||||||||||ASP3662 / Astellas Journal: IMAGING THE ENZYME 11β-HYDROXYSTEROID DEHYDROGENASE TYPE 1 WITH POSITRON EMISSION TOMOGRAPHY: EVALUATION OF THE NOVEL RADIOTRACER C-AS2471907 IN HUMAN BRAIN. (Pubmed Central) - Apr 14, 2020 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. 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.
||||||||||ASP3662 / Astellas Preclinical, Journal: Analgesic effect of ASP3662, a novel 11β-HSD1 inhibitor, in rat models of neuropathic and dysfunctional pain. (Pubmed Central) - Oct 18, 2019 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.
||||||||||ASP3662 / Astellas Trial completion: A Positron Emission Tomography Occupancy Study Using Ligand [11C]AS2471907 and Following Oral Dosing of ASP3662 (clinicaltrials.gov) - Jun 28, 2016 P1, N=18, Completed, Sponsor: Astellas Pharma Global Development, Inc. 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. Recruiting --> Completed
||||||||||ASP3662 / Astellas Phase classification, Enrollment change, Trial termination, Trial primary completion date: Study to Assess Analgesic Efficacy and Safety of ASP3662 in Subjects With Painful Diabetic Peripheral Neuropathy (clinicaltrials.gov) - Jun 10, 2016 P2a, N=116, Terminated, Sponsor: Astellas Pharma Global Development, Inc. Recruiting --> Completed Phase classification: P2 --> P2a | N=210 --> 116 | Recruiting --> Terminated | Trial primary completion date: Oct 2016 --> May 2016; The study was terminated due to futility analysis.
||||||||||ASP3662 / Astellas Trial primary completion date: A Positron Emission Tomography Occupancy Study Using Ligand [11C]AS2471907 and Following Oral Dosing of ASP3662 (clinicaltrials.gov) - Oct 28, 2015 P1, N=18, Recruiting, Sponsor: Astellas Pharma Global Development, Inc. Phase classification: P2 --> P2a | N=210 --> 116 | Recruiting --> Terminated | Trial primary completion date: Oct 2016 --> May 2016; The study was terminated due to futility analysis. Trial primary completion date: Oct 2015 --> Apr 2016