Details of the Drug-Related molecule(s) Interaction Atlas

General Information of Drug (ID: DMCEPUA)

• Drug Name: ERB-041 Drug Info
• Synonyms: 2-(3-Fluoro-4-hydroxyphenyl)-7-vinylbenzoxazol-5-ol

Indication

Disease Entry	ICD 11	Status	REF
Inflammatory bowel disease	DD72	Phase 2	[1] , [2]

• Cross-matching ID:
  PubChem CID: 656954
  CAS Number: CAS 524684-52-4
  TTD Drug ID: DMCEPUA

Molecule-Related Drug Atlas

Drug(s) Targeting Estrogen receptor beta (ESR2)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Conjugated estrogens	DMLT0E1	Menopause symptom	GA30.0	Approved	[5]
Trilostane	DMQZ9GF	Cushing disease	5A70	Approved	[6]
ARZOXIFENE	DMOKCVI	Breast cancer	2C60-2C65	Approved	[7]
Estrogen	DMGY0UT	Menopause symptom	GA30.0	Approved	[8]
Premarin/Pravachol	DMLSOB7	Hyperlipidaemia	5C80	Phase 3	[9]
MF-101	DM8Z0I3	Hepatitis virus infection	1E50-1E51	Phase 3	[10]
Genistein	DM0JETC	Menopause symptom	GA30.0	Phase 2/3	[11]
AUS-131	DMZMSQJ	Hot flushes	GA30	Phase 2	[12]
Erteberel	DMU1XZD	Prostate hyperplasia	GA90	Phase 2	[13]
VG-101	DMAN21O	Menopause symptom	GA30.0	Phase 1/2	[14]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Estrogen receptor beta (ESR2)	TTOM3J0	ESR2_HUMAN	Agonist	[3] , [4]

References

• [1] URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 6700).
• [2] ClinicalTrials.gov (NCT00318500) Study Evaluating the Safety and Efficacy of ERB-041 on Reduction of Symptoms Associated With Endometriosis in Reproductive-Aged Women. U.S. National Institutes of Health.
• [3] Erb-041, an estrogen receptor-beta agonist, inhibits skin photocarcinogenesis in SKH-1 hairless mice by downregulating the WNT signaling pathway. Cancer Prev Res (Phila). 2014 Feb;7(2):186-98.
• [4] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
• [5] Differential biochemical and cellular actions of Premarin estrogens: distinct pharmacology of bazedoxifene-conjugated estrogens combination. Mol Endocrinol. 2009 Jan;23(1):74-85.
• [6] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
• [7] Benzothiophene selective estrogen receptor modulators with modulated oxidative activity and receptor affinity. J Med Chem. 2007 May 31;50(11):2682-92.
• [8] Estrogen inhibits the vascular injury response in estrogen receptor beta-deficient female mice. Proc Natl Acad Sci U S A. 1999 Dec 21;96(26):15133-6.
• [9] Lovastatin and beyond: the history of the HMG-CoA reductase inhibitors. Nat Rev Drug Discov. 2003 Jul;2(7):517-26.
• [10] MF101, a selective estrogen receptor beta modulator for the treatment of menopausal hot flushes: a phase II clinical trial. Menopause. 2009 May-Jun;16(3):458-65.
• [11] Company report (Axcentua)
• [12] S-equol, a potent ligand for estrogen receptor beta, is the exclusive enantiomeric form of the soy isoflavone metabolite produced by human intestinal bacterial flora. Am J Clin Nutr. 2005 May;81(5):1072-9.
• [13] Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800031986)
• [14] Update on alternative therapies for vulvovaginal atrophy. Patient Prefer Adherence. 2011; 5: 533-536.