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1. (3-((4-benzoyl-1-piperazinyl)(oxo)acetyl)-4-methoxy-7-(3-methyl-1h-1,2,4-triazol-1-yl)-1h-pyrrolo(2,3-c)pyridin-1-yl)methyl Dihydrogen Phosphate
2. 1,2-ethanedione, 1-(4-benzoyl-1-piperazinyl)-2-(4-methoxy-7-(3-methyl-1h-1,2,4-triazol-1-yl)-1-((phosphonooxy)methyl)-1h-pyrrolo(2,3-c)pyridin-3-yl)-
3. Bms-663068
1. 864953-29-7
2. Bms-663068
3. Bms-663068 Free Acid
4. Bms 663068
5. Fostemsavir [usan]
6. Rukobia
7. Fostemsavir(bms-663068)
8. 97iq273h4l
9. 864953-29-7(free Base)
10. Fostemsavir (usan)
11. [3-[2-(4-benzoylpiperazin-1-yl)-2-oxoacetyl]-4-methoxy-7-(3-methyl-1,2,4-triazol-1-yl)pyrrolo[2,3-c]pyridin-1-yl]methyl Dihydrogen Phosphate
12. Bms663068
13. Piperazine, 1-benzoyl-4-((4-methoxy-7-(3-methyl-1h-1,2,4-triazol-1-yl)-1-((phosphonooxy)methyl)-1h-pyrrolo(2,3-c)pyridin-3-yl)oxoacetyl)-
14. (3-(2-(4-benzoylpiperazin-1-yl)-2-oxoacetyl)-4-methoxy-7-(3-methyl-1h-1,2,4-triazol-1-yl)-1h-pyrrolo[2,3-c]pyridin-1-yl)methyl Dihydrogen Phosphate
15. Unii-97iq273h4l
16. Fostemsavir & N6
17. [3-[2-(4-benzoylpiperazin-1-yl)-2-oxo-acetyl]-4-methoxy-7-(3-methyl-1,2,4-triazol-1-yl)pyrrolo[2,3-c]pyridin-1-yl]methyl Dihydrogen Phosphate
18. 1,2-ethanedione, 1-(4-benzoyl-1-piperazinyl)-2-(4-methoxy-7-(3-methyl-1h-1,2,4-triazol-1-yl)-1-((phosphonooxy)methyl)-1h-pyrrolo(2,3-c)pyridin-3-yl)-
19. 1,2-ethanedione, 1-(4-benzoyl-1-piperazinyl)-2-[4-methoxy-7-(3-methyl-1h-1,2,4-triazol-1-yl)-1-[(phosphonooxy)methyl]-1h-pyrrolo[2,3-c]pyridin-3-yl]-
20. Gsk3684934
21. Fostemsavir & Pg16
22. Fostemsavir & 4dm2m
23. Fostemsavir & Vrc03
24. Fostemsavir & Ch106
25. Fostemsavir & 35o22
26. Fostemsavir & Pgt128
27. Fostemsavir [mi]
28. Fostemsavir [inn]
29. Fostemsavir & 3bnc117
30. Fostemsavir & Pg16-imab
31. Fostemsavir [who-dd]
32. Fostemsavir & Pgt128-imab
33. Fostemsavir & Vrc07-523
34. Schembl754395
35. Fostemsavir; Bms-663068
36. Chembl3301594
37. Gtpl11100
38. Dtxsid40235596
39. Fostemsavir & Nih45-46g54w
40. Bcp13226
41. Ex-a1973
42. Bms-626529 & 4dm2m
43. Hy-15440a
44. S7220
45. Zinc14210883
46. Bms-626529 & Pg16-imab
47. Bms-663038
48. Cs-1059
49. Db11796
50. Sb11250
51. Bms-626529 & Pgt128-imab
52. Bms626-529 & Vrc03
53. Gsk-3684934
54. Bms-626529 & N6
55. Bms-626529 & Pg16
56. Compound 35 [pmid: 29271653]
57. Ncgc00510187-01
58. Ac-30663
59. Bms-626529 & Pgt128
60. Bms-626529 & Ch106
61. Bms-626529 & 3bnc117
62. Bms-626529 & 35o22
63. Bms-626529 & Vrc07-523
64. Bms626-529 & Nih45-46g54w
65. D10707
66. A863152
67. Q17001240
68. ({3-[2-(4-benzoylpiperazin-1-yl)-2-oxoacetyl]-4-methoxy-7-(3-methyl-1h-1,2,4-triazol-1-yl)-1h-pyrrolo[2,3-c]pyridin-1-yl}methoxy)phosphonic Acid
69. (3-((4-benzoyl-1-piperazinyl)(oxo)acetyl)-4-methoxy-7-(3-methyl-1h-1,2,4-triazol-1-yl)-1h-pyrrolo(2,3-c)pyridin-1-yl)methyl Dihydrogen Phosphate
70. (3-((4-benzoylpiperazin-1-yl)-oxoacetyl)-4-methoxy- 7-(3-methyl-1h-1,2,4-triazol-1-yl)-1h-pyrrolo(2,3-c)pyridin- 1-yl)methyl Dihydrogen Phosphate
71. 1-(4-benzoyl-1-piperazinyl)-2-[4-methoxy-7-(3-methyl-1h-1,2,4-triazol-1-yl)-1-[(phosphonooxy)methyl]-1h-pyrrolo[2,3-c]pyridin-3-yl]-1,2-ethanedione
| Molecular Weight | 583.5 g/mol |
|---|---|
| Molecular Formula | C25H26N7O8P |
| XLogP3 | -0.1 |
| Hydrogen Bond Donor Count | 2 |
| Hydrogen Bond Acceptor Count | 11 |
| Rotatable Bond Count | 8 |
| Exact Mass | 583.15804781 g/mol |
| Monoisotopic Mass | 583.15804781 g/mol |
| Topological Polar Surface Area | 182 Ų |
| Heavy Atom Count | 41 |
| Formal Charge | 0 |
| Complexity | 1020 |
| 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 |
Fostemsavir is indicated, in combination with other antiretrovirals, for the treatment of multidrug-resistant HIV-1 infection in heavily treatment-experienced adults failing their current antiretroviral therapy due to resistance, intolerance, or safety concerns.
Rukobia, in combination with other antiretrovirals, is indicated for the treatment of adults with multidrug resistant HIV-1 infection for whom it is otherwise not possible to construct a suppressive anti-viral regimen.
Temsavir inhibits the first stage in the HIV-1 viral lifecycle: attachment. It has a moderate duration of action necessitating twice-daily dosing. Fostemsavir, administered at roughly 4x the recommended human dose, has been observed to significantly prolong the QTc-interval. Patients with a history of QTc-prolongation, those receiving other QTc-prolonging medications, and/or those with pre-existing cardiac disease should use fostemsavir with caution, and should be monitored at baseline and throughout therapy for signs or symptoms suggestive of QTc-prolongation. Fostemsavir should also be used with caution in patients with hepatitis B or C co-infection as elevations in hepatic transaminases were observed in greater proportions in these populations in clinical trials.
Anti-HIV Agents
Agents used to treat AIDS and/or stop the spread of the HIV infection. These do not include drugs used to treat symptoms or opportunistic infections associated with AIDS. (See all compounds classified as Anti-HIV Agents.)
HIV Fusion Inhibitors
Inhibitors of the fusion of HIV to host cells, preventing viral entry. This includes compounds that block attachment of HIV ENVELOPE PROTEIN GP120 to CD4 RECEPTORS. (See all compounds classified as HIV Fusion Inhibitors.)
J05AX
J - Antiinfectives for systemic use
J05 - Antivirals for systemic use
J05A - Direct acting antivirals
J05AX - Other antivirals
J05AX29 - Fostemsavir
Absorption
The absorption of temsavir is significantly limited by suboptimal dissolution and solubility following oral administration. Fostemsavir, a phosphonooxymethyl prodrug of temsavir, has improved aqueous solubility and stability under acidic conditions as compared to its parent drug - following oral administration of fostemsavir, the absolute bioavailability is approximately 26.9%. The Cmax and AUCtau following oral administration of fostemsavir 600mg twice daily was 1770 ng/mL and 12,900 ng.h/L, respectively, with a Tmax of approximately 2 hours. Co-administration of fostemsavir with a standard meal increases its AUC by approximately 10%, while co-administration with a high-fat meal increases its AUC by approximately 81%.
Route of Elimination
Temsavir is highly metabolized, after which it is excreted in the urine and feces as inactive metabolites. Approximately 51% of a given dose is excreted in the urine, with <2% comprising unchanged parent drug, and 33% is excreted in the feces, of which 1.1% is unchanged parent drug.
Volume of Distribution
The steady-state volume of distribution of temsavir following intravenous administration is approximately 29.5 L.
Clearance
The mean clearance and apparent clearance of temsavir, the active metabolite of fostemsavir, are 17.9 L/h and 66.4 L/h, respectively.
Fostemsavir is rapidly hydrolyzed to temsavir, its active metabolite, by alkaline phosphatase(s) present at the brush border membrane of the intestinal lumen. Temsavir undergoes further biotransformation to two predominant inactive metabolites: BMS-646915, a product of hydrolysis by esterases, and BMS-930644, an N-dealkylated metabolite generated via oxidation by CYP3A4. Approximately 36.1% of an administered oral dose is metabolized by esterases, 21.2% is metabolized by CYP3A4, and <1% is conjugated by UDP-glucuronosyltransferases (UGT) prior to elimination. Both temsavir and its two predominant metabolites are known to inhibit BCRP.
The half-life of temsavir is approximately 11 hours. Fostemsavir is generally undetectable in plasma following oral administration.
The gp120 subunit within the gp160 envelope glycoprotein of HIV-1 is a new and novel target in the treatment of HIV-1 infection. These subunits are responsible for facilitating the first step in the viral life cycle, attachment, by mediating the interaction between the virus and host cell CD4 receptors. Following attachment, HIV-1 undergoes assembly, budding, and maturation within the host cell, after which mature viral particles are released to continue the viral life cycle. Fostemsavir's active metabolite, temsavir, is an HIV-1 attachment inhibitor. It binds directly to the gp120 subunit to inhibit viral interaction with host CD4 receptors, thereby preventing the initial attachment required for viral replication. It has also been shown to inhibit other gp120-dependent post-attachment steps required for viral entry.
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