TABLE 3

Percentages of lemborexant and its metabolites recovered in excreta after a single oral dose of [14C]lemborexant

Urine samples at 0–120 h and fecal samples at 0–264 h postdose were used. Each value represents the mean ± S.D. of eight subjects.

AnalyteM No.Dose
UrineFecesTotal
%
Met4—0.5 ± 0.4ND0.5 ± 0.4
Met5—0.7 ± 0.4ND0.7 ± 0.4
Met6M230.5 ± 0.4ND0.5 ± 0.4
Met7—0.2 ± 0.3ND0.2 ± 0.3
Met9aM16b, M22b1.7 ± 0.4ND1.7 ± 0.4
Met10—ND0.3 ± 0.40.3 ± 0.4
Met11cM17d0.6 ± 0.3ND0.6 ± 0.3
Met12M1811.0 ± 2.5ND11.0 ± 2.5
Met13M240.9 ± 0.2ND0.9 ± 0.2
Met14e—ND0.8 ± 0.50.8 ± 0.5
Met15f—ND1.7 ± 0.41.7 ± 0.4
Met16gM13h0.9 ± 0.2ND0.9 ± 0.2
Met17M200.5 ± 0.4ND0.5 ± 0.4
Met19—ND1.1 ± 0.41.1 ± 0.4
Met20M211.4 ± 0.7ND1.4 ± 0.7
Met21iM11j, M14j0.8 ± 0.3ND0.8 ± 0.3
Met22kM1lND2.5 ± 0.72.5 ± 0.7
Met24mM12n, M4n4.0 ± 1.312.0 ± 2.116.0 ± 1.8
Met25M7ND1.4 ± 0.31.4 ± 0.3
Met26oM3p, M9pND4.7 ± 1.84.7 ± 1.8
Met28M8ND0.7 ± 0.50.7 ± 0.5
Lemborexant + Met29q—ND13.0 ± 5.313.0 ± 5.3

  • —, not applicable; ND, below the lower limit of detection.

  • ↵a Met9 was a mixture of Met9-1, Met9-2, Met9-3, and Met9-4.

  • ↵b Met9-1 and Met9-4 were identified as M16 and M22, respectively.

  • ↵c Met11 was a mixture of Met11-1, Met11-2, and Met11-3.

  • ↵d Met11-1 was identified as M17.

  • ↵e Met14 was a mixture of Met14-1 and Met14-2

  • ↵f Met15 was a mixture of Met15-1 and Met15-2.

  • ↵g Met16 was a mixture of Met16-1 and Met16-2.

  • ↵h Met16-2 was identified as M13.

  • ↵i Met21 was a mixture of Met21-1 and Met21-2.

  • ↵j Met21-1 and Met21-2 were identified as M11 and M14, respectively.

  • ↵k Met22 was a mixture of Met22-1 and Met22-2.

  • ↵l Met22-1 was identified as M1.

  • ↵m Met24 was a mixture of Met24-1 and Met24-2. Met24-2 was not detected in feces.

  • ↵n Met24-1 and Met24-2 were identified as M12 and M4, respectively.

  • ↵o Met26 was a mixture of Met26-1 and Met26-2.

  • ↵p Met26-1 and Met26-2 were identified as M3 and M9, respectively.

  • ↵q Met29 was eluted as a mixture with lemborexant.