Erteberel

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Erteberel
Clinical data
Other namesSelective estrogen receptor beta agonist-1; SERBA-1; LY-500307; (3aS,4R,9bR)-1,2,3,3a,4,9b-Hexahydro-4-(4-hydroxyphenyl)cyclopenta(c)(1)benzopyran-8-ol; (2R,3S,4R)-SERBA[1]
Routes of
administration
By mouth
Identifiers
  • (3aS,4R,9bR)-4-(4-Hydroxyphenyl)-1,2,3,3a,4,9b-hexahydrocyclopenta[c]chromen-8-ol
JSmol)
  • C1C[C@H]2[C@@H](C1)C3=C(C=CC(=C3)O)O[C@H]2C4=CC=C(C=C4)O
  • InChI=1S/C18H18O3/c19-12-6-4-11(5-7-12)18-15-3-1-2-14(15)16-10-13(20)8-9-17(16)21-18/h4-10,14-15,18-20H,1-3H2/t14-,15+,18+/m1/s1
  • Key:XIESSJVMWNJCGZ-VKJFTORMSA-N

Erteberel (

negative symptoms and cognitive impairment associated with the condition.[2] As of 2015, it is in phase II clinical trials for this indication in the United States.[2] Erteberel was also under investigation for the treatment of benign prostatic hyperplasia and reached phase II clinical studies for this use but failed to improve symptoms in men with the condition and development for this indication was discontinued.[2][5] The drug has also been proposed as a potential novel treatment for glioblastoma.[6]

Erteberel has 14-fold

full agonist of both the ERβ and ERα (Emax = 101% versus 94%, respectively).[3][7] Although selective for the ERβ, erteberel loses its selectivity at high dosages and activates the ERα as well, producing effects such as suppression of gonadal testosterone production in men.[8]

See also

References

  1. S2CID 6259593
    .
  2. ^ a b c d "Erteberel - AdisInsight". adisinsight.springer.com. Archived from the original on 31 December 2016. Retrieved 22 May 2022.
  3. ^
    S2CID 3841877
    .
  4. .
  5. .
  6. .
  7. ^ .
  8. .

External links