ArticleRapid communications in mass spectrometry : RCM2025
Synthesis and In Vitro Metabolic Profiling of the Selective Androgen Receptor Modulator (SARM) LY305.
Article in Rapid communications in mass spectrometry : RCM, 2025. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 2 papers.
What it found
Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.
The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.
Who cites it
2 citing papers in PubMed.
- Annual Banned-Substance Review 18th Edition-Analytical Approaches in Human Sports Drug Testing 2024/2025.Drug testing and analysis · 2026Review
- Synthesis and In Vitro Metabolic Profiling of the Selective Androgen Receptor Modulator (SARM) LY305.Rapid communications in mass spectrometry : RCM · 2025Article
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
5 authors.
Funding
Abstract
rationale2-Chloro-4-[[(1R,2R)-2-hydroxy-2-methyl-cyclopentyl]amino]-3-methyl-benzonitrile (LY305) is a transdermal selective androgen receptor modulator (SARM) that has been under development as a potential therapeutic for conditions involving muscle wasting, osteoporosis, or hypogonadism. Due to its proven anabolic effects, its potential (and illicit) use in sport must be taken into consideration, necessitating information on its biotransformation for the implementation of adequate target analytes into routine doping control analytical procedures. In this study, the synthesis of LY305 and in vitro-derived metabolites of the SARM are described.
methodsLY305 was synthesized by a Buchwald-Hartwig amination using 2-chloro-4-iodo-3-methylbenzonitrile and (1R,2R)-2-amino-1-methyl-cyclopentanol. The in vitro metabolism experiments were conducted using human liver microsomes (HLM) and the S9 fraction to allow for studying phase-I and phase-II biotransformations. For the detection and separation of LY305 and its metabolites, liquid chromatography-high-resolution tandem mass spectrometry was used.
resultsOverall, 18 metabolites were detected, nine of which were identified as phase-I metabolites and an additional nine were attributed to phase-II conjugates. Metabolic reactions were as follows: hydroxylation, dehydrogenation, oxidation, oxidation and hydroxylation, O-glucuronidation, hydroxylation with subsequent glucuronidation, and bis-hydroxylation with subsequent glucuronidation.
conclusionsThe transdermal SARM LY305 was successfully synthesized and subjected to in vitro metabolic studies, yielding chromatographic and mass spectral data that support improving comprehensive anti-doping tests. To the best of our knowledge, no published experimental data exist that report on the in vitro metabolic profile of LY305, a substance that might undergo further (pre)clinical evaluation.
Indexed as
Identifiers
What OpenQuestion holds
Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.