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.
Theropeutic Class
Cytotoxic Chemotherapy
Pharmacology
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.
Dosage & Administration of Mylostat 500 mg
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.
Dosage of Mylostat 500 mg
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.
Interaction of Mylostat 500 mg
Impairs immune response to vaccines; possible infection with live vaccines, zidovudine, zalcitabine. May alter action of oral anticoagulants and phenytoin.
Contraindications
Severe bone-marrow suppression, severe anaemia, WBC <3000/mm3 or platelet count <100,000/mm3. Pregnancy and lactation. Hypersensitivity.
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
Precautions & Warnings
Regular monitoring of uric acid concentrations, blood counts, renal and hepatic function is recommended. Prior irradiation therapy. Elderly. Avoid use of live vaccines.
Drug Classes
Cytotoxic Chemotherapy
Mode Of Action
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
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
Frequently Asked Questions
What is Mylostat 500 mg used for?
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.
What is the dosage of Mylostat 500 mg?
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.
Severe bone-marrow suppression, severe anaemia, WBC <3000/mm3 or platelet count <100,000/mm3. Pregnancy and lactation. Hypersensitivity.
What precautions should be taken with Mylostat 500 mg?
Regular monitoring of uric acid concentrations, blood counts, renal and hepatic function is recommended. Prior irradiation therapy. Elderly. Avoid use of live vaccines.
Is Mylostat 500 mg safe during pregnancy and breastfeeding?
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
Disclaimer
The information provided is accurate to our best practices, but it does not replace professional medical advice. We cannot guarantee its completeness or accuracy. The absence of specific information about a drug should not be seen as an endorsement. We are not responsible for any consequences resulting from this information, so consult a healthcare professional for any concerns or questions.