| 词条 | Arterolane |
| 释义 |
| verifiedrevid = 451552022 | IUPAC_name = [(N-(2-amino-2-methylpropyl)-2-cis-dispiro(adamantane-2,3'-[1,2,4]trioxolane-5',1"-cyclohexan)-4"-yl]acetamide | image = Arterolane.svg | tradename = | pregnancy_AU = | pregnancy_US = | pregnancy_category = | legal_AU = | legal_CA = | legal_UK = | legal_US = | legal_status = | routes_of_administration = Oral | bioavailability = | protein_bound = | metabolism = | elimination_half-life = | excretion = | CAS_number_Ref = {{cascite|correct|??}} | CAS_number = 664338-39-0 | ATC_prefix = P01 | ATC_suffix = BX02 | ATC_supplemental = (combination with piperaquine) | PubChem = 10475633 | DrugBank_Ref = {{drugbankcite|correct|drugbank}} | DrugBank = | ChemSpiderID_Ref = {{chemspidercite|correct|chemspider}} | ChemSpiderID = 25069705 | UNII_Ref = {{fdacite|correct|FDA}} | UNII = 3N1TN351VB | C=22 | H=36 | N=2 | O=4 | molecular_weight = 392.531 g/mol | smiles = C2C1CC5CC2CC(C5)C1(O3)OOC3(CC4)CCC4CC(=O)NCC(C)(C)N | StdInChI_Ref = {{stdinchicite|correct|chemspider}} | StdInChI = 1S/C22H36N2O4/c1-20(2,23)13-24-19(25)12-14-3-5-21(6-4-14)26-22(28-27-21)17-8-15-7-16(10-17)11-18(22)9-15/h14-18H,3-13,23H2,1-2H3,(H,24,25)/t14-,15-,16+,17-,18+,21+,22- | StdInChIKey_Ref = {{stdinchicite|correct|chemspider}} | StdInChIKey = VXYZBLXGCYNIHP-SSPKTAKCSA-N }}Arterolane, also known as OZ277 or RBx 11160, is a substance that was tested for antimalarial activity[1] by Ranbaxy Laboratories.[2] It was discovered by US and European scientists who were coordinated by the Medicines for Malaria Venture (MMV).[3] Its molecular structure is uncommon for pharmacological compounds in that it has both a ozonide (trioxolane) group and an adamantane substituent.[4] Initial results were disappointing, and in 2007 MMV withdrew support, after having invested $20M in the research;[5] Ranbaxy said at the time that it intended to continue developing the drug combination on its own.[2] Ranbaxy started a Phase II clinical trial of arterolane, in combination with piperaquine in 2009 that published in 2015.[5][6] In 2012, Ranbaxy obtained approval to market the arterolane/piperaquine combination drug in India, under the brand name Synriam,[7] and in 2014 received approval to market it in Nigeria, Uganda, Senegal, Cameroon, Guinea, Kenya and Ivory Coast; it had already received approval in Uganda.[8] References1. ^{{cite journal |doi= 10.1021/jm901473s |title= The Structure−Activity Relationship of the Antimalarial Ozonide Arterolane (OZ277) |year= 2010 |last1= Dong |first1= Yuxiang |last2= Wittlin |first2= Sergio |last3= Sriraghavan |first3= Kamaraj |last4= Chollet |first4= Jacques |last5= Charman |first5= Susan A. |last6= Charman |first6= William N. |last7= Scheurer |first7= Christian |last8= Urwyler |first8= Heinrich |last9= Santo Tomas |first9= Josefina |last10= Snyder |first10= Christopher |last11= Creek |first11= Darren J. |last12= Morizzi |first12= Julia |last13= Koltun |first13= Maria |last14= Matile |first14= Hugues |last15= Wang |first15= Xiaofang |last16= Padmanilayam |first16= Maniyan |last17= Tang |first17= Yuanqing |last18= Dorn |first18= Arnulf |last19= Brun |first19= Reto |last20= Vennerstrom |first20= Jonathan L. |journal= Journal of Medicinal Chemistry |volume= 53 |pages= 481–91 |pmid= 19924861 |issue= 1 |display-authors= 8}} {{Antimalarials}}{{antiinfective-drug-stub}}2. ^1 Blow to Ranbaxy drug research plans at LiveMint.com, Sep 21 2007 3. ^{{cite journal |doi= 10.1038/nature02779 |title= Identification of an antimalarial synthetic trioxolane drug development candidate |year= 2004 |last1= Vennerstrom |first1= Jonathan L. |last2= Arbe-Barnes |first2= Sarah |last3= Brun |first3= Reto |last4= Charman |first4= Susan A. |last5= Chiu |first5= Francis C. K. |last6= Chollet |first6= Jacques |last7= Dong |first7= Yuxiang |last8= Dorn |first8= Arnulf |last9= Hunziker |first9= Daniel |last10= Matile |first10= Hugues |last11= McIntosh |first11= Kylie |last12= Padmanilayam |first12= Maniyan |last13= Santo Tomas |first13= Josefina |last14= Scheurer |first14= Christian |last15= Scorneaux |first15= Bernard |last16= Tang |first16= Yuanqing |last17= Urwyler |first17= Heinrich |last18= Wittlin |first18= Sergio |last19= Charman |first19= William N. |journal= Nature |volume= 430 |issue= 7002 |pages= 900–4 |pmid= 15318224 |display-authors= 8}} 4. ^In the Pipeline: "Ozonides As Drugs: What Will They Think Of Next?", by Derek Lowe; published November 23, 2009; retrieved November 17, 2015; at Sciencemag.org 5. ^India Clinical trials registry CTRI/2009/091/000531 6. ^Toure OA et al. Efficacy and safety of fixed dose combination of arterolane maleate and piperaquine phosphate dispersible tablets in paediatric patients with acute uncomplicated Plasmodium falciparum malaria: a phase II, multicentric, open-label study. Malar J. 2015 Nov 25;14(1):469. Clinical Trial Registry India: CTRI/2009/091/000531. {{PMID|26608469}} [https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4660726/ PMC4660726] 7. ^1 Akshat Rathi for Chemistry World. 3 May 2012 Ranbaxy launches new anti-malarial Synriam 8. ^Staff, Business Standard. December 16, 2014 Ranbaxy receives approval for malaria drug Synriam from 7 African countries 7 : Antimalarial agents|Adamantanes|Organic peroxides|Spiro compounds|Carboxamides|Amines|Cyclohexanes |
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