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1. Mk-1439
2. Pifeltro
1. 1338225-97-0
2. Mk-1439
3. Pifeltro
4. 3-chloro-5-((1-((4-methyl-5-oxo-4,5-dihydro-1h-1,2,4-triazol-3-yl)methyl)-2-oxo-4-(trifluoromethyl)-1,2-dihydropyridin-3-yl)oxy)benzonitrile
5. 3-chloro-5-[1-[(4-methyl-5-oxo-1h-1,2,4-triazol-3-yl)methyl]-2-oxo-4-(trifluoromethyl)pyridin-3-yl]oxybenzonitrile
6. Mk1439
7. Doravirine (mk-1439)
8. Mk-1439a
9. 913p6lk81m
10. 3-chloro-5-({1-[(4-methyl-5-oxo-4,5-dihydro-1h-1,2,4-triazol-3-yl)methyl]-2-oxo-4-(trifluoromethyl)-1,2-dihydropyridin-3-yl}oxy)benzonitrile
11. Benzonitrile, 3-chloro-5-((1-((4,5-dihydro-4-methyl-5-oxo-1h-1,2,4-triazol-3-yl)methyl)-1,2-dihydro-2-oxo-4-(trifluoromethyl)-3-pyridinyl)oxy)-
12. Doravirine [usan]
13. Doravirine [usan:inn]
14. Unii-913p6lk81m
15. 4ncg
16. Pifeltro (tn)
17. 2kw
18. Mk 1439
19. Doravirine [mi]
20. Doravirine [inn]
21. Doravirine [jan]
22. Doravirine; Mk-1439
23. Mk-1439(doravirine)
24. Doravirine [who-dd]
25. C17h11clf3n5o3
26. Doravirine (jan/usan/inn)
27. Schembl2509885
28. Chembl2364608
29. Doravirine [orange Book]
30. Dtxsid30158386
31. Amy16781
32. Bcp02296
33. Ex-a1968
34. Bdbm50508293
35. Delstrigo Component Doravirine
36. Mfcd22417167
37. S6492
38. Zinc72317283
39. Akos030528603
40. Cs-5924
41. Db12301
42. Sb17104
43. Doravirine Component Of Delstrigo
44. Ncgc00508866-01
45. Ac-33637
46. Hy-16767
47. Db-091410
48. D10624
49. F53303
50. A856128
51. Q6885419
52. S900006160
53. 3-chloro-5-[[1-[(4-methyl-5-oxo-1h-1,2,4-triazol-3-yl)methyl]-2-oxo-4-(trifluoromethyl)-3-pyridyl]oxy]benzonitrile
| Molecular Weight | 425.7 g/mol |
|---|---|
| Molecular Formula | C17H11ClF3N5O3 |
| XLogP3 | 2.1 |
| Hydrogen Bond Donor Count | 1 |
| Hydrogen Bond Acceptor Count | 8 |
| Rotatable Bond Count | 4 |
| Exact Mass | 425.0502514 g/mol |
| Monoisotopic Mass | 425.0502514 g/mol |
| Topological Polar Surface Area | 98 Ų |
| Heavy Atom Count | 29 |
| Formal Charge | 0 |
| Complexity | 860 |
| 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 |
Doravirine is indicated, in combination with other antiretroviral agents, for the treatment of HIV-1 infection in adult patients with no prior antiretroviral treatment history. It is also indicated to replace the current antiretroviral regimen in those who are virologically suppressed (HIV-1 RNA less than 50 copies per mL) on a stable antiretroviral regimen with no history of treatment failure and no known substitutions associated with resistance to doravirine.
FDA Label
Pifeltro is indicated, in combination with other antiretroviral medicinal products, for the treatment of adults, and adolescents aged 12 years and older weighing at least 35 kg infected with HIV 1 without past or present evidence of resistance to the NNRTI class.
In a clinical phase 2 trial evaluating a dose range of 0.25-2x the recommended dose of doravirine (in combination with emtricitabine/tenofovir) in HIV-1 infected subjects with no antiretroviral treatment history, no exposure-response relationship for efficacy was identified for doravirine. Furthermore, at a dose of 1200 mg, which provides approximately 4 times the peak concentration observed following the recommended dose, doravirine does not prolong the QT interval to any clinically relevant extent.
J05AG06
J - Antiinfectives for systemic use
J05 - Antivirals for systemic use
J05A - Direct acting antivirals
J05AG - Non-nucleoside reverse transcriptase inhibitors
J05AG06 - Doravirine
Absorption
The absolute bioavailability of doravirine is 64% with a Tmax of 2 hours. Following oral [14C]doravirine administration, all of the administered dose was recovered and the agent is considered to be well absorbed. Moreover, its co-administration with food did not greatly alter doravirine's pharmacokinetic profile during clinical studies.
Route of Elimination
The primary route of elimination for doravirine is via cytochrome P450 3A4/5 metabolism. Only 6% of an administered dose is recovered in the urine unchanged, with even less unchanged drug found in the feces.
Volume of Distribution
The steady-state volume of distribution of doravirine following intravenous administration is 60.5 L.
Clearance
The oral and renal clearances of doravirine are 106 ml/min and 9.3 ml/min, respectively.
Following absorption, unchanged parent drug is the major circulating component in plasma. Its M9 metabolite - a product of cytochrome P450 3A4/5 mediated oxidative metabolism - is the most abundant doravirine metabolite in the circulation.
The elimination half-life determined of doravirine is 15 hours.
Doravirine is a pyridinone non-nucleoside reverse transcriptase inhibitor of HIV-1. Reverse transcriptase is the enzyme with which HIV generates complementary DNA (cDNA) to its RNA genome - this cDNA is then inserted into the host cell genome, where it can be transcribed into viral RNA for the purposes of replication. Doravirine inhibits HIV-1 replication by non-competitively inhibiting HIV-1 reverse transcriptase. Doravirine does not, however, inhibit the human cellular DNA polymerases , , and mitochondrial DNA polymerase .
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