ライフサイエンスコーパス: DOTA

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

2 DOTA-antibody constructs were labeled to a wide range of

3 DOTA-E-[c(RGDfK)]2 was radiolabeled with (111)In ((111)I

4 DOTA-E-[c(RGDfK)]2 was radiolabeled with (111)In ((111)I

5 DOTA-human IgG (hIgG) was also prepared as a control, wh

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

7 DOTA-Z09591 was stably labeled with (111)In with preserv

8 [DOTA]LTT-SS28 exhibited a pansomatostatin-like profile b

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

10 lododecane-1,4,7,10-tetraacetic acid (In-111-DOTA) accumulate within target cells due to the residual

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

12 In conclusion, the somatostatin mimic [111In-DOTA]LTT-SS28 specifically localizes in sst2-, sst3-, an

13 Radioligand [111In-DOTA]LTT-SS28 showed good stability in the mouse bloodst

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

15 diHSG peptide (RDC018) equipped with both a DOTA chelate for radiolabeling purposes and a fluorophor

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

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

18 Radiolabeling of a DOTA-folate conjugate (cm09) was performed at 95 degrees

19 An in vivo proof-of-concept study using a DOTA-folate conjugate demonstrated the excellent feature

20 rein, we present a novel strategy in which a DOTA-folate conjugate with an albumin-binding entity (cm

21 ed (177)Lu- or (90)Y-anti-CD45 antibody (Ab; DOTA-30F11) was administered by tail vein injection to a

22 Affibody-based construct, ZHER2:2891-ABD035-DOTA (ABY-027), was created by fusion of the reengineere

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

24 aazacyclododecane-1,4,7,10-tetraacetic acid (DOTA) at the N-terminus of GRP(13/14/17/18-27) fragments

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

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

27 acyclod odecane-1,4,7-triyl) triacetic acid (DOTA-NHS-ester) and subsequently tagged with Eu.

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

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

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

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

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

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

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

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

36 Although DOTA-Sug-hAb47 demonstrated the highest receptor binding

37 TA(3), PCTA(4), Oxo-DO3A(5), CB-TE2A(6), and DOTA(7), in an effort to determine which provides the mo

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

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

40 s-hAb47, DOTA-Cys-hAb47, DOTA-Sug-hAb47, and DOTA-Lys-hAb131, respectively).

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

42 8.5 MBq of the (90)Y-labeled GRPr antagonist DOTA-AR and underwent in vivo and ex vivo CLI at 1-48 h

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

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

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

46 ed with lanthanide metals using bifunctional DOTA-based (1,4,7,10-tetraazacyclododecane-1,4,7,10-tetr

47 The chelator DOTA was used in all cases.

48 proach, a model Eu(DOTA-tetraamide) complex (DOTA = 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacet

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

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

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

52 2)=21.3h), whereas surface-conjugated (64)Cu-DOTA cleared only slightly faster and non-significantly,

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

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

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

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

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

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

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

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

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

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

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

64 e response to radioimmunotherapy with (64)Cu-DOTA-cetuximab in KRAS-mutated HCT116 tumor-bearing mice

65 ion of (64)Cu from (64)Cu-acetate and (64)Cu-DOTA-cetuximab to the tumor cell nuclei.

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

67 rafts, both (64)Cu-DOTA-Lys-hAb47 and (64)Cu-DOTA-Cys-hAb47 demonstrated prominent tumor accumulation

68 The (64)Cu-DOTA-DAPTA tracer showed specific PET imaging of CCR5 in

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

70 The targeted (64)Cu-DOTA-DAPTA-comb nanoparticles showed extended blood sign

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

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

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

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

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

76 Moreover, (64)Cu-DOTA-Lys-hAb131 (29.48 +/- 2.60 %ID/g) demonstrated sign

77 (64)Cu-DOTA-Lys-hAb131 was also found to specifically accumulat

78 In HT29 xenografts, both (64)Cu-DOTA-Lys-hAb47 and (64)Cu-DOTA-Cys-hAb47 demonstrated pr

79 y higher HT29 tumor accumulation than (64)Cu-DOTA-Lys-hAb47.

80 In contrast, (64)Cu-DOTA-Lys-hIgG had a low tumor accumulation, thus demonst

81 average, tumor uptake was similar for (64)Cu-DOTA-trastuzumab and (18)F-FDG (SUVmax and range, 8.1 an

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

83 45-mg trastuzumab predose provides a (64)Cu-DOTA-trastuzumab biodistribution favorable for tumor ima

84 this study was to evaluate PET/CT of (64)Cu-DOTA-trastuzumab for detecting and measuring tumor uptak

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

86 For 6 of the 8 patients, (64)Cu-DOTA-trastuzumab injection (364-512 MBq, 5 mg of trastuz

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

88 -25 (day 1) and 47-49 (day 2) h after (64)Cu-DOTA-trastuzumab injection.

89 -25 (day 1) and 47-49 (day 2) h after (64)Cu-DOTA-trastuzumab injection.

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

91 (64)Cu-DOTA-trastuzumab PET/CT warrants further evaluation for

92 (64)Cu-DOTA-trastuzumab visualizes HER2-positive metastatic bre

93 ed, and estimated radiation dose from (64)Cu-DOTA-trastuzumab was similar to (18)F-FDG.

94 (64)Cu-DOTA-vMIP-II exhibited fast in vivo pharmacokinetics wit

95 dentified chemokine receptor-mediated (64)Cu-DOTA-vMIP-II uptake and verified the presence of 8 chemo

96 (64)Cu-DOTA-vMIP-II was proven a sensitive and useful PET imagi

97 icantly less tracer accumulation than (64)Cu-DOTA-vMIP-II, with no difference observed between injury

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

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

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

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

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

103 tic acid 1-(2,5-dioxo-1-pyrrolidinyl) ester (DOTA-NHS) to the surface of a water-soluble glycol chito

104 To demonstrate this approach, a model Eu(DOTA-tetraamide) complex (DOTA = 1,4,7,10-tetraazacyclod

105 hich turns on upon DNA intercalation, and Eu-DOTA-Phen, which turns off.

106 , 98.93% +/- 3.75%, and 82.09% +/- 4.14% for DOTA-Lys-hAb47, DOTA-Cys-hAb47, DOTA-Sug-hAb47, and DOTA

107 Furthermore, [DOTA]LTT-SS28 behaved as an agonist at hsst2, hsst3, and

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

109 ostatin receptor PET tracers such as [(68)Ga-DOTA,1-Nal(3)]-octreotide ((68)Ga-DOTANOC) and [(68)Ga-D

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

111 (3)]-octreotide ((68)Ga-DOTANOC) and [(68)Ga-DOTA,Tyr(3)]-octreotate ((68)Ga-DOTATATE) have shown pro

112 simetry of (68)Ga-bombesin antagonist (68)Ga-DOTA-4-amino-1-carboxymethylpiperidine-d-Phe-Gln-Trp-Ala

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

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

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

116 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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

132 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.

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

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

135 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

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

137 Gd-DOTA-PE nanoparticles had an ionic r1 of 13.3 L . mmol(-

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

139 m tetraazacyclododecane tetraacetic acid (Gd-DOTA) phosphatidylethanolamine (PE) into the surfactant

140 A-PE nanoparticles (n = 4) or nontargeted Gd-DOTA-PE nanoparticles (n = 4).

141 mplantation by using alphavbeta3-targeted Gd-DOTA-PE nanoparticles (n = 4) or nontargeted Gd-DOTA-PE

142 surface volume with alphavbeta3-targeted Gd-DOTA-PE nanoparticles and 3.0% +/- 0.3 with alphavbeta3-

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

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

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

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

147 the same time, the CE-MRI of kidney with Gd-DOTA showed significantly improved signal enhancement fo

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

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

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

151 /- 4.14% for DOTA-Lys-hAb47, DOTA-Cys-hAb47, DOTA-Sug-hAb47, and DOTA-Lys-hAb131, respectively).

152 5%, and 82.09% +/- 4.14% for DOTA-Lys-hAb47, DOTA-Cys-hAb47, DOTA-Sug-hAb47, and DOTA-Lys-hAb131, res

153 ibe the Ugi-assisted synthesis of [I-125]HIP-DOTA, a 4-hydroxy-3-iodophenyl (HIP) derivative of DOTA,

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

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

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

157 140-fold lower renal uptake than the (111)In-DOTA label at 4 after injection.

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

159 (111)In-DOTA-(betaAla)2-JMV594 achieved the highest tumor values

160 The amount of intact [(111)In-DOTA-Ala(1)]SS14 detected in the mouse circulation at 5

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

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

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

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

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

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

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

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

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

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

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

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

173 The dissociation constant for (111)In-DOTA-Z09591 binding to U-87 MG cells was determined to b

174 7 MG xenografts, the tumor uptake of (111)In-DOTA-Z09591 was 7.2 +/- 2.4 percentage injected dose per

175 U-87 MG glioblastoma cell line using (111)In-DOTA-Z09591 was evaluated in vitro and in vivo.

176 PC-3 xenografts in SCID mice, with [(111)In-DOTA]GRP(17-27) exhibiting the most favorable pharmacoki

177 The shorter chain [(111)In-DOTA]GRP(17/18-27) analogs showed higher metabolic stabi

178 ually impressive increase in intact [(111)In-DOTA]MG11 levels in the mouse bloodstream-from less than

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

180 Trp-Ala-Val-Gly-His-Sta-Leu-NH2], JMV4168 is DOTA-betaAla-betaAla-[H-D-Phe-Gln-Trp-Ala-Val-Gly-His-St

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

182 that nuclear localization of (64)Cu-labeled DOTA-cetuximab was enhanced in p53 wild-type tumor cells

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

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

185 of ICPMS together with the specificity of Ln-DOTA-Dimedone and Ln-MeCAT toward sulfenic acid and thio

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

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

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

189 in patients with NETs treated with [(177)Lu-DOTA(0),Tyr(3)]octreotate ((177)Lu-octreotate).

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

191 a single treatment or combined with [(177)Lu-DOTA,Tyr3]octreotate ((177)Lu-DOTATATE), where the latte

192 /s/cm(2)/sr for (90)Y-DOTA-30F11 and (177)Lu-DOTA-30F11, respectively, compared with undetectable sig

193 injection of approximately 1 GBq of (177)Lu-DOTA-[Cpa-c(DCys-Aph(Hor)-DAph(Cbm)-Lys-Thr-Cys)-DTyr-NH

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

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

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

197 s to investigate the distribution of (177)Lu-DOTA-BR96 monoclonal antibodies targeting the Lewis Y an

198 intravenously given 25 or 50 MBq of (177)Lu-DOTA-BR96 per kilogram of body weight and were sacrifice

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

215 (177)Lu-DOTA-JR11 showed a 1.7-10.6 times higher tumor dose than

216 higher tumor-to-organ dose ratio for (177)Lu-DOTA-JR11 than for (177)Lu-DOTATATE was the prerequisite

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

218 Reversible minor adverse effects of (177)Lu-DOTA-JR11 were observed.

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

220 r)-DAph(Cbm)-Lys-Thr-Cys)-DTyr-NH2] ((177)Lu-DOTA-JR11) and (177)Lu-DOTATATE, 3-dimensional voxel dos

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

222 All 4 patients were treated with (177)Lu-DOTA-JR11, resulting in partial remission in 2 patients,

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

224 the prerequisite for treatment with (177)Lu-DOTA-JR11.

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

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

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

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

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

230 61, and 71 d for the control group, (177)Lu-DOTA-octreotate group, and the (177)Lu-DOTA-JR11-treated

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

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

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

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

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

236 to explore the clinical response to (177)Lu-DOTA-rituximab in the treatment of patients with relapse

237 strate the safety and feasibility of (177)Lu-DOTA-rituximab treatment for the lymphoma entities teste

238 The MTD using (177)Lu-DOTA-rituximab was 1,665 MBq/m(2) of BSA.

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

240 trastuzumab compared to (111)In- and (177)Lu-DOTA-trastuzumab, with increased tumor uptake and higher

241 mpared to 0.93-0.95 for (111)In- and (177)Lu-DOTA-trastuzumab.

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

243 cteriophage P22, equipped with a luminescent DOTA[Tb(3+)] macrocyclic complex and a sensitizing trypt

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

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

246 is study, we present the somatostatin mimic [DOTA]LTT-SS28 {[(DOTA)Ser1,Leu8,D-Trp22,Tyr25]SS28} and

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

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

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

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

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

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

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

254 For this purpose a novel DOTA-folate conjugate (cm10) with an albumin-binding ent

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

256 Site-specific coupling of DOTA provides a uniform conjugate and creates the potent

257 ly conjugated with a maleimido derivative of DOTA and labeled with (111)In.

258 finity ABD035, and a maleimido-derivative of DOTA was conjugated at the C terminus of the construct.

259 a 4-hydroxy-3-iodophenyl (HIP) derivative of DOTA, and demonstration of its residualizing properties

260 ed representative antibodies with 2 forms of DOTA as well as other chelators as controls.

261 Labeling kinetics of DOTA-antibody constructs linked through a benzyl isothio

262 c at a quality suitable for radiolabeling of DOTA-functionalized biomolecules.

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

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

265 ns (15 min, RT, ~94-95%) than those based on DOTA-trastuzumab (60 min, 37 degrees C, ~50-88%).

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

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

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

269 Compared with the previous DOTA derivative, the new (64)Cu probes FBP8 and FBP9 sho

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

271 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

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

273 ent the somatostatin mimic [DOTA]LTT-SS28 {[(DOTA)Ser1,Leu8,D-Trp22,Tyr25]SS28} and its 111In radioli

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

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

276 10 complete responses were observed for the DOTA-PRIT-treated animals within 30 d.

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

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

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

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

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

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

283 chemokine receptors through conjugation with DOTA for (64)Cu radiolabeling and PET.

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

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

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

287 10(3) +/- 7.0 x 10(2) p/s/cm(2)/sr for (90)Y-DOTA-30F11 and (177)Lu-DOTA-30F11, respectively, compare

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

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

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

291 with 800 muCi of anti-CD38 pretargeted (90)Y-DOTA-biotin achieved long-term myeloma-free survival (>7

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

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

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

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

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

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

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

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

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