BC8 (176-406 MBq) into 52 adult patients with hemat

163 Conclusion: (111)In-DOTA-BC8 had a long retention time in liver, spleen, kid

164 differ significantly (250-280), but (111)In-DOTA-Cys(59)-ADAPT6 provided significantly higher tumor-

165 sulinoma in 4 of 4 patients, whereas (111)In-DOTA-exendin-4 SPECT/CT correctly identified the insulin

166 (111)In-DOTA-exendin-4 SPECT/CT has been shown to be highly effi

167 (68)Ga-DOTA-exendin-4 PET/CT and (111)In-DOTA-exendin-4 SPECT/CT were performed in a randomized c

168 own significantly elevated uptake of (111)In-DOTA-IA in the area of VX2 tumors pretreated by pHIFU co

169 ent 24h after systematic delivery of (111)In-DOTA-IA in VX2 tumors pretreated by pHIFU compared with

170 peptidomimetic integrin antagonist, (111)In-DOTA-IA, was used following pHIFU treatment in our study

171 Tyr(3)-octreotate (SSTR agonist) and (111)In-DOTA-JR11 (SSTR antagonist) to 40 human BC specimens was

172 Results:(111)In-DOTA-JR11 binding to human BC tissue was significantly h

173 in contrast, higher for both of the (111)In-DOTA-labeled ADAPT variants in other organs.

174 Binding of (111)In-DOTA-Tyr(3)-octreotate (SSTR agonist) and (111)In-DOTA-J

175 tissue was significantly higher than (111)In-DOTA-Tyr(3)-octreotate binding (P < 0.001).

176 Cold standards were prepared by incubating DOTA-conjugated peptides with GaCl3.

177 udy, the SSTR2 antagonist OPS201 (DOTA-JR11; DOTA-[Cpa-c(DCys-Aph(Hor)-DAph(Cbm)-Lys-Thr-Cys)-DTyr-NH

178 (68)Ga-labeled DOTA-4-amino-1-carboxymethyl-piperidine-d-Phe-Gln-Trp-Al

179 (68)Ga-labeled DOTA-4-amino-1-carboxymethyl-piperidine-D-Phe-Gln-Trp-Al

180 Methods: (68)Ga-labeled DOTA-conjugated lysine-ureido-glutamate-based PSMA-targe

181 y in uveal melanoma cells, and the lanthanum-DOTA-MC1RL analog was tested for binding affinity.

182 A new metal-containing reagent (Ln-DOTA-Dimedone) devised to react specifically with SA has

183 Lutetium 177 ((177)Lu) DOTA-0-Tyr3-Octreotate (DOTATATE) peptide receptor radio

184 (177)Lu-DOTATOC, respectively) and [(177)Lu-DOTA(0),Tyr(3)]octreotate ((177)Lu-DOTATATE).

185 lvement, neoadjuvant treatment with [(177)Lu-DOTA(0),Tyr(3)]octreotate ((177)Lu-octreotate) may be an

186 [(90)Y-DOTA(0),Tyr(3)]octreotide or [(177)Lu-DOTA(0),Tyr(3)]octreotide ((90)Y- or (177)Lu-DOTATOC, re

187 whether improved minigastrin analog (177)Lu-DOTA-(d-Glu)(6)-Ala-Tyr-Gly-Trp-Nle-Asp-PheNH(2) ((177)L

188 -Phe-NH(2)) and (177)Lu-DOTA-PP-F11 ((177)Lu-DOTA-(dGlu)(6)-Ala-Tyr-Gly-Trp-Met-Asp-Phe-NH(2)), and w

189 bilized analog (177)Lu-DOTA-PP-F11N ((177)Lu-DOTA-(dGlu)(6)-Ala-Tyr-Gly-Trp-Nle-Asp-Phe-NH(2)) perfor

190 OTA-PRIT regimen (total administered (177)Lu-DOTA-Bn activity, 167 MBq/mouse; estimated radiation abs

191 atment groups (i.e., no treatment or (177)Lu-DOTA-Bn only), leading to euthanasia due to excessive tu

192 raazacyclododecane tetraacetic acid ((177)Lu-DOTA-Bn), that leads to high TIs for radiosensitive tiss

193 stability, namely (177)Lu-DOTA-MG11 ((177)Lu-DOTA-dGlu-Ala-Tyr-Gly-Trp-Met-Asp-Phe-NH(2)) and (177)Lu

194 than (177)Lu-DOTA-trastuzumab Fab or (177)Lu-DOTA-EGF.

195 (177)Lu-DOTA-Fab-PEG24-EGF bound specifically to HER2 and EGFR o

196 (177)Lu-DOTA-Fab-PEG24-EGF inhibited tumor growth more effective

197 istant TrR1 tumors were treated with (177)Lu-DOTA-Fab-PEG24-EGF or (111)In-DTPA-Fab-PEG24-EGF at the

198 cells was measured after exposure to (177)Lu-DOTA-Fab-PEG24-EGF or (111)In-DTPA-Fab-PEG24-EGF or to m

199 TrR1 tumors were growth-inhibited by (177)Lu-DOTA-Fab-PEG24-EGF or (111)In-DTPA-Fab-PEG24-EGF.

200 The maximum injected amount of (177)Lu-DOTA-Fab-PEG24-EGF that caused no observable adverse eff

201 The binding of (177)Lu-DOTA-Fab-PEG24-EGF to tumor cells (MDA-MB-231, SK-OV-3,

202 The NOAEL for (177)Lu-DOTA-Fab-PEG24-EGF was 11.1 MBq (10 mug).

203 The tumor uptake of (177)Lu-DOTA-Fab-PEG24-EGF was 2-fold greater than (177)Lu-DOTA-

204 (177)Lu-DOTA-Fab-PEG24-EGF was more cytotoxic than (111)In-DTPA-

205 and normal tissue biodistribution of (177)Lu-DOTA-Fab-PEG24-EGF was studied at 48 h after injection i

206 Biodistribution studies with (177)Lu-DOTA-JR11 (0.5 mug/30 MBq) resulted in the highest tumor

207 tively larger necrotic fractions for (177)Lu-DOTA-JR11 despite further tumor growth.

208 onist (177)Lu-DOTATOC and antagonist (177)Lu-DOTA-JR11 longitudinally in an orthotopic murine pancrea

209 tic agent when labeled with (177)Lu ((177)Lu-DOTA-JR11 or (177)Lu-OPS201).

210 ies with (177)Lu-DOTA-octreotate and (177)Lu-DOTA-JR11 resulted in a tumor growth delay time of 18 +/

211 Cells treated with (177)Lu-DOTA-JR11 showed 2 times more p53-binding protein 1 foci

212 Conclusion: (177)Lu-DOTA-JR11 showed a higher tumor-to-kidney ratio and a mo

213 We found a 5-times-higher uptake of (177)Lu-DOTA-JR11 than of (177)Lu-DOTA-octreotate.

214 ults: Compared with (177)Lu-DOTATOC, (177)Lu-DOTA-JR11 treatment resulted in an increased accumulatio

215 gnificantly lower (P = 0.01) whereas (177)Lu-DOTA-JR11 uptake remained stable.

216 ffect of (177)Lu-DOTA-octreotate and (177)Lu-DOTA-JR11 were performed in this same animal model.

217 MBq of (177)Lu-DOTATOC, or 20 MBq of (177)Lu-DOTA-JR11 with an interval of 3 wk.

218 OTA-octreotate, an SSTR agonist, and (177)Lu-DOTA-JR11, an SSTR antagonist.

219 ast amount of viable tumor tissue in (177)Lu-DOTA-JR11-treated animals, at 6.2% (IQR, 2%-23%).

220 77)Lu-DOTA-octreotate group, and the (177)Lu-DOTA-JR11-treated group, respectively.

221 th (177)Lu-DOTA-Tyr(3)-octreotate or (177)Lu-DOTA-JR11.

222 ic acid, (177)Lu-DOTA-octreotate, or (177)Lu-DOTA-JR11.

223 th varying in vivo stability, namely (177)Lu-DOTA-MG11 ((177)Lu-DOTA-dGlu-Ala-Tyr-Gly-Trp-Met-Asp-Phe

224 ors is as good as the performance of (177)Lu-DOTA-MG11 in the presence of inhibitors.

225 hosphoramidon or thiorphan increases (177)Lu-DOTA-MG11 uptake significantly in the CCK2R(+) tumors an

226 For (177)Lu-DOTA-MGS5, additional metabolic studies were performed o

227 In the blood of mice injected with (177)Lu-DOTA-MGS5, at least 70% intact radiopeptide was detected

228 r extended internal irradiation with (177)Lu-DOTA-octreotate (LuTate) peptide receptor radionuclide t

229 vo growth properties and response to (177)Lu-DOTA-octreotate (LuTate) PRRT to identify models with fe

230 In vivo therapy studies with (177)Lu-DOTA-octreotate and (177)Lu-DOTA-JR11 resulted in a tumo

231 experiments comparing the effect of (177)Lu-DOTA-octreotate and (177)Lu-DOTA-JR11 were performed in

232 61, and 71 d for the control group, (177)Lu-DOTA-octreotate group, and the (177)Lu-DOTA-JR11-treated

233 ly compare the therapeutic effect of (177)Lu-DOTA-octreotate, an SSTR agonist, and (177)Lu-DOTA-JR11,

234 iethylene triamine pentaacetic acid, (177)Lu-DOTA-octreotate, or (177)Lu-DOTA-JR11.

235 otein 1 foci than cells treated with (177)Lu-DOTA-octreotate.

236 uptake of (177)Lu-DOTA-JR11 than of (177)Lu-DOTA-octreotate.

237 ghest tumor radiation dose found for (177)Lu-DOTA-octreotate.

238 a-Tyr-Gly-Trp-Met-Asp-Phe-NH(2)) and (177)Lu-DOTA-PP-F11 ((177)Lu-DOTA-(dGlu)(6)-Ala-Tyr-Gly-Trp-Met-

239 Less profound was the effect on (177)Lu-DOTA-PP-F11, whereas no influence or even reduction was

240 F11N had the same biodistribution as (177)Lu-DOTA-PP-F11; however, uptake in the MZ-CRC-1 tumors was

241 her the chemically stabilized analog (177)Lu-DOTA-PP-F11N ((177)Lu-DOTA-(dGlu)(6)-Ala-Tyr-Gly-Trp-Nle

242 e or even reduction was observed for (177)Lu-DOTA-PP-F11N (20.7 +/- 1.71 vs. 15.6 +/- 3.80 [with phos

243 Autoradiography of (177)Lu-DOTA-PP-F11N (without and with phosphoramidon) and NanoS

244 The first clinical data show high (177)Lu-DOTA-PP-F11N accumulation in tumors, stomach, kidneys, a

245 First human data on (177)Lu-DOTA-PP-F11N are also reported.

246 (177)Lu-DOTA-PP-F11N had the same biodistribution as (177)Lu-DOT

247 SPECT/CT images of (177)Lu-DOTA-PP-F11N in a metastatic MTC patient were also acqui

248 Conclusion: The performance of (177)Lu-DOTA-PP-F11N without protease inhibitors is as good as t

249 ab-PEG24-EGF was 2-fold greater than (177)Lu-DOTA-trastuzumab Fab or (177)Lu-DOTA-EGF.

250 ibution studies after injection with (177)Lu-DOTA-Tyr(3)-octreotate or (177)Lu-DOTA-JR11.

251 novel (177)Lu-labeled conjugate ([(177)Lu]Lu-DOTA-SP714).

252 Results: (nat)Lu-DOTA-PP-F11N is less of a substrate for neprilysins than

253 The tailor-made DOTA-conjugated PSMA inhibitor PSMA-617 presented here i

254 Methods: DOTA-D-Glu-Ala-Tyr-Gly-Trp-(N-Me)Nle-Asp-1-Nal-NH(2) (DO

255 Val-betaAla-His-Phe-Nle-NH2), and DOTA-MG11 (DOTA-dGlu-Ala-Tyr-Gly-Trp-Met-Asp-Phe-NH2) were labeled

256 vivo evaluation, here of the chelates (52)Mn-DOTA and (64)Cu-DOTA.

257 Liposomes with surface-conjugated (52)Mn-DOTA exhibited a significantly shorter plasma half-life

258 mes with (52)Mn, and furthermore that (52)Mn-DOTA may be unstable in vivo whereas (64)Cu-DOTA appears

259 odecane-1,4,7,10-tetraacetic acid monoamide (DOTA-MA), or a diethylenetriamine ligand (DETA-propanoic

260 , DOTA-PEG4-[D-Phe(6), Sta(13)]-BN(6-14)NH2 (DOTA-AR), and DOTA-(4-amino-1-carboxymethyl-piperidine)-

261 piperidine)-[D-Phe(6), Sta(13)]-BN(6-14)NH2 (DOTA-RM2).

262 NeoBOMB1 is a novel DOTA-coupled GRPR antagonist with high affinity for GRPR

263 Conjugation of DOTA and NODAGA chelators at positions Lys(27) and Lys(4

264 usion: The excellent targeting properties of DOTA-MGS5 support future clinical studies evaluating the

265 Mbq/nmol) suitable for the radiolabeling of DOTA-conjugated vectors.

266 microcalcification targeting specificity of DOTA-alendronate and elucidate the histologic and ultras

267 , and the increasing availability and use of DOTA analogs in the therapy of neuroendocrine tumors, we

268 clinical study, the SSTR2 antagonist OPS201 (DOTA-JR11; DOTA-[Cpa-c(DCys-Aph(Hor)-DAph(Cbm)-Lys-Thr-C

269 acyclododecane-1,4,7,10-tetraacetic acid) or DOTA-like chelator-modified peptide.

270 he-Trp-Lys-Thr-Phe-Thr-Ser-Cys]-OH), PanSB1 (DOTA-PEG2-dTyr-Gln-Trp-Ala-Val-betaAla-His-Phe-Nle-NH2),

271 The bombesin-based pseudopeptide DOTA-4-amino-1-carboxymethylpiperidine-d-Phe-Gln-Trp-Ala

272 mitter radioimmunotherapy using radiolabeled DOTA-daratumumab in a preclinical model of disseminated

273 D-Phe(6), Sta(13)]-BN(6-14)NH2), by reacting DOTA-Lys-PEG4-[D-Phe(6), Sta(13)]-BN(6-14)NH2 (HZ219) wi

274 Results: DOTA-MGS5 radiolabeled with (111)In and (177)Lu showed a

275 The peptide conjugates [DOTA-Ala(1)]SS14 (DOTA-Ala-Gly-c[Cys-Lys-Asn-Phe-Phe-Trp-Lys-Thr-Phe-Thr-S

276 It has already been shown that DOTA-bearing FAP inhibitors (FAPIs) generate high-contra

277 The DOTA conjugates were labeled with (111)In and (68)Ga.

278 s: (a) the affinity of the fragments and the DOTA conjugates was measured via flow cytometry, (b) the

279 10 complete responses were observed for the DOTA-PRIT-treated animals within 30 d.

280 Linkage of the DOTA-based LBT to a cysteine residue induces pseudo-cont

281 high affinity and long tumor retention, the DOTA-conjugated ligand PSMA-617 has low kidney uptake, m

282 logic purposes, is frequently made using the DOTA-derived somatostatin analogs DOTATOC or DOTATATE fo

283 bodies by enzymatic digestion, conjugated to DOTA, and labeled with (64)Cu.

284 tibody by enzymatic digestion, conjugated to DOTA, and labeled with (64)Cu.

285 tion of PSMA-targeting ligands conjugated to DOTA-chelates of Europium.

286 th polyethyleneglycol (PEG) chains linked to DOTA for complexing the beta-particle emitter (177)Lu an

287 These immunoconjugates were conjugated with DOTA and radiolabeled with (111)In.

288 Ex(9-39)NH2-based antagonists, modified with DOTA or NODAGA chelators at positions Lys(27) and Lys(40

289 timal doses of 2H7-Fc-C825 followed by (90)Y-DOTA were cured by 150 days, whereas the growth of tumor

290 h radiolabeled sstr agonists, such as [(90)Y-DOTA(0),Tyr(3)]octreotide or [(177)Lu-DOTA(0),Tyr(3)]oct

291 Mice treated with 200 muCi (90)Y-DOTA-30F11 had a median overall survival of 73 days, whi

292 mia-bearing mice treated with 400 muCi (90)Y-DOTA-30F11, CY, and haploidentical BMT were cured and li

293 (90)Y-DOTA-AR concentration in the 3 tumor models ranged from

294 red activity for a therapy infusion of (90)Y-DOTA-BC8 were 0.35 +/- 0.20 cGy/MBq for red marrow, 0.80

295 to 1,200 muCi of anti-CD38 pretargeted (90)Y-DOTA-biotin, including 100% complete remissions (no dete

296 Patients received one cycle of (90)Y-DOTA-epratuzumab on days 1 and 8 (give or take 2 days) s

297 (90)Y-DOTA-epratuzumab radioimmunotherapy is well tolerated.

298 lled anti-CD22 epratuzumab tetraxetan ((90)Y-DOTA-epratuzumab) radioimmunotherapy in refractory or re

299 identify the maximum tolerated dose of (90)Y-DOTA-epratuzumab.

300 the tumor-specific, integrin-targeting (90)Y-DOTA-RGD and the localized activation of Cy7 azide.

301 -bearing mice were injected first with (90)Y-DOTA-RGD, targeting alphavbeta3 integrins, and then with

302 OTA) captured by a very high-affinity anti-Y-DOTA scFv antibody (C825).

303 l trap for a radiolabeled ligand (yttrium[Y]-DOTA) captured by a very high-affinity anti-Y-DOTA scFv