A Double-Blind, Placebo-Controlled, Crossover Pilot Study of the Efficacy and Safety of Fluasterone Buccal Tablet in the Control of Hyperglycemia in Adults with Endogenous Cushing’s Syndrome - ST002-51

Start Date-

Sponsor / Collaborator

SteroTherapeutics LLCStartup

100 Clinical Results associated with Fluasterone

100 Translational Medicine associated with Fluasterone

100 Patents (Medical) associated with Fluasterone

Literatures (Medical) associated with Fluasterone

01 Jan 2010·Chemico-Biological InteractionsQ2 · MEDICINE

Pharmacokinetic and tissue distribution study of [14C]fluasterone in male Beagle dogs following intravenous, oral and subcutaneous dosing routes

Q2 · MEDICINE

Article

Author: Schwartz, Arthur ; Kapetanovic, Izet M. ; Lyubimov, Alexander ; Zakharov, Alexander D. ; Thomas, Brian F. ; Lindeblad, Matthew O. ; Bauer, Kenneth S. ; Green, Jonathan S. ; Hill, Judith M.

The purpose of this work was to compare the pharmacokinetics (PK) and tissue distribution of [14C]fluasterone following intravenous (iv), subcutaneous (sc) and oral (po) administration in male Beagle dogs. The main goal of the investigation was to discover if non-oral routes would alter parameters observed in this study following the administration of [14C]fluasterone. The oral formulation had a lower bioavailability (47%) compared to the sc formulation (84%). Po and sc administration resulted in a similar t(max); however, the observed C(max) following sc dosing was less than half of that after oral dosing. The sc route had the greatest overall exposure (AUC(0-infinity)). Tissue distribution analysis 2 h post-intravenous dosing showed that connective tissue (adipose and bone), liver, and skeletal muscle accumulated relatively high levels of fluasterone. The majority of the dose was retained during the first 24 h. Elimination of [14C]fluasterone-derived radioactivity following intravenous dosing resulted in urine and feces containing 7.6% and 28%, respectively, of the total dose over the first 24 h. Elimination of [14C]fluasterone-derived radioactivity following subcutaneous dosing resulted in 4.6% in urine and 7.8% in feces of the total dose over the first 24 h. Following oral dosing, elimination resulted in 3.8% in urine and 36% in feces over the first 24h. In conclusion, the sc route of administration offers some advantages to po and iv due to the prolonged release and increased retention through 24 h.

01 May 2009·Drug Metabolism and DispositionQ2 · MEDICINE

Identification of [¹⁴C]Fluasterone Metabolites in Urine and Feces Collected from Dogs after Subcutaneous and Oral Administration of [¹⁴C]Fluasterone

Q2 · MEDICINE

Article

Author: Hill, Judith M. ; Zhan, Qiao ; Schwartz, Arthur ; Lindeblad, Matthew ; Thomas, Brian F. ; Kapetanovic, Izet M. ; Burgess, Jason P. ; Lyubimov, Alexander ; Green, Jonathan S.

The objective of this research was the identification of the metabolic profile of fluasterone, a synthetic derivative of dehydroepiandrosterone, in dogs treated orally or subcutaneously with [4-(14)C]fluasterone. Separation and characterization techniques used to identify the principal metabolites of fluasterone in urine and feces included high-performance liquid chromatography (HPLC), liquid scintillation spectrometry, HPLC/tandem mass spectrometry, and NMR. In urine, the majority of the radioactivity was present as two components that had apparent molecular weights consistent with their tentative identification as monoglucuronide conjugates of 4alpha-hydroxy-16alpha-fluoro-5-androsten-17beta-ol and X(alpha or beta)-4alpha-dihydroxy-16alpha-fluoro-5-androsten-17beta-ol. The identification of the monoglucuronide conjugate of 4alpha-hydroxy-16alpha-fluoro-5-androsten-17beta-ol was also supported by NMR data. In support of this identification, these metabolites were cleaved with glucuronidase enzyme treatment, which gave rise to components with molecular weights again consistent with the aglycones of a monohydroxylated, 17-keto reduced (dihydroxy) fluasterone metabolite and a dihydroxylated, 17-keto reduced (trihydroxy) fluasterone metabolite. In feces, nonconjugated material predominated. The primary metabolites eliminated in feces were the two hydroxy fluasterone metabolites arising from 17-reduction (16alpha-fluoro-5-androsten-17beta-ol and 16alpha-fluoro-5-androsten-17alpha-ol) and 4alpha-hydroxy-16alpha-fluoro-5-androsten-17beta-ol that was present in urine in glucuronide form.

01 Nov 2006·Magnetic Resonance in ChemistryQ3 · CHEMISTRY

Complete ¹H and ¹³C assignments of fluorinated analogs of dehydroepiandrosterone

Q3 · CHEMISTRY

Article

Author: Burgess, Jason P. ; Thomas, Brian F. ; Wintermute, James S. ; Kapetanovic, Izet M.

AbstractThe complete assignments of all 1H and 13C chemical shifts were made for the fluorinated dehydroepiandrosterone (DHEA) analog fluasterone, 2, and two potential in vivo metabolites 3 and 4. The assignments were made using a combination of one‐ and two‐dimensional NMR techniques (1H, 13C, gDQCOSY, gHSQC, gHMBC). Once the proton chemical shifts were assigned, the stereochemistry of the two hydroxylated analogs was determined using 2D ROESY experiments. Copyright © 2006 John Wiley & Sons, Ltd.

100 Deals associated with Fluasterone

External Link

KEGG	Wiki	ATC	Drug Bank
-	-	-	DB06250

R&D Status

10 top R&D records.

to view more data

Indication	Highest Phase	Country/Location	Organization	Date
Actinic Keratosis	Phase 2	-	Harbor	-
Metabolic Syndrome	Phase 2	-	Harbor	-
Multiple Sclerosis	Phase 2	US	Harbor Therapeutics, Inc.	-

Clinical Result

Indication

Phase

Evaluation

View All Results

Translational Medicine

Boost your research with our translational medicine data.

view full example data

Deal

Boost your decision using our deal data.

view full example data

Core Patent

Boost your research with our Core Patent data.

view full example data

Clinical Trial

Identify the latest clinical trials across global registries.

view full example data

Approval

Accelerate your research with the latest regulatory approval information.

view full example data

Regulation

Understand key drug designations in just a few clicks with Synapse.

view full example data

Chat with Hiro

Get started for free today!

Accelerate Strategic R&D decision making with Synapse, PatSnap’s AI-powered Connected Innovation Intelligence Platform Built for Life Sciences Professionals.

Start your data trial now!

Synapse data is also accessible to external entities via APIs or data packages. Empower better decisions with the latest in pharmaceutical intelligence.

Bio

Bio Sequences Search & Analysis

Chemical

Chemical Structures Search & Analysis