Clinical and pharmacological group: & nbsp

Antineoplastic agents - inhibitors of protein kinases

Included in the formulation
  • Xalcorie®
    capsules inwards 
    Pfizer Inc.     USA
  • АТХ:

    L.01.X.E.16   Crysotinib

    Pharmacodynamics:

    Crysotinib is an antitumor agent, a selective low molecular weight inhibitor of tyrosine kinase receptors and an inhibitor of growth factor receptors of hepatocytes.

    Cryotinib has potent and selective inhibitory activity and induces apoptosis of tumor cell lines.

    Pharmacokinetics:

    With a single administration of cryotinib, the terminal half-life from the blood plasma was 42 hours.

    Cryotinib is largely metabolized in the liver.

    Indications:Common non-small cell lung cancer expressing anaplastic lymphoma kinase.

    II.C30-C39.C34   Malignant neoplasm of bronchi and lungs

    Contraindications:

    Violation of the function of the liver.

    Violation of the function of the kidneys of a serious degree.

    Simultaneous application with powerful inducers or inhibitors of the isoenzyme CYP3A, as well as with substrates of the isoenzyme CYP3A.

    Pregnancy.

    Breast-feeding.

    Children and adolescence under 18 years.

    Individual intolerance.

    Carefully:

    Caution should be applied cryotinib in patients with a history of episodes of prolongation of the QTc interval,predisposed to this condition (patients with congestive heart failure, bradycardia, electrolyte balance disorders) or receiving medicines that extend the QT interval, as well as in case of liver function disorder; in combination with preparations, mainly metabolized isoenzymes CYP3A.

    Pregnancy and lactation:

    Action category for the fetus by FDA - С. The drug is contraindicated for use during pregnancy and the period of breastfeeding.

    Dosing and Administration:

    Dosage of the drug is selected individually, as a rule, it is 250 mg 2 times a day.

    Treatment with the drug is prolonged, as long as there is a positive effect of therapy.

    Side effects:

    The cardiovascular system: bradycardia, prolongation of the QT interval on the ECG.

    Sense organs: very often there are visual impairments (fear of light, double vision, reduced vision, floating opacities of the vitreous, photophobia, the appearance of iridescent circles around the light source, a violation of the perception of the brightness of light).

    Digestive system: very often - nausea and vomiting, diarrhea or constipation,gastroesophageal reflux and esophagitis, violation and pain when swallowing, pain in the esophagus, esophageal spasm, esophageal ulcer), abdominal pain, stomatitis, often - indigestion, rarely - liver failure.

    Laboratory indicators: very often - an increase in the activity of hepatic transaminases, gamma-glutamyl transferase, impaired hepatic functional tests, impaired liver function, often - increased alkaline phosphatase activity.

    Blood: often - neutropenia, leukopenia, lymphopenia, infrequently - thrombocytopenia.

    Nervous system: very often - neuropathy, impaired gait, neurotoxicity, creeping sensation in the body, decreased muscle tone, optic neuritis, sensory change, sensory and motor disorder, peroneal nerve palsy, polyneuropathy, vertigo, imbalance, lightheadedness, headache, and insomnia.

    Respiratory system: often - interstitial lung diseases, upper respiratory tract infections, dyspnea, cough.

    Leather: very often - a rash.

    Urinary system: often - multiple renal cysts.

    Musculoskeletal system: very often - pain in the joints, in the back, in the chest, muscle weakness until atrophy.

    Others: very often - swelling, fatigue, discomfort and chest pain, asthenia, fever, decreased appetite.

    Overdose:No data.
    Interaction:

    It is recommended to avoid simultaneous use of crizotinib with itraconazole, atazanavir, clarithromycin, ketoconazole, nefazodone, indinavir, nelfinavir, saquinavir, telithromycin, ritonavir, troleandomycin and voriconazole.

    Grapefruit or grapefruit juice increases the concentration of cryotinib in the blood plasma, it is necessary to abandon their use for the entire treatment period.

    It is necessary to avoid simultaneous application of rifabutin, carbamazepine, phenobarbital, rifampicin, phenytoin and preparations of St. John's wort perforated, as well as alfentanil, cyclosporin, fentanyl, quinidine, sirolimus, tacrolimus.

    With simultaneous use with pimozide, dihydroergotamine, ergotamine, as well as with astemizole, cisapride and terfenadine, the risk of life-threatening arrhythmias is high.

    Special instructions:

    With caution apply the drug in patients with congestive heart failure, bradycardia, electrolyte balance disorders.

    Cases with drug-induced hepatotoxicity with a lethal outcome have been documented in patients receiving cryotinib.

    Against the background of cryotinib therapy, there have been cases of development of severe, life-threatening or fatal interstitial lung diseases or pneumonitis. Therefore, long-term treatment requires constant monitoring of the lungs.

    If there is a double vision, a fear of light, a decrease in the clarity of vision that occurs during the first 2 weeks of taking the drug, it is recommended that you consult with the oculist.

    When there are side effects from the digestive system, symptomatic agents are prescribed (laxatives, antidiarrheals, antiemetics).

    On the background of cryotinib therapy, monitoring of the values ​​of functional liver samples, regular conduct of a clinical blood test.

    Instructions
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