Regoraphanib (Regorafenib)

Pharmacodynamics Pharmacokinetics Indications Carefully Contraindications Dosing and Administration Side effects
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Clinical and pharmacological group: & nbsp

Antineoplastic agents - inhibitors of protein kinases

Included in the formulation
  • Stevingra®
    pills inwards 
    Bayer Pharma AG     Germany
    • АТХ:

    L.01.X.E.21   Regoraphanib

    Pharmacodynamics:

    It blocks protein kinases involved in oncogenesis, angiogenesis and tumor microenvironment. Suppresses the main oncogene (KIT), stimulating the development of gastrointerstitial stromal tumors, as a result of which the proliferation of tumor cells ceases.

    Pharmacokinetics:

    After oral administration, an empty stomach is absorbed up to 80% in the gastrointestinal tract. The maximum concentration in the blood plasma is achieved in 3-4 hours. The connection with plasma proteins is 99.5%.

    Metabolism in the liver.

    The half-life is 60 hours. Elimination by the kidneys.

    Indications:

    It is used to treat metastatic colorectal cancer.

    ICD-10

    II.C76-C80.C78.5   Secondary malignant neoplasm of large intestine and rectum

    II.C15-C26.C20   Malignant neoplasm of rectum

    Contraindications:

    Severe renal failure, age under 18, pregnancy and lactation, individual intolerance.

    Carefully:

    Arterial hypertension, skin diseases, increased bleeding, unstable angina.

    Pregnancy and lactation:

    Recommendations for FDA - Category D. Contraindicated in pregnancy and lactation.

    Dosing and Administration:

    Inside, at the same time, 4 tablets (each 40 mg) 1 time per day for 3 weeks.

    The highest daily dose: 160 mg.

    The highest single dose: 160 mg.

    Side effects:

    Central and peripheral nervous system: asthenia, depression, peripheral sensory neuropathy, rarely - reversible encephalopathic syndrome.

    Respiratory system: hoarseness, rhinorrhea, interstitial pneumonia.

    Hemopoietic system: lymphopenia, neutropenia, anemia, thrombocytopenia, and leukopenia.

    The cardiovascular system: bleeding from the respiratory tract, gastrointestinal tract, hemorrhages in the brain, congestive cardiovascular failure, myocardial infarction, rarely - hypertensive crisis.

    Digestive system: nausea, vomiting, diarrhea, stomatitis, glossodinia, dysphagia, anorexia, intestinal perforation, constipation, rarely - gastritis, pancreatitis, cholecystitis, drug-induced hepatitis, weight loss.

    Musculoskeletal system: arthralgia, myalgia, rhabdomyolysis.

    Dermatological reactions: alopecia, erythema, acne, exfoliative dermatitis, eczema, palmar-plantar skin syndrome of erythrodysesthesia, folliculitis, erythema multiforme, Stevens-Johnson syndrome, toxic epidermal necrolysis.

    Reproductive system: erectile dysfunction, gynecomastia.

    Sense organs: noise in ears.

    Endocrine system: hyperthyroidism, hypothyroidism.

    Allergic reactions.

    Overdose:

    Increased side effects.

    Treatment is symptomatic, drug cancellation.

    Interaction:

    Increase the concentration of regorafenib in the blood serum inhibitors CYP 3A4 and Pgp: voriconazole, intraconazole, ketoconazole, clarithromycin, telithromycin, ritonavir.

    Reduces the concentration of the drug in blood plasma inducers of activity CYP 3A4: carbamazepine, rifampicin, phenytoin, phenobarbital, preparations of St. John's wort.

    Special instructions:

    Optimal reception of the drug - 1 hour before or 2 hours after eating. It is not recommended to drink grapefruit juice.

    During treatment, patients need to use reliable contraceptive methods. If the drug is dizzy, you should stop driving the car and work with moving mechanisms.

    Instructions
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