Development of a Radiolabeled Cyclin-Dependent Kinases 4 and 6 (CDK4/6) Inhibitor for Brain and Cancer PET Imaging.

The synthesis, biochemical evaluation and radiosynthesis of a cyclin-dependent kinases 4 and 6 (CDK4/6) inhibitor and radioligand was performed. NT431, a newly synthesized 4-fluorobenzyl-abemaciclib, exhibited high potency to CDK4/6 and against four cancer cell lines with IC similar to that of the parent abemaciclib. We performed a two-step one-pot radiosynthesis to produce [F]NT431 with good radiochemical yield (9.

Design and radiosynthesis of class-IIa HDAC inhibitor with high molar activity via repositioning the F-radiolabel.

The design and radiosynthesis of [F]NT376, a high potency inhibitor of class-IIa histone deacetylases (HDAC) is reported. We utilized a three-step radiochemical approach that led to the radiosynthesis of [F]NT376 in a good radiochemical yield, (17.0 ± 3%, decay corrected), high radiochemical purity (> 97%) and relatively high molar activity of 185.

Pubic Aneurysmal Bone Cyst Following Penile Inversion Vaginoplasty: A Case Report.

Background: Aneurysmal bone cysts (ABCs) are aggressive, expansile, and locally destructive vascular lesions. The exact etiology of ABCs is currently unknown and hypothesized to be related to vascular malformations or disruption of osseous vascularity. To date, there have been no reports describing the development of pubic ABCs following penile inversion vaginoplasty (PIV).

Coordinated single-cell tumor microenvironment dynamics reinforce pancreatic cancer subtype.

Bulk analyses of pancreatic ductal adenocarcinoma (PDAC) samples are complicated by the tumor microenvironment (TME), i.e. signals from fibroblasts, endocrine, exocrine, and immune cells.

A Multicenter Phase 1 Trial Evaluating Nanoliposomal Irinotecan for Heated Intraperitoneal Chemotherapy Combined with Cytoreductive Surgery for Patients with Peritoneal Surface Disease.

Background: Nanoliposomal irinotecan (nal-IRI) is a promising novel hyperthermic intraperitoneal chemotherapy (HIPEC) agent given its enhanced efficacy against gastrointestinal tumors, safety profile, thermo-synergy, and heat stability. This report describes the first in-human phase 1 clinical trial of nal-IRI during cytoreductive surgery (CRS) and HIPEC.

Methods: Patients with peritoneal surface disease (PSD) from appendiceal and colorectal neoplasms were enrolled in a 3 + 3 dose-escalation trial using nal-IRI (70-280 mg/m) during HIPEC for 30 min at 41 ± 1 °C.