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Inocoterone

Inocoterone
Inocoterone.svg
Clinical data
Other namesRU-29294; 2,5-Seco-A-dinorestr-9-en-17β-ol-5-one
Routes of
administration
Topical
Drug classNonsteroidal antiandrogen
Identifiers
CAS Number
PubChem CID
ChemSpider
UNII
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC16H24O2
Molar mass248.36056 g/mol g·mol−1
3D model (JSmol)

Inocoterone (INN; developmental code name RU-29294) is a steroid-like nonsteroidal antiandrogen (NSAA) that was never marketed.[1][2] An acetate ester, inocoterone acetate, shows greater antiandrogen activity and was developed as a topical medication for the treatment of acne but showed only modest effectiveness in clinical trials and similarly was never marketed.[3]

Relative affinities (%) of antiandrogens at steroid-hormone receptors

Antiandrogen AR PR ER GR MR
Cyproterone acetate 8–10 60 <0.1 5 1
Chlormadinone acetate 5 175 <0.1 38 1
Megestrol acetate 5 152 <0.1 50 3
Spironolactone 7 0.4a <0.1 2a 182
Trimethyltrienolone 3.6 <1 <1 <1 <1
Inocoterone 0.8 <0.1 <0.1 <0.1 <0.1
Inocoterone acetate <0.1 <0.1 <0.1 <0.1 <0.1
Flutamide <0.1 <0.1 <0.1 <0.1 <0.1
Hydroxyflutamide 0.5–0.8 <0.1 <0.1 <0.1 <0.1
Nilutamide 0.5–0.8 <0.1 <0.1 <0.1 <0.1
Bicalutamide 1.8 <0.1 <0.1 <0.1 <0.1
Notes: (1): Reference ligands (100%) were testosterone for the AR, progesterone for the PR, estradiol for the ER, dexamethasone for the GR, and aldosterone for the MR. (2): Tissues were rat prostate (AR), rabbit uterus (PR), mouse uterus (ER), rat thymus (GR), and rat kidney (MR). (3): Incubation times (0°C) were 24 hours (AR, a), 2 hours (PR, ER), 4 hours (GR), and 1 hour (MR). (4): Assay methods were different for bicalutamide for receptors besides the AR. Sources: See template.

See also

References

  1. ^ J. Elks (14 November 2014). The Dictionary of Drugs: Chemical Data: Chemical Data, Structures and Bibliographies. Springer. pp. 686–. ISBN 978-1-4757-2085-3.
  2. ^ P. Michael Conn (23 July 2010). Techniques in Confocal Microscopy. Academic Press. pp. 215–. ISBN 978-0-12-384659-4.
  3. ^ Annual Reports in Medicinal Chemistry. Academic Press. 2 September 1987. pp. 358–. ISBN 978-0-08-058366-2.