Included in the formulation
АТХ:L.01.X.E.31 Nintedanib
Pharmacodynamics:Competitively binds to the ATP-binding sites of the following receptors: PDGFR-α and PDGFR-β-platelet growth factor, VEGFR-1, VEGFR-2, VEGFR-3 vascular endothelial growth factor, FGFR-1, FGFR-2, FGFR-3 - fibroblast growth factor. As a result, it blocks the transmission of signals within the cell, preventing the proliferation and survival of pericytes and vascular smooth muscle cells, as well as the proliferation, migration and transformation of fibroblasts involved in the formation of pulmonary fibrosis. Inhibits kinases: Flt-3, Lck and Src.
Prevents the formation and development of tumor vessels, which leads to a slowing and cessation of tumor growth.
Pharmacokinetics:After oral ingestion, up to 4.7% is absorbed in the gastrointestinal tract. The maximum concentration in the blood plasma is achieved in 2-4 hours. The connection with plasma proteins is 97.8%.
Metabolism in the liver.
The half-life is 9.5 hours. Elimination with feces.
Indications:It is used to treat locally advanced, metastatic or recurrent non-small cell lung cancer (adenocarcinoma) as a second-line chemotherapy agent in combination with docetaxel.Used for idiopathic pulmonary fibrosis for the purpose of treatment to slow the progression of the disease.
II.C30-C39.C34 Malignant neoplasm of bronchi and lungs
II.C76-C80.C78.0 Secondary malignant neoplasm of lung
X.J80-J84.J84.1 Other interstitial lung diseases with mention of fibrosis
Contraindications:Metastases to the brain, severe renal and hepatic insufficiency, age to 18 years, pregnancy and lactation, individual intolerance.
Carefully:Hepatic and renal insufficiency of moderate severity, treatment with anticoagulants, in anamnesis - perforation of the gastrointestinal tract, arterial thromboembolism.
Pregnancy and lactation:Recommendations for FDA - category D. Contraindicated in pregnancy and lactation.
Dosing and Administration:Inside on an empty stomach, 150 mg 2 times a day.
The highest daily dose: 300 mg.
The highest single dose: 150 mg.
Side effects:Central and peripheral nervous system: headache, asthenia, peripheral polyneuropathy.
Respiratory system: shortness of breath, interstitial pneumonia.
Hemopoietic system: neutropenia, leukopenia.
The cardiovascular system: arterial hypertension, bleeding, thromboembolism.
Digestive system: anorexia, weight loss, nausea, vomiting, diarrhea, abdominal pain.
urinary system: renal failure.
Allergic reactions.
Overdose:Increased side effects.
Treatment is symptomatic.
Interaction:When used simultaneously with inducers CYP3A4 (carbamazepine, rifampicin, phenytoin) careful monitoring of the condition of patients is recommended in order to prevent undesirable side reactions.
With simultaneous use with anticoagulants, the risk of bleeding increases.
Special instructions:Before treatment and then monthly monitored the activity of transaminases, alkaline phosphatase, and bilirubin.
During treatment and a month after the end of taking the drug it is recommended to use reliable methods of contraception.