Mylostat500 mg

Mylostat 500 mg is indicated for the treatment of resistant chronic myeloid leukemia, locally advanced squamous cell carcinomas of the head and neck (excluding the lip) in combination with chemoradiation.

Cytotoxic Chemotherapy

Mylostat 500 mg is converted to a free radical nitroxide (NO) in vivo, and transported by diffusion into cells where it quenches the tyrosyl free radical at the active site of the M2 protein subunit of ribonucleotide reductase, inactivating the enzyme. The entire replicase complex, including ribonucleotide reductase, is inactivated and DNA synthesis is selectively inhibited, producing cell death in S phase and synchronization of the fraction of cells that survive. Repair of DNA damaged by chemicals or irradiation is also inhibited by Mylostat 500 mg, offering potential synergy between Mylostat 500 mg and radiation or alkylating agents. Mylostat 500 mg also increases the level of fetal hemoglobin, leading to a reduction in the incidence of vasoocclusive crises in sickle cell anemia. Levels of fetal hemoglobin increase in response to activation of soluble guanylyl cyclase (sGC) by Mylostat 500 mg-derived NO.

Malignancies Chronic myeloid leukaemia: 20-30 mg/kg/day.Solid tumours: 80 mg/kg every third day. With radiotherapy, start treatment 7 days before initiation of radiotherapy.Sickle-cell disease: Initial: 15 mg/kg/day. Max: 35 mg/kg/ day. Adjust based on response and blood counts.Essential thrombocythemia: 15 mg/kg/day. Adjust based on platelet counts.

Malignancies Chronic myeloid leukaemia: 20-30 mg/kg/day.Solid tumours: 80 mg/kg every third day. With radiotherapy, start treatment 7 days before initiation of radiotherapy.Sickle-cell disease: Initial: 15 mg/kg/day. Max: 35 mg/kg/ day. Adjust based on response and blood counts.Essential thrombocythemia: 15 mg/kg/day. Adjust based on platelet counts.

Impairs immune response to vaccines; possible infection with live vaccines, zidovudine, zalcitabine. May alter action of oral anticoagulants and phenytoin.

Severe bone-marrow suppression, severe anaemia, WBC <3000/mm3 or platelet count <100,000/mm3. Pregnancy and lactation. Hypersensitivity.

Gl disturbances, Nausea, Vomiting, Constipation, Diarrhea, Hyperuricemia, Renal failure, Rash, Hyperpigmentation. Pulmonary oedema, dermatological reactions, headache, dizziness. Disorientation, drowsiness, hallucinations, convulsions, alopecia.

Pregnancy category D. There is positive evidence of human fetal risk based on adverse reaction data from investigational or marketing experience or studies in humans, but potential benefits may warrant use of the drug in pregnant women despite potential risks.Lactation: Excreted in breast milk, do not nurse

Regular monitoring of uric acid concentrations, blood counts, renal and hepatic function is recommended. Prior irradiation therapy. Elderly. Avoid use of live vaccines.

Cytotoxic Chemotherapy

Mylostat 500 mg is converted to a free radical nitroxide (NO) in vivo, and transported by diffusion into cells where it quenches the tyrosyl free radical at the active site of the M2 protein subunit of ribonucleotide reductase, inactivating the enzyme. The entire replicase complex, including ribonucleotide reductase, is inactivated and DNA synthesis is selectively inhibited, producing cell death in S phase and synchronization of the fraction of cells that survive. Repair of DNA damaged by chemicals or irradiation is also inhibited by Mylostat 500 mg, offering potential synergy between Mylostat 500 mg and radiation or alkylating agents. Mylostat 500 mg also increases the level of fetal hemoglobin, leading to a reduction in the incidence of vasoocclusive crises in sickle cell anemia. Levels of fetal hemoglobin increase in response to activation of soluble guanylyl cyclase (sGC) by Mylostat 500 mg-derived NO.

Pregnancy category D. There is positive evidence of human fetal risk based on adverse reaction data from investigational or marketing experience or studies in humans, but potential benefits may warrant use of the drug in pregnant women despite potential risks.Lactation: Excreted in breast milk, do not nurse