Detection of the selective androgen receptor modulator GSK2881078 and metabolites in urine and hair after single oral administration

• Published in: Drug testing and analysis 2021-01, Vol.13 (1), p.217-222
• Main Authors: Rading, Alina, Anielski, Patricia, Thieme, Detlef, Keiler, Annekathrin Martina
• Format: Article
• Language: English
• Subjects: Androgens; doping control; GSK2881078; hair; metabolism; Metabolites; Oral administration; Urine
• ISSN: 1942-7603; 1942-7611
• DOI: 10.1002/dta.2943

Hair and urine concentrations of the nonsteroidal selective androgen receptor modulator GSK2881078 were examined following single oral administration to investigate its hair incorporation and estimate the general suitability of hair testing for selected androgen receptor modulators. Hair segments were collected following a single dose of 1.5 mg GSK2881078 by repeated shaving of scalp hair at Week 0 (blank), Week 1 (representing the pre‐application period), Week 3 (ideally focusing the time of incorporation), and Weeks 5 and 9 (post‐administration period). The intact compound and various (at least 4) hydroxy‐metabolites exhibited similar elimination profiles. The peak urinary concentration (approximately 920 pg/ml) was observed after 8 h and is reduced to the detection limit (2 pg/ml) on Day 42 following administration of 760 μg GSK2881078. Correspondingly, hair concentrations of GSK2881078 (intact compound only) following a single oral dose of 1.5 mg GSK2881078 reached a peak concentration of 1.7 pg/mg in the segments collected 3 weeks post administration, representing the time of ingestion. The concentration rapidly declined to trace amounts of 0.7 (Week 5) and 0.2 pg/mg (Week 9), respectively. In conclusion, measurement of the intact compound GSK2881078 is feasible for both urine and hair analysis. However, concentrations in hair after single oral administration are in the low pg/mg range and can only be detected, if the segments cover the administration period. The excretion and metabolism of the selective androgen receptor modulator GSK2881078 was investigated after oral administration by one volunteer. Beside urinary excretion of the intact compound and identified metabolites, the potential incorporation in the hair matrix was evaluated.