Sipasterol

Sipasterol
Clinical data
Other namesAndrotriol; Triol; Annaosanchun; YC-6; YC6; 5α-Androstane-3β,5α,6β-triol; 5α-Androst-3β,5,6β-triol
Routes of
administration		Intravenous infusion
Drug classAnti-inflammatory steroid; Neuroprotective agent
Identifiers
  • (3S,5R,6R,8S,9S,10R,13S,14S)-10,13-dimethyl-1,2,3,4,6,7,8,9,11,12,14,15,16,17-tetradecahydrocyclopenta[a]phenanthrene-3,5,6-triol
CAS Number
PubChem CID
ChemSpider
Chemical and physical data
FormulaC19H32O3
Molar mass308.462 g·mol−1
3D model (JSmol)
  • C[C@@]12CCC[C@H]1[C@@H]3C[C@H]([C@]4(C[C@H](CC[C@@]4([C@H]3CC2)C)O)O)O
  • InChI=1S/C19H32O3/c1-17-7-3-4-14(17)13-10-16(21)19(22)11-12(20)5-9-18(19,2)15(13)6-8-17/h12-16,20-22H,3-11H2,1-2H3/t12-,13-,14-,15-,16+,17-,18+,19-/m0/s1
  • Key:IFRIPYPBJCUNAG-OTMXHXQLSA-N

Sipasterol (INNTooltip International Nonproprietary Name; developmental code name YC-6), also known as androtriol, 5α-androstane-3β,5α,6β-triol, or annaosanchun, is an experimental anti-inflammatory steroid which is under development for the treatment of ischaemic stroke. It is given by intravenous infusion.

The drug has shown neuroprotective, anti-inflammatory, anti-excitotoxic, and anti-edema effects in preclinical research. The exact mechanism of action of sipasterol is undefined.

The chemical synthesis of sipasterol from dehydroepiandrosterone (DHEA) has been described. It is a synthetic analogue of the endogenous neuroprotective steroid and major cholesterol metabolite cholestane-3β,5α,6β-triol, which is known to produce neuroprotective effects by acting as a negative allosteric modulator of the NMDA receptor and inhibitor of acid-sensing ion channels and is known to inhibit neuronal hyperexcitability and produce anticonvulsant effects by negatively modulating voltage-gated sodium channels.

Sipasterol was first described in the scientific literature by 2013. It is under development by Guangzhou Cellprotek Pharmaceutical and Xiuhe Medical Technique. As of November 2024, no recent development has been reported. However, the findings of a phase 2 clinical trial were published in October 2025 and the drug's INN was designated in July 2026.

See also

References

  1. 1 2 3 4 5 6 7 "Androtriol - Guangzhou Cellprotek Pharmaceutical". adisinsight.springer.com. Retrieved 27 October 2026.
  2. 1 2 "WHO2026" (PDF). cdn.who.int.
  3. 1 2 3 Hou H, Feng B, Zang D, Li Z, Wang Y, Zhao X, et al. (November 2025). "Safety and Feasibility of YC-6 in Patients With Large Hemispheric Infarction: A Randomized Clinical Trial". Journal of the American Heart Association. 14 (21) e039157. doi:10.1161/JAHA.124.039157. PMC 12684777. PMID 41147407.
  4. 1 2 3 4 Chen J, Leng T, Chen W, Yan M, Yin W, Huang Y, et al. (October 2013). "A synthetic steroid 5α-androst-3β,5,6β-triol blocks hypoxia/reoxygenation-induced neuronal injuries via protection of mitochondrial function". Steroids. 78 (10): 996–1002. doi:10.1016/j.steroids.2013.06.004. PMID 23811019.
  5. ↑ Yan M, Leng T, Tang L, Zheng X, Lu B, Li Y, et al. (February 2017). "Neuroprotectant androst-3β, 5α, 6β-triol suppresses TNF-α-induced endothelial adhesion molecules expression and neutrophil adhesion to endothelial cells by attenuation of CYLD-NF-κB pathway". Biochemical and Biophysical Research Communications. 483 (2): 892–896. Bibcode:2017BBRC..483..892Y. doi:10.1016/j.bbrc.2017.01.030. PMID 28082198.
  6. 1 2 Zhang P, Chen JS, Li QY, Sheng LX, Gao YX, Lu BZ, et al. (January 2020). "Neuroprotectants attenuate hypobaric hypoxia-induced brain injuries in cynomolgus monkeys". Zoological Research. 41 (1): 3–19. doi:10.24272/j.issn.2095-8137.2020.012. PMC 6956719. PMID 31840949.
  7. ↑ Xue D, Wei C, Zhou Y, Wang K, Zhou Y, Chen C, et al. (July 2022). "TRIOL Inhibits Rapid Intracellular Acidification and Cerebral Ischemic Injury: The Role of Glutamate in Neuronal Metabolic Reprogramming". ACS Chemical Neuroscience. 13 (14): 2110–2121. doi:10.1021/acschemneuro.2c00119. PMID 35770894.
  8. ↑ Hu H, Zhou Y, Leng T, Liu A, Wang Y, You X, et al. (August 2014). "The major cholesterol metabolite cholestane-3β,5α,6β-triol functions as an endogenous neuroprotectant". The Journal of Neuroscience. 34 (34): 11426–11438. doi:10.1523/JNEUROSCI.0344-14.2014. PMC 6615515. PMID 25143622.
  9. ↑ Sun H, Yang T, Simon R, Xiong ZG, Leng T (June 2024). "Cholestane-3β,5α,6β-Triol Inhibits Acid-Sensing Ion Channels and Reduces Acidosis-Mediated Ischemic Brain Injury". Stroke. 55 (6): 1660–1671. doi:10.1161/STROKEAHA.124.046963. PMC 11126354. PMID 38660789.
  10. ↑ Tang L, Wang Y, Leng T, Sun H, Zhou Y, Zhu W, et al. (June 2015). "Cholesterol metabolite cholestane-3β,5α,6β-triol suppresses epileptic seizures by negative modulation of voltage-gated sodium channels". Steroids. 98: 166–172. doi:10.1016/j.steroids.2014.12.025. PMID 25578735.
  11. ↑ Tang L, Yan M, Leng T, Yin W, Cai S, Duan S, et al. (January 2018). "Cholestane-3β, 5α, 6β-triol suppresses neuronal hyperexcitability via binding to voltage-gated sodium channels". Biochemical and Biophysical Research Communications. 496 (1): 95–100. Bibcode:2018BBRC..496...95T. doi:10.1016/j.bbrc.2018.01.004. PMID 29307820.