Last update 21 Nov 2024

Mesterolone

Last update 21 Nov 2024

Overview

R&D Status

Clinical Result

Translational Medicine

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Mesterolone (USAN/INN)

+ [1]

Target

Mechanism

AR agonists(Androgen Receptor agonists)

Therapeutic Areas

Urogenital Diseases

Active Indication

Infertility

Inactive Indication-

Originator Organization-

Active Organization-

Inactive Organization-

Drug Highest PhaseApproved

First Approval Date-

Regulation-

Structure

Molecular FormulaC20H32O2

InChIKeyUXYRZJKIQKRJCF-TZPFWLJSSA-N

CAS Registry1424-00-6

100 Clinical Results associated with Mesterolone

100 Translational Medicine associated with Mesterolone

100 Patents (Medical) associated with Mesterolone

147

Literatures (Medical) associated with Mesterolone

24 Nov 2023·International Journal of Analytical Chemistry

Chemical Application of Topological Indices in Infertility Treatment Drugs and QSPR Analysis

Article

Author: Sultana, Sobia

The main challenges faced by medical researchers while producing novel drugs are time commitment, amplified costs, creating a safety profile for the medications, reduced solubility, and a lack of experimental data. Chemical graph theory makes an important theoretical contribution to drug development and design by investigating the structural properties of molecules. To improve drug research and assess the effectiveness of treatments, topological indices aim to provide a mathematical representation of molecular structures. In this study, the author examined a number of recently used drugs, including tamoxifen, mesterolone, anastrozole, and letrozole which are used to treat infertility. We compute the topological descriptors with the limiting behaviors associated with these pharmaceutical drugs and offer degree-based topological parameters for them. We conducted a QSPR investigation on the prospective degree-based topological descriptors using quadratic, cubic, exponential, and logarithmic regression models.

01 Aug 2023·Drug testing and analysis

Detection time comparison of non-hydrolysed sulphated metabolites of metenolone, mesterolone and 17α-methyltestosterone analysed by four different mass spectrometric techniques.

Article

Author: Van Gansbeke, Wim ; Van Eenoo, Peter ; Polet, Michael ; Albertsdottir, Adalheidur Dora

The frequent detection of anabolic androgenic steroids (AAS) indicates their popularity among rule-breaking athletes. The so called long-term metabolites play a crucial role in their detection, and non-hydrolysed sulphated metabolites have gained renewed interest, as research has demonstrated their extended detection time compared to the more conventional markers (e.g., for metenolone and mesterolone). Their potential has been investigated using liquid and gas chromatography-mass spectrometry (LC- and GC-MS). However, due to their complementary nature, chances are that the most promising metabolite on one technique does not necessarily exhibit the same behaviour on the other and vice versa. Therefore, a comparison was carried out where as a trial model, metenolone, mesterolone and 17α-methyltestosterone were selected and the most likely long-term sulphated metabolites identified on four mass spectrometric instruments. Additionally, using a modified sample preparation procedure, comparison between conventional and non-hydrolysed sulphated metabolites between different GC-MS instruments was also included. When focusing on each individual marker, no cases were observed where a single metabolite provided a superior detection time on all instruments. Furthermore, for each AAS, there were incidences where a metabolite provided the best detection time on one instrument but could only be detected for a shorter period or not at all on other instruments. This demonstrates that metabolite detection windows and hence their added-value as target substance are unique and dependent on the analytical technique and not only on their pharmacokinetic behaviour. Consequently, in each case, a metabolite versus instrument evaluation is needed to maximise the probabilities of detecting doping offences.

01 Jun 2023·Drug Testing and Analysis

LC‐MS/(MS) confirmatory doping control analysis of intact phase II metabolites of methenolone and mesterolone after Girard's Reagent T derivatization

Article

Author: Angelis, Yiannis S. ; Fragkaki, Argyro G. ; Sakellariou, Panagiotis ; Kiousi, Polyxeni ; Christophoridis, Christophoros

AbstractIn the present study, the application and evaluation of Girard's Reagent T (GRT) derivatization for the simultaneous detection and significantly important identification of different phase II methenolone and mesterolone metabolites by LC‐MS/(MS) are presented. For the LC‐MS analysis of target analytes two complementary isolation methods were developed; a derivatization and shoot method in which native urine is diluted with derivatization reagent and is injected directly to LC‐MS and a liquid–liquid extraction method, using ethyl acetate at pH 4.5, for the effective isolation of both sulfate and glucuronide metabolites of the named steroids as well as of their free counterparts. For the evaluation of the proposed protocols, urine samples from methenolone and mesterolone excretion studies were analyzed against at least one sample from a different excretion study. Retention times, along with product ion ratios, were evaluated according to the WADA TD2021IDCR requirements, in order to determine maximum detection and identification time windows for each metabolite. Established identification windows obtained after LC‐MS/(MS) analysis were further compared with those obtained after GC‐MS/(MS) analysis of the same samples from the same excretion studies, for the most common analytes monitored by GC‐MS/(MS). Full validation was performed for the developed derivatization and shoot method for the identification of methenolone metabolite, 3α‐hydroxy‐1‐methylen‐5α‐androstan‐17‐one‐3‐glucuronide (mth3). Overall, the GRT derivatization presented herein offers a tool for the simultaneous sensitive detection of free, intact glucuronide and sulfate metabolites by LC‐MS/(MS) that enhance significantly the detection and identification time windows of specific methenolone and mesterolone metabolites for doping control analysis.

100 Deals associated with Mesterolone

External Link

KEGG	Wiki	ATC	Drug Bank
D04947	Mesterolone	G03BB01	DB13587

R&D Status

10 top approved records.

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Indication	Country/Location	Organization	Date
Infertility	-	-	-

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