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1. 4-((6-amino-5-bromo-2-((4-cyanophenyl)amino)-4-pyrimidinyl)oxy)-3,5-dimethyl-benzonitrile
2. Benzonitrile, 4-((6-amino-5-bromo-2-((4-cyanophenyl)amino)-4-pyrimidinyl)oxy)-3,5-dimethyl-
3. Intelence
4. R165335
5. Tmc 125
6. Tmc-125
7. Tmc125 Cpd
1. 269055-15-4
2. Intelence
3. Tmc-125
4. Tmc125
5. Etravirine (tmc125)
6. Tmc 125
7. R165335
8. R-165335
9. 4-((6-amino-5-bromo-2-((4-cyanophenyl)amino)pyrimidin-4-yl)oxy)-3,5-dimethylbenzonitrile
10. 4-({6-amino-5-bromo-2-[(4-cyanophenyl)amino]pyrimidin-4-yl}oxy)-3,5-dimethylbenzonitrile
11. 4-[[6-amino-5-bromo-2-[(4-cyanophenyl)amino]-4-pyrimidinyl]oxy]-3,5-dimethylbenzonitrile
12. 0c50hw4fo1
13. Chembl308954
14. Chebi:63589
15. Etravirine-d8
16. 4-((6-amino-5-bromo-2-((4-cyanophenyl)amino)-4-pyrimidinyl)oxy)-3,5-dimethyl-benzonitrile
17. 4-(6-amino-5-bromo-2-(4-cyanoanilino)pyrimidin-4-yloxy)-3,5-dimethylbenzonitrile
18. Benzonitrile, 4-((6-amino-5-bromo-2-((4-cyanophenyl)amino)-4-pyrimidinyl)oxy)-3,5-dimethyl-
19. Benzonitrile, 4-[[6-amino-5-bromo-2-[(4-cyanophenyl)amino]-4-pyrimidinyl]oxy]-3,5-dimethyl-
20. Benzonitrile,4-[[6-amino-5-bromo-2-[(4-cyanophenyl)amino]-4-pyrimidinyl]oxy]-3,5-dimethyl-
21. 65b
22. Intelence(tm)
23. Dapy Deriv
24. 4-(6-amino-5-bromo-2-(4-cyanophenylamino)pyrimidin-4-yloxy)-3,5-dimethylbenzonitrile
25. Intelence (tn)
26. Diaminopyrimidine Deriv
27. Tmc125 Cpd
28. Unii-0c50hw4fo1
29. Etravirine (jan/usan/inn)
30. Etravirine [usan:inn:ban:jan]
31. Etravirine [inn]
32. Etravirine- Bio-x
33. R 165335
34. Etravine; Etravirine
35. 4-[6-amino-5-bromo-2-(4-cyanoanilino)pyrimidin-4-yl]oxy-3,5-dimethylbenzonitrile
36. R165335-tmc125
37. 3m8p
38. Etravirine [mi]
39. Tmc-125/r-165335
40. Etravirine [jan]
41. Etravirine [usan]
42. Etravirine [vandf]
43. Etravirine [mart.]
44. Etravirine [who-dd]
45. Schembl52691
46. Etravirine [ema Epar]
47. Etravirine [orange Book]
48. Dtxsid30181412
49. Hms3651p20
50. Zinc602632
51. Bcp03562
52. Ex-a4282
53. Bdbm50103642
54. S3080
55. 4-({6-amino-5-bromo-2-[(4-
56. Akos015896355
57. Ac-8503
58. Bcp9000006
59. Ccg-269074
60. Cs-0435
61. Db06414
62. He-0088
63. Pb32778
64. 4-[[4-amino-5-bromo-6-(4-cyano-2,6-dimethylphenyloxy)-2-pyrimidinyl]amino]benzonitrile
65. 4-[6-amino-5-bromo-2-(4-cyanoanilino)pyrimidin-4-yl]oxy-3,5-dimethyl-benzonitrile
66. Ncgc00345885-02
67. Ncgc00345885-04
68. Ba164437
69. Hy-90005
70. Bcp0726000193
71. Db-067700
72. Am20080899
73. Cyanophenyl)amino]pyrimidin-4-yl}oxy)-3,5-
74. Ft-0658058
75. Ft-0668442
76. Ft-0668443
77. Sw219570-1
78. A26965
79. D04112
80. Ab01566873_01
81. A818671
82. Q414762
83. Sr-01000944895
84. J-513179
85. Sr-01000944895-1
86. 4-(6-amino-5-bromo-2-(4-cyanophenylamino)pyrimidin-4-ylamino)-3,5-dimethylbenzonitrile
87. 4-[[4-amino 5-bromo-6-(4-cyano-2,6-dimethylphenyloxy)-2-pyrimidinyl]amino]benzonitrile
88. 4-[[4-amino-5-bromo-6-(4-cyano-2,6-dimethylphenyloxy)-2-pyrimidinyl]-amino]benzonitrile
89. 4-[[6-amino-5-bromo-2-(4-cyanoanilino)-4-pyrimidinyl]oxy]-3,5-dimethylbenzonitrile
90. 4-[6-amino-5-bromo-2-(4-cyano-phenylamino)-pyrimidin-4-yloxy]-3,5-dimethyl-benzonitrile
91. 4-((6-amino-5-bromo-2-((4-cyanophenyl) Amino) Pyrimidin-4-yl) Oxy)-3, 5-dimethylbenzonitrile
92. 4-[[6-amino-5-bromo-2-[(4-cyanophenyl)amino]-4-pyrimidinyl]oxy]-3, 5 Cdimethylbenzonitrile
93. 4-[[6-amino-5-bromo-2-[(4-cyanophenyl)amino]-4-pyrimidinyl]oxy]-3,5-dimethyl -benzonitrile
94. 4-[6-azanyl-5-bromanyl-2-[(4-cyanophenyl)amino]pyrimidin-4-yl]oxy-3,5-dimethyl-benzenecarbonitrile
Molecular Weight | 435.3 g/mol |
---|---|
Molecular Formula | C20H15BrN6O |
XLogP3 | 4.5 |
Hydrogen Bond Donor Count | 2 |
Hydrogen Bond Acceptor Count | 7 |
Rotatable Bond Count | 4 |
Exact Mass | 434.04907 g/mol |
Monoisotopic Mass | 434.04907 g/mol |
Topological Polar Surface Area | 121 Ų |
Heavy Atom Count | 28 |
Formal Charge | 0 |
Complexity | 609 |
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 |
1 of 2 | |
---|---|
Drug Name | Intelence |
PubMed Health | Etravirine (By mouth) |
Drug Classes | Antiretroviral Agent |
Drug Label | INTELENCE (etravirine) is a non-nucleoside reverse transcriptase inhibitor (NNRTI) of human immunodeficiency virus type 1 (HIV-1).The chemical name for etravirine is 4-[[6-amino-5-bromo-2-[(4-cyanophenyl)amino]-4-pyrimidinyl]oxy]-3,5-dimethylbenzon... |
Active Ingredient | Etravirine |
Dosage Form | Tablet |
Route | Oral |
Strength | 200mg; 25mg; 100mg |
Market Status | Prescription |
Company | Janssen R And D |
2 of 2 | |
---|---|
Drug Name | Intelence |
PubMed Health | Etravirine (By mouth) |
Drug Classes | Antiretroviral Agent |
Drug Label | INTELENCE (etravirine) is a non-nucleoside reverse transcriptase inhibitor (NNRTI) of human immunodeficiency virus type 1 (HIV-1).The chemical name for etravirine is 4-[[6-amino-5-bromo-2-[(4-cyanophenyl)amino]-4-pyrimidinyl]oxy]-3,5-dimethylbenzon... |
Active Ingredient | Etravirine |
Dosage Form | Tablet |
Route | Oral |
Strength | 200mg; 25mg; 100mg |
Market Status | Prescription |
Company | Janssen R And D |
Indicated as an adjunct therapy in the treatment of adult HIV-1 infections resistant to therapy with other NNRTIs and antiretroviral agents.
FDA Label
Intelence, in combination with a boosted protease inhibitor and other antiretroviral medicinal products, is indicated for the treatment of human-immunodeficiency-virus-type-1 (HIV-1) infection in antiretroviral-treatment-experienced adult patients and in antiretroviral-treatment-experienced paediatric patients from six years of age.
This indication is based on week-48 analyses from two phase-III trials in highly pretreated patients where Intelence was investigated in combination with an optimised background regimen (OBR) which included darunavir/ritonavir. The indication in paediatric patients is based on 48-week analyses of a single-arm, phase-II trial in antiretroviral-treatment-experienced paediatric patients.
Clinical trials have shown no prolongation of QT intervals on electrocardiograms after 8 days of dosing.
Reverse Transcriptase Inhibitors
Inhibitors of reverse transcriptase (RNA-DIRECTED DNA POLYMERASE), an enzyme that synthesizes DNA on an RNA template. (See all compounds classified as Reverse Transcriptase Inhibitors.)
J05AG04
J05AG04
S76 | LUXPHARMA | Pharmaceuticals Marketed in Luxembourg | Pharmaceuticals marketed in Luxembourg, as published by d'Gesondheetskeess (CNS, la caisse nationale de sante, www.cns.lu), mapped by name to structures using CompTox by R. Singh et al. (in prep.). List downloaded from https://cns.public.lu/en/legislations/textes-coordonnes/liste-med-comm.html. Dataset DOI:10.5281/zenodo.4587355
J - Antiinfectives for systemic use
J05 - Antivirals for systemic use
J05A - Direct acting antivirals
J05AG - Non-nucleoside reverse transcriptase inhibitors
J05AG04 - Etravirine
Absorption
Maximum oral absorption is achieved in 2.5-4 hours. Absorption is unaffected by the concomitant use of oral ranitidine or omeprazole, which decrease gastric acidity. Administration under fasting conditions resulted in a near 50% decrease in systemic exposure (AUC) when compared to administration after a meal.
Route of Elimination
After a 800mg dose of radio-labelled etraverine, 93.7% was found to undergo fecal elimination, with 81.2% - 86.4% eliminated unchanged. 1.2% of the dose was renally eliminated, changed. Etravirine is dialyzable (hemodialysis).
Volume of Distribution
Distribution of etravirine into compartments other than plasma has not been evaluated in humans.
Clearance
Renal clearance of etravirine is negligible (<1.2%), thus no dose adjustments are required in patients with renal impairment. Clearance is shown to be reduced in patients with Hepatitis B and/or co-infection, however, the safety profile of etravirine does not call for dosage adjustments.
Metabolized (in vitro) by the liver CYP450 enzymes: CYP3A4, CYP2C9, CYP2C19. The major metabolites formed by a methyl hydroxylation of the dimethylbenzonitrile moiety retained less than 90% of etravirine's activity.
Half life of 9.05-41 hours.
Etravirine exerts its effects via direct inhibition of the reverse transcriptase enzyme of human immunodeficiency virus type 1 (HIV-1). It directly binds reverse transcriptase and consequently blocks DNA-dependent and RNA-dependent polymerase activity. Etravirine does not inhibit human DNA polymerase alpha, beta or gamma.
API Imports and Exports
Importing Country | Total Quantity (KGS) |
Average Price (USD/KGS) |
Number of Transactions |
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ABOUT THIS PAGE
A Etravirine manufacturer is defined as any person or entity involved in the manufacture, preparation, processing, compounding or propagation of Etravirine, including repackagers and relabelers. The FDA regulates Etravirine manufacturers to ensure that their products comply with relevant laws and regulations and are safe and effective to use. Etravirine API Manufacturers are required to adhere to Good Manufacturing Practices (GMP) to ensure that their products are consistently manufactured to meet established quality criteria.
click here to find a list of Etravirine manufacturers with USDMF, JDMF, KDMF, CEP, GMP, COA and API Price related information on PhamaCompass.
A Etravirine supplier is an individual or a company that provides Etravirine active pharmaceutical ingredient (API) or Etravirine finished formulations upon request. The Etravirine suppliers may include Etravirine API manufacturers, exporters, distributors and traders.
click here to find a list of Etravirine suppliers with USDMF, JDMF, KDMF, CEP, GMP, COA and API Price related information on PharmaCompass.
A Etravirine DMF (Drug Master File) is a document detailing the whole manufacturing process of Etravirine active pharmaceutical ingredient (API) in detail. Different forms of Etravirine DMFs exist exist since differing nations have different regulations, such as Etravirine USDMF, ASMF (EDMF), JDMF, CDMF, etc.
A Etravirine DMF submitted to regulatory agencies in the US is known as a USDMF. Etravirine USDMF includes data on Etravirine's chemical properties, information on the facilities and procedures used, and details about packaging and storage. The Etravirine USDMF is kept confidential to protect the manufacturer’s intellectual property.
click here to find a list of Etravirine suppliers with USDMF on PharmaCompass.
In Korea, the Ministry of Food and Drug Safety (MFDS) is in charge of regulating pharmaceutical products and services.
Pharmaceutical companies submit a Etravirine Drug Master File in Korea (Etravirine KDMF) to the MFDS, which includes comprehensive information about the production, processing, facilities, materials, packaging, and testing of Etravirine. The MFDS reviews the Etravirine KDMF as part of the drug registration process and uses the information provided in the Etravirine KDMF to evaluate the safety and efficacy of the drug.
After submitting a Etravirine KDMF to the MFDS, the registered manufacturer can provide importers or distributors with the registration number without revealing confidential information to Korean business partners. Applicants seeking to register their Etravirine API can apply through the Korea Drug Master File (KDMF).
click here to find a list of Etravirine suppliers with KDMF on PharmaCompass.
A Etravirine written confirmation (Etravirine WC) is an official document issued by a regulatory agency to a Etravirine manufacturer, verifying that the manufacturing facility of a Etravirine active pharmaceutical ingredient (API) adheres to the Good Manufacturing Practices (GMP) regulations of the importing country. When exporting Etravirine APIs or Etravirine finished pharmaceutical products to another nation, regulatory agencies frequently require a Etravirine WC (written confirmation) as part of the regulatory process.
click here to find a list of Etravirine suppliers with Written Confirmation (WC) on PharmaCompass.
National Drug Code is a comprehensive database maintained by the FDA that contains information on all drugs marketed in the US. This directory includes information about finished drug products, unfinished drug products, and compounded drug products, including those containing Etravirine as an active pharmaceutical ingredient (API).
The FDA updates the NDC directory daily. The NDC numbers for Etravirine API and other APIs are published in this directory by the FDA.
The NDC unfinished drugs database includes product listing information submitted for all unfinished drugs, such as active pharmaceutical ingredients (APIs), drugs intended for further processing and bulk drug substances for compounding.
Pharmaceutical companies that manufacture Etravirine as an active pharmaceutical ingredient (API) must furnish the FDA with an updated record of all drugs that they produce, prepare, propagate, compound, or process for commercial distribution in the US at their facilities.
The NDC directory also contains data on finished compounded human drug products that contain Etravirine and are produced by outsourcing facilities. While these outsourcing facilities are not mandated to assign a Etravirine NDC to their finished compounded human drug products, they may choose to do so.
click here to find a list of Etravirine suppliers with NDC on PharmaCompass.
Etravirine Active pharmaceutical ingredient (API) is produced in GMP-certified manufacturing facility.
GMP stands for Good Manufacturing Practices, which is a system used in the pharmaceutical industry to make sure that goods are regularly produced and monitored in accordance with quality standards. The FDA’s current Good Manufacturing Practices requirements are referred to as cGMP or current GMP which indicates that the company follows the most recent GMP specifications. The World Health Organization (WHO) has its own set of GMP guidelines, called the WHO GMP. Different countries can also set their own guidelines for GMP like China (Chinese GMP) or the EU (EU GMP).
PharmaCompass offers a list of Etravirine GMP manufacturers, exporters & distributors, which can be sorted by USDMF, JDMF, KDMF, CEP (COS), WC, API price, and more, enabling you to easily find the right Etravirine GMP manufacturer or Etravirine GMP API supplier for your needs.
A Etravirine CoA (Certificate of Analysis) is a formal document that attests to Etravirine's compliance with Etravirine specifications and serves as a tool for batch-level quality control.
Etravirine CoA mostly includes findings from lab analyses of a specific batch. For each Etravirine CoA document that a company creates, the USFDA specifies specific requirements, such as supplier information, material identification, transportation data, evidence of conformity and signature data.
Etravirine may be tested according to a variety of international standards, such as European Pharmacopoeia (Etravirine EP), Etravirine JP (Japanese Pharmacopeia) and the US Pharmacopoeia (Etravirine USP).
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