Pharmacokinetic considerations in the treatment of multiple sclerosis with interferon-β

Abstract

IFNβ has a bioavailability of ∼ 30% after subcutaneous or intramuscular administration, shows peak serum concentrations within several hours, has a half-life of < 1 day and is eliminated by a renal and hepatic pathway. PK parameters do not substantially differ between the types of IFNβ and routes of administration; only pegylation of IFNβ results in substantially increased and prolonged PK. Although no clinical dose-effect relationship could be established, there is an association of IFNβ dose with magnetic resonance imaging outcome parameters. Furthermore, there is an association of IFNβ serum levels with the occurrence of adverse events and anti-drug antibodies.

Management of flu-like syndrome with cetirizine in patients with relapsing-remitting multiple sclerosis during therapy with interferon beta: Results of a randomized, cross-over, placebo-controlled pilot study

“…Differences in the frequency of FLS with different IFNβ administration modes cannot be excluded either, as the occurrence of FLS appears to correlate with the frequency of IFNβ injections. With regard to the serum IFNβ levels achieved with different formulations, a recent review of the pharmacokinetic data of the three formulations used in the present study showed that the occurrence of flu-like symptoms after IFNβ injection clearly correlates with an increase of IFNβ serum concentrations [21]. According to this review, however, the pharmacokinetic characteristics of the different types of IFNβ and routes of administration are similar.…”

Current immunotherapies for multiple sclerosis and neuromyelitis optica spectrum disorders: the similarities and differences

“…The biological activity of IFN-β1a is 10 times higher than that of IFN-β1b. However, pegylated IFN-β1a, which consists of covalently linked IFN and polyethylene glycol, has a long half-life, which decreases the required frequency of administration [99,100] . IFN-β and GA, which were approved more than 20 years ago, are safe and effective.…”

“…It causes fewer adverse reactions, so it is a safe and generally well tolerated drug for NMOSD [169] . The efficacy of rituximab is better than that of azathioprine regulates T-, B-, natural killer, and dendritic cells; blocks leukocyte migration to the central nervous system [99][100][101] RRMS [87][88][89][90][91][92][93] , SPMS [94][95][96] , PPMS [97,98] [102][103][104] RRMS [105][106][107][108][109] , PPMS [110] Mitoxantrone Novantrone, 2000 12 mg/m 2 , once every 3 months, iv…”

Advances in the treatment of relapsing&ndash;remitting multiple sclerosis: the role of pegylated interferon &beta;-1a

“… 52 Systemic administration of IFNβ is believed to primarily modulate immune cell function in the periphery. 62 In general, IFNβ appears to oppose the pathogenic processes associated with MS disease progression by shifting from a pro-inflammatory to an anti-inflammatory immune profile ( Figure 1 ). A key player in MS pathology are auto-reactive T cells that migrate across the blood–brain barrier (BBB), initiating inflammatory cascades in the CNS inflicting damage on axons, neurons and myelin sheaths.…”