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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

Corresponding Author:[email protected]

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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.
28 Apr 2021Submitted to British Journal of Clinical Pharmacology
27 Jul 2021Submission Checks Completed
27 Jul 2021Assigned to Editor
13 Aug 2021Reviewer(s) Assigned
10 Sep 2021Review(s) Completed, Editorial Evaluation Pending
12 Sep 2021Editorial Decision: Revise Major
21 Oct 20211st Revision Received
22 Oct 2021Assigned to Editor
22 Oct 2021Submission Checks Completed
22 Oct 2021Review(s) Completed, Editorial Evaluation Pending
27 Oct 2021Editorial Decision: Revise Minor
19 Nov 20212nd Revision Received
29 Nov 2021Submission Checks Completed
29 Nov 2021Assigned to Editor
29 Nov 2021Review(s) Completed, Editorial Evaluation Pending
30 Nov 2021Editorial Decision: Revise Minor
03 Dec 20213rd Revision Received
03 Dec 2021Submission Checks Completed
03 Dec 2021Assigned to Editor
03 Dec 2021Review(s) Completed, Editorial Evaluation Pending
03 Dec 2021Editorial Decision: Accept
May 2022Published in British Journal of Clinical Pharmacology volume 88 issue 5 on pages 2396-2407. 10.1111/bcp.15176