Perspectives in Evaluating Selective Androgen Receptor Modulators in Human Hair: A Short Communication

Abstract

Background: As hair testing increases the window of drug detection and permits the differentiation of long-term use from a single exposure when performing segmental analyses (which also allows establishing the pattern of use), this matrix should be considered as a suitable complement to standard investigations in clinical, forensic, and sport toxicology. The authors were recently involved in 3 cases where hair analysis was used to demonstrate the use of selective androgen receptor modulators (SARMs), including ligandrol (LGD-4033), andarine (S-4), and ostarine (S-22). SARMs are increasingly being abused as "safe" alternatives to steroids.Methods: After decontamination using dichloromethane, hair specimens were segmented, cut into very small segments (,1 mm), incubated overnight in a buffer, and extracted using a mixture of organic solvents. Drugs were tested using liquid chromatography-tandem mass spectrometry and confirmed using liquid chromatography/HRMS. Results:The determined concentrations were as follows: ligandrol, 14-42 pg/mg; andarine, 0.1-0.7 pg/mg; and ostarine, 3-21 pg/mg. Conclusions:To enhance performance, SARMs must be used on a long-term basis, which can have serious clinical consequences, including liver damage, myocardial infarction, and blood clots. Hair testing for SARMs has additional benefits versus urine analysis as it can detect the parent compound and numerous metabolites.

Peroxisome Proliferator-Activated Receptor Delta Agonist (PPAR- δ) and Selective Androgen Receptor Modulator (SARM) Abuse: Clinical, Analytical and Biological Data in a Case Involving a Poisonous Combination of GW1516 (Cardarine) and MK2866 (Ostarine)

“…In a case of a subject abusing cardarine for improving athletic performances, concentrations of 32 and 22 pg/mg were measured in 2 × 2 cm segments [ 21 ]. Ostarine has been identified on several occasions, including doping challenges or drug trafficking [ 9 , 18 , 19 , 20 ]. Concentrations ranged from 1 to 168 pg/mg and individual results are presented in Table 4 .…”

“…The biological specimens (blood, urine and hair) were tested by liquid chromatography coupled to tandem mass spectrometry (LC-MS/MS), using previously described methods for ostarine [ 18 , 19 ] and cardarine [ 20 ]. Briefly, 1 mL of blood or hydrolyzed urine (with 20,000 UI of ß-glucuronidase at pH 5.2) was extracted in 1 mL borate pH 9.5 buffer and 5 mL of diethyl ether/dichloromethane/hexane (50/30/20, v / v ) in presence of 100 ng of bicalutamide-d 4 used as internal standard.…”

“…The conditions of use of the equipment (Waters Acquity class I ultra-high performance liquid chromatography and XEVO TQS micro triple quadrupole mass spectrometer) have been described in previous papers [ 18 , 19 , 20 ]. Briefly, separation was achieved using a Waters Acquity HSS C18 column (150 × 2.1 mm × 1.8 µm) at 50 °C using a gradient elution with pH 3 formate buffer (phase A) and 0.1% formic acid in acetonitrile (phase B) and a flow rate at 0.4 mL/min.…”

“…As a consequence, in the limited case reports involving SARMs or PPAR- δ, there is no toxicological data (identification of the substance and evaluation of its concentration). Testing for ostarine [ 9 , 18 , 19 , 20 ] and GW1516 [ 21 ] in human hair is the privilege of our laboratory as no other citation is available in the scientific literature.…”

Annual banned‐substance review: Analytical approaches in human sports drug testing 2020/2021

“…Further to the urine analysis, scalp hair was sampled before and up to 9 weeks by shaving, demonstrating the traceability of GSK2881078 only between 3 and 9 weeks after ingestion at 0.2–1.7 pg/mg. Since hair testing has been considered in several cases of AAFs lately, such information is of continuously increasing importance concerning result interpretation in anti‐doping 132 …”