Dataset Information

Pharmacokinetics comparison of two pegylated interferon alfa formulations in healthy volunteers.

ABSTRACT:

Background

Several countries have used pegylation technology to improve the pharmacokinetic properties of essential drugs. Recently, a novel interferon alfa-2b protein conjugated to four-branched 12 kDa polyethylene glycol molecules was developed jointly between Cuba and Brazil. The aim of this study was to compare the pharmacokinetic properties of BIP48 (pegylated interferon alfa-2b from Bio-Manguinhos/Fiocruz, Brazil) to those of PEGASYS® (commercially available pegylated interferon alfa-2a from Roche Pharmaceutical).

Methods

This phase I, single-centre, randomized, double-blind crossover trial enrolled 31 healthy male volunteers aged 19 to 35 who were allocated to two stages, either side of a 5-week wash-out period, with each arm lasting 14 consecutive days after subcutaneous administration of 180 μg of one formulation or the other (study or comparator). The main outcome variable was serum pegylated interferon concentrations in 15 samples collected during the course of the study and tested using an enzyme immunoassay.

Results

There were no differences between formulations in terms of magnitude or absorption parameters. Analysis of time parameters revealed that BIP48 remained in the body significantly longer than PEGASYS® (T_max: 73 vs. 54 h [p = 0.0010]; MRT: 133 vs. 115 h [p = 0.0324]; ke: 0.011 vs. 0.013 h(-1) [p = 0.0153]; t_1/2: 192 vs. 108 h [p = 0.0218]).

Conclusion

BIP48 showed the expected pharmacokinetic profile for a pegylated product with a branched molecular structure. Compared to PEGASYS®, the magnitude absorption was similar, but time parameters were consistent with slower elimination. Further studies should be conducted to evaluate the clinical implications of these findings. A phase II-III repeated-dose clinical trial is ongoing to study these findings in patients with chronic hepatitis C virus infection.

Trial registration

This study is registered on the ClinicalTrials.gov platform (accession number NCT01889849 ). This trial was retrospectively registered in June 2013.

SUBMITTER: Costa MB

PROVIDER: S-EPMC5755306 | biostudies-literature | 2018 Jan

REPOSITORIES: biostudies-literature

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Publications

Pharmacokinetics comparison of two pegylated interferon alfa formulations in healthy volunteers.

Costa Marisa Boff MB Picon Paulo Dornelles PD Sander Guilherme Becker GB Cuni Hugo Nodarse HN Silva Carmen Valenzuela CV Meireles Rolando Páez RP Góes Ana Carolina Magalhães Andrade ACMA Batoreu Nadia Maria NM Maia Maria de Lourdes de Sousa MLS Albuquerque Elizabeth Maciel EM Matos Denise Cristina de Souza DCS Saura Pedro Lopez PL

BMC pharmacology & toxicology 20180104 1

<h4>Background</h4>Several countries have used pegylation technology to improve the pharmacokinetic properties of essential drugs. Recently, a novel interferon alfa-2b protein conjugated to four-branched 12 kDa polyethylene glycol molecules was developed jointly between Cuba and Brazil. The aim of this study was to compare the pharmacokinetic properties of BIP48 (pegylated interferon alfa-2b from Bio-Manguinhos/Fiocruz, Brazil) to those of PEGASYS® (commercially available pegylated interferon al ...[more]

PMID: 29301580

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Dataset Information

Pharmacokinetics comparison of two pegylated interferon alfa formulations in healthy volunteers.

Background

Methods

Results

Conclusion

Trial registration

Publications

Pharmacokinetics comparison of two pegylated interferon alfa formulations in healthy volunteers.

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