Lack of effect of dalcetrapib on QT interval in healthy subjects following multiple dosing.

Evaluate dalcetrapib's potential to prolong QT intervals in healthy subjects. This was a single-center, randomized, active and placebo-controlled, six-sequence, three-period cross-over study. Participants [18-65 years; body mass index (BMI) 18-30 kg/m2] were randomized to daily doses of dalcetrapib...

Descripción completa

Detalles Bibliográficos
Publicado en:European Journal of Clinical Pharmacology Vol. 66; no. 8; pp. 775 - 784
Autores principales: Derks M, Abt M, Mwangi A, Meneses-Lorente G
Formato: clinical trial research Journal Article
Publicado: Springer Nature Aug2010
Acceso en línea:Ver este registro en EBSCOhost
fields @attributes:
  recordID: 1
pdfLink:
plink: https://search.ebscohost.com/login.aspx?direct=true&db=ccm&AN=105057532&site=ehost-live
header:
  @attributes:
    shortDbName: ccm
    uiTerm: 105057532
    longDbName: CINAHL Complete
    uiTag: AN
  controlInfo:
    bkinfo:
    dissinfo:
    jinfo:
      jid:
        00316970
        NP9
      jtl: European Journal of Clinical Pharmacology
      issn: 00316970
      maglogo: N
    pubinfo:
      dt: Aug2010
      vid: 66
      iid: 8
      pid: 237
      pub: Springer Nature
      place: New York, New York
    artinfo:
      ui:
        105057532
        2010717660
        10.1007/s00228-010-0841-2
        NLM20521033
        105057532
      ppf: 775
      ppct: 9
      formats:
        fmt:
          @attributes:
            type: P
      tig:
        atl: Lack of effect of dalcetrapib on QT interval in healthy subjects following multiple dosing.
      aug:
        au:
          Derks M
          Abt M
          Mwangi A
          Meneses-Lorente G
        affil: F. Hoffmann-La Roche Ltd, Building 663, Office 2139 Basel 4070 Switzerland
      sug:
        subj:
          Drugs, Investigational
          Electrocardiography Methods
          Hyperlipidemia Therapy
          Clinical Trials
          Funding Source
          Human
          Risk Management Methods
      ab: Evaluate dalcetrapib's potential to prolong QT intervals in healthy subjects. This was a single-center, randomized, active and placebo-controlled, six-sequence, three-period cross-over study. Participants [18-65 years; body mass index (BMI) 18-30 kg/m2] were randomized to daily doses of dalcetrapib 600 mg (therapeutic) or 3,900 mg (supratherapeutic) or to dalcetrapib-matched placebo for 7 days. On Day 8, subjects received single-dose moxifloxacin 400 mg (active control) or placebo, following the placebo or dalcetrapib, respectively. Electrocardiographic parameters were recorded on Days -1, 1, 7, and 8. The primary endpoint was the difference to placebo of time-matched change from baseline in the study-specific corrected QT interval (QTcS) at seven time-points within 24 h after dalcetrapib 3,900 mg on Day 7. An upper 95% confidence interval (CI) <10 ms confirmed the absence of a significant effect. Pharmacokinetic and lipid-related parameters were measured. Subjects ( n = 49) were predominantly male (71%), and all were white, with a mean age of 45 years and mean BMI of 25 kg/m2. For the primary analysis, the upper 95% CI for dalcetrapib 3,900 mg was <10 ms at all time-points. Similar findings were obtained for dalcetrapib 600 mg. Following the administration of moxifloxacin, the QTcS increased by >5 ms. At Day 7, exposure for dalcetrapib 3,900 mg was approximately eightfold higher than that for dalcetrapib 600 mg [mean area under the plasma concentration-time curve between time 0 and 24 h 68,500 vs. 8,280 ng*h/mL; mean peak concentration 6,810 vs. 861 ng/mL]. Cholesteryl ester transfer protein activity was inhibited by 30%, and high-density lipoprotein cholesterol increased by 26% for dalcetrapib 600 mg. Dalcetrapib was well tolerated. Dalcetrapib is not associated with QT interval prolongation, even at doses markedly greater than intended therapeutically.
      pubtype: Academic Journal
      doctype:
        clinical trial
        research
        Journal Article
      ougenre: Article
    language: English
    refInfo:
    holdings:
      @attributes:
        islocal: N