Included in the formulation
АТХ:L.01.X.X Other antineoplastic agents
L.01.X.X.44 Afleibercept
Pharmacodynamics:Rapid development of the tumor requires accelerated growth of the blood vessels, so the indicator of tumor growth is the vascular endothelial growth factor (VEGF). Afleibercept inhibits angiogenesis by binding to all types of vascular endothelial growth factor: VEGF-A, VEGF-B and PIGF. The drug acts as a "receptor-trap": having greater affinity for VEGF, than native receptors, interacts with this factor. After binding of the molecules of endothelial growth factors, stable inert complexes are formed that do not possess biological activity. This suppresses the formation of new vessels that feed the tumor.
Vascular growth is a pathophysiological basis for the development of macular degeneration. In this case, anti-VEGF drugs, in particular, aflibercept. With intravitreal introduction aflibercept does not have a systemic effect.
Pharmacokinetics: | Half-Elimination (half-life) of the drug is 6 days. Metabolism is not investigated. |
Indications:It is used to treat metastatic colorectal cancer, age-related wet macular degeneration.
II.C15-C26.C18 Malignant neoplasm of colon
II.C15-C26 Malignant neoplasms of the digestive system
VII.H30-H36.H35.3 Degeneration of the macula and posterior pole
Contraindications:Severe renal and hepatic insufficiency. Chronic heart failure. Malignant arterial hypertension.
For ophthalmic practice - inflammatory diseases of the eye.
Individual intolerance.
Carefully:Arterial hypertension, hepatic insufficiency of mild degree.
Pregnancy and lactation:Recommendations for Food and Drug Administration (US Food and Drug Administration) - category D - not applicable. There is no data on the ingestion of the drug in breast milk - during intravenous laxation, intravenous administration of aflibercept is contraindicated.
Dosing and Administration:At 4 mg / kg of body weight every 2 weeks. The drug is administered intravenously for 1 hour. The cycles of chemotherapy are repeated every 2 weeks.
In ophthalmology: 2 mg intravitreal for 3 months of treatment with an interval of 4 weeks. Then 2 mg every 8 weeks.
The highest daily dose: 4 mg / kg.
The highest single dose: 4 mg / kg.
Side effects:Central and peripheral nervous system: fatigue, headache, dysphonia.
The hemopoietic system: leukopenia, thrombocytopenia.
Cardiovascular system: increase of arterial pressure, thromboembolism of arterial vessels.
Metabolism: decreased appetite, dehydration, weight loss.
Urinary system: proteinuria, nephrotic syndrome.
With local application in ophthalmic practice, cases of hemorrhage under the conjunctiva have been noted.
Allergic reactions.
Overdose:Not checked.
Antidote is absent, treatment is symptomatic.
Interaction:Clinically significant interactions are not described.
Special instructions:Monitoring of kidney function, blood pressure.
Preparation protein - shelf life after opening the bottle - no more than 24 hours. Unused remnants of aflibercept are disposed of.