| 词条 | Aplaviroc |
| 释义 |
| verifiedrevid = 451871816 | IUPAC_name = 4-(4- | image = Aplaviroc structure.svg | width = 300 | pregnancy_category = | legal_status = Development terminated | routes_of_administration = Oral | bioavailability = | protein_bound = | metabolism = | elimination_half-life = | excretion = | IUPHAR_ligand = 805 | CAS_number_Ref = {{cascite|correct|??}} | CAS_number = 461023-63-2 | ATC_prefix = none | ATC_suffix = | PubChem = 3001322 | ChEMBL = 1255794 | DrugBank_Ref = {{drugbankcite|correct|drugbank}} | DrugBank = | ChemSpiderID_Ref = {{chemspidercite|correct|chemspider}} | ChemSpiderID = 2272720 | UNII_Ref = {{fdacite|correct|FDA}} | UNII = 98B425P30V | KEGG_Ref = {{keggcite|correct|kegg}} | KEGG = D06557 | C=33 | H=43 | N=3 | O=6 | molecular_weight = 577.711 g/mol | smiles = CCCCN1C(=O)[C@H](NC(=O)C12CCN(CC2)CC3=CC=C(C=C3)OC4=CC=C(C=C4)C(=O)O)[C@@H](C5CCCCC5)O | StdInChI_Ref = {{stdinchicite|correct|chemspider}} | StdInChI = 1S/C33H43N3O6/c1-2-3-19-36-30(38)28(29(37)24-7-5-4-6-8-24)34-32(41)33(36)17-20-35(21-18-33)22-23-9-13-26(14-10-23)42-27-15-11-25(12-16-27)31(39)40/h9-16,24,28-29,37H,2-8,17-22H2,1H3,(H,34,41)(H,39,40)/t28-,29-/m1/s1 | StdInChIKey_Ref = {{stdinchicite|correct|chemspider}} | StdInChIKey = GWNOTCOIYUNTQP-FQLXRVMXSA-N }} Aplaviroc (INN, codenamed AK602 and GSK-873140) is a CCR5 entry inhibitor that belongs to a class of 2,5-diketopiperazines[1] developed for the treatment of HIV infection.[2][3] It was developed by GlaxoSmithKline. In October 2005, all studies of aplaviroc were discontinued due to liver toxicity concerns.[4][5] Some authors have claimed that evidence of poor efficacy may have contributed to termination of the drug's development;[6] the ASCENT study, one of the discontinued trials, showed aplaviroc to be under-effective in many patients even at high concentrations.[7] See also
References1. ^{{Cite journal | title = 2,5-Diketopiperazines: Synthesis, Reactions, Medicinal Chemistry, and Bioactive Natural Products | author = Borthwick AD | journal = Chemical Reviews | year = 2012 | volume = 112 | issue = 7 | pages = 3641–3716 | doi = 10.1021/cr200398y | pmid = 22575049}} 2. ^{{cite web |url=http://www.retroconference.org/2004/cd/PDFs/540.pdf |title=Determination of binding sites of a unique CCR5 inhibitor AK602 / ONO-4128/ GW873140 on human CCR5 |first1=Kenji |last1=Maeda |first2=Hiromi |last2=Ogata |first3=Shigeyoshi |last3=Harada |first4=Toshikazu |last4=Miyakawa |first5=Hirotomo |last5=Nakata |first6=Yasuhiro |last6=Koh |first7=Yasushi |last7=Tojo |first8=Shiro |last8=Shibayama |first9=Yoshikazu |last9=Takaoka |first10=Kenji |last10=Sagawa |first11=Fukushima |last11=Daikichi |first12=Joseph |last12=Moravek |first13=Edward |last13=Arnold |first14=Hiroaki |last14=Mitsuya |display-authors=3 |archiveurl=https://web.archive.org/web/20051103110511/http://www.retroconference.org/2004/cd/PDFs/540.pdf |format=PDF |archivedate=November 3, 2005 |year=2004 |publisher=Conference on Retroviruses and Opportunistic Infections |deadurl=yes }} 3. ^{{cite journal |url=http://jvi.asm.org/cgi/content/abstract/79/4/2087 |title=Potent Anti-R5 Human Immunodeficiency Virus Type 1 Effects of a CCR5 Antagonist, AK602/ONO4128/GW873140, in a Novel Human Peripheral Blood Mononuclear Cell Nonobese Diabetic-SCID, Interleukin-2 Receptor γ-Chain-Knocked-Out AIDS Mouse Model |first1=Hirotomo |last1=Nakata |first2=Kenji |last2=Maeda |first3=Toshikazu |last3=Miyakawa |first4=Shiro |last4=Shibayama |first5=Masayoshi |last5=Matsuo |first6=Yoshikazu |last6=Takaoka |first7=Mamoru |last7=Ito |first8=Yoshio |last8=Koyanagi |first9=Hiroaki |last9=Mitsuya |display-authors=3 |volume=79 |issue=4 |pages=2087–96 |date=February 2005 |journal=Journal of Virology |doi=10.1128/jvi.79.4.2087-2096.2005 |pmid=15681411 |pmc=546550}} 4. ^{{cite web|url=http://www.aidsmeds.com/drugs/aplaviroc.htm |title=Aplaviroc (GSK-873,140) |date=October 25, 2005 |publisher=AIDSmeds.com |accessdate=September 5, 2008 |deadurl=yes |archiveurl=https://web.archive.org/web/20070113173331/http://www.aidsmeds.com/drugs/aplaviroc.htm |archivedate=January 13, 2007 }} 5. ^{{cite journal |author=Nichols WG |title=Hepatotoxicity Observed in Clinical Trials of Aplaviroc (GW873140) |journal=Antimicrobial Agents and Chemotherapy |volume=52 |issue=3 |pages=858–65 |date=March 2008 |pmid=18070967 |pmc=2258506 |doi=10.1128/aac.00821-07 |author2=Steel HM |author3=Bonny T |display-authors=3 |last4=Adkison |first4=K. |last5=Curtis |first5=L. |last6=Millard |first6=J. |last7=Kabeya |first7=K. |last8=Clumeck |first8=N. }} 6. ^{{cite web |url=http://www.thebody.com/content/treat/art39205.html |title=The Last Word on Aplaviroc: A CCR5 Antagonist With Poor Efficacy |date=December 19, 2006 |author=Moyle, Graeme |publisher=The Body |accessdate=September 5, 2008 |archiveurl=https://web.archive.org/web/20081006093337/http://www.thebody.com/content/treat/art39205.html |archivedate=6 October 2008 |deadurl=no }} 7. ^{{cite journal |last1=Currier |first1=Judith |title=Antiviral activity and safety of aplaviroc with lamivudine/zidovudine in HIV-infected, therapy-naive patients: the ASCENT (CCR102881) study |journal=Antiviral Therapy (Lond.) |volume=13 |issue=2 |pages=297–306 |year=2008 |pmid=18505181 |url=http://www.intmedpress.com/serveFile.cfm?sUID=176d0ac2-96c4-4498-97dc-f19874756f4e |last2=Lazzarin |first2=Adriano |last3=Sloan |first3=Louis |display-authors=3 |last4=Clumeck |first4=Nathan |last5=Slims |first5=Jihad |last6=McCarty |first6=Deb |last7=Steel |first7=Helen |last8=Kleim |first8=Jörg-Peter |last9=Bonny |first9=Tab |last10=Millary |first10=Judith }} Further reading
11 : Abandoned drugs|Alcohols|Benzoic acids|Diketopiperazines|Entry inhibitors|Ethers|Hepatotoxins|Spiro compounds|Phenol ethers|Piperidines|Cyclohexanes |
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