Ansofaxine
Clinical data
Other namesLY03005; LPM570065; 4-Methylbenzoate desvenlafaxine
Routes of
administration		By mouth
Identifiers
  • 4-[2-(Dimethylamino)-1-(1-hydroxycyclohexyl)ethyl]phenyl 4-methylbenzoate
CAS Number
PubChem CID
ChemSpider
UNII
Chemical and physical data
FormulaC24H31NO3
Molar mass381.516 g·mol−1
3D model (JSmol)
  • Cc1ccc(cc1)C(=O)Oc2ccc(cc2)C(CN(C)C)C3(CCCCC3)O
  • InChI=1S/C24H31NO3/c1-18-7-9-20(10-8-18)23(26)28-21-13-11-19(12-14-21)22(17-25(2)3)24(27)15-5-4-6-16-24/h7-14,22,27H,4-6,15-17H2,1-3H3
  • Key:QKYBZJLEMOZFFU-UHFFFAOYSA-N

Toludesvenlafaxine, also formerly known as ansofaxine and sold under the brand name Ruoxinlin, is an antidepressant which is approved for the treatment of major depressive disorder in China.[1] It is also under development for use in other countries like the United States.[1] It is a serotonin–norepinephrine–dopamine reuptake inhibitor (SNDRI) and was developed by Luye Pharma Group.[1][2][3][4]

Toludesvenlafaxine is described as an SNDRI and prodrug to desvenlafaxine.[2] However, unlike desvenlafaxine, which has in vitro IC50Tooltip half-maximal inhibitory concentration values of 53 nM and 538 nM for inhibition of serotonin and norepinephrine reuptake, respectively, toludesvenlafaxine has respective in vitro IC50 values of 723 nM, 763 nM, and 491 nM for serotonin, norepinephrine, and dopamine reuptake inhibition.[2] As such, toludesvenlafaxine appears to be a more balanced reuptake inhibitor of serotonin, norepinephrine, and dopamine than desvenlafaxine.[2]

As of July 2018, toludesvenlafaxine is in preregistration for the treatment of depression in the United States, the European Union, and Japan.[1] As of January 2023, it is also in phase 3 clinical trials for the treatment of generalized anxiety disorder.[1] In March 2020, the United States Food and Drug Administration accepted Luye Pharma's New Drug Application for toludesvenlafaxine, which remains under review.[1][5] In November 2022, toludesvenlafaxine was approved for the treatment of depression in China under the brand name Ruoxinlin.[6][7]

References

  1. 1 2 3 4 5 6 "Toludesvenlafaxine extended release - Luye Pharma". AdisInsight. Springer Nature Switzerland AG.
  2. 1 2 3 4 Zhang R, Li X, Shi Y, Shao Y, Sun K, Wang A, et al. (2014). "The effects of LPM570065, a novel triple reuptake inhibitor, on extracellular serotonin, dopamine and norepinephrine levels in rats". PLOS ONE. 9 (3): e91775. Bibcode:2014PLoSO...991775Z. doi:10.1371/journal.pone.0091775. PMC 3948889. PMID 24614602.
  3. ↑ Dale E, Bang-Andersen B, Sánchez C (May 2015). "Emerging mechanisms and treatments for depression beyond SSRIs and SNRIs". Biochemical Pharmacology. 95 (2): 81–97. doi:10.1016/j.bcp.2015.03.011. PMID 25813654.
  4. ↑ Completion of Phase 1 Clinical Studies of Ansofaxine Hydrochloride Extended Release Tablets (LY03005) in the U.S.
  5. ↑ "Luye Pharma Releases Top-Line Results from a Phase II Clinical Trial of Its New Antidepressant Ansofaxine Hydrochloride Extended-Release Tablets". BioSpace. Retrieved 2022-02-08.
  6. ↑ "Luye Pharma's Class 1 Innovative Antidepressant Ruoxinlin® Approved for Launch in China - Press Releases - Luye Pharma Group". www.luye.cn. Retrieved 2022-12-04.
  7. ↑ "R&D - Luye Pharma Group". www.luye.cn. Retrieved 2022-10-06.
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