title: Preparation of (99m)Tc-labelled methotraxate by a direct labeling technique as a potential diagnostic agent for breast cancer and preliminary clinical results.
abstract: Methotrexate (MTX) is being used in clinical oncology for the treatment of a wide variety of cancers. The aim of the present study was to label directly MTX with (99m)Tc by using Sn/pyrophosphate as reducing agent and to use this labeled compound as a potential anticancer radiopharmaceutical for breast cancer imaging. We studied the labeling efficiency of the (99m)Tc-MTX compound by paper chromatography and instant thin layer chromatography (ITLC) in acetone and saline and found it to be more than 95%. In vitro stability of labeled MTX in serum was studied up to 5h. Partition coefficient in n-octanol and saline indicated that the labeled radiopharmaceutical was hydrophilic. We then tested (99m)Tc-MTX in 5 breast cancer female patients. Protein bound (99m)Tc-MTX showed rapid clearance from blood. The biodistibution data suggested that (99m)Tc-MTX was cleared by the kidneys and the liver. Patients ' data also showed highly significant uptake of (99m)Tc-MTX in breast cancer. In conclusion, this study indicated that (99m)Tc-MTX may be used as a potential diagnostic agent for breast cancer patients imaging and may show treatment efficiency in case MTX is to be used for treatment.
authors.affiliation: Gujranwala Institute of Nuclear Medicine (GINUM), Cancer Hospital, Nizampur, Sialkot road, Gujranwala, Pakistan. dr.nmd.paec@gmail.com
authors.forename: Rashid
authors.initials: R
authors.lastname: Rasheed
authors.forename: Muhammad
authors.initials: M
authors.lastname: Javed
authors.forename: Fayyaz
authors.initials: F
authors.lastname: Ahmad
authors.forename: Asima
authors.initials: A
authors.lastname: Sohail
authors.forename: Sohail
authors.initials: S
authors.lastname: Murad
authors.forename: Misbah
authors.initials: M
authors.lastname: Masood
authors.forename: Shahid
authors.initials: S
authors.lastname: Rasheed
authors.forename: Saqib
authors.initials: S
authors.lastname: Rasheed
mesh_terms: D000328:Adult; D001943:Breast Neoplasms / Q000000981:diagnostic imaging*; D005260:Female; D006801:Humans; D007553:Isotope Labeling / Q000379:methods*; D008727:Methotrexate / Q000009:adverse effects / Q000737:chemistry; D008875:Middle Aged; D015609:Organotechnetium Compounds; D011786:Quality Control; D011877:Radionuclide Imaging; D012449:Safety
chemical_list: D015609:Organotechnetium Compounds; D008727:Methotrexate