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Novel Long-Acting Ropeginterferon Alfa-2b: Pharmacokinetics, Pharmacodynamics, and Safety in a Phase I Clinical Trial
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  • Yi-Wen Huang,
  • Chung-Wei Tsai,
  • Albert Qin,
  • Jane Fang,
  • Chingleou Teng,
  • Richard Larouche
Yi-Wen Huang
National Taiwan University College of Medicine
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Chung-Wei Tsai
Pharmaessentia Corp.
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Albert Qin
Pharmaessentia Corp.
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Jane Fang
Athenex Inc
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Chingleou Teng
Pharmaessentia Corp.
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Richard Larouche
Syneos Health Inc
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AIM Ropeginterferon alfa-2b is a new site-specific conjugated 40 kDa branched polyethylene-glycol recombinant interferon (IFN). The aim of the study was to determine its safety, pharmacokinetics (PK) and pharmacodynamic (PD). METHODS Ropeginterferon alfa-2b was evaluated first in human in 48 healthy male volunteers after a single dose subcutaneous injection by either 24, 48, 90, 180, 225, 270mcg of the product or 180mcg of marketed pegylated (peg)-IFN alfa-2a. Within each dosing group, 6 subjects received ropeginterferon alfa-2b and 2 subjects received peg-IFN alfa-2a. RESULTS Dose-related increases in ropeginterferon alfa-2b PK parameters (Cmax, AUC, and AUC0-t) were observed over the dose range 24 to 270mcg. The geometric mean values for these PK parameters of ropeginterferon alfa-2b were higher than that of peg-IFN alfa-2a at the 180mcg dose level of 176%, 166%, and 182%, respectively. Mean PD parameters (Emax, Tmax, and AUC0-t) for ropeginterferon alfa-2b increased with dose for both biomarkers neopterin and 2’, 5’-OAS. Ropeginterferon alfa-2b has similar PD profiles as peg-IFN alfa-2a. The treatment related adverse events are similar between the two study drugs, but the overall incidence was numerically lower for ropeginterferon alfa-2b (83%) than peg-IFN alfa-2a (100%) at the 180mcg dose level. CONCLUSIONS Single subcutaneous dose of Ropeginterferon alfa-2b of up to 270mcg is safe and well tolerated. It displays dose related increase in PK and PD parameters, potentially less frequent injection, and better safety profiles. Ropeginterferon alfa-2b is being developed for diseases in which previous peg-IFN use has been limited by side effects.

Peer review status:IN REVISION

28 Apr 2021Submitted to British Journal of Clinical Pharmacology
27 Jul 2021Assigned to Editor
27 Jul 2021Submission Checks Completed
13 Aug 2021Reviewer(s) Assigned
10 Sep 2021Review(s) Completed, Editorial Evaluation Pending
12 Sep 2021Editorial Decision: Revise Major