Bezisterim

Bezisterim
Clinical data
Other names	NE3107; NE-3107; HE3286; HE-3286; 17α-Ethynyl-5-androstene-3β,7β,17β-triol;
Legal status
Legal status	Investigational;
Identifiers
	IUPAC name (3S,7R,8R,9S,10R,13S,14S,17R)-17-Ethynyl-10,13-dimethyl-1,2,3,4,7,8,9,11,12,14,15,16-dodecahydrocyclopenta[a]phenanthrene-3,7,17-triol;
CAS Number	1001100-69-1;
PubChem CID	16739648;
DrugBank	DB05212;
ChemSpider	20571043;
UNII	PH8858757I;
KEGG	D12932;
ChEMBL	ChEMBL4297284;
CompTox Dashboard (EPA)	DTXSID501267252 ;
Chemical and physical data
Formula	C21H30O3
Molar mass	330.468 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES C[C@]12CC[C@@H](CC1=C[C@@H]([C@@H]3[C@@H]2CC[C@]4([C@H]3CC[C@]4(C#C)O)C)O)O;
	InChI InChI=1S/C21H30O3/c1-4-21(24)10-7-16-18-15(6-9-20(16,21)3)19(2)8-5-14(22)11-13(19)12-17(18)23/h1,12,14-18,22-24H,5-11H2,2-3H3/t14-,15-,16-,17-,18+,19-,20-,21-/m0/s1; Key:JJKOQZHWYLMASZ-FJWDNACWSA-N;

Bezisterim (developmental code names NE3107, HE3286) is a synthetic analogue of androstenetriol that is believed to have anti-inflammatory and insulin-sensitizing effects in the brain.^[1] The compound crosses the blood–brain barrier and does not activate any neurotransmitter receptors.^[2] It has been tested as a treatment for Alzheimer's disease,^[3]^[4]^[5]^[6] Parkinson's disease,^[1] and traumatic brain injury.^[7] The drug is under development for a variety of conditions and its highest developmental phase is phase 3 for Alzheimer's disease.^[1]

References

^ ^a ^b ^c "Bezisterim". AdisInsight. 5 September 2024. Retrieved 26 September 2024.
^ Reading, Chris L; Ahlem, Clarence N; Parameswaran, Narayanan (December 2021). "Rationale for an anti-inflammatory insulin sensitizer in a phase 3 Alzheimer's disease trial". Alzheimer's & Dementia. 17 (S9). doi:10.1002/alz.057438.
^ Stoiljkovic, Milan; Horvath, Tamas L.; Hajós, Mihály (July 2021). "Therapy for Alzheimer's disease: Missing targets and functional markers?". Ageing Research Reviews. 68: 101318. doi:10.1016/j.arr.2021.101318. PMC 8131215. PMID 33711510.
^ Balzano, Tiziano; Esteban-García, Noelia; Blesa, Javier (2 January 2023). "Neuroinflammation, immune response and α-synuclein pathology: how animal models are helping us to connect dots". Expert Opinion on Drug Discovery. 18 (1): 13–23. doi:10.1080/17460441.2023.2160440. PMID 36538833. S2CID 254959175.
^ Liu, Ping; Wang, Yunyun; Sun, Yan; Peng, Guoping (April 2022). "Neuroinflammation as a Potential Therapeutic Target in Alzheimer's Disease". Clinical Interventions in Aging. 17: 665–674. doi:10.2147/CIA.S357558. PMC 9064449. PMID 35520949.
^ Xi, Yilong; Chen, Yun; Jin, Yi; Han, Guochen; Song, Mingjie; Song, Tingting; Shi, Yang; Tao, Ling; Huang, Zewei; Zhou, Jianping; Ding, Yang; Zhang, Huaqing (May 2022). "Versatile nanomaterials for Alzheimer's disease: Pathogenesis inspired disease-modifying therapy". Journal of Controlled Release. 345: 38–61. doi:10.1016/j.jconrel.2022.02.034. PMID 35257810. S2CID 247285338.
^ "U.S. Clinical Trial: Neurological Associates of West Los Angeles Listed a New Clinical Trial to Study Insulin-sensitizing NE3107 in Improving Sleep and Fatigue in Subjects With Traumatic Brain Injury." Contify Life Science News, 1 Aug. 2023, p. NA. Gale OneFile: Health and Medicine, link.gale.com/apps/doc/A759542006/HRCA?u=anon~bb46c85&sid=sitemap&xid=0c315c7e. Accessed 14 Dec. 2023.

[AdisInsight-1] "Bezisterim". AdisInsight. 5 September 2024. Retrieved 26 September 2024.

[2] Reading, Chris L; Ahlem, Clarence N; Parameswaran, Narayanan (December 2021). "Rationale for an anti-inflammatory insulin sensitizer in a phase 3 Alzheimer's disease trial". Alzheimer's & Dementia. 17 (S9). doi:10.1002/alz.057438.

[3] Stoiljkovic, Milan; Horvath, Tamas L.; Hajós, Mihály (July 2021). "Therapy for Alzheimer's disease: Missing targets and functional markers?". Ageing Research Reviews. 68: 101318. doi:10.1016/j.arr.2021.101318. PMC 8131215. PMID 33711510.

[4] Balzano, Tiziano; Esteban-García, Noelia; Blesa, Javier (2 January 2023). "Neuroinflammation, immune response and α-synuclein pathology: how animal models are helping us to connect dots". Expert Opinion on Drug Discovery. 18 (1): 13–23. doi:10.1080/17460441.2023.2160440. PMID 36538833. S2CID 254959175.

[5] Liu, Ping; Wang, Yunyun; Sun, Yan; Peng, Guoping (April 2022). "Neuroinflammation as a Potential Therapeutic Target in Alzheimer's Disease". Clinical Interventions in Aging. 17: 665–674. doi:10.2147/CIA.S357558. PMC 9064449. PMID 35520949.

[6] Xi, Yilong; Chen, Yun; Jin, Yi; Han, Guochen; Song, Mingjie; Song, Tingting; Shi, Yang; Tao, Ling; Huang, Zewei; Zhou, Jianping; Ding, Yang; Zhang, Huaqing (May 2022). "Versatile nanomaterials for Alzheimer's disease: Pathogenesis inspired disease-modifying therapy". Journal of Controlled Release. 345: 38–61. doi:10.1016/j.jconrel.2022.02.034. PMID 35257810. S2CID 247285338.

[7] "U.S. Clinical Trial: Neurological Associates of West Los Angeles Listed a New Clinical Trial to Study Insulin-sensitizing NE3107 in Improving Sleep and Fatigue in Subjects With Traumatic Brain Injury." Contify Life Science News, 1 Aug. 2023, p. NA. Gale OneFile: Health and Medicine, link.gale.com/apps/doc/A759542006/HRCA?u=anon~bb46c85&sid=sitemap&xid=0c315c7e. Accessed 14 Dec. 2023.

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