1. (3s,11ar)-n-((2,6-difluoropyridin-3-yl)methyl)-6-hydroxy-3-methyl-5,7-dioxo-2,3,5,7,11,11a-hexahydro(1,3)oxazolo(3,2-a)pyrido(1,2-d)pyrazine-8-carboxamide
2. Apretude
3. Cabotegravir Extended-release Injectable Suspension
4. Cabotegravir Sodium
5. Gsk-1265744
6. Gsk-1265744a
7. Gsk-1265744b
8. Gsk1265744
9. Gsk1265744a
10. Gsk1265744b
11. Gsk744
12. N-((2,4-difluorophenyl)methyl)-6-hydroxy-3-methyl-5,7-dioxo-2,3,5,7,11,11a-hexahydro(1,3)oxazolo(3,2-a)pyrido(1,2-d)pyrazine-8-carboxamide
13. S-265744
14. S-265744b
15. Sodium (3s,11ar)-8-(((2,4-difluorophenyl)methyl)carbamoyl)-3-methyl-5,7-dioxo-2,3,5,7,11,11a-hexahydrooxazolo(3,2-a)pyrido(1,2-d)pyrazin-6-olate
16. Vocabria
1. 1051375-10-0
2. Gsk1265744
3. Gsk744
4. Gsk-1265744
5. Gsk1265744a
6. S-265744
7. Gsk744 Lap
8. Gsk-1265744a
9. Gsk744 La
10. Gsk 744
11. S/gsk1265744
12. Gsk 1265744
13. Cabotegravir (gsk744, Gsk1265744)
14. Gsk744 (s/gsk1265744)
15. Hmh0132z1q
16. (3s,11ar)-n-(2,4-difluorobenzyl)-6-hydroxy-3-methyl-5,7-dioxo-2,3,5,7,11,11a-hexahydrooxazolo[3,2-a]pyrido[1,2-d]pyrazine-8-carboxamide
17. Cab
18. (3s,11ar)-n-((2,4-difluorophenyl)methyl)-6-hydroxy-3-methyl-5,7-dioxo-2,3,5,7,11,11a-hexahydrooxazolo(3,2-a)pyrido(1,2-d)pyrazine-8-carboxamide
19. Unii-hmh0132z1q
20. Cabotegravir [usan:inn]
21. Cabotegravirum
22. 744 La
23. Cabotegravir [inn]
24. Cabotegravir [jan]
25. Cabotegravir [usan]
26. Schembl82803
27. Cabotegravir [who-dd]
28. Cabotegravir (jan/usan/inn)
29. Cabotegravir; Gsk1265744
30. Chembl2403238
31. Gtpl11386
32. Dtxsid50146982
33. Chebi:172944
34. Cabotegravir [orange Book]
35. Amy27899
36. Bcp08631
37. Ex-a2330
38. Bdbm50492496
39. Mfcd25976748
40. S7766
41. Zinc96927633
42. Cabenuva Component Cabotegravir
43. S/gsk-1265744
44. Cabenuva (cabotegravir + Rilpivirine)
45. Ccg-268708
46. Cs-5078
47. Db11751
48. Cabotegravir Component Of Cabenuva
49. Ncgc00386434-02
50. Ac-30895
51. As-61279
52. Hy-15592
53. S/gsk1265744; Gsk744
54. D10548
55. P14046
56. A902375
57. Q15411012
58. (3r,6s)-n-[(2,4-difluorophenyl)methyl]-10-hydroxy-6-methyl-8,11-dioxo-4-oxa-1,7-diazatricyclo[7.4.0.0?,?]trideca-9,12-diene-12-carboxamide
59. (3r,6s)-n-[(2,4-difluorophenyl)methyl]-10-hydroxy-6-methyl-8,11-dioxo-4-oxa-1,7-diazatricyclo[7.4.0.03,7]trideca-9,12-diene-12-carboxamide
60. (3s,11ar)-n-((2,6-difluoropyridin-3-yl)methyl)-6-hydroxy-3-methyl-5,7-dioxo-2,3,5,7,11,11a-hexahydro(1,3)oxazolo(3,2-a)pyrido(1,2-d)pyrazine-8-carboxamide
61. (3s,11ar)-n-(2,4-difluorobenzyl)-6-hydroxy-3-methyl-5,7-dioxo-2,3,5,7,11,11a-hexahydro[1,3]oxazolo[3,2-a]pyrido[1,2-d]pyrazine-8-carboxamide
62. (3s,11ar)-n-[(2,4-difluorophenyl)methyl]-2,3,5,7,11,11a-hexahydro-6-hydroxy-3-methyl-5,7-dioxo-oxazolo[3,2-a]pyrido[1,2-d]pyrazine-8-carboxamide
63. (3s,11ar)-n-[(2,4-difluorophenyl)methyl]-6-hydroxy-3-methyl-5,7-dioxo-2,3,11,11a-tetrahydrooxazolo[[?]]pyrido[[?]]pyrazine-8-carboxamide
64. (3s,11ar)-n-[(2,4-difluorophenyl)methyl]-6-hydroxy-3-methyl-5,7-dioxo-2,3,5,7,11,11a-hexahydro[1,3]oxazolo[3,2-a]pyrido[1,2-d]pyrazine-8-carboxamide
65. 1264720-72-0
66. N-((2,4-difluorophenyl)methyl)-6-hydroxy-3-methyl-5,7-dioxo-2,3,5,7,11,11a-hexahydro(1,3)oxazolo(3,2-a)pyrido(1,2-d)pyrazine-8-carboxamide
67. Oxazolo(3,2-a)pyrido(1,2-d)pyrazine-8-carboxamide, N-((2,4-difluorophenyl)methyl)-2,3,5,7,11,11a-hexahydro-6-hydroxy-3-methyl-5,7-dioxo-, (3s,11ar)-
| Molecular Weight | 405.4 g/mol |
|---|---|
| Molecular Formula | C19H17F2N3O5 |
| XLogP3 | 2.1 |
| Hydrogen Bond Donor Count | 2 |
| Hydrogen Bond Acceptor Count | 8 |
| Rotatable Bond Count | 3 |
| Exact Mass | 405.11362698 g/mol |
| Monoisotopic Mass | 405.11362698 g/mol |
| Topological Polar Surface Area | 99.2 Ų |
| Heavy Atom Count | 29 |
| Formal Charge | 0 |
| Complexity | 814 |
| Isotope Atom Count | 0 |
| Defined Atom Stereocenter Count | 2 |
| Undefined Atom Stereocenter Count | 0 |
| Defined Bond Stereocenter Count | 0 |
| Undefined Bond Stereocenter Count | 0 |
| Covalently Bonded Unit Count | 1 |
Oral cabotegravir is indicated in combination with rilpivirine for the short term treatment of HIV-1 in virologically suppressed adults with no history of treatment failure to assess tolerability of cabotegravir or who have missed an injected dose of cabotegravir. Intramuscular extended-release cabotegravir is indicated in combination with rilpivirine as a complete regimen for virologically suppressed adults with no history of treatment failure. The intramuscular form is meant to replace their current antiretroviral treatment.
Treatment of human immunodeficiency virus (HIV-1) infection
Vocabria tablets are indicated in combination with rilpivirine tablets for the short-term treatment of Human Immunodeficiency Virus type 1 (HIV-1) infection in adults who are virologically suppressed (HIV-1 RNA < 50 copies/mL) on a stable antiretroviral regimen without present or past evidence of viral resistance to, and no prior virological failure with agents of the NNRTI and INI class for:
- oral lead in to assess tolerability of Vocabria and rilpivirine prior to administration of long acting cabotegravir injection plus long acting rilpivirine injection.
- oral therapy for adults who will miss planned dosing with cabotegravir injection plus rilpivirine injection.
Vocabria injection is indicated, in combination with rilpivirine injection, for the treatment of Human Immunodeficiency Virus type 1 (HIV-1) infection in adults who are virologically suppressed (HIV-1 RNA < 50 copies/mL) on a stable antiretroviral regimen without present or past evidence of viral resistance to, and no prior virological failure with agents of the NNRTI and INI class.
Treatment of human immunodeficiency virus (HIV-1) infection
Prevention of human immunodeficiency virus (HIV-1) infection
Cabotegravir is an inhibitor of HIV integrase, which reduces viral replication. It has a long duration of action as the oral tablet is given daily and the intramuscular suspension is given monthly. Patients should be counselled regarding the risk of hypersensitivity, hepatotoxicity, and depression.
HIV Integrase Inhibitors
Inhibitors of HIV INTEGRASE, an enzyme required for integration of viral DNA into cellular DNA. (See all compounds classified as HIV Integrase Inhibitors.)
J05AX
J - Antiinfectives for systemic use
J05 - Antivirals for systemic use
J05A - Direct acting antivirals
J05AJ - Integrase inhibitors
J05AJ04 - Cabotegravir
Absorption
Oral cabotegravir has a Tmax of 3 hours, reaches a Cmax of 8.0 g/mL, and has an AUC of 145 g\*h/mL. Intramuscular extended-release cabotegravir has a Tmax of 7 days, reaches a Cmax of 8.0 g/mL, and has an AUC of 1591 g\*h/mL.
Route of Elimination
An oral radiolabelled dose of cabotegravir is 58.5% recovered in the feces and 26.8% recovered in the urine.
Volume of Distribution
Data regarding the volume of distribution of cabotegravir is not readily available.
Clearance
Data regarding the clearance of cabotegravir is not readily available. Clearance in dogs was 0.34 mL/min/kg and in cynomolgus monkeys was 0.32 mL/min/kg.
Cabotegravir is O-glucuronidated to the M1 and M2 metabolites, with 67% of glucuronidation performed by UGT1A1, and 33% by UGT1A9.
The mean half life of oral cabotegravir is 41 hours. The mean half life of intramuscular extended-release cabotegravir is 5.6-11.5 weeks.
Cabotegravir binds to the active site of HIV integrase, preventing strand transfer of the viral genome into the host genome, and preventing replication of the virus.
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