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).Completion of Phase 1 Clinical Studies of Ansofaxine Hydrochloride Extended Release Tablets (LY03005) in the U.S.
/ref> It is described as an SNDRI and

prodrug A prodrug is a medication or compound that, after intake, is metabolized (i.e., converted within the body) into a pharmacologically active drug. Instead of administering a drug directly, a corresponding prodrug can be used to improve how the drug ...

desvenlafaxine Desvenlafaxine, sold under the brand name Pristiq among others, is a medication used to treat depression. It is an antidepressant of the serotonin-norepinephrine reuptake inhibitor (SNRI) class and is taken by mouth. It is recommended that the ...

. However, unlike desvenlafaxine, which has '' in vitro'' values of 53 nM and 538 nM for inhibition of

serotonin Serotonin () or 5-hydroxytryptamine (5-HT) is a monoamine neurotransmitter. Its biological function is complex and multifaceted, modulating mood, cognition, reward, learning, memory, and numerous physiological processes such as vomiting and vas ...

and norepinephrine reuptake, respectively, toludesvenlafaxine has respective ''in vitro'' IC₅₀ values of 723 nM, 763 nM, and 491 nM for serotonin, norepinephrine, and

dopamine Dopamine (DA, a contraction of 3,4-dihydroxyphenethylamine) is a neuromodulatory molecule that plays several important roles in cells. It is an organic compound, organic chemical of the catecholamine and phenethylamine families. Dopamine const ...

reuptake inhibition. As of July 2018, the drug is in preregistration for MDD in the United States, the European Union,

Japan Japan ( ja, 日本, or , and formally , ''Nihonkoku'') is an island country in East Asia. It is situated in the northwest Pacific Ocean, and is bordered on the west by the Sea of Japan, while extending from the Sea of Okhotsk in the north ...

, and

China China, officially the People's Republic of China (PRC), is a country in East Asia. It is the world's most populous country, with a population exceeding 1.4 billion, slightly ahead of India. China spans the equivalent of five time zones and ...

. In December 2018 the drug is in phase III trial in the United States and China. In March of 2020 the FDA accepted Luye Pharma's new drug application for ansofaxine. In December 2021 Luye Pharma released results from phase II clinical trials on ansofaxine. Luye Pharma Group has issued the brand name Ruoxinlin for the upcoming medication Ansofaxine. In November of 2022 Ruoxinlin was approved for MDD in China.

References

External links

Toludesvenlafaxine hydrochloride extended release - AdisInsight
Antidepressants Cyclohexanols Experimental drugs Phenethylamines Phenols Serotonin–norepinephrine–dopamine reuptake inhibitors Tertiary alcohols {{Nervous-system-drug-stub

See also

References

External links