An overview of translational (radio)pharmaceutical research related to certain oncological and non-oncological applications

Table 1 Evaluation of physical properties of different formulations of ¹²³Hyp/Hyp examined by macroscopic digital imaging under white light and ultraviolet light (254 nm) and by microscopy over a corresponding drop in bright field and fluorescence illumination mode

Formulation	Macroscopic digital imaging	Microscopy
DMSO/saline (20/80, v/v)	Cloudy brownish solution, no fluorescence	Massive formation of aggregates reduced fluorescent intensity
DMSO/water (25/75, v/v)	Cloudy brownish solution, no fluorescence	Massive formation of aggregate reduced fluorescent intensity
DMSO/D10W (25/75, v/v)	Cloudy brownish solution, no fluorescence	Massive formation of aggregates reduced fluorescent intensity
DMSO/D20W (25/75, v/v)	Cloudy brownish solution, no fluorescence	Massive formation of aggregates reduced fluorescent intensity
DMSO/serum (25/75, v/v)	Cloudy brownish solution, moderate fluorescence signal	Massive formation of aggregates moderate fluorescent intensity
DMSO/PEG 400/water (25/60/15, v/v/v)	Bright red solution, highly fluorescent	No aggregates formation; strong, homogeneous fluorescence
EtOH/PEG 400/water (10/50/40, v/v/v)	Dark red solution, moderate fluorescence	Aggregate formation; moderate, heterogeneous fluorescence,
EtOH/PEG 400/water (10/60/30, v/v/v)	Red solution, minimum aggregation, high fluorescence	Some aggregates; strong, homogeneous fluorescence
PEG 400/water (60/40, v/v)	Red solution, high fluorescence	Some aggregates; strong, homogeneous fluorescence
PEG 400/water (70/30, v/v)	Bright red solution, highly fluorescent	Some aggregates; strong, homogeneous fluorescence
PVP-10000	Dark red solution, moderate fluorescence	Aggregate formation; reduced fluorescence intensity
PVP-29000	Dark red solution, moderate fluorescence	Aggregate formation; reduced fluorescence intensity
β-Cyclodextrins	Cloudy brownish solution, no fluorescence	Massive formation of aggregates reduced fluorescent intensity

DMSO: Dimethyl sulfoxide; D10W: 10% dextrose; D20W: 20% dextrose; EtOH: Ethanol; PEG 400: Polyethylene glycol 400; PVP: Polyvinylpyrrolidone.

Table 2 Dosimetry aspects of different anticancer therapeutic agents under pre-clinical and clinical investigation

Therapeutics	Dosimetry calculations	Species	Targeting tissue	Pathology	Dose to tumor(mGy/MBq)	Ref.
131I-Hyp	OLINDA/EXM software	RPLI rats	Necrotic tissue	Solid tumors	276–93600	[79]
131I-Labeled TNT-1 monoclonal antibody	Organ uptake-time integration by trapezoid method Whole body image analysis	Nude mice bearing ME-180 human cervical tumors	Histone fraction H1 in necrotic tissues	Cervical carcinoma cell	366–3610	[31]
131I-m-iodobenzylguanidine (MIBG)	MicroPET/CT 124I-MIBG OLINDA/EXM software	Mice bearing A431 human epithelial carcinoma xenografts	Norepinephrine transporter	Neuroblastoma	97–380	[80]
131I- labeled monoclonal antibody MN-14	MIRDOSE3 software	Nude mice with intraperitoneal LS174T tumors	Carcinoembryonic antigen	Peritoneal metastases of colorectal origin	-16200	[89]
131I-tositumomab	SPECT/CT Imaging DPM Monte Carlo electron and photon transport program	Humans	CD20-positive B-cells	Refractory B-cell NHL	2.81 (mean)	[81]
177Lu-DOTA-AE105	Organ uptake-time integration by trapezoid method Sphere model	Nude mice bearing colorectal HT-29 tumor	uPAR-positive HT-29 xenograft	Colorectal cancer	5.8	[82]
177Lu-pertuzumab	Organ uptake-time integration by trapezoid method Sphere model	BALB/c (nu/nu) Mice with HER-2–overexpressing xenografts	HER-2 tyrosine kinase receptor	Breast cancer	-6900	[83]
186Re-1-hydroxy- ethylidene-1,1 diphosphonic acid	MIRDOSE 3.1 software	Humans	Bone mineral metabolite	Skeletal metastases	23–34	[84]
90Y-ibritumomab tiuxetan	PET/CT Imaging DPM 89Zr-ibritumomab tiuxetan OLINDA/EXM software	Humans	CD20-positive B-cells	Relapsing NHL	8.6–28.6	[85]
90Y- DOTA0-DPhe1-Tyr3- octreotide	SPECT/CT Imaging DPM 111In-DOTA-TOC	Humans	Somatostatin receptor subtype 2	NETs	4-31 (mean 10)	[86]

CT: Computed tomography; DOTA: 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid;

¹³¹I: Iodine-131;

¹⁷⁷Lu: Lutetium-177; NETs: Neuroendocrine tumors; OLINDA/EXM: Organ level internal dose assessment/exponential modeling; PET: Positron emission tomography;

¹⁸⁶Re: Rhenium-186; RPLI: Reperfused partial liver infarction; SPECT: Single-photon emission computed tomography; TNT: Tumor necrosis treatment; DPM: Dose planning method; NHL: Non-Hodgkin lymphoma; DOTA-TOC:

⁹⁰Y- DOTA0-DPhe1-Tyr3-octreotide; ⁹⁰Y: Yttrium-90.