Table 1.
Commercially available interferons approved for the treatment of RRMS
| Product | Active substance | Adm. | Dosing | PK assessments | Qualitative composition | Neutralizing antibodies | Reduction of the annual attack rate (ITT)a | Reduction of disability progression (EDSS)b | Common adverse effects | References | |
|---|---|---|---|---|---|---|---|---|---|---|---|
| Flu‐like symptoms | Injection site reactions | ||||||||||
| Plegridy® | Pegylated IFN beta‐1a | SC | 125 μg/2 weeks |
T½: 78 ± 15 hr T max: 1–1.5 days (SmPC Plegridy) |
Recombinant from CHO‐K1 covalently linked with methoxy‐polyethyleneglycol (SmPC Plegridy) | <1% (SmPC Plegridy) | 36% (Calabresi et al., 2014) |
38% (12 w‐CDP; Calabresi et al., 2014) 54% (24 w‐CDP; SmPC Plegridy, 2014) |
47% (SmPC Plegridy, 2014) | 66% (SmPC Plegridy, 2014) |
SmPC Calabresi et al. (2014) Kieseier et al. (2014) |
| Betaferon®/Extavia® | IFN beta‐1b | SC | 250 μg/every other day |
T½: 5 hr T max: 1–8 hr Bioavailability: ~50% (SmPC Betaferon) |
Recombinant from Escherichia coli (SmPC Betaferon) | 23%–41% (SmPC Betaferon) | 30% (The IFNB Multiple Sclerosis Study Group, 1993) | 31% (The IFNB Multiple Sclerosis Study Group, 1993) (12 w‐CDP; SmPC Betaferon, 2016) NS | 52% (SmPC Betaferon, 2016) | 85% (SmPC Betaferon, 2016) |
SmPC The IFNB Multiple Sclerosis Study Group (1993) |
| Avonex® | IFN beta‐1a | IM | 30 μg weekly |
T½: 10 hr T max: 5–15 hr Bioavailability: ~40% (SmPC Avonex) |
Recombinant from CHO‐K1 (SmPC Avonex) | 5%–8% (SmPC Avonex) | 32% (Jacobs et al., 1996) | 37% (24 w‐CDP; Jacobs et al., 1996) | 61% (Jacobs et al., 1996) | 15% (Jacobs et al., 1996) |
SmPC Jacobs et al. (1996) Rudick et al. (1997) |
| Rebif® | IFN beta‐1a | SC |
22 μg 3 × weekly 44 μg 3 × weekly |
Apparent T½: 50–60 hr T max: 8 hr (SmPC Rebif, 2015) |
Recombinant from CHO‐K1 (SmPC Rebif, 2015) |
24% (SmPC Rebif, 2015) 13‐14% (SmPC Rebif, 2015) |
27% (PRISMS Study Group, 1998) 33% (PRISMS Study Group, 1998) |
30% (12w‐CDP; SmPC Rebif, 2015) 39% (12w‐CDP; SmPC Rebif, 2015) |
70% (SmPC Rebif, 2015) | 30% (SmPC Rebif, 2015) |
SmPC PRISMS Study Group, (1998) |
The data are extracted from the respective summary of product characteristics and the pivotal registration studies performed in RRMS. IFN, Interferon; T½, half‐life assessed with neopterin; T max, time to peak concentration assessed with neopterin; CHO‐K1, Chinese hamster ovary cells; ITT, intention‐to‐treat. SC, subcutaneous; IM, intramuscular ITT, intention‐to‐treat analysis; CDP, confirmed disability progression. Data in the columns Active substance, Administration, Dosing, PK assessments, Qualitative composition and neutralizing antibodies are collected from the respective Summary of Product Characteristics (SmPC). NS, not significant.
Compared to placebo.
Proportion with ≥1‐point progression on EDSS.