Ansofaxine

Ansofaxine
Clinical data
Other names	LY03005; LPM570065; 4-Methylbenzoate desvenlafaxine hydrochloride
Routes of; administration	By mouth
Identifiers
	IUPAC name 4-[2-(Dimethylamino)-1-(1-hydroxycyclohexyl)ethyl]phenyl 4-methylbenzoate;
CAS Number	916918-84-8 (hydrochloride);
PubChem CID	56955395;
ChemSpider	13114670;
UNII	V6Z6K3OQX4;
Chemical and physical data
Formula	C24H31NO3
Molar mass	381.516 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES Cc1ccc(cc1)C(=O)Oc2ccc(cc2)C(CN(C)C)C3(CCCCC3)O;
	InChI 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 (former developmental code names LY03005, LPM570065), also known as ansofaxine or as 4-methylbenzoate desvenlafaxine, is a serotonin–norepinephrine–dopamine reuptake inhibitor (SNDRI) which is under development by Luye Pharma Group for the treatment of major depressive disorder (MDD).^[1]^[2]^[3]^[4] It is described as an SNDRI and prodrug to desvenlafaxine.^[2] However, unlike desvenlafaxine, which has in vitro IC₅₀ 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 of July 2018, the drug is in preregistration for MDD in the United States, the European Union, Japan, and China.^[1] In December 2018 the drug is in phase III trial in the United States and China.^[5] In March of 2020 the FDA approved Luye Pharma's new drug application for ansofaxine.^[6] In December 2021 Luye Pharma released results from phase II clinical trials on ansofaxine. ^[7]

References[]

^ ^a ^b "Toludesvenlafaxine extended release - Luye Pharma - AdisInsight".
^ ^a ^b ^c Zhang R, Li X, Shi Y, Shao Y, Sun K, Wang A, Sun F, Liu W, Wang D, Jin J, Li Y (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.
^ Dale, Elena; Bang-Andersen, Benny; Sánchez, Connie (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. ISSN 0006-2952. PMID 25813654.
^ Completion of Phase 1 Clinical Studies of Ansofaxine Hydrochloride Extended Release Tablets (LY03005) in the U.S.
^ "Luye Pharma's Global Strategy For CNS-Focused Products Gathers Pace: Rotigotine Extended Release Microspheres Submitted to Japan's PMDA for Clinical Trials Approval - Press Releases - Luye Pharma Group". www.luye.cn. Retrieved 2022-02-08.
^ "NDA Filing for Luye Pharma's Antidepressant Drug LY03005 Accepted by the U.S. FDA - Press Releases - Luye Pharma Group". www.luye.cn. Retrieved 2022-02-08.
^ "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.

External links[]

Toludesvenlafaxine hydrochloride extended release - AdisInsight

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[AdisInsight-1] "Toludesvenlafaxine extended release - Luye Pharma - AdisInsight".

[pmid24614602-2] Zhang R, Li X, Shi Y, Shao Y, Sun K, Wang A, Sun F, Liu W, Wang D, Jin J, Li Y (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.

[DaleBang-Andersen2015-3] Dale, Elena; Bang-Andersen, Benny; Sánchez, Connie (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. ISSN 0006-2952. PMID 25813654.

[evaluategroup-4] Completion of Phase 1 Clinical Studies of Ansofaxine Hydrochloride Extended Release Tablets (LY03005) in the U.S.

[5] "Luye Pharma's Global Strategy For CNS-Focused Products Gathers Pace: Rotigotine Extended Release Microspheres Submitted to Japan's PMDA for Clinical Trials Approval - Press Releases - Luye Pharma Group". www.luye.cn. Retrieved 2022-02-08.

[6] "NDA Filing for Luye Pharma's Antidepressant Drug LY03005 Accepted by the U.S. FDA - Press Releases - Luye Pharma Group". www.luye.cn. Retrieved 2022-02-08.

[7] "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.

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v t Phenethylamines
Phenethylamines	Psychedelics: 25B-NBOMe 25C-NBOMe 25D-NBOMe 25I-NBOMe 25N-NBOMe 2C-B 2C-C 2C-CP 2C-D 2C-E 2C-EF 2C-F 2C-G 2C-G-1 2C-G-2 2C-G-3 2C-G-4 2C-G-5 2C-G-6 2C-G-N 2C-H 2C-I 2C-iP 2C-N 2C-O 2C-O-4 2C-P 2C-SE 2C-T 2C-T-2 2C-T-3 2C-T-4 2C-T-7 2C-T-8 2C-T-9 2C-T-13 2C-T-15 2C-T-16 2C-T-17 2C-T-19 2C-T-21 2C-T-28 2C-TFE 2C-TFM 2C-YN 2C-V Allylescaline DESOXY Escaline Isoproscaline Jimscaline Macromerine MEPEA Mescaline Metaescaline Methallylescaline Proscaline Psi-2C-T-4 TCB-2 Stimulants: Phenylethanolamine Hordenine Phenethylamine Phenpromethamine α-Methylphenethylamine (amphetamine) β-Methylphenethylamine m-Methylphenethylamine N-Methylphenethylamine o-Methylphenethylamine p-Methylphenethylamine Methylphenidate Entactogens: Lophophine MDPEA MDMPEA Others: BOH DMPEA
Amphetamines	Psychedelics: 3C-AL 3C-BZ 3C-E 3C-MAL 3C-P Aleph Beatrice Bromo-DragonFLY D-Deprenyl DMA DMCPA DMMDA DOB DOC DOEF DOET DOI DOM DON DOPR DOTFM Ganesha MMDA MMDA-2 Psi-DOM TMA TeMA ZDCM-04 Stimulants: 2-FA 2-FMA 3-FA 3-FMA Acridorex Alfetamine Amfecloral Amfepentorex Amphetamine (Dextroamphetamine, Levoamphetamine) Amphetaminil Benfluorex Benzphetamine Cathine Clobenzorex Dimethylamphetamine Ephedrine Etilamfetamine Fencamfamin Fencamine Fenethylline Fenfluramine (Dexfenfluramine, Levofenfluramine) Fenproporex Flucetorex Fludorex Formetorex Furfenorex Gepefrine 4-Hydroxyamphetamine Iofetamine Isopropylamphetamine Lefetamine Lisdexamfetamine Mefenorex Metaraminol Methamphetamine (Dextromethamphetamine, Levomethamphetamine) Methoxyphenamine MMA Morforex Norfenfluramine L-Norpseudoephedrine N,alpha-Diethylphenylethylamine Oxifentorex Oxilofrine Ortetamine PBA PCA PFA PFMA PIA PMA PMEA PMMA Phenylpropanolamine Pholedrine Prenylamine Propylamphetamine Pseudoephedrine Sibutramine Tiflorex Tranylcypromine Xylopropamine Zylofuramine Entactogens: 4-FA 4-FMA 4-MA 4-MMA 4-MTA 5-APB 5-APDB 5-EAPB 5-IT 5-MAPB 5-MAPDB 6-APB 6-APDB 6-Chloro-MDMA 6-EAPB 6-IT 6-MAPB 6-MAPDB EDA IAP 2,3-MDA 3,4-MDA (tenamfetamine) MDEA MDHMA MDMA (midomafetamine) MDOH Methamnetamine MMDMA Naphthylaminopropane TAP Others: 3,4-DCA Amiflamine DiFMDA Selegiline (also D-Deprenyl)
Phentermines	Stimulants: Chlorphentermine Cloforex Clortermine Etolorex Mephentermine Pentorex Phentermine Entactogens: MDPH MDMPH Others: Cericlamine
Cathinones	Stimulants: 3-FMC 4-MC 4-BMC 4-CMC 4-EMC 4-FMC 4-MEC 4-MeMABP 4-MPD Amfepramone Benzedrone Brephedrone Buphedrone Bupropion Cathinone Dimethylcathinone Ethcathinone Eutylone Hydroxybupropion Methcathinone Methedrone NEB N-Ethylhexedrone N-Ethylpentedrone Pentedrone Pentylone Radafaxine Entactogens: 3,4-DMMC 3-MMC Butylone Ethylone Methylone Methylenedioxycathinone Mephedrone
Phenylisobutylamines	Entactogens: 4-CAB 4-MAB Ariadne BDB Butylone EBDB Eutylone MBDB Stimulants: Phenylisobutylamine
Phenylalkylpyrrolidines	Stimulants: α-PBP α-PHP α-PPP α-PVP MDPBP MDPPP MDPV 4-MePBP 4-MePHP 4-MePPP MOPPP MOPVP MPBP MPHP MPPP Naphyrone PEP Prolintane Pyrovalerone
Catecholamines (and close relatives)	6-FNE 6-OHDA a-Me-DA a-Me-TRA Adrenochrome Ciladopa D-DOPA (Dextrodopa) Dimetofrine Dopamine Epinephrine Epinine Etilefrine Ethylnorepinephrine Fenclonine Ibopamine Isoprenaline Isoetarine L-DOPA (Levodopa) L-DOPS (Droxidopa) L-Phenylalanine L-Tyrosine m-Tyramine Metanephrine Metaraminol Metaterol Metirosine Methyldopa N,N-Dimethyldopamine Nordefrin (Levonordefrin) Norepinephrine Norfenefrine (m-Octopamine) Normetanephrine Orciprenaline p-Octopamine p-Tyramine Phenylephrine Synephrine
Miscellaneous	AL-LAD Amidephrine Arbutamine Cafedrine Denopamine Desvenlafaxine Diphenidine Dizocilpine Dobutamine Dopexamine Ephenidine Etafedrine ETH-LAD Famprofazone Fluorolintane Hexapradol IP-LAD Lysergic acid amide Lysergic acid 2-butyl amide Lysergic acid 2,4-dimethylazetidide Lysergic acid diethylamide Methoxamine Methoxphenidine MT-45 PARGY-LAD Phenibut PRO-LAD Pronethalol Salbutamol (Levosalbutamol) Solriamfetol Theodrenaline Thiamphenicol UWA-101 Venlafaxine

Clinical data

Other names	LY03005; LPM570065; 4-Methylbenzoate desvenlafaxine hydrochloride
Routes of administration	By mouth
Identifiers
IUPAC name 4-[2-(Dimethylamino)-1-(1-hydroxycyclohexyl)ethyl]phenyl 4-methylbenzoate
CAS Number	916918-84-8 (hydrochloride)
PubChem CID	56955395
ChemSpider	13114670
UNII	V6Z6K3OQX4
Chemical and physical data
Formula	C₂₄H₃₁NO₃
Molar mass	381.516 g·mol⁻¹
3D model (JSmol)	Interactive image
SMILES Cc1ccc(cc1)C(=O)Oc2ccc(cc2)C(CN(C)C)C3(CCCCC3)O
InChI 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

Ansofaxine

See also[]

References[]

External links[]