Tyrokin 400mg 10pcs(Box)

✔️ Uses

• Chronic myeloid leukemia (CML)
• Acute lymphocytic leukemia (ALL)
• Gastrointestinal stromal tumors (GISTs)

✔️ How does

Tyrokin 400 works by inhibiting the activity of a specific protein enzyme, bcr-abl tyrosine kinase, which promotes the growth and spread of cancer cells. By targeting this enzyme, the medication prevents the proliferation of cancer cells and induces their planned death (apoptosis).

✔️ Side Effects:

• Rash
• Vomiting
• Abdominal pain
• Diarrhea
• Fatigue
• Water retention and swelling (report rapid weight gain to your doctor)

✔️ Acute Lymphoblastic Leukemia (ALL)

• Relapsed or refractory Philadelphia chromosome-positive (Ph+) ALL.
• Dose: 600 mg orally once daily (PO qDay).

✔️ Myelodysplastic/Myeloproliferative Diseases (MDS/MPD)

• Indication: MDS/MPD associated with platelet-derived growth factor receptor (PDGFR) gene rearrangements (confirmed via FDA-approved test).
• Dose: 400 mg PO qDay.

✔️ Hypereosinophilic Syndrome/Eosinophilic Leukemia (HES/CEL)

• Indication:
  • With FIP1L1-PDGFR-alpha fusion kinase (via mutational analysis or CHIC2 allele deletion):
    • Starting Dose: 100 mg PO qDay.
    • Adjustments: Increase to 400 mg PO qDay in the absence of adverse effects if the response is insufficient.
  • Fusion kinase negative or unknown: 400 mg PO qDay.

✔️ Chronic Myeloid Leukemia (CML)

Chronic Phase (Newly Diagnosed)

• Adults and Pediatrics: 400 mg PO qDay.

Chronic Phase (After Failure of Interferon-Alpha Therapy)

• Dose Increase: Up to 600 mg/day if there is disease progression, failure to achieve a hematologic response after 3 months, cytogenetic response after 6-12 months, or loss of response.

Accelerated Phase or Blast Crisis

• Dose: 600 mg PO qDay.
• Increase: Up to 400 mg PO every 12 hours (q12hr) under the same circumstances as above.

✔️ Dermatofibrosarcoma Protuberans (DFSP)

• Indication: Unresectable, recurrent, or metastatic DFSP.
• Dose: 400 mg PO q12hr.

✔️ Aggressive Systemic Mastocytosis (ASM)

• Indication: ASM without D816V c-Kit mutation or with unknown c-Kit mutation status.
  • Without D816V mutation: 100 mg PO qDay.
  • Unknown mutation status: 400 mg PO qDay.
  • ASM with eosinophilia related to FIP1L1-PDGFR-alpha fusion kinase:
    • Starting Dose: 100 mg PO qDay.
    • Adjustments: Increase to 400 mg PO qDay if needed.

✔️ Gastrointestinal Stromal Tumors (GISTs)

Unresectable/Metastatic Malignant GIST

• Dose: 400 mg PO qDay.
• Adjustments: Increase to 400 mg twice daily (BID) in cases of disease progression without severe side effects.

Adjuvant Therapy (Post-GIST Resection)

• Dose: 400 mg PO qDay for 3 years.

✔️ Hepatic Impairment

• Severe impairment: Reduce dose by 25%.

✔️ Pediatric Dosage Guidelines: Chronic Myeloid Leukemia (CML)

• Indication: Newly diagnosed pediatric patients with Ph+ CML in the chronic phase.
• Dose: 340 mg/m²/day PO, not exceeding 600 mg/day.
• Age: Not established for children under 1 year.

✔️ Pediatric Dosage Guidelines: Acute Lymphoblastic Leukemia (ALL)

• Indication: Newly diagnosed pediatric patients with Ph+ ALL.
• Dose: 340 mg/m²/day PO, not exceeding 600 mg/day.
• Age: Not established for children under 1 year.

✔️ Drug Interactions

CYP3A4 Inhibitors:

• Effect: Increased serum levels of imatinib.
• Examples: Azole antifungals (e.g., ketoconazole), and macrolide antibiotics (e.g., clarithromycin).

CYP3A4 Inducers:

• Effect: Reduced serum levels of imatinib.
• Examples: Carbamazepine, dexamethasone, phenobarbital, phenytoin, rifampicin.

CYP3A4 Substrates:

• Effect: Imatinib may increase serum levels of drugs metabolized by CYP3A4.
• Examples: Ciclosporin, pimozide, triazole-benzodiazepines, dihydropyridine calcium channel blockers, and certain statins.

CYP2C9 Substrates:

• Effect: May elevate serum levels of drugs metabolized by CYP2C9.
• Examples: Warfarin.

CYP2D6 Substrates:

• Effect: Imatinib may increase serum levels of CYP2D6-metabolized drugs.

✔️ Contraindications:

Hypersensitivity. Lactation.

✔️ Precautions & Warnings

• Patients with cardiac disease or an elevated risk for congestive heart failure (CHF) should be closely monitored for severe fluid retention.
• Regularly monitor complete blood count (CBC) to detect cytopenias.
• Monitor liver function tests (LFTs) and renal function periodically.
• Use only if necessary. Potential harm to the fetus exists; advise effective contraception during treatment.
• Imatinib and its active metabolite are excreted into human milk. Advise lactating women not to breastfeed during treatment and for 1 month after the last dose.

✔️ Storage:

Store below 30°C, in a cool and dry place. Keep away from light. Keep out of the reach of children.