Table 2.

Comparative analysis of paper published with other radiolabelled antibiotics in animals

Type of radiopharmaceutical	Radiopharmaceutical	First author (ref)	Labelling method	Specific activity (MBq/mmol)	Stability		Animal model	Metabolic route
					Saline	Serum
Fluoroquinolones	99mTc-gatifloxacin	M. A. Motaleb [95]	Direct labelling—SnCl2·2H2O	5.45 × 104	81.3 % at 8 h	77.4 % at 24 h	Rat	Liver (+), kidneys (++)
	99mTc-pefloxacin	E. A. El-Ghany [61]	Direct labelling—SnCl2·2H2O	6.53 × 105	96 % at 12 h	n. a.	Mouse	Liver (++)
	99mTc-ofloxacin	M. Erfani [63]	Carbonil core	6.05 × 102	90 % at 6 h	80 % at 6 h	Mouse	Liver (++), kidneys (+)
	99mTc-ofloxacin	M. A. Motaleb [62]	Direct labelling—SnCl2·2H2O	7.02 × 104	96 % at 2 h	n. a.	Rat	Kidneys (++)
	99mTc-lomefloxacin	M. A. Motaleb [62]	Direct labelling—SnCl2·2H2O	5.34 × 104	80 % at 2 h	n. a.	Rat	Kidneys (++)
	99mTc-enrofloxacin	R. H. Siaens [64]	Direct labelling-stannous tartrate	5.76 × 104	n. a.	72 % at 24 h	Rat	Kidneys (++)
	99mTc-enrofloxacin	S. Shahzad [65]	Direct labelling—SnCl2·2H2O	6.5 × 104	98 % at 5 h	98 % at 5 h	Rabbit	Liver (+), kidneys (++)
	99mTc-norfloxacin	I. T. Ibrahim [66]	Direct labelling—SnCl2·2H2O	2.53 × 104	78.6 % at 6 h	84 % at 24 h	Rat	Liver (+), kidneys (++)
	99mTc-norfloxacin	S. I. Sazonova [67]	Direct labelling—SnCl2·2H2O	n. a.	n. a.	91 % at 8 h	Rat	Liver (+), kidneys (++)
	99mTcN-norfloxacin dithiocarbamate	S. Zhang [68]	SnCl2·2H2O, succinic dihydrazide, propylenediamine tetraacetic acid	n. a.	96 % at 6 h	95 % at 6 h	Mouse	Liver (++), kidneys (+)
	99mTc-sparafloxacin	M. A. Motaleb [9]	Direct labelling—SnCl2·2H2O	6.33 × 104	n. a.	75 % at 24 h	Rat	Liver and kidneys
	99mTc-rufloxacin	M. A. Motaleb [71]	Direct labelling—SnCl2·2H2O	2.52 × 103	93.4 % at 8 h	82 % at 24 h	Mouse	Liver (++), kidneys (+)
	18F-fleroxacin	A. J. Fischman [72]	Potassius fluoride	n. a.	n. a.	n. a.	Mouse, rat, rabbit	Intestine (++), liver (+), kidneys (+)
	99mTc-sitafloxacin	S. S. Qaiser [74]	Direct labelling—SnCl2·2H2O	2.17 × 104	87.2 % at 4 h	n. a.	Rat	Liver (+), kidneys (++)
	99mTc-levofloxacin	S. Shahzad [70]	Direct labelling—SnCl2·2H2O	1.35 × 105	98 % at 6 h	98 % at 6 h	Rabbit	Liver (+), kidneys (++)
	99mTcN-sitafloxacin dithiocarbamate	S. S. Qaiser [75]	Direct labelling—SnCl2·2H2O	7.32 × 103	91 % at 4 h	90 % at 4 h	Rat	Liver (+), kidneys (++)
	99mTc-sarafloxacin	M. E. Moustapha [79]	Direct labelling—SnCl2·2H2O	1.47 × 105	65 % at 8 h	85 % at 24 h	Mouse	Liver and kidneys
	99mTc-moxifloxacin	S. Chattopadhyay [76]	Direct labelling—SnCl2·2H2O	1.05 × 104	84 % at 3 h	n. a.	Rat/rabbit	Liver (+), kidneys(++)
	99mTc-gemifloxacin	S. Shahzad [78]	SnCl2·2H2O-D-penicillamine	1.46 × 105	98 % at 6 h	98 % at 6 h	Rabbit	Liver (+), kidneys(++)
	99mTc-gemifloxacin	S. S. Qaiser [77]	Direct labelling—SnCl2·2H2O	2.15 × 104	91 % at 4 h	94 % at 2 h	Rat	Liver and kidneys
Cephalosporins	99mTc-cefazolin	M. El-Tawoosy [80]	Direct labelling—SnCl2·2H2O	1.63 × 105	n. a.	n. a.	Mouse	Liver (++), kidneys (+)
	99mTc-cefuroxime acetil	F. Yurt Lambrecht [81]	Direct labelling—SnCl2·2H2O	3.81 × 104	n. a.	n. a.	Rat	Liver and kidneys
	99mTc-cefuroxime	S. Chattopadhyay [82]	Direct labelling-stannous tartrate	8 × 104	95 % at 5 h	n. a.	Rat	Liver and kidneys
	99mTc-ceftizoxime	V. Gomes Barreto [84]	Na-dithionite	4.38 × 104	n. a.	n. a.	Rat	Kidneys (++)
	99mTc-ceftizoxime	P. H. N. Costa [85]	Na-dithionite	n. a.	n. a.	n. a.	Rat	n. a.
	99mTc-ceftizoxime	L. E. M. Teixeira [86]	Na-dithionite	5.3 × 104	n. a.	n. a.	Rat	n. a.
	99mTc-cefotaxime	S. F. Mirshojaei [87]	Na-dithionite	9.4 × 104	92 % at 12 h	85 % at 24 h	Mouse	Liver (+), kidneys (++)
	99mTc-cefotaxime sodium	D. Ilem-Ozdemir [88]	Stannous tartrate/Stannous chloride	3.4 × 103	92 % at 24 h	85 % at 24 h	Rat	Liver (+), kidneys (++)
	99mTc-ceftriaxone	M. Mostafa [89]	Direct labelling—SnCl2·2H2O	1.90 × 102	n. a.	n. a.	Mouse	Kidneys (++)
	99mTc-ceftriaxone	A. Kaul [90]	Stannous tartrate and gentisic acid	8.95 × 104	95 % at 24 h	95 % at 24 h	Rabbit	Liver (++), kidneys (+)
	99mTc-ceftriaxone	A. Fazli [91]	Direct labelling—SnCl2·2H2O	n. a.	80 % at 24 h	71.2 % at 24 h	Mouse	Liver (+), kidneys (++)
	99mTc-ceftriaxone	M. Sohaib [92]	Direct labelling—SnCl2·2H2O	6.5 × 103	92.8 at 24 h	90.5 at 24 h	Rat	Liver (+), kidneys (++)
	99mTc-ceftazimide	S. F. Mirshojaei [93]	Na-dithionite	1.17 × 105	n. a.	85 % at 24 h	Mouse	Liver (+), kidneys (++)
	99mTc-cefoperazone	M. A. Motaleb [94]	Direct labelling—SnCl2·2H2O	8.51 × 104	98 % at 6 h	n. a.	Rat	Kidneys (++)
	99mTc-cefepime	M. A. Motaleb [95]	Direct labelling—SnCl2·2H2O	3.92 × 104	98 % at 8 h	86.8 % at 24 h	Rat	Liver (+), kidneys (++)
Inhibitors of nucleic acid synthesis	99mTc-rifampicin	S. S. Qaiser [98]	Direct labelling—SnCl2·2H2O	5.48 × 104	90 % at 2 h	n. a.	Rat	Liver and kidneys
	99mTc-nitrofurantoin	S. S. Qaiser [100]	Direct labelling—SnCl2·2H2O	9.01 × 103	90 % at 2 h	87.5 % at 2 h	Rat	Liver and kidneys
Inhibitors of bacterial cell wall synthesis	99mTc-amoxicillin	S. K. Shahzadi [103]	SnCl2·2H2O-Sodium/Potassium pyrophosphate	7.25 × 104	92 % at 6 h	92 % at 6 h	Rabbit	Liver (+), kidneys (++)
	99mTc-alafosfalin	C. Tsopelas [105]	Direct labelling—SnCl2·2H2O	4.01 × 103	n. a.	n. a.	Rat	Kidneys (++)
	99mTc-vancomycin	S. Roohi [108]	Direct labelling—SnCl2·2H2O	1.35 × 105	95 % at 6 h	n. a.	Rat	Liver (+), kidneys (++)
	[18F]fluoroacetamido-D-glucopyranose	M. E. Martìnez [106]	Microwave irradiation	1.80 × 104	n. a.	n. a.	Rat	Liver and kidneys
Inhibitors of protein synthesis	99mTc-kanamycin	S. Roohi [110]	Direct labelling—SnCl2·2H2O	3.62 × 104	98 % at 6 h	96.4 % at 24 h	Rat	Liver (++), kidneys (+)
	99mTc-doxycycline hyclate (DOX)	D. Ilem-Ozdemir [111]	Stannous tartrate-ascorbic acid	3.70 × 105	90 % at 6 h	94 % at 24 h	Rat	Kidneys (++)
	99mTc-erythromycin	I. Y. Abdel-Ghaney [112]	Direct labelling—SnCl2·2H2O	1.94 × 105	97 % at 2 h	87 % at 24 h	Mouse	Liver (+), kidneys (++)
	99mTc-clarithromycin	E. H. Borai [116]	Direct labelling—SnCl2·2H2O	1.5 × 105	90 % at 2 h	90 % at 24 h	Mouse	Liver (+), kidneys (++)
	99mTc-vibramycin	S. Hina [113]	Direct labelling—SnCl2·2H2O	7.8 × 105	95 % at 12 h	98 % at 24 h	Rat	Liver (++), kidneys (+)
	99mTc-azithromycin	M. H. Sanad [115]	Direct labelling—SnCl2·2H2O	1.44 × 105	97.5 % at 2 h	85.5 % at 24 h	Mouse	Liver (+), kidneys (++)
	99mTc-clindamycin	S. Hina [118]	Direct labelling—SnCl2·2H2O	1.56 × 106	95 % at 5 h	92 % at 24 h	Rat	Liver (+), kidneys (++)
Others	6-[18F]-fluoromaltose	G. Gowrishankar [122]	Nucleophilic displacement	n. a.	n. a.	n. a.	Mouse	Liver and kidneys
	68Ga-triacetylfusarinine C (TAFC)	M. Petrik [124]	Direct labelling-sodium acetate	92 × 106	n. a.	80 % at 2 h	Rat	Lungs
	68Ga-ferrioxamine E (FOXE)	M. Petrik [124]	Direct labelling-sodium acetate	3.4 × 106	n. a.	90 % at 2 h	Rat	Lungs
	99mTc-mebendazole	T. Inceboz [120]	Direct labelling—SnCl2·2H2O	2.3–4.6 × 10−2	n. a.	n. a.	Rat	Liver (++), kidneys (+)
	99mTc-HQMADA	M. A. Motaleb [125]	Direct labelling—SnCl2·2H2O	765.8 (MBq/mg)	89.7 % at 8 h	83.4 % at 24 h	Mouse	Liver (++), kidneys (+)

Type of radiopharmaceutical	Max T/NT ratio							Final comment by the authors
	Time	Bacteria (CFU—strain)	Infection site	BKG	T/NT	Control experiment	T/NT (control)
Fluoroquinolones	3 h	108—E. coli	Left thigh	Muscle	4.5	Turpentine oil/heat killed bacteria	4.1/4.4	Low specificity
	24 h	n. a.—E. coli	Right thigh	Muscle	5.6	Turpentine oil	0.75	Good specificity
	2 h	108—S. aureus	Right thigh	Muscle	2.02	n. a.	n. a.	Suitable radiopharmaceutical
	n. a.	105–106—S. aureus	Left thigh	Muscle	4.3	n. a.	n. a.	Specificity to be improved
	n. a.	105–106—S. aureus	Left thigh	Muscle	6.5	n. a.	n. a.	Good specificity
	22 h	5 × 108—S. aureus	Left thigh	Muscle	4.8	Turpentine oil/heat killed bacteria	3.85/3.8	Non specific
	1 h	3 × 108—S. typhi	Thigh	Muscle	4.8	Normal	n. a.	Suitable radiopharmaceutical
	2 h	107–108—S. aureus	Left thigh	Muscle	6.9	Turpentine oil/heat killed bacteria	4.5/6	Non specific
	18 h	109—S. aureus	Left thigh	Muscle	2.87	Turpentine oil	1	Promising radiotracer
	4 h	108—S. aureus	Left thigh	Muscle	3.46	Turpentine oil	1.23	Promising radiotracer
	30 min	105–106—S. aureus	Left thigh	Muscle	5.9	None	n. a.	Specificity to be improved
	3 h	105–106—E. coli	Left thigh	Muscle	8.5	Turpentine oil/heat killed bacteria	3/4.5	Specific
	n. a.	109—E. coli	Right thigh	Muscle	n. a.	n. a.	n. a.	Promising radiotracer for PET imaging
	2 h	2 × 108—S. aureus	Right thigh	Muscle	23.13	Turpentine oil	1.13	Specific at early stage
	1 h	3 × 108—E.coli, P. aeruginosa	Thigh	Muscle	1.3/8.09	Normal	n. a.	Promising for lung, sinus bone infections
	90 min	105—S. aureus	Left thigh	Muscle	7.6	Heat killed bacteria	1	Recommended imaging agent
	2 h	n. a.—S. aureus	Left thigh	Muscle	4.2	Turpentine oil/heat killed bacteria	3.4/3.3	Non specific
	1 h	106–108—E. coli	Left thigh	Muscle	1.62	n. a.	n. a.	Specificity to be improved
	4 h	3 × 108—S. typhi, P. aeruginosa, K. pneumoniae	Thigh	Muscle	8/8.8/16	Normal	n. a.	Specific for respiratory tract infections
	90 min	n. a.—S. pneumoniae	Left thigh	Muscle	4.88	Heat killed bacteria	1.4	Specific for S. Pneumoniae
Cephalosporins	30 min	107–108—S. aureus	Left thigh	Muscle	8.57	Turpentine oil	1.4	Specific at early stage
	4 h	2 × 108—S. aureus	Right thigh	Muscle	2.5	Turpentine oil	1.2	Specific
	3 h	108—E. coli	Left thigh	Muscle	1.8	Normal	n. a.	Potential imaging agent
	6 h	2 × 108—E. coli	Left thigh	Muscle	3.24	Zymosan	1.65	Specific
	n. a.	n. a.	n. a.	n. a.	n. a.	Bone wax	n. a.	Good for deep sternal infection
	n. a.	109—S. aureus	n. a.	n. a.	n. a.	Sterile implant	n. a.	Specificity to be improved
	1 h	108—S. aureus	Right thigh	Muscle	2.89	Normal	n. a.	Potential imaging agent
	1 h	4 × 1010—E. coli	Right thigh	Muscle	3.77	Turpentine oil	3.30	Non specific
	4 h	n.a.—E. coli	Left thigh	Muscle	5.6	Turpentine oil/heat killed bacteria	1.49	Good specificity
	24 h	107—S. aureus	Left forearm	Right forearm	4.5	Turpentine oil	1.4	Specific
	3 h	108—S. aureus	Left thigh	Muscle	3.39	Turpentine oil/heat killed bacteria	3.12/2.48	Potential imaging Agent
	4 h	108—E. coli, S. aureus	Left thigh	Muscle	12.6/2.36	Turpentine oil	1.4	Specific
	1 h	108—S. aureus	Left thigh	Muscle	1.4	n. a.	n. a.	Suitable radiopharmaceutical
	45 min	105–106—S. aureus	Left thigh	Muscle	4.66	n. a.	n. a.	Good specificity
	3 h	108–E. coli	Left thigh	Muscle	8.4	Turpentine oil/heat killed bacteria	3.31/4.13	Specific
Inhibitors of nucleic acid synthesis	90 min	2 × 108—methicillin-res S. aureus	Thigh	Muscle	7.34	Turpentine oil	1.20	Specific for MRSA
	90 min	108—E. coli	Right thigh	Muscle	4.83	Turpentine oil/normal	1	Promising radiotracer
Inhibitors of bacterial cell wall synthesis	2 h	3 × 108—S. pneumoniae	Thigh	Muscle	4.6	n. a.	–	Suitable radiopharmaceutical
	4 h	108—S. aureus	Right thigh	Muscle	4.32	99mTc-DTPA/99mTc-WBC	1.93/20.09	Good for imaging osteomyelitis
	1 h	108—S. aureus	Right thigh	Muscle	5.1	Turpentine oil	1.2	Enough specific
	n. a.	107—E. coli	Right thigh	Muscle	n. a.	Turpentine oil	–	Specific
Inhibitors of protein synthesis	30 min	2 × 108—S. aureus	Right thigh	Muscle	2.5	n. a.	–	Able to localize bacterial infection
	5 h	4 × 1010—E. coli	Right thigh	Muscle	2.24	n. a.	n. a.	Non specific
	30 min	105–106—S. aureus	Left thigh	Muscle	5	Turpentine oil	4.8	Non specific
	2 h	108—S. aureus	Left thigh	Muscle	7.33	Turpentine oil/heat killed bacteria	3.1/3.26	Specific
	1 h	2 × 108—S. aureus	Left thigh	Muscle	2.64	Turpentine oil/heat killed bacteria	1.80/2.15	Good bacterial imaging agent
	2 h	n. a.—S. aureus	Left thigh	Muscle	6.2	Turpentine oil/heat killed bacteria	2.60/3.13	Specific
	1 h	2 × 108—S. aureus	Left thigh	Muscle	3.1	Turpentine oil/heat killed bacteria	2.47/1.6	Potential imaging agent
Others	n. a.	5 × 107—E. coli	Right thigh	Muscle	n. a.	Turpentine oil/heat killed bacteria	–	Specific
	n. a.	109—A. fumigatus	Left calf	Muscle	n. a.	Turpentine oil	n. a.	Specific for A. Fumigatus
	n. a.	109—A. fumigatus	Left calf	Muscle	n. a.	Turpentine oil	n. a.	Specific for A. Fumigatus
	n. a.	750–1000 larvae T. spiralis	Diaphragm	Muscle	n. a.	n. a.	n. a.	Specific for T. Spiralis
	2 h	n. a.—E. coli	Left thigh	Muscle	5.52	Turpentine oil/heat killed bacteria	2.5/2.2	Potential substitute of ciprofloxacin

We found 53 published studies in animals and none in man (of which 18 were classified as “good”, 23 as “average” and 12 as “poor” on the basis of the reported specificity to tested bacteria)