Tyronib 100 mg (Tablet)
Medicine Details
| Category | Details |
|---|---|
| Generic | Imatinib mesylate |
| Company | Healthcare pharmaceuticals ltd |
| Also available as |
Indications
- Newly diagnosed adult and pediatric patients with Philadelphia chromosome positive chronic myeloid leukemia (Ph+CML) in chronic phase
- Patients with Philadelphia chromosome positive chronic myeloid leukemia in blast crisis, accelerated phase, or in chronic phase after failure of interferon-alpha therapy
- Adult patients with relapsed or refractory Philadelphia chromosome positive acute lymphoblastic leukemia (Ph+ ALL)
- Pediatric patients with newly diagnosed Philadelphia chromosome positive acute lymphoblastic leukemia (Ph+ ALL)
- Adult patients with myelodysplastic/myeloproliferative diseases associated with platelet-derived growth factor receptor (PDGFR) gene re-arrangements
- Adult patients with aggressive systemic mastocytosis without the D816V c-Kit mutation or with c-Kit mutational status unknown
- Adult patients with hypereosinophilic syndrome and/or chronic eosinophilic leukemia who have the FIP1L1-PDGFR a fusion kinase (mutational analysis or fluorescence in situ hybridization [FISH] demonstration of CHIC2 allele deletion) and for patients with HES and/or CEL who are FIP1L1-PDGFRa fusion kinase negative or unknown
- Adult patients with unresectable, recurrent and/or metastatic dermatofibrosarcoma protuberans
- Patients with Kit (CD117) positive unresectable and/or metastatic malignant gastrointestinal stromal tumors
- Adjuvant treatment of adult patients following complete gross resection of Kit (CD117) positive GIST
Pharmacology
Imatinib is a small molecule protein-tyrosine kinase inhibitor that potently inhibits the activity of the Bcr-Abl tyrosine kinase (TK), as well as several receptor TKs: Kit, the receptor for stem cell factor (SCF) coded for by the c-Kit proto-oncogene, the discoidin domain receptors (DDR1 and DDR2), the colony stimulating factor receptor (CSF-1R) and the platelet-derived growth factor receptors alpha and beta (PDGFR-alpha and PDGFR-beta). Imatinib can also inhibit cellular events mediated by activation of these receptor kinases.
Dosage & Administration
Adults with Ph+ CML CP: 400 mg/day, Adults with Ph+ CML AP or BC: 600 mg/day, Pediatrics with Ph+ CML CP: 340 mg/m2/day, Adults with Ph+ ALL: 600 mg/day, Pediatrics with Ph+ ALL: 340 mg/m2/day, Adults with MDS/MPD: 400 mg/day, Adults with ASM: 100 mg/day or 400 mg/day, Adults with HES/CEL: 100 mg/day or 400 mg/day, Adults with DFSP: 800 mg/day, Adults with metastatic and/or unresectable GIST: 400 mg/day, Adjuvant treatment of adults with GIST: 400 mg/day, Patients with mild to moderate hepatic impairment: 400 mg/day, Patients with severe hepatic impairment: 300 mg/day
Interaction
- Agents Inducing CYP3A Metabolism
- Agents Inhibiting CYP3A Metabolism
- Interactions with Drugs Metabolized by CYP3A4
- Interactions with Drugs Metabolized by CYP2D6
Side Effects
- Fluid Retention and Edema
- Hematologic Toxicity
- Congestive Heart Failure and Left Ventricular Dysfunction
- Hepatotoxicity
- Hemorrhage
- Gastrointestinal Disorders
- Hypereosinophilic Cardiac Toxicity
- Dermatologic Toxicities
- Hypothyroidism
- Growth Retardation in Children and Adolescents
- Tumor Lysis Syndrome
- Impairments Related to Driving and Using Machinery
- Renal Toxicity
Pregnancy & Lactation
- Women of childbearing potential must use effective contraception during treatment and for at least 15 days after stopping treatment with Imatinib
- Limited data on the use of imatinib in pregnant women, potential risk for the fetus is unknown, should not be used during pregnancy unless clearly necessary
- Limited information on imatinib distribution in human milk, potential effects of low-dose exposure of the infant to imatinib are unknown, women should not breast-feed during treatment and for at least 15 days after stopping treatment with Imatinib
- Effects of imatinib on fertility and gametogenesis have not been performed
Precautions & Warnings
- Edema and severe fluid retention
- Cytopenias
- Severe congestive heart failure and left ventricular dysfunction
- Severe hepatotoxicity
- Grade 3/4 hemorrhage
- Cardiogenic shock/left ventricular dysfunction
- Bullous dermatologic reactions
- Hypothyroidism
- Fetal harm
- Growth retardation in children and pre-adolescents
- Tumor Lysis Syndrome
- Reports of motor vehicle accidents
- Renal Toxicity
Overdose Effects
Experience with doses higher than the recommended therapeutic dose is limited. In the event of overdose the patient should be observed and an appropriate symptomatic treatment given.
Therapeutic Class
Targeted Cancer Therapy, Tyrosine Kinase Inhibitor
Storage Conditions
Store below 30°C, in a cool and dry place. Keep away from light. Keep out of the reach of children.