Oprelvekin

(USAN, rINN)
Synonyms: Oprelvekina; Oprelvékine; Oprelvekinum. 2-178-Interleukin 11 (human clone pXM/IL-11).
Cyrillic synonym: Опрельвекин.

💊 Chemical information

Chemical formula: C854H1411N253O235S2 = 19047.0.
CAS — 145941-26-0.
ATC — L03AC02.
ATC Vet — QL03AC02.

💊 Adverse Effects and Precautions

Fluid retention may occur and lead to peripheral oedema, dyspnoea and pulmonary oedema, capillary leak syndrome, and exacerbation of pre-existing pleural effusions; caution is required when giving oprelvekin to patients with a history or signs of heart failure. Dilutional anaemia may occur. Fluid balance and electrolytes should be monitored in patients receiving long-term diuretic therapy. Transient atrial arrhythmias commonly occur; there have also been some reports of ventricular arrhythmias occurring within 2 to 7 days of starting oprelvekin. Other adverse effects include exfoliative dermatitis, blurred vision, and conjunctival injection. Hypersensitivity reactions, including anaphylaxis, have been reported with the use of oprelvekin. Papilloedema has been reported, and oprelvekin should be used with caution in patients with pre-existing papilloedema or tumours involving the CNS. Use of oprelvekin after myeloablative chemotherapy and bone marrow transplantation is considered to be contra-indicated because of an increased incidence of adverse effects. Fetotoxicity has been reported in animals.
1. Smith JW. Tolerability and side-effect profile of rhIL-11. Oncology (Huntingt) 2000; 14 (suppl 8): 41–7.

Effects on the eyes.

Papilloedema has been reported in patients treated with oprelvekin,1 and was found to be a dose-limiting adverse effect in a study of safety and pharmacokinetics in children.2
1. Peterson DC, et al. Oprelvekin-associated bilateral optic disk edema. Am J Ophthalmol 2005; 139: 367–8
2. Cairo MS, et al. Phase I/II dose escalation study of recombinant human interleukin-11 following ifosfamide, carboplatin and etoposide in children, adolescents and young adults with solid tumours or lymphoma: a clinical, haematological and biological study. Br J Haematol 2005; 128: 49–58.

💊 Pharmacokinetics

The bioavailability of oprelvekin after subcutaneous injection is about 80%, peak serum concentrations are reached after about 3 hours, and it has a terminal half-life of about 7 hours. Oprelvekin is metabolised before excretion by the kidneys, and its clearance is reduced in renal impairment.

💊 Uses and Administration

Oprelvekin, a recombinant human interleukin-11, is a platelet growth factor that stimulates the proliferation and maturation of megakaryocytes and thus increases the production of platelets. Oprelvekin is given by subcutaneous injection in a dose of 50 micrograms/kg daily to prevent severe thrombocytopenia and reduce the need for platelet transfusions in high-risk patients after myelosuppressive, but not myeloablative, chemotherapy for non-myeloid malignancies. The dose should be reduced in severe renal impairment (see below). The initial dose should be given 6 to 24 hours after the last dose of antineoplastic, and continued up to a maximum of 21 days. Treatment with oprelvekin should be stopped at least 2 days before starting the next planned cycle of chemotherapy. Oprelvekin is under investigation for the treatment of Crohn’s disease, rheumatoid arthritis, and chronic hepatitis C.

Administration in renal impairment.

In severe renal impairment (creatinine clearance less than 30 mL/min) the recommended dose of oprelvekin is 25 micrograms/kg daily by subcutaneous injection.

Thrombocytopenia.

References.
1. Tepler I, et al. A randomized placebo-controlled trial of recombinant human interleukin-11 in cancer patients with severe thrombocytopenia due to chemotherapy. Blood 1996; 87: 3607–14
2. Isaacs C, et al. Randomized placebo-controlled study of recombinant human interleukin-11 to prevent chemotherapy-induced thrombocytopenia in patients with breast cancer receiving doseintensive cyclophosphamide and doxorubicin. J Clin Oncol 1997; 15: 3368–77
3. Reynolds CH. Clinical efficacy of rhIL-11. Oncology (Huntingt) 2000; 14 (suppl 8): 32–40.

💊 Preparations

Proprietary Preparations

Arg.: Neumega†; Braz.: Neumega; Chile: Neumega†; Mex.: Neumega†; USA: Neumega; Venez.: Neumega.
Published December 13, 2018.