Wikipedia preview

出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2013/07/08 00:51:32」(JST)

wiki en

Rilpivirine (TMC278, trade name Edurant) is a pharmaceutical drug, developed by Tibotec, for the treatment of HIV infection.^[1]^[2] 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.^[3]^[4]

Rilpivirine entered phase III clinical trials in April 2008,^[5]^[6] and was approved for use in the United States in May 2011.^[7] A fixed-dose drug combining rilpivirine with emtricitabine and tenofovir, was approved by the U.S. Food and Drug Administration in August 2011 under the brand name Complera.^[8]

Like etravirine, a second-generation NNRTI approved in 2008, rilpivirine is a diarylpyrimidine (DAPY). Rilpivirine in combination with emtricitabine and tenofovir has been shown to have higher rates of virologic failure than Atripla in patients with baseline HIV viral loads greater than 100,000 copies.

External links[edit]

Rilpivirine bound to proteins in the PDB

References[edit]

^ "TMC278 - A new NNRTI". Tibotec. Retrieved 2010-03-07.
^ 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.
^ 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.
^ 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.
^ ClinicalTrials.gov A Clinical Trial in Treatment naïve HIV-1 Patients Comparing TMC278 to Efavirenz in Combination With Tenofovir + Emtricitabine
^ ClinicalTrials.gov A Clinical Trial in Treatment naïve HIV-Subjects Patients Comparing TMC278 to Efavirenz in Combination With 2 Nucleoside/Nucleotide Reverse Transcriptase Inhibitors
^ "FDA approves new HIV treatment". FDA. Retrieved 2011-05-20.
^ "Approval of Complera: emtricitabine/rilpivirine/tenofovir DF fixed dose combination". FDA. August 10, 2011.

This antiinfective drug article is a stub. You can help Wikipedia by expanding it.

UpToDate Contents

全文を閲覧するには購読必要です。 To read the full text you will need to subscribe.

1. 非ヌクレオシド系逆転写酵素阻害剤の薬理学 pharmacology of non nucleoside reverse transcriptase inhibitors
2. 未治療HIV感染患者のための抗レトロウイルス療法の選択 selecting antiretroviral regimens for the treatment naive hiv infected patient
3. HIV抗レトロウイルス療法に関する臨床試験：非ヌクレオシド系逆転写酵素阻害剤 clinical trials of hiv antiretroviral therapy non nucleoside reverse transcriptase inhibitors
4. HIV抗レトロウイルス療法の変更 modifying hiv antiretroviral therapy regimens
5. 錠剤を嚥下できないHIV感染成人患者の治療：液剤、チュアブル、および砕くことができる剤形の薬剤 treatment of hiv infected adults who have trouble swallowing pills liquid chewable and crushable formulations

English Journal

Key drug-drug interactions with direct-acting antiviral in HIV-HCV coinfection.

El-Sherif O1, Khoo S, Solas C.
Current opinion in HIV and AIDS.Curr Opin HIV AIDS.2015 Sep;10(5):348-54. doi: 10.1097/COH.0000000000000185.
PURPOSE OF REVIEW: We reviewed the most recent data on pharmacokinetic interactions between hepatitis C direct-acting antiviral (DAA) agents and HIV antiretrovirals (ARVs).RECENT FINDINGS: Drug interactions between DAAs and HIV ARVs are extrapolated from phase 1 drug-drug interaction (DDI) studies i
PMID 26248122

Safety, tolerability and pharmacokinetics of rilpivirine following administration of a long-acting formulation in healthy volunteers.

Verloes R1, Deleu S2, Niemeijer N1, Crauwels H1, Meyvisch P1, Williams P1.
HIV medicine.HIV Med.2015 Sep;16(8):477-84. doi: 10.1111/hiv.12247. Epub 2015 May 18.
OBJECTIVES: This phase I healthy volunteer study (NCT01031589) was carried out to investigate the safety/tolerability and pharmacokinetics of a rilpivirine (RPV; TMC278) long-acting (LA) formulation after single and multiple intramuscular (IM) injections.METHODS: In the first part of the study, whic
PMID 25988676

Comparative Safety and Neuropsychiatric Adverse Events Associated With Efavirenz Use in First-Line Antiretroviral Therapy: A Systematic Review and Meta-Analysis of Randomized Trials.

Ford N1, Shubber Z, Pozniak A, Vitoria M, Doherty M, Kirby C, Calmy A.
Journal of acquired immune deficiency syndromes (1999).J Acquir Immune Defic Syndr.2015 Aug 1;69(4):422-9. doi: 10.1097/QAI.0000000000000606.
INTRODUCTION: Efavirenz (EFV) is widely used for the treatment of antiretroviral-naive HIV-positive individuals, but there are concerns about the risk of adverse neuropsychiatric events. We systematically reviewed the safety of EFV in first-line therapy.METHODS: Four databases were searched until Oc
PMID 25850607

Japanese Journal

Mass Spectrometric Characterization of HIV-1 Reverse Transcriptase Interactions with Non-nucleoside Reverse Transcriptase Inhibitors

Biological and Pharmaceutical Bulletin 39(3), 450-454, 2016
NAID 130005132309

非ヌクレオシド系逆転写酵素阻害剤RPV(エジュラント^【○!R】錠25mg)の薬理学的特徴および臨床試験成績

日本薬理學雜誌 = Folia pharmacologica Japonica 141(4), 205-211, 2013-04-01
NAID 10031165477

Development and application of a simple LC-MS method for the determination of plasma rilpivirine (TMC-278) concentrations

The journal of medical investigation : JMI 60(1-2), 35-40, 2013-02
NAID 120005380899

Related Pictures

hivpositivemagazine.com Edurant Full Prescribing Information, Dosage & Side Effects | MIMS.com Singapore RILPIVIRINE TABLETS images galleries - healthgalleries.com DRUG SYNTHESIS INTERNATIONAL: RILPIVIRINE TMC 25 Pill - Edurant 25 mg Edurant (Rilpivirine) Manufacturer, Supplier, Exporter In Seven Wells, Chennai, India Rilpivirine | FDA Label - Tablet (film coated) | AIDSinfo

★リンクテーブル★

リンク元

「リルピビリン」

Rilpivirine
Systematic (IUPAC) name
	4-{[4-({4-[(E)-2-cyanovinyl]-2,6-dimethylphenyl}amino)pyrimidin-2-yl]amino}benzonitrile
Clinical data
Trade names	Edurant
AHFS/Drugs.com	Consumer Drug Information
MedlinePlus	a611037
Licence data	US FDA:link
Pregnancy cat.	B (US)
Legal status	℞-only (US)
Routes	Oral
Pharmacokinetic data
Half-life	38 hours
Identifiers
CAS number	500287-72-9
ATC code	J05AG05
PubChem	CID 6451164
ChemSpider	4953643
UNII	FI96A8X663
ChEBI	CHEBI:68606
ChEMBL	CHEMBL175691
NIAID ChemDB	169030
Chemical data
Formula	C22H18N6
Mol. mass	366.42 g/mol
	InChI InChI=1S/C22H18N6/c1-15-12-18(4-3-10-23)13-16(2)21(15)27-20-9-11-25-22(28-20)26-19-7-5-17(14-24)6-8-19/h3-9,11-13H,1-2H3,(H2,25,26,27,28)/b4-3+ ; Key:YIBOMRUWOWDFLG-ONEGZZNKSA-N ;
(what is this?) (verify);

　　[★]

英: rilpivirine
化: リルピビリン塩酸塩 rilpivirine hydrochloride
商: エジュラント
関: 抗ウイルス剤

[1] "TMC278 - A new NNRTI". Tibotec. Retrieved 2010-03-07.

[pmid17933730-2] 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.

[3] 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.

[4] 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.

[5] ClinicalTrials.gov A Clinical Trial in Treatment naïve HIV-1 Patients Comparing TMC278 to Efavirenz in Combination With Tenofovir + Emtricitabine

[6] ClinicalTrials.gov A Clinical Trial in Treatment naïve HIV-Subjects Patients Comparing TMC278 to Efavirenz in Combination With 2 Nucleoside/Nucleotide Reverse Transcriptase Inhibitors

[7] "FDA approves new HIV treatment". FDA. Retrieved 2011-05-20.

[8] "Approval of Complera: emtricitabine/rilpivirine/tenofovir DF fixed dose combination". FDA. August 10, 2011.

匿名

検索

案内

案内

rilpivirine