Discovery of [18F]N-(2-(Diethylamino)ethyl)-6-fluoronicotinamide: A Melanoma Positron Emission Tomography Imaging Radiotracer with High Tumor to Body Contrast Ratio and Rapid Renal Clearance

被引：49

作者：

Greguric, Ivan ^{[1
]}

Taylor, Stephen R. ^{[1
]}

Denoyer, Delphine ^{[2
]}

Ballantyne, Patrice ^{[1
]}

Berghofer, Paula ^{[1
]}

Roselt, Peter ^{[2
]}

Pham, Tien Q. ^{[1
]}

Mattner, Filomena ^{[1
]}

Bourdier, Thomas ^{[1
]}

Neels, Oliver C. ^{[2
]}

Dorow, Donna S. ^{[2
]}

Loc'h, Christian ^{[1
]}

Hicks, Rodney J. ^{[2
]}

Katsifis, Andrew ^{[1
]}

机构：

[1] Australian Nucl Sci & Technol Org, Radiopharmaceut Res Inst, Menai, NSW 2234, Australia

[2] Peter MacCallum Canc Ctr, Ctr Mol Imaging, Melbourne, Vic 3002, Australia

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 2009年 / 52卷 / 17期

关键词：

CUTANEOUS MALIGNANT-MELANOMA; PET;

D O I：

10.1021/jm9008423

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The high melanoma uptake and rapid body clearance displayed by our series of [I-123]liodonicotinamides prompted the development of [F-18]N-(2-(diethylamino)ethyl)-6-fluoronicotinamide ([F-18]2), a novel radiotracer for PET melanoma imaging. Significantly, unlike fluorobenzoates, [F-18]fluorine incorporation on the nicotinamide ring is one step, facile, and high yielding. [F-18]2 displayed high tumor uptake, rapid body clearance via predominantly renal excretion, and is currently being evaluated in preclinical studies for progression into clinical trials to assess the responsiveness of therapeutic agents.

引用

页码：5299 / 5302

页数：4

共 9 条

[1]

Belhocine TZ, 2006, J NUCL MED, V47, P957

[2] Cutaneous malignant melanoma [J].

Cummins, DL ;

Cummins, JM ;

Pantle, H ;

Silverman, MA ;

Leonard, AL ;

Chanmugam, A .

MAYO CLINIC PROCEEDINGS, 2006, 81 (04) :500-507

[3]

Dimitrakopoulou-Strauss A, 2001, J NUCL MED, V42, P248

[4] Design, Synthesis, and Preliminary in Vitro and in Vivo Evaluation of N-(2-diethylaminoethyl)-4-[18F]fluorobenzamide ([18F]-DAFBA): A Novel Potential PET Probe to Image Melanoma Tumors [J].

Garg, Sudha ;

Kothari, Kanchan ;

Thopate, Shankar R. ;

Doke, Aniruddha K. ;

Garg, Pradeep K. .

BIOCONJUGATE CHEMISTRY, 2009, 20 (03) :583-590

[5] Baseline staging in cutaneous malignant melanoma [J].

Hafner, J ;

Schmid, MH ;

Kempf, W ;

Burg, G ;

Künzi, W ;

Meuli-Simmen, C ;

Neff, P ;

Meyer, V ;

Mihic, D ;

Garzoli, E ;

Jungius, KP ;

Siefert, B ;

Dummer, R .

BRITISH JOURNAL OF DERMATOLOGY, 2004, 150 (04) :677-686

[6] Synthesis and evaluation of novel radioiodinated nicotinamides for malignant melanoma [J].

Liu, Xiang ;

Pham, Tien Q. ;

Berghofer, Paula ;

Chapman, Janette ;

Greguric, Ivan ;

Mitchell, Peter ;

Mattner, Filomena ;

Loc'h, Christian ;

Katsifis, Andrew .

NUCLEAR MEDICINE AND BIOLOGY, 2008, 35 (07) :769-781

[7]

MICHELOT JM, 1993, J NUCL MED, V34, P1260

[8] Preparation and biologic evaluation of a novel radioiodinated benzylpiperazine, 123I-MEL037, for malignant melanoma [J].

Pham, Tien Q. ;

Berghofer, Paula ;

Liu, Xiang ;

Greguric, Ivan ;

Dikic, Branko ;

Ballantyne, Patrice ;

Matmer, Filornena ;

Nguyen, Vu ;

Loc'h, Christian ;

Katsifis, Andrew .

JOURNAL OF NUCLEAR MEDICINE, 2007, 48 (08) :1348-1356

[9] Phase 2 clinical study of 123l-N-(2-diethylaminoethyl)-2-iodobenzamide in the diagnostic of primary and metastatic ocular melanoma [J].

Sillaire-Houtmann, I ;

Bonafous, J ;

Veyre, A ;

Mestas, D ;

d'Incan, M ;

Moins, N ;

Kerneny, J ;

Chossat, F ;

Bacin, F .

JOURNAL FRANCAIS D OPHTALMOLOGIE, 2004, 27 (01) :34-39

← 1 →