Comparison of radioactivity-based quantification and LESA quantification of figopitant and its metabolites in different tissues of two different animals
| Tissue | Metabolite | Relative Abundance | LESA CV | LESA Accuracy | LESA | ||||
|---|---|---|---|---|---|---|---|---|---|
| Organ Extraction | LESA1 | LESA2 | LESA3 | LESA Mean | |||||
| % | % | nmol/kg | |||||||
| Lung | M474 | 42.2 | 57.9 | 51.6 | 40.5 | 50.0 | 18 | 118 | 13,242 |
| M490 | 3.2 | 3.2 | 2.7 | 2.1 | 2.7 | 21 | 83 | 706 | |
| Figopitant | 48.6 | 32.1 | 37.2 | 47.4 | 38.9 | 20 | 80 | 10,302 | |
| M542 | 1.0 | BLQ | 1.3 | 1.6 | 1.5 | 15 | 145 | 384 | |
| M544 | 5.0 | 6.8 | 7.2 | 8.4 | 7.5 | 11 | 149 | 1977 | |
| Spleen | M474 | 42.8 | 54.7 | 58.4 | 60.5 | 57.9 | 5 | 135 | 22,196 |
| M490 | 7.5 | 5.5 | 5.6 | 5.5 | 5.5 | 1 | 74 | 2122 | |
| Figopitant | 45.2 | 33.7 | 31.1 | 27.8 | 30.9 | 10 | 68 | 11,840 | |
| M544 | 4.5 | 6.1 | 4.9 | 6.2 | 5.7 | 13 | 127 | 2199 | |
| Kidney (outer medulla) | M474 | 59.2 | 69.9 | 71.5 | 69.2 | 70.2 | 2 | 119 | 18,250 |
| M490 | 9.7 | 8.3 | 9.1 | 9.8 | 9.1 | 8 | 93 | 2357 | |
| Figopitant | 31.1 | 21.9 | 19.4 | 21 | 20.8 | 6 | 67 | 5399 | |
| Salivary gland | M474 | 24.1 | 50.7 | 47.7 | 45.2 | 47.9 | 6 | 199 | 12,949 |
| M488 | 3.2 | 1.5 | 1.2 | 1.1 | 1.3 | 16 | 40 | 461 | |
| M490 | 3.2 | 4.2 | 3.6 | 3.2 | 3.7 | 14 | 115 | 1413 | |
| Figopitant | 67.5 | 39.2 | 42.4 | 45.8 | 42.5 | 8 | 63 | 11,718 | |
| M544 | 2.0 | 4.4 | 5.1 | 4.8 | 4.8 | 7 | 238 | 2307 | |
| White fat | M474 | 10.9 | BLQ | BLQ | BLQ | N.A. | N.A. | N.A. | N.A. |
| Figopitant | 89.1 | 100.0 | 100.0 | 100.0 | 100.0 | N.A. | 112 | 1257 | |
| Myocardium | M474 | 66.0 | 77.0 | 76.7 | 78.5 | 77.4 | 1 | 117 | 9136 |
| Figopitant | 34.0 | 23.0 | 23.3 | 21.5 | 22.6 | 4 | 66 | 2668 | |
| Liver | M448 | 8.6 | 3.6 | 3.4 | 2.9 | 3.3 | 11 | 38 | 1006 |
| M474 | 53.6 | 62.1 | 61.4 | 63.2 | 62.2 | 1 | 116 | 18,978 | |
| M488 | 3.5 | BLQ | BLQ | 0.9 | 0.9 | N.A. | 26 | 274 | |
| M490 | 19.5 | 12.4 | 11.7 | 15.6 | 13.2 | 16 | 68 | 4036 | |
| Figopitant | 9.3 | 14.4 | 14.7 | 9.6 | 12.9 | 22 | 139 | 3934 | |
| M542 | 1.6 | BLQ | BLQ | BLQ | N.A. | N.A. | N.A. | N.A. | |
| M544 | 3.9 | 7.5 | 8.8 | 7.9 | 8.1 | 8 | 207 | 2460 | |
| Pancreas | M448 | 2.4 | BLQ | BLQ | 1.4 | 1.4 | N.A. | 58 | 437 |
| M474 | 40.6 | 56.5 | 58.1 | 53.0 | 55.9 | 5 | 138 | 17,437 | |
| M488 | 4.9 | BLQ | 0.5 | 1.5 | 1.0 | 71 | 20 | 312 | |
| M490 | 9.1 | 7.6 | 9.3 | 6.7 | 7.9 | 17 | 86 | 2455 | |
| Figopitant | 29.7 | 22.8 | 20.7 | 27.7 | 23.7 | 15 | 80 | 7407 | |
| M542 | 3.5 | BLQ | BLQ | BLQ | N.A. | N.A. | N.A. | N.A. | |
| M544 | 9.7 | 13.1 | 11.4 | 9.7 | 11.4 | 15 | 118 | 3561 | |
| Thymus | M474 | 20.9 | 17.9 | 27.3 | 23.3 | 22.8 | 21 | 109 | 2785 |
| Figopitant | 72.2 | 69.7 | 63.1 | 68.7 | 67.2 | 5 | 93 | 8192 | |
| M542 | 4.4 | 1.8 | 0.9 | 0.9 | 1.2 | 43 | 27 | 146 | |
| M544 | 2.5 | 10.6 | 8.7 | 7.1 | 8.8 | 20 | 352 | 1073 | |
| Stomach | M474 | 46.4 | 44.1 | 44.7 | 50.2 | 46.3 | 7 | 100 | N.A. |
| M488 | 5.8 | 1.9 | 1.9 | 2 | 1.9 | 3 | 33 | N.A. | |
| M490 | 7.7 | 7.6 | 6.3 | 11.3 | 8.4 | 31 | 109 | N.A. | |
| Figopitant | 32.6 | 39.6 | 35.6 | 28.7 | 34.6 | 16 | 106 | N.A. | |
| M542 | 4.7 | 0.6 | 4.5 | BLQ | 2.6 | 108 | 54 | N.A. | |
| M544 | 2.9 | 6.3 | 7 | 7.9 | 7.1 | 11 | 244 | N.A. | |
| Testis | M474 | 7.7 | 4.4 | 8.1 | 7.2 | 6.6 | 29 | 85 | 131 |
| Figopitant | 72.8 | 78.9 | 78.5 | 81.1 | 79.5 | 2 | 109 | 1591 | |
| M544 | 19.6 | 16.7 | 13.4 | 11.7 | 13.9 | 18 | 71 | 279 | |
| Harder's gland | M474 | 12.7 | 16.0 | 19.8 | 24.5 | 20.1 | 21 | 158 | 6884 |
| Figopitant | 87.3 | 84.0 | 80.2 | 75.5 | 79.9 | 5 | 92 | 27,367 | |
| Epididymis | M474 | 14.4 | 13.0 | 28.6 | 28.3 | 23.3 | 38 | 162 | 1162 |
| Figopitant | 74.1 | 70.2 | 62.5 | 53.5 | 62.1 | 13 | 84 | 3095 | |
| M544 | 11.5 | 16.7 | 8.8 | 18.2 | 14.6 | 35 | 127 | 726 | |
| Muscle | M488 | 4.1 | 0.9 | 0.9 | 0.9 | 0.9 | 0 | 22 | 62 |
| M474 | 38.9 | 56.9 | 50.7 | 59.1 | 55.6 | 8 | 143 | 3851 | |
| M490 | 3.7 | 2.6 | 0.9 | 4.1 | 2.5 | 63 | 68 | 176 | |
| Figopitant | 53.7 | 35.4 | 44.0 | 30.2 | 36.5 | 19 | 68 | 2532 | |
| M542 | 1.5 | BLQ | BLQ | BLQ | N.A. | N.A. | N.A. | N.A. | |
| M544 | 2.1 | 4.2 | 3.5 | 5.6 | 4.4 | 24 | 211 | 307 | |
| Pituitary | M448 | 0.8 | 0.2 | 0.2 | 0.3 | 0.2 | 25 | 29 | 95 |
| M474 | 31.4 | 44.0 | 43.3 | 37.3 | 41.5 | 9 | 132 | 16,974 | |
| M488 | 2.7 | 1.1 | 0.8 | 0.6 | 0.8 | 30 | 31 | 341 | |
| M490 | 4.6 | 3.5 | 3.3 | 3.2 | 3.3 | 5 | 72 | 1362 | |
| Figopitant | 48.8 | 46.1 | 46.5 | 50.8 | 47.8 | 5 | 98 | 19,535 | |
| M542 | 2.3 | 0.6 | 0.2 | 0.4 | 0.4 | 50 | 17 | 163 | |
| M544 | 9.4 | 4.5 | 6.0 | 7.4 | 6.0 | 24 | 63 | 2439 | |
| Brain (total) | M474 | 27.7 | 11.4 | 34.3 | 27.6 | 24.4 | 48 | 88 | 97 |
| Figopitant | 72.3 | 88.6 | 65.7 | 72.4 | 75.6 | 16 | 105 | 301 | |
| Brown fat | M474 | 60.0 | 53.7 | 50.8 | 54.2 | 52.9 | 3 | 88 | 7095 |
| Figopitant | 40.0 | 46.3 | 49.2 | 45.8 | 47.1 | 4 | 118 | 6318 | |
BLQ, below limit of quantification; N.A., not applicable.