Oprelvekin
Recombinant interleukin-11 for chemotherapy-induced thrombocytopenia, stimulating megakaryocyte proliferation.
Chemical Identity
| Property | Value |
|---|---|
| Molecular Weight | ~19 kDa |
| Amino Acids | 177 |
| CAS Number | 145941-26-0 |
| Gene | IL11 |
| Route | SC injection |
Structure
Oprelvekin (Neumega) is recombinant human interleukin-11 (IL-11), a 177-amino acid cytokine produced in E. coli. It lacks the N-terminal proline of native IL-11 but retains full biological activity. IL-11 belongs to the gp130 family of cytokines.
Mechanism of Action
IL-11 binds IL-11R-alpha and gp130, activating JAK/STAT signaling in megakaryocyte progenitors and hepatocytes. This stimulates megakaryocyte proliferation, differentiation, and maturation, increasing platelet production. IL-11 also has mucosal protective effects in the gastrointestinal tract.
Clinical Applications
- Chemotherapy-induced thrombocytopenia: Prevention of severe thrombocytopenia
- Autologous transplant: Platelet recovery support
- Mucositis: Gastrointestinal protective effects (investigational)
- Limited use: Replaced by TPO receptor agonists
Pharmacokinetics
- Half-life: 6.9 hours
- Tmax: 3.2 hours (SC)
- Bioavailability: >80%
- Dosing: 25-50 mcg/kg SC daily
- Route: SC
Safety and Side Effects
Fluid retention (dose-limiting), edema, dyspnea, atrial arrhythmias (10%), papilledema, and headache. Cardiovascular monitoring required. Rarely used now due to side effect profile.
References
- Tepler, I., et al. (1996). IL-11 for chemotherapy thrombocytopenia. Journal of Clinical Oncology, 14, 312-319.
- Du, X., & Williams, D.A. (1997). Interleukin-11: a multifunctional growth factor. Blood, 89, 3897-3908.
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