Lack of ethnic differences in the pharmacokinetics and pharmacodynamics of inclacumab in healthy Japanese and Caucasian subjects.

Purpose: Inclacumab, a novel monoclonal antibody against P-selectin, is in development for the treatment and prevention of atherosclerotic cardiovascular diseases. This study was conducted to investigate potential differences in the safety, tolerability, pharmacokinetics (PK), and pharmacodynamics (...

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Published in:European Journal of Clinical Pharmacology Vol. 71; no. 11; pp. 1365 - 1375
Main Authors: Morrison, Mary, Palermo, Guiseppe, Schmitt, Christophe
Format: equations & formulas research tables/charts Journal Article
Published: Springer Nature Nov2015
Online Access:View this record in EBSCOhost
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        00316970
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      jtl: European Journal of Clinical Pharmacology
      issn: 00316970
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      dt: Nov2015
      vid: 71
      iid: 11
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      pub: Springer Nature
      place: New York, New York
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        110465311
        110465311
        110465311
        10.1007/s00228-015-1938-4
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        110465311
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        atl: Lack of ethnic differences in the pharmacokinetics and pharmacodynamics of inclacumab in healthy Japanese and Caucasian subjects.
      aug:
        au:
          Morrison, Mary
          Palermo, Guiseppe
          Schmitt, Christophe
        affil: Roche Innovation Center Welwyn, Roche Products Ltd, Welwyn Garden City UK
      sug:
        subj:
          Antibodies, Monoclonal Pharmacodynamics
          Antibodies, Monoclonal Metabolism
          Japanese Persons
          White Persons
          Human
          Male
          Female
          Japan
          Ethnic Groups
          Administration, Intravenous
          Antibodies, Monoclonal Administration and Dosage
          Biological Availability
          Race Factors
          Male
          Female
      ab: Purpose: Inclacumab, a novel monoclonal antibody against P-selectin, is in development for the treatment and prevention of atherosclerotic cardiovascular diseases. This study was conducted to investigate potential differences in the safety, tolerability, pharmacokinetics (PK), and pharmacodynamics (PD) of single intravenous doses of inclacumab between Japanese and Caucasian healthy volunteers. Method: Sixty-two subjects (31 Japanese and 31 Caucasian) were enrolled in a single-center, open-label, parallel, three dose groups (0.3, 3.0, and 20 mg/kg), single-dose study in Japanese and Caucasian healthy volunteers. Inclacumab concentrations, platelet-leukocyte aggregates (PLA), free/total soluble P-selectin (sP-selectin) ratio, and antibody formation were measured along with routine safety monitoring during the conduct of the study. Results: The PK profiles of inclacumab in Caucasian and Japanese subjects were similar following single-dose intravenous infusion. The statistical analysis of peak ( C) and total exposure (AUC) indicated that bioavailability was similar for both races when corrected for body weight. The geometric mean ratios for AUC and C in the Japanese versus Caucasian cohort were 101 and 111 %, respectively, in 0.3 mg/kg dose group, 108 and 107 %, respectively, in 3.0 mg/kg dose group, and 97 and 96 %, respectively, in 20 mg/kg dose group. No differences were observed in the level of PLA inhibition and mean free/total soluble P-selectin ratio between Japanese and Caucasian subjects. PK/PD relationship between the free/total sP-selectin ratio or PLA and plasma concentration of inclacumab appeared to be similar in both Japanese and Caucasian populations. The effect of race as a covariate was explored on both PK/PD models for PLA and free/total sP-selectin ratio and did not have a significant effect over the reduced model without race as a covariate. Conclusions: Ethnicity had no clinically relevant influence on inclacumab pharmacokinetics or pharmacodynamics. No dose adjustment of inclacumab is required for differences in race.
      pubtype: Academic Journal
      doctype:
        equations & formulas
        research
        tables/charts
        Journal Article
      ougenre: Article
    language: English
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