Tubulysins are highly toxic tubulin-targeting agents with a narrow therapeutic window that are interesting for application in antibody-drug conjugates (ADC). For full control over drug-antibody ratio (DAR) and the effect thereof on pharmacokinetics and tumor targeting, a dual-labeling approach was developed, wherein the drug, tubulysin variants, and the antibody, the anti-HER2 monoclonal antibo...

Abstract We developed a novel method for production of no-carrier-added (n.c.a.) [ 188, 189, 191 Pt]Pt II Cl 4 2− from an Ir target material, and then synthesized n.c.a. [*Pt]cis-[Pt 2 (NH 3 ) ] ([*Pt]cisplatin) [*Pt]Pt . was prepared as synthetic precursor *Pt complex by combination resin extraction anion-exchange chromatography after the selective reduction IV 6 with ascorbic acid. The ligand...

Significant dephosphorylation of glucose 6-phosphate due to glucose-6-phosphatase activity in rat brain in vivo was recently reported (Huang, M., and Veech, R. L. (1982) J. Biol. Chem. 257, 1135811363). The evidence was an apparent more rapid 3H than '"C loss from the glucose pool and faster [2-3H] glucose than [U-'"C]glucose utilization following pulse labeling of the brain with [2-SH...

This review article covers a concise account on fludeoxyglucose ((18)F-FDG) synthesis and quality control procedures with emphasis on practical synthesis Currently, (18)F-FDG is the most successful PET radiopharmaceutical so far. The advancement in synthesis and quality control of (18)F-FDG, together with its approval by the US FDA and the availability of reimbursement, are probably the main re...

UNLABELLED Breast and endometrial cancers are the most common invasive malignancies in women, with more than 217,000 new diagnoses per year in the United States. These cancers are often classified into 2 subtypes based on the expression of the classical estrogen receptor. In this study, we describe a new structural class of neutral tridentate 99mTc(I)-estradiol-pyridin-2-yl hydrazine derivative...

Tubulysins are highly toxic tubulin-targeting agents with a narrow therapeutic window that are interesting for application in antibody–drug conjugates (ADC). For full control over drug–antibody ratio (DAR) and the effect thereof on pharmacokinetics and tumor targeting, a dual-labeling approach was developed, wherein the drug, tubulysin variants, and the antibody, the anti-HER2 monoclonal antibo...

UNLABELLED Small-molecule ligands specific for prostate-specific membrane antigen (PSMA) have the potential to improve prostate cancer imaging. However, highly charged ligands are difficult to label with 99mTc and to purify. In this study, we present an adamantane-trimerized small molecule that has nanomolar binding to PSMA and also has 12 negative charges. METHODS To convert this molecule in...

PURPOSE Bufalin, the main component of a Chinese traditional medicine chansu, shows convincing anticancer effects in a lot of tumor cell lines. However, its in vivo behavior is still unclear. This research aimed to evaluate how bufalin was dynamically absorbed after intravenous injection in animal models. We developed a radiosynthesis method of [18F]fluoroethyl bufalin to noninvasively evaluate...

UNLABELLED The use of (99m)Tc-sulfur colloid lymphoscintigraphy for the determination of lymph flow patterns from a tumor site and localization of the sentinel node has been widely adopted. However, the effects of multiple injections of the radiopharmaceutical can range from mild discomfort to pain. pH-adjusted lidocaine HCl coadministered with (99m)Tc-sulfur colloid presents a risk of introduc...

Purpose: To evaluate whether Zr can be used as a PET surrogate label for quantification of Yibritumomab tiuxetan (Y-Zevalin) biodistribution and dosimetry before myeloablative radioimmunotherapy. Methods: Zevalin was labelled with Zr by introducing Nsuccinyldesferal (N-sucDf) as a second chelate. For comparison of the in vitro stability of Zr-Zevalin and Y-Zevalin (as a substitute for Y), sampl...