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Nilotinib Antitumor agent, protein tyrosine kinase inhibitor. Bcr-Аbl oncoprotein tyrosine kinase activity of cell lines primary positive for Philadelphia chromosome inhibits selectively.
International name of medicinal substance:
The list of drugs containing the active substance Nilotinib, is given after the description.
Antitumor agent, protein tyrosine kinase inhibitor. Bcr-Аbl oncoprotein tyrosine kinase activity of cell lines primary positive for Philadelphia chromosome inhibits selectively. It has a pronounced inhibitory effect on the free type of Br-Abl oncoprotein due to its high affinity for ATP binding sites. Active against imatinib-resistant 32/33 mutant forms of Bcr-Abl-tyrosine kinase, with the exception of T315I mutation. Selectively inhibits proliferation and induces apoptosis of cell lines in Philadelphia chromosome-positive leukemic cells. It has no or little effect on other protein kinases (including the protein kinase of the Src family), except for kinases that have receptors for platelet growth factors, Kit receptors, and afrin receptors. Inhibition of this type of protein kinase occurs at drug concentrations within the therapeutic doses recommended for the treatment of chronic myeloid leukemia when taken orally. The cytogenetic response when nilotinib is used, in patients with intolerance or resistance to imatinib occurs during the first 3 months of therapy, lasts until the end of treatment and is 52%.
Absorption - about 30%. Taking the drug 30 minutes or 2 hours after a meal increases bioavailability by 29% and 15%, respectively. Meal increases Cmax and AUC of 112% and 82% respectively in comparison with use on an empty stomach. TCmax - 3 hours. The ratio <blood-plasma> is 0.68. Communication with plasma proteins - 98%. TCss - 8 days. Css is 35% higher when applied at a dose of 400 mg 2 times / day than when applied at a dose of 800 mg 1 time / day. There is no significant increase in Css nilotinib with increasing doses from 400 mg 2 times / day to 600 mg 2 times / day. Plasma concentration in the period between the use of the first dose and the achievement of Css increases by 2 times when taken 1 time / day and 3.8 times when taken 2 times / day. The main metabolic pathways are oxidation and hydroxylation. In the blood plasma circulates mostly unchanged. All metabolites have negligible pharmacological activity. Excreted mainly (69%) with feces in unchanged form. More than 90% of the dose is eliminated within 7 days (with a single use). T1 / 2 - 17 h (with repeated use). Buy Nilotinib directly from India without intermediaries, the price of Nilotinib directly from the manufacturer!
Chronic myeloid leukemia positive for Philadelphia chromosome in the chronic phase and acceleration phase (with intolerance or resistance to previous therapy, including imatinib).
Hypersensitivity, pregnancy, lactation, childhood and adolescence (up to 18 years).
Frequency: very often (more than 1/10), often (more than 1/100 and less than 1/10), infrequently (more than 1/1000 and less than 1/100), the frequency is unknown (side effects with an unknown frequency). From the side of blood-forming organs: very often - thrombocytopenia, neutropenia, anemia; often - febrile neutropenia, pancytopenia; frequency is unknown - thrombocythemia, leukocytosis. From the side of water and electrolyte metabolism: often - hypomagnesemia, hyperkalemia, hyperglycemia; infrequently - hypokalemia, hyponatremia, hypocalcemia, hypophosphatemia, dehydration; frequency is unknown - hypercalcemia, hyperphosphatemia. On the part of metabolism: infrequently - hyperthyroidism; frequency is unknown - hypothyroidism, thyroiditis, diabetes mellitus. From the nervous system: very often - headache; often - dizziness, paresthesia, insomnia; infrequently - intracranial hemorrhage, migraine, tremor, hypoesthesia, hyperesthesia, depression, anxiety; frequency is unknown - cerebral edema, loss of consciousness, optic neuritis, peripheral neuropathy, confusion, disorientation. From the senses: often - vertigo; infrequently - intraocular hemorrhage, reduced visual acuity, periorbital edema, conjunctivitis, eye irritation, dry eye syndrome; frequency is unknown - edema of the optic nerve, diplopia, blurred vision, photophobia, eyelid swelling, blepharitis, eye pain, hearing loss, ear pain. On the part of the cardiovascular system: often - the heartbeat, the increase in the interval Q-T, hot flashes, increased blood pressure; infrequently - heart failure, angina pectoris, atrial fibrillation, pericardial effusion, ischemic heart disease, cardiomegaly, heart murmur, bradycardia, hypertensive crisis, hematomas; frequency is unknown - myocardial infarction, pericarditis, atrial flutter, extrasystole, hemorrhagic shock, decrease in blood pressure, thrombosis. On the part of the respiratory system: often - shortness of breath at rest and during physical exertion, cough, dysphonia; infrequently - pulmonary edema, pleural effusion, interstitial lung disease, pleurisy, pneumonia, nose bleeding, pain in the pharynx and / or larynx, pharyngitis, irritation of the pharyngeal mucosa; frequency is unknown - pulmonary hypertension, bronchitis. On the part of the digestive system: very often - nausea, constipation, diarrhea, often - vomiting, abdominal pain, anorexia, abdominal discomfort, dyspepsia, flatulence; infrequently - pancreatitis, hepatitis, gastroenteritis, gastrointestinal bleeding, melena, gastroesophageal reflux, stomatitis, dryness of the oral mucosa, increased or decreased appetite; frequency is unknown - hepatomegaly, jaundice, perforation of gastrointestinal ulcers, retroperitoneal hemorrhage, vomiting with blood, stomach ulcer, ulcerative esophagitis, partial intestinal obstruction. For the skin: very often - rash, itching; often - alopecia, eczema, urticaria, hyperhidrosis, dry skin; infrequently - exfoliative rash, ecchymosis; frequency is unknown - erythema nodosum, skin ulcers, petechiae, increased photosensitivity. On the part of the musculoskeletal system: often - myalgia, arthralgia, bone pain, muscle spasm; infrequently - muscle weakness; frequency is unknown - arthritis, swelling of the joints. From the urinary system: infrequently - dysuria, urinary tract infections, painful urge to urinate, nocturia, pollakiuria; frequency is unknown - renal failure, hematuria, urinary incontinence. Reproductive system: Infrequently - pain in the mammary glands, erectile dysfunction, gynecomastia. Laboratory indicators: very often - increased lipase activity; often - increased activity of amylase, CK, alkaline phosphatase, ALT, AST, GGT, LDH hyperbilirubinemia, hyperglycemia; infrequently - hypoglycemia, increased concentration of creatinine, urea; unknown frequency - increased concentrations of troponin, conjugated bilirubin. Other: very often - increased fatigue; often - asthenia, fluid retention and edema, fever, night sweats, weight loss or weight gain; infrequently - chest pain, swelling of the face, swelling of the legs, flu-like syndrome, chills, general malaise; frequency is unknown - sepsis, herpes infection (herpes simplex), candidiasis. Buy Nilotinib Price Nilotinib India
Nilotinib is metabolized in the liver with the participation of the CYP3A4 isoenzyme, and is also a substrate of P-glycoprotein for the system of elimination of many drugs. The absorption and subsequent elimination of nilotinib may be affected by drugs acting on the CYP3A4 isoenzyme and / or P glycoprotein. The simultaneous use of nilotinib with drugs that are potent inhibitors of CYP3A4 (ketoconazole, itraconazole, voriconazole, ritonavir, clarithromycin and telithromycin) should be avoided. The bioavailability of nilotinib is increased by 3 times, while applying with a powerful inhibitor of the CYP3A4 isoenzyme ketoconazole. If necessary, treatment with drugs that are powerful inhibitors of CYP3A4 isoenzyme, treatment with nilotinib, if possible, is suspended or carried out under close supervision. Buy Nilotinib Price Nilotinib