Pharmacodynamic effects of steady-state fingolimod on antibody response in healthy volunteers: a 4-week, randomized, placebo-controlled, parallel-group, multiple-dose study

J Clin Pharmacol. 2012 Dec;52(12):1879-90. doi: 10.1177/0091270011427908. Epub 2011 Dec 15.

Abstract

Fingolimod, a first-in-class oral sphingosine 1-phosphate receptor (S1PR) modulator, is approved in many countries for relapsing-remitting multiple sclerosis, at a once-daily 0.5-mg dose. A reduction in peripheral lymphocyte count is an expected consequence of the fingolimod mechanism of S1PR modulation. The authors investigated if this pharmacodynamic effect impacts humoral and cellular immunogenicity. In this double-blind, parallel-group, 4-week study, 72 healthy volunteers were randomized to steady state, fingolimod 0.5 mg, 1.25 mg, or to placebo. The authors compared T-cell dependent and independent responses to the neoantigens, keyhole limpet hemocyanin (KLH), and pneumococcal polysaccharides vaccine (PPV-23), respectively, and additionally recall antigen response (tetanus toxoid [TT]) and delayed-type hypersensitivity (DTH) to KLH, TT, and Candida albicans. Fingolimod caused mild to moderate decreases in anti-KLH and anti-PPV-23 IgG and IgM levels versus placebo. Responder rates were identical between placebo and 0.5-mg groups for anti-KLH IgG (both > 90%) and comparable for anti-PPV-23 IgG (55% and 41%, respectively). Fingolimod did not affect anti-TT immunogenicity, and DTH response did not differ between placebo and fingolimod 0.5-mg groups. Expectedly, lymphocyte count reduced substantially in the fingolimod groups versus placebo but reversed by study end. Fingolimod was well tolerated, and the observed safety profile was consistent with previous reports.

Publication types

  • Randomized Controlled Trial

MeSH terms

  • Administration, Oral
  • Adult
  • Antigens / administration & dosage
  • Antigens, Fungal / administration & dosage
  • Candida albicans / immunology
  • Double-Blind Method
  • Female
  • Fingolimod Hydrochloride
  • Hemocyanins / administration & dosage
  • Humans
  • Hypersensitivity, Delayed / etiology
  • Hypersensitivity, Delayed / immunology
  • Immunoglobulin G / blood*
  • Immunoglobulin M / blood*
  • Immunosuppressive Agents / administration & dosage*
  • Immunosuppressive Agents / blood
  • Immunosuppressive Agents / pharmacokinetics
  • Male
  • Pneumococcal Vaccines / administration & dosage
  • Propylene Glycols / administration & dosage*
  • Propylene Glycols / blood
  • Propylene Glycols / pharmacokinetics
  • Sphingosine / administration & dosage
  • Sphingosine / analogs & derivatives*
  • Sphingosine / blood
  • Sphingosine / pharmacokinetics
  • T-Lymphocytes / drug effects*
  • T-Lymphocytes / immunology
  • Tetanus Toxoid / administration & dosage
  • Young Adult

Substances

  • Antigens
  • Antigens, Fungal
  • Immunoglobulin G
  • Immunoglobulin M
  • Immunosuppressive Agents
  • Pneumococcal Vaccines
  • Propylene Glycols
  • Tetanus Toxoid
  • Hemocyanins
  • keyhole-limpet hemocyanin
  • Fingolimod Hydrochloride
  • Sphingosine