ASP3662 / Astellas - LARVOL DELTA

Safety, Pharmacokinetics, and Pharmacodynamics of ASP3662, a Novel 11β-HSD1 Inhibitor, in Healthy Young and Elderly Subjects. (PubMed, Clin Transl Sci) - "A marked dissociation between pharmacokinetics and pharmacodynamics was observed after single, but not multiple doses of ASP3662. ASP3662 was generally safe and well tolerated."

Clinical • Journal • PK/PD data • Pain

A Novel F-Labeled Radioligand for Positron Emission Tomography Imaging of 11β-Hydroxysteroid Dehydrogenase (11β-HSD1): Synthesis and Preliminary Evaluation in Nonhuman Primates. (PubMed, ACS Chem Neurosci) - "In monkey brain, [F]AS2471907 displayed high uptake and heterogenous distribution, while administration of the 11β-HSD1 inhibitor ASP3662 significantly reduced uptake, thus demonstrating the binding specificity of [F]AS2471907. Given the longer half-life of F-18 and feasibility for central production and distribution, [F]AS2471907 holds great promise to be a valuable PET radiotracer to image 11β-HSD1 in the brain."

Journal • Alzheimer's Disease • CNS Disorders • Depression • Diabetes • Genetic Disorders • Metabolic Disorders • Obesity • Type 2 Diabetes Mellitus

IMAGING THE ENZYME 11β-HYDROXYSTEROID DEHYDROGENASE TYPE 1 WITH POSITRON EMISSION TOMOGRAPHY: EVALUATION OF THE NOVEL RADIOTRACER C-AS2471907 IN HUMAN BRAIN. (PubMed, J Nucl Med) - "Two subjects underwent an additional scan after blockade with the selective and high-affinity 11β-HSD1 inhibitor ASP3662 to evaluate C-AS2471907 nondisplaceable distribution volume...C-AS2471907 has a very high fraction of specific binding in vivo in humans, and reasonable within-day reproducibility of binding parameters."

Journal

Analgesic effect of ASP3662, a novel 11β-HSD1 inhibitor, in rat models of neuropathic and dysfunctional pain. (PubMed, Br J Pharmacol) - "These results indicate that ASP3662 is a potent, selective and CNS-penetrable inhibitor of 11β-HSD1. The effects of ASP3662 suggest that selective inhibition of 11β-HSD1 may be an attractive approach for the treatment of neuropathic and dysfunctional pain, such as that observed in fibromyalgia."

Journal • Preclinical