IMAVEC

IMAVEC

Imatinib 400mg
Net Qty- 3x10 Tablets
Self-Life- 2 Years

Imavec (Imatinib) is a first-generation tyrosine kinase inhibitor (TKI) used to treat certain types of cancers, primarily Chronic Myeloid Leukemia (CML) and Gastrointestinal Stromal Tumors (GISTs). It is commonly sold under the brand name Imavec by MedOnco Pharma.

USE

Uses of Imatinib 400mg

✅ Chronic Myeloid Leukemia (CML) (Philadelphia Chromosome-Positive)

  • First-line treatment for newly diagnosed CML in the chronic phase.
  • Used in accelerated or blast phase when other treatments fail.

✅ Acute Lymphoblastic Leukemia (ALL) (Ph+ ALL)

  • Used in combination with chemotherapy for Philadelphia chromosome-positive ALL.

✅ Gastrointestinal Stromal Tumors (GISTs)

  • Effective against CD117 (c-KIT) positive GISTs.
  • Used in unresectable or metastatic cases.

✅ Other Uses

  • Hypereosinophilic Syndrome (HES)
  • Dermatofibrosarcoma Protuberans (DFSP)
  • Systemic Mastocytosis

Mechanism
of Action

Imavec (Imatinib) is a tyrosine kinase inhibitor (TKI) that blocks specific proteins involved in cancer growth, primarily BCR-ABL, c-KIT, and PDGFR.

 1. Targets of Imavec (Imatinib)

✅ BCR-ABL Tyrosine Kinase (Main Target in CML & Ph+ ALL)

  • In Chronic Myeloid Leukemia (CML) and Philadelphia chromosome-positive Acute Lymphoblastic Leukemia (Ph+ ALL), an abnormal BCR-ABL fusion protein is created due to a genetic mutation (Philadelphia Chromosome, t(9;22)).
  • This BCR-ABL protein is a constitutively active tyrosine kinase, which triggers uncontrolled cancer cell division.
  • Imavec (Imatinib) binds to the ATP-binding site of BCR-ABL, preventing it from activating downstream signaling pathways like RAS/MAPK and PI3K/AKT, which promote leukemia cell growth.
    ✔ Result: Cancer cell growth is halted, and apoptosis (cell death) is triggered.

✅ c-KIT Tyrosine Kinase (Main Target in GISTs)

  • In Gastrointestinal Stromal Tumors (GISTs), cancer cells have mutations in the c-KIT gene, leading to continuous activation of the KIT receptor tyrosine kinase, which fuels tumor growth.
  • Imavec (Imatinib) blocks c-KIT, stopping tumor cell proliferation.
    ✔ Result: Tumor shrinkage and slowed disease progression.

✅ PDGFR (Platelet-Derived Growth Factor Receptor)

  • In some cancers like Hypereosinophilic Syndrome (HES) and Dermatofibrosarcoma Protuberans (DFSP), PDGFR mutations cause abnormal cell proliferation.
  • Imavec (Imatinib) inhibits PDGFR, blocking the growth signals.
    ✔ Result: Prevention of tumor formation.

2. How Imavec (Imatinib) Works at the Cellular Level

💊 Imavec (Imatinib) competes with ATP at the kinase’s active site → Prevents phosphorylation of downstream signaling proteins → Stops cancer cell proliferation and induces apoptosis.

Key Takeaways

✔ Blocks BCR-ABL in CML & Ph+ ALL (stops leukemia cell growth)
✔ Inhibits c-KIT in GISTs (prevents tumor growth)
✔ Targets PDGFR in other cancers (stops abnormal cell division)
✔ Results in apoptosis (cancer cell death) and prevents disease progression

Dosage and Administration

Imavec (Imatinib) should be taken under the supervision of Doctors only, Imavec (Imatinib) is not advisable with out Doctors prescription-


💊 Standard Dose for CML & GISTs: 400mg once daily (can be increased to 600-800mg if needed).

💊 Take with food and a full glass of water to reduce stomach irritation.
💊 Do not crush or chew the tablet.

Common Side Effects

Most common side effects of Imavec (Imatinib)

✅ Mild Side Effects:

  • Nausea, vomiting
  • Fatigue
  • Muscle cramps, joint pain
  • Diarrhea

🚨 Serious Side Effects (Call a Doctor):

  • Severe swelling (fluid retention) (around the eyes, ankles, lungs)
  • Unusual bleeding or bruising
  • Liver problems (yellowing of skin, dark urine)
  • Heart issues (shortness of breath, chest pain)

Monitoring

If you’re taking Dasatinib 50mg, regular monitoring is essential to ensure safety and effectiveness. Below are the key tests and parameters that should be checked:

1. Blood Tests (Complete Blood Count – CBC)

✅ Frequency: Weekly for the first 2 months, then monthly
✅ Purpose:

  • Check for low white blood cell (WBC) count (neutropenia)
  • Detect low platelet levels (thrombocytopenia)
  • Identify anemia (low RBC count)

2. Liver Function Tests (LFTs)

✅ Frequency: Every 4-6 weeks or as needed
✅ Purpose:

  • Monitor for elevated liver enzymes (AST, ALT, bilirubin)
  • Ensure no drug-induced liver damage

3. Kidney Function Tests

✅ Frequency: Every 3-6 months
✅ Purpose:

  • Monitor creatinine and blood urea nitrogen (BUN) levels
  • Check for kidney impairment

4. Electrolytes (Sodium, Potassium, Calcium, Magnesium, Phosphorus)

✅ Frequency: Every 4-6 weeks
✅ Purpose:

  • Prevent electrolyte imbalances that may cause heart problems

5. ECG (Electrocardiogram)

✅ Frequency: Before starting treatment and periodically
✅ Purpose:

  • Monitor for QT prolongation, which can lead to heart rhythm issues

6. Chest X-ray or Lung Function Tests

✅ Frequency: If symptoms develop
✅ Purpose:

  • Detect pleural effusion (fluid in the lungs), a common side effect

7. Bone Marrow Examination (For CML patients)

✅ Frequency: Every 3-6 months
✅ Purpose:

  • Assess response to treatment and check for disease progression

8. BCR-ABL1 Mutation Testing (If resistance is suspected)

✅ Frequency: If treatment is not working
✅ Purpose:

  • Identify mutations that may cause resistance to Dasatinib
  • Determine if a different TKI (like Ponatinib or Bosutinib) is needed

9. Pregnancy Test (For Women of Childbearing Age)

✅ Frequency: Before starting treatment and as needed
✅ Purpose:

  • Dasatinib is harmful during pregnancy, so women must avoid pregnancy during treatment

Important Precautions During Monitoring:

❌ Avoid grapefruit juice, as it can increase Dasatinib levels
❌ Do not take with antacids or proton pump inhibitors (PPIs) (reduces drug absorption)
✔ Stay hydrated to prevent kidney-related side effects

Precautions

If you are taking Imavec (Imatinib 400mg), following these precautions can help ensure safety and effectiveness while minimizing side effects.

1. Before Starting Imatinib

✔ Inform your doctor if you have:

  • Liver, kidney, or heart disease
  • History of infections or low blood counts
  • Bleeding disorders

✔ Pregnancy & Breastfeeding

  • Avoid pregnancy – Imatinib can harm the unborn baby.
  • Use effective contraception while on treatment.
  • Do not breastfeed while taking Imatinib.

2. How to Take Imatinib Safely

✔ Take with food and a full glass of water to prevent stomach irritation.
✔ Swallow the tablet whole – do not crush, chew, or break it.
✔ Take at the same time every day to maintain steady drug levels.
✔ Avoid grapefruit juice, as it can increase side effects.

3. Monitoring & Regular Checkups

📌 Complete Blood Count (CBC) – Monitor WBCs, RBCs, and platelets.
📌 Liver & Kidney Function Tests – To detect any organ toxicity.
📌 ECG (if needed) – For patients at risk of heart issues.

4. Managing Side Effects

💊 For Swelling & Fluid Retention:
✔ Limit salt intake to reduce swelling.
✔ Report severe swelling or shortness of breath immediately.

💊 For Stomach Problems (Nausea, Vomiting, Diarrhea):
✔ Eat small, frequent meals.
✔ Stay hydrated and take anti-nausea medications if needed.

💊 For Muscle Cramps & Joint Pain:
✔ Stay hydrated and eat potassium-rich foods (bananas, nuts).
✔ Light stretching or gentle massage can help.

💊 For Fatigue & Weakness:
✔ Get enough rest and avoid overexertion.
✔ Light exercise (like walking) can improve energy levels.

5. Drug & Food Interactions (Avoid These)

🚫 Do not take with acid-reducing medications (PPIs, H2 blockers).
🚫 Avoid NSAIDs (Ibuprofen, Naproxen) – Use paracetamol for pain relief.
🚫 Avoid alcohol and smoking – can worsen liver and lung issues.

6. When to Contact Your Doctor 🚨

❌ Severe swelling, breathing problems, or chest pain
❌ Persistent fever, infections, or unusual bruising
❌ Dark urine, yellowing of skin (signs of liver issues)
❌ Severe diarrhea, dehydration, or vomiting

Key Takeaways

✔ Take with food & water to avoid stomach upset.
✔ Monitor side effects & blood tests regularly.
✔ Avoid grapefruit, smoking, alcohol, and pregnancy.
✔ Stay hydrated & eat well to reduce side effects.

Drug Interactions

Imavec (Imatinib) interacts with various drugs, affecting its absorption, metabolism, and effectiveness. Below are the key interactions to watch out for:

1. Acid-Reducing Agents (Reduce Imatinib Absorption) – AVOID

💊 Proton Pump Inhibitors (PPIs): Omeprazole, Pantoprazole, Esomeprazole
💊 H2 Blockers: Ranitidine, Famotidine
💊 Antacids: Aluminum hydroxide, Magnesium hydroxide

✅ Solution: If antacids are needed, take them at least 2 hours before or after Imatinib.

2. CYP3A4 Inhibitors (Increase Imatinib Levels – Risk of Toxicity) – AVOID

💊 Antifungals: Ketoconazole, Itraconazole, Voriconazole
💊 Antibiotics: Clarithromycin, Erythromycin
💊 HIV Medications: Ritonavir, Indinavir, Saquinavir

✅ Solution: Dose adjustments may be needed if these drugs must be taken.

3. CYP3A4 Inducers (Reduce Imatinib Effect – Risk of Treatment Failure) – AVOID

💊 Anticonvulsants: Phenytoin, Carbamazepine, Phenobarbital
💊 Tuberculosis Drugs: Rifampin, Rifabutin
💊 Herbal Products: St. John’s Wort

✅ Solution: Avoid these drugs or switch to alternatives.

4. Blood Thinners & Antiplatelets (Increase Bleeding Risk) – CAUTION

💊 Warfarin, Heparin
💊 Aspirin, Clopidogrel
💊 NSAIDs (Ibuprofen, Naproxen, Diclofenac)

✅ Solution: Use paracetamol (acetaminophen) instead of NSAIDs for pain relief. Monitor for bleeding signs.

5. Cardiovascular Drugs (May Increase Heart Side Effects) – CAUTION

💊 QT-Prolonging Drugs: Amiodarone, Sotalol, Moxifloxacin
💊 Calcium Channel Blockers: Diltiazem, Verapamil (also CYP3A4 inhibitors)

✅ Solution: ECG monitoring may be needed if taken together.

6. Immunosuppressants (Increase Risk of Infection) – CAUTION

💊 Tacrolimus, Cyclosporine

✅ Solution: Monitor immune function closely.

7. Other Cancer Drugs (Possible Increased Toxicity) – CAUTION

💊 Other Tyrosine Kinase Inhibitors: Dasatinib, Nilotinib, Ponatinib
💊 Chemotherapy Agents: Doxorubicin, Cyclophosphamide

✅ Solution: Careful dose adjustments and monitoring are required.

8. Food & Drink Interactions

🚫 Avoid grapefruit juice, as it increases Imatinib levels and side effects.
🚫 Avoid alcohol, as it may worsen liver toxicity.

Key Takeaways

❌ Avoid acid reducers, CYP3A4 inducers/inhibitors, and grapefruit juice.
⚠ Be cautious with blood thinners, heart medications, and NSAIDs.
✔ Consult your doctor before adding new medications.

Clinical Effectiveness

Imavec (Imatinib) is a first-generation tyrosine kinase inhibitor (TKI) used primarily for Chronic Myeloid Leukemia (CML) and Gastrointestinal Stromal Tumors (GISTs). Clinical trials and real-world studies have confirmed its high effectiveness in treating these conditions.

1. Effectiveness in Chronic Myeloid Leukemia (CML)

✅ First-Line Treatment (Newly Diagnosed CML)

  • IRIS Trial (2003, 5-year follow-up)
    • Complete Cytogenetic Response (CCyR): 83% of patients achieved CCyR after 5 years.
    • Overall Survival (OS): 89% survival rate at 5 years.
    • Progression-Free Survival (PFS): 87% of patients remained in chronic phase without disease progression.
    • Conclusion: Imavec (Imatinib) revolutionized CML treatment, significantly increasing survival rates.
  • 10-Year Follow-up of IRIS Trial (2013)
    • 10-year survival rate: 83% of patients were still alive, showing long-term effectiveness.

✅ Key Finding: Imavec (Imatinib) transformed CML from a fatal disease into a manageable chronic condition with normal life expectancy in most patients.

✅ Second-Line Treatment (Imavec (Imatinib)-Resistant Cases)

  • For patients resistant or intolerant to Imavec (Imatinib), second-generation TKIs like Dasatinib or Nilotinib are used.
  • Effectiveness in Resistant Cases: Around 30-40% of patients who switch to higher doses (800mg daily) show improved response.

2. Effectiveness in Gastrointestinal Stromal Tumors (GISTs)

  • GIST Clinical Trials (B2222 Study, 2002)
    • Progression-Free Survival (PFS) at 2 years: 75% of patients had no tumor progression.
    • Overall Survival: 88% at 2 years, significantly higher than historical survival rates.
    • Tumor Size Reduction: 50-70% of patients experienced partial or complete tumor shrinkage.

✅ Key Finding: Imavec (Imatinib) is the first-line treatment for metastatic or unresectable GISTs and greatly improves survival.

3. Effectiveness in Other Cancers

  • Philadelphia Chromosome-Positive Acute Lymphoblastic Leukemia (Ph+ ALL):
    • Increases remission rates when combined with chemotherapy.
    • Long-term survival is better than chemotherapy alone.
  • Hypereosinophilic Syndrome (HES) & Systemic Mastocytosis
    • Effective in patients with PDGFR mutations.

Summary of Clinical Effectiveness

✔ CML: 10-year survival >80% (life expectancy near normal).
✔ GISTs: Significant tumor reduction and extended survival.
✔ Ph+ ALL & Other Cancers: Improves remission and survival rates.

Tips for Patients

If you are taking Imavec (Imatinib) 400mg, following these tips can help maximize effectiveness and minimize side effects.

1. How to Take Imavec (Imatinib) Correctly

✔ Take with food and a full glass of water to reduce stomach irritation.
✔ Swallow the tablet whole—do not crush, break, or chew it.
✔ Take it at the same time each day to maintain stable drug levels.
✔ If you miss a dose, take it as soon as you remember. If it’s almost time for the next dose, skip the missed dose (do not double the dose).

2. Managing Side Effects

✅ Stomach Problems (Nausea, Vomiting, Diarrhea)

  • Eat small, frequent meals to prevent nausea.
  • Stay hydrated (drink at least 2–3 liters of water daily).
  • If diarrhea occurs, electrolyte drinks can help.

✅ Swelling & Fluid Retention (Face, Legs, Eyes)

  • Limit salt intake to reduce swelling.
  • If severe swelling or breathing issues occur, contact your doctor immediately.

✅ Muscle Cramps & Joint Pain

  • Stay hydrated and eat foods rich in potassium & magnesium (bananas, nuts, spinach).
  • Light stretching or massage can help relieve muscle pain.

✅ Fatigue & Weakness

  • Get enough rest and avoid overexertion.
  • Light exercise (like walking) can help improve energy levels.

✅ Skin Rash & Dryness

  • Use a mild moisturizer and wear sunscreen outdoors.
  • If the rash worsens, inform your doctor.

✅ Low Blood Counts (Anemia, Neutropenia, Thrombocytopenia)

  • Regular blood tests are needed to monitor counts.
  • Report unusual bruising, bleeding, or infections immediately.

3. Lifestyle Tips

✔ Avoid alcohol and smoking, as they may worsen side effects.
✔ Eat a balanced diet with fruits, vegetables, and protein-rich foods.
✔ Avoid grapefruit & St. John’s Wort, as they can interfere with Imavec (Imatinib).
✔ Use effective birth control, as Imavec (Imatinib) can harm unborn babies.

4. Regular Monitoring is Key

📌 Complete Blood Count (CBC) – Monitor WBCs, RBCs, and platelets.
📌 Liver & Kidney Function Tests – To detect any organ toxicity.
📌 Heart Monitoring (ECG, if needed) – For patients at risk of heart issues.

5. When to Call Your Doctor 🚨

❌ Severe swelling, breathing problems, or chest pain
❌ Persistent fever, infections, or unusual bruising
❌ Dark urine, yellowing of skin (signs of liver issues)
❌ Severe diarrhea, dehydration, or vomiting

Key Takeaways

✔ Take with food & water to avoid stomach upset.
✔ Monitor side effects & blood tests regularly.
✔ Avoid grapefruit, smoking, alcohol, and pregnancy.
✔ Stay hydrated & eat well to reduce side effects.