Rilpivirine

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Rilpivirine
File:Rilpivirine.svg
File:Rilpivirine3D.PNG
Systematic (IUPAC) name
4-{[4-({4-[(E)-2-cyanovinyl]-2,6-dimethylphenyl}amino)pyrimidin-2-yl]amino}benzonitrile
Clinical data
Routes of
administration		 Oral
Pharmacokinetic data
Biological half-life 38 hours
Identifiers
CAS Number 500287-72-9
ATC code none
PubChem CID 6451164
Chemical data
Formula C22H18N6
Molar mass 366.42 g/mol[[Script error: No such module "String".]]
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Rilpivirine (TMC278) is an investigational new drug, developed by Tibotec, for the treatment of HIV infection.[1] It is a second-generation non-nucleoside reverse transcriptase inhibitor (NNRTI) with higher potency, longer half-life and reduced side-effect profile compared with older NNRTIs, such as efavirenz.[2][3] It entered phase III clinical trials in April 2008, with an estimated study completion date in January 2011.[4][5] Like etravirine, a second-generation NNRTI approved in 2008, rilpivirine is a diarylpyrimidine (DAPY).

References

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Antiviral drugs: antiretroviral drugs used against HIV (primarily J05)
Entry/fusion inhibitors
(Discovery & development)
Reverse transcriptase
inhibitors (RTIs)
(1st gen) Efavirenz°# · Nevirapine#  · Loviride◊ · Delavirdine◊ ·
(2nd gen) diarylpyrimidines (Etravirine, Rilpivirine†)  · Lersivirine†
Integrase inhibitors
Raltegravir · Elvitegravir† · Globoidnan A (experimental)  · MK-2048†  · GSK-572†
Maturation inhibitors
Bevirimat† · Vivecon†
Protease Inhibitors (PI)
(Discovery and development)
Combined formulations
Experimental agents
TRIM5alpha (gene)
Other
Failed agents
°DHHS preferred first-line agent. ◊Formerly or rarely used agent.


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  1. ↑ Stellbrink HJ (2007). "Antiviral drugs in the treatment of AIDS: what is in the pipeline ?". Eur. J. Med. Res. 12 (9): 483–95. PMID 17933730. 
  2. ↑ Goebel F, Yakovlev A, Pozniak AL, Vinogradova E, Boogaerts G, Hoetelmans R, de Béthune MP, Peeters M, Woodfall B (2006). "Short-term antiviral activity of TMC278--a novel NNRTI--in treatment-naive HIV-1-infected subjects". AIDS. 20 (13): 1721–6. doi:10.1097/01.aids.0000242818.65215.bd. PMID 16931936. 
  3. ↑ Pozniak A, Morales-Ramirez J, Mohap L et al. 48-Week Primary Analysis of Trial TMC278-C204: TMC278 Demonstrates Potent and Sustained Efficacy in ART-naïve Patients. Oral abstract 144LB.
  4. ↑ ClinicalTrials.gov A Clinical Trial in Treatment naïve HIV-1 Patients Comparing TMC278 to Efavirenz in Combination With Tenofovir + Emtricitabine
  5. ↑ ClinicalTrials.gov A Clinical Trial in Treatment naïve HIV-Subjects Patients Comparing TMC278 to Efavirenz in Combination With 2 Nucleoside/Nucleotide Reverse Transcriptase Inhibitors
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