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1. 5-chloro-2,4-dihydroxypyridine
2. 5-chloro-4-hydroxy-2(1h)-pyridinone
1. 103766-25-2
2. Gimestat
3. 5-chloro-2,4-dihydroxypyridine
4. 5-chloropyridine-2,4-diol
5. 5-chloro-4-hydroxy-2(1h)-pyridone
6. 5-chloro-4-hydroxy-2(1h)-pyridinone
7. Gimeracil [inn]
8. 5-chloro-4-hydroxy-1h-pyridin-2-one
9. 5-chloro-2,4-pyridinediol
10. 5-chloro-2-hydroxypyridin-4(1h)-one
11. 2(1h)-pyridinone, 5-chloro-4-hydroxy-
12. 5-chloro-4-hydroxy-2-pyridone
13. Ua8se1325t
14. 5-chloro-4-hydroxypyridin-2(1h)-one
15. Mfcd08458352
16. 1349387-07-0
17. Ncgc00181011-01
18. Dsstox_cid_26799
19. Dsstox_rid_81914
20. Dsstox_gsid_46799
21. Cdhp Compound
22. Cas-103766-25-2
23. Unii-ua8se1325t
24. Gimeracil (cdhp)
25. Gimeracil (jan/inn)
26. Gimeracil [jan]
27. Gimeracil [mi]
28. Gimeracil [who-dd]
29. Gimeracil Impurity 1
30. Gimeracil [ema Epar]
31. Schembl124438
32. Ts-1 (tn)
33. Chembl1730601
34. Dtxsid8046799
35. Gimeracil, >=98% (hplc)
36. Chebi:31652
37. Amy2406
38. Teysuno Component Gimeracil
39. Hms3655b15
40. Act04735
41. Bcp05824
42. Tox21_112661
43. Ac-475
44. Stl452964
45. Zinc13831809
46. Gimeracil Component Of Teysuno
47. Akos006346735
48. Akos015891515
49. Akos026749993
50. Tox21_112661_1
51. Bcp9000727
52. Ccg-266172
53. Cs-1822
54. Db09257
55. Ks-5133
56. Ncgc00181011-02
57. Hy-17469
58. Sy029154
59. Ft-0645353
60. S2055
61. Sw219483-1
62. D01846
63. Ab01566858_01
64. 766g252
65. A800802
66. A935098
67. Sr-01000945072
68. Q-100034
69. Sr-01000945072-1
70. Q22075887
| Molecular Weight | 145.54 g/mol |
|---|---|
| Molecular Formula | C5H4ClNO2 |
| XLogP3 | -0.1 |
| Hydrogen Bond Donor Count | 2 |
| Hydrogen Bond Acceptor Count | 2 |
| Rotatable Bond Count | 0 |
| Exact Mass | 144.9930561 g/mol |
| Monoisotopic Mass | 144.9930561 g/mol |
| Topological Polar Surface Area | 49.3 Ų |
| Heavy Atom Count | 9 |
| Formal Charge | 0 |
| Complexity | 207 |
| Isotope Atom Count | 0 |
| Defined Atom Stereocenter Count | 0 |
| Undefined Atom Stereocenter Count | 0 |
| Defined Bond Stereocenter Count | 0 |
| Undefined Bond Stereocenter Count | 0 |
| Covalently Bonded Unit Count | 1 |
Gimeracil is used as an adjunct to antineoplastic therapy. When used within the product Teysuno, gimeracil is indicated for the treatment of adults with advanced gastric (stomach) cancer when given in combination with cisplatin.
Absorption
Mean 5-FU maximum plasma concentration (Cmax) and area under the concentration-time curve (AUC) values were approximately 3-fold higher after Teysuno administration than after administration of tegafur alone, despite a 16-fold lower Teysuno dose (50 mg of tegafur) compared to tegafur alone (800 mg), and are attributed to inhibition of DPD by gimeracil. Maximum plasma uracil concentration was observed at 4 hours, with a return to baseline levels within approximately 48 hours after dosing, indicating the reversibility of the DPD inhibition by gimeracil. After administration of a single dose of 50 mg Teysuno (expressed as tegafur content), median Tmax for Teysuno components tegafur, gimeracil, and oteracil was 0.5, 1.0, and 2.0 hours, respectively.
Route of Elimination
Following a single dose of Teysuno, approximately 3.8% to 4.2% of administered tegafur, 65% to 72% of administered gimeracil, and 3.5% to 3.9% of administered oteracil were excreted unchanged in the urine.
Volume of Distribution
Although no intravenous data are available for Teysuno in humans, the volume of distribution could be roughly estimated from the apparent volume of distribution and urinary excretion data as 16 l/m2, 17 l/m2, and 23 l/m2 for tegafur, gimeracil and oteracil, respectively.
Following a single dose of Teysuno, T1/2 values ranged from 6.7 to 11.3 hours for tegafur, from 3.1 to 4.1 hours for gimeracil, and from 1.8 to 9.5 hours for oteracil.
Gimeracil's main role within Teysuno is to prevent the breakdown of [DB00544] (5-FU), which helps to maintin high enough concentrations for sustained effect against cancer cells. It functions by reversibly blocking the enzyme dihydropyrimidine dehydrogenase (DPD), which is involved in the degradation of 5-FU.
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