GEFIMED

GEFIMED

Gefitinib 250mg
Net Qty- 30 Tablets
Shelf-Life- 2 Years

Gefimed (Gefitinib 250mg) is a targeted therapy drug used primarily for treating certain types of lung cancer. It is a tyrosine kinase inhibitor (TKI) that works by blocking specific proteins involved in cancer growth.. It is commonly sold under the brand name Gefimed by MedOnco Pharma.

USE

Uses of Gefimed (Gefitinib 250mg)

1. Primary Use of Gefitinib 250mg

✅ Non-Small Cell Lung Cancer (NSCLC) – EGFR Mutation Positive

  • Used for advanced (metastatic) or locally advanced NSCLC.
  • Works best in patients with EGFR mutations (Exon 19 deletion or Exon 21 L858R mutation).
  • First-line treatment in patients who are not suitable for chemotherapy.

2. Other Possible Uses (Off-Label)

  • Head and Neck Cancers (In some cases, when EGFR is overexpressed).
  • Breast Cancer (Under research, not a standard treatment).

3. Who Should Take Gefitinib?

✔ Patients with NSCLC confirmed to have EGFR mutations.
✔ Those unable to tolerate chemotherapy due to age or other health issues.
✔ Patients with advanced or metastatic lung cancer.

🚫 Not effective for lung cancer without EGFR mutations.

Key Takeaways

✔ First-line treatment for EGFR-positive NSCLC.
✔ Oral tablet, taken once daily (250mg).
✔ Less toxic than chemotherapy, but requires genetic testing.

Mechanism
of Action

Gefimed (Gefitinib) is a tyrosine kinase inhibitor (TKI) that specifically targets the epidermal growth factor receptor (EGFR), a protein involved in cancer cell growth and survival.

1. Target: EGFR Tyrosine Kinase

  • EGFR (Epidermal Growth Factor Receptor) is a protein found on the surface of cells.
  • When EGFR is activated by growth factors, it triggers cell division and survival pathways.
  • In certain cancers (especially EGFR-mutated NSCLC), EGFR is overactive, leading to uncontrolled tumor growth.

2. How Gefitinib Works

💊 Gefitinib binds to the ATP-binding site of EGFR, preventing its activation.
💊 This blocks downstream signaling pathways like:

  • RAS/MAPK Pathway (involved in cell proliferation)
  • PI3K/AKT Pathway (prevents apoptosis)
  • JAK/STAT Pathway (involved in inflammation and survival)
    💊 As a result, cancer cells stop dividing and undergo apoptosis (cell death).

✅ Gefitinib is highly effective in tumors with EGFR mutations (Exon 19 deletion & Exon 21 L858R mutation).
🚫 Does not work well in tumors without EGFR mutations or those with T790M resistance mutations.

3. Summary of Gefitinib’s Action

 

✔ Blocks EGFR signaling → Stops tumor growth
✔ Prevents cancer cell survival → Induces apoptosis
✔ Targets only EGFR-mutant cancer cells → Fewer side effects than chemotherapy

Dosage and Administration

Gefimed (Gefitinib 250mg) is a targeted therapy used primarily for EGFR-mutated non-small cell lung cancer (NSCLC). Proper dosing and administration ensure maximum effectiveness and minimal side effects.

1. Standard Dosage

💊 Recommended Dose: 250mg once daily
💊 Maximum Dose: 250mg/day (Higher doses do not increase effectiveness but may cause more side effects.)

2. How to Take Gefitinib

✔ Take it at the same time every day for consistent blood levels.
✔ Swallow the tablet whole with water—do not crush, break, or chew.
✔ Can be taken with or without food (food does not affect absorption).
✔ If you have trouble swallowing, dissolve the tablet in half a glass of water, stir for 10 minutes, and drink immediately.

3. Missed Dose Instructions

  • If you miss a dose, take it as soon as you remember.
  • If it’s close to your next dose, skip the missed dose.
  • Do not take a double dose to make up for the missed one.

4. Special Administration Considerations

🚫 Avoid taking Gefitinib with acid-reducing agents (PPIs, H2 blockers, antacids) as they reduce drug absorption.
🚫 Do not take with grapefruit juice, as it increases drug levels and side effects.
✔ Patients with liver or kidney issues may require close monitoring.

5. Duration of Treatment

  • Continue as long as the cancer responds and side effects are manageable.
  • If cancer progresses or severe side effects occur, your doctor may adjust the dose or switch to another therapy.

Key Takeaways

✔ 250mg once daily, same time each day.
✔ Take whole with water, with or without food.
✔ Avoid acid reducers & grapefruit juice.
✔ Do not double dose if missed.

Common Side Effects

Gefimed (Gefitinib 250mg) is a targeted therapy, and while it’s generally well-tolerated, it can still cause side effects. Below are the common side effects and how to manage them.

1. Skin-Related Issues

✅ Rash or Acne-like Eruptions

  • Frequency: Occurs in about 30-40% of patients.
  • Management:
    • Use gentle skincare products and moisturizers.
    • Avoid sun exposure and use sunscreen.
    • Over-the-counter hydrocortisone cream or prescribed treatments can help.

✅ Dry Skin or Itching

  • Frequency: Mild to moderate dryness is common.
  • Management:
    • Apply moisturizers regularly.
    • Avoid hot showers to prevent further drying.

2. Gastrointestinal Issues

✅ Diarrhea

  • Frequency: Occurs in around 30% of patients.
  • Management:
    • Stay hydrated with fluids that replace electrolytes.
    • Use anti-diarrheal medications (with doctor approval).
    • Avoid fatty, spicy foods that can irritate the digestive system.

✅ Nausea or Vomiting

  • Frequency: Common but often mild.
  • Management:
    • Take with food to reduce nausea.
    • Ask your doctor about anti-nausea medications.

3. Fatigue and Weakness

  • Frequency: Moderate fatigue is a common side effect.
  • Management:
    • Rest regularly and avoid overexertion.
    • Light exercise like walking may help boost energy levels.

4. Liver Function Changes

✅ Elevated Liver Enzymes

  • Frequency: Seen in some patients (mild to moderate elevation).
  • Management:
    • Regular liver function tests (LFTs) to monitor levels.
    • If liver enzymes become too elevated, your doctor may adjust the dose or stop the treatment.
    • Report yellowing of the skin/eyes or dark urine immediately.

5. Eye Problems

✅ Eye Irritation (Dry eyes or Conjunctivitis)

  • Frequency: Occurs in a small percentage of patients.
  • Management:
    • Use artificial tears or eye lubricants.
    • Consult an ophthalmologist if irritation persists.

6. Respiratory Issues

✅ Interstitial Lung Disease (ILD)

  • Frequency: Rare, but potentially serious.
  • Management:
    • Monitor for shortness of breath, persistent cough, or fever.
    • Seek medical help immediately if these symptoms occur.
    • Your doctor may stop treatment if ILD develops.

7. Loss of Appetite

  • Frequency: May cause mild loss of appetite in some patients.
  • Management:
    • Eat small, frequent meals.
    • Consume nutrient-dense foods to maintain weight and energy.

Key Takeaways

 

✔ Skin rash, diarrhea, and nausea are the most common side effects.
✔ Monitor for liver and lung problems through regular check-ups.
✔ Manage fatigue with rest and light exercise.
✔ Contact your doctor immediately if you notice severe symptoms like shortness of breath, jaundice, or persistent cough.

Monitoring

Patients taking Gefimed (Gefitinib 250mg) for EGFR-mutated non-small cell lung cancer (NSCLC) should undergo regular monitoring to ensure the drug’s effectiveness and detect any potential side effects early. Below are the key aspects of monitoring during treatment with Gefitinib.

1. Liver Function Tests (LFTs)

  • Why: Gefitinib can cause liver toxicity, resulting in elevated liver enzymes.
  • When: Before starting treatment, then every 2-4 weeks during the first few months of treatment, and periodically thereafter.
  • What to Watch For:
    • Elevated AST (aspartate aminotransferase), ALT (alanine aminotransferase), or bilirubin.
    • Report yellowing of the skin/eyes or dark urine, which may indicate liver problems.

2. Lung Function Monitoring (Interstitial Lung Disease – ILD)

  • Why: Gefitinib can cause Interstitial Lung Disease (ILD), a serious side effect that affects the lungs.
  • When: Regular checkups for breathing issues (especially at the start of treatment) and after any signs or symptoms of ILD develop.
  • What to Watch For:
    • Persistent cough, shortness of breath, or fever.
    • If ILD symptoms appear, discontinue Gefitinib immediately and consult your doctor.

3. Dermatological Monitoring (Skin Rash & Acne)

  • Why: A common side effect of Gefitinib is skin rash or acne-like eruptions.
  • When: Monitor the skin daily for any signs of rash or dryness.
  • What to Watch For:
    • Severe or spreading rash, redness, or blistering.
    • Manage with topical treatments, but seek medical advice if severe.

4. Gastrointestinal Function (Diarrhea & Nausea)

  • Why: Gefitinib can cause diarrhea, nausea, and vomiting, which can lead to dehydration and electrolyte imbalances.
  • When: Monitor daily for gastrointestinal symptoms.
  • What to Watch For:
    • Frequent or severe diarrhea.
    • Loss of appetite or dehydration.
    • Electrolyte testing may be needed if diarrhea is persistent.

5. ECG (Electrocardiogram)

  • Why: Rarely, Gefitinib may cause QT prolongation, which affects heart rhythm.
  • When: ECG monitoring may be needed if you have a history of heart disease or are taking other medications that may cause QT prolongation.
  • What to Watch For:
    • Irregular heartbeats, dizziness, or fainting.
    • If these symptoms occur, an ECG will be required to assess the heart’s electrical activity.

6. General Symptom Monitoring

  • Why: To detect potential side effects early.
  • When: Ongoing monitoring throughout treatment.
  • What to Watch For:
    • Fatigue, weakness, or loss of appetite.
    • Unusual bleeding, bruising, or infections due to potential impacts on blood cells.

7. Regular Clinical Assessments

  • Why: Monitor the overall effectiveness of Gefitinib.
  • When: Every 2-3 months, or as needed based on disease progression.
  • What to Watch For:
    • CT scans or MRIs may be used to assess tumor size and response to treatment.
    • Symptom improvement or worsening should be reported to the doctor.

Key Takeaways

 

✔ Monitor liver function regularly to prevent toxicity.
✔ Watch for lung issues (ILD), skin reactions, and gastrointestinal symptoms.
✔ Be vigilant about heart function and other general side effects.
✔ Frequent clinical checkups and imaging are important to track cancer response.

Precautions

Gefimed (Gefitinib 250mg) is a targeted therapy used for EGFR-mutated non-small cell lung cancer (NSCLC), and it is important to follow specific precautions to ensure safety and minimize risks associated with the treatment.

1. Before Starting Treatment

✅ Liver Problems

  • Precaution: Inform your doctor if you have a history of liver disease or liver problems.
  • Reason: Gefitinib can cause elevated liver enzymes and liver toxicity.
  • Action: Liver function tests should be conducted before and during treatment.

✅ Lung Issues

  • Precaution: Tell your doctor if you have a history of lung disease or breathing problems.
  • Reason: Gefitinib may cause Interstitial Lung Disease (ILD), which can lead to severe breathing problems.
  • Action: Be vigilant for signs of ILD (persistent cough, shortness of breath, or fever).

✅ Pregnancy & Breastfeeding

  • Precaution: Avoid pregnancy during treatment, and do not breastfeed while taking Gefitinib.
  • Reason: Gefitinib can harm an unborn baby and is excreted in breast milk.
  • Action: Use effective contraception during treatment, and consult your doctor about stopping breastfeeding.

✅ Kidney Problems

  • Precaution: If you have kidney disease, inform your doctor.
  • Reason: Gefitinib is metabolized by the liver and excreted by the kidneys, and any kidney impairment may affect the drug’s elimination.
  • Action: Kidney function tests should be conducted periodically.

2. During Treatment

✅ Skin Reactions (Rash & Dry Skin)

  • Precaution: Monitor your skin for rash, dryness, or itching.
  • Reason: Skin-related issues like acneiform rash are common.
  • Action: Use moisturizers and sunscreen to protect skin. Contact your doctor if the rash becomes severe.

✅ Gastrointestinal Issues (Diarrhea, Nausea)

  • Precaution: Be mindful of gastrointestinal side effects like diarrhea and nausea.
  • Reason: These side effects are common and can lead to dehydration or electrolyte imbalances.
  • Action: Stay hydrated and consult your doctor for anti-nausea medications or anti-diarrheal treatments.

✅ Monitoring for Lung Toxicity (ILD)

  • Precaution: Monitor for breathing issues such as shortness of breath, cough, or fever.
  • Reason: ILD is a serious but rare side effect.
  • Action: Report any respiratory symptoms immediately to your doctor. Discontinuation of Gefitinib may be necessary if ILD develops.

3. Drug Interactions

✅ Avoid Certain Medications

  • CYP3A4 Inhibitors: (e.g., Ketoconazole, Clarithromycin) – May increase Gefitinib levels and risk of side effects.
  • CYP3A4 Inducers: (e.g., Rifampin, Phenytoin) – May reduce the effectiveness of Gefitinib.
  • Antacids & PPIs: Can reduce Gefitinib absorption.
  • Grapefruit Juice: Increases Gefitinib levels, leading to possible toxicity.
  • Action: Always inform your doctor about any other medications, including over-the-counter drugs and supplements.

4. Heart & Eye Issues

✅ Heart Monitoring (QT Prolongation)

  • Precaution: If you have a history of heart problems, especially QT prolongation, discuss this with your doctor.
  • Reason: Gefitinib may affect the heart’s electrical activity.
  • Action: ECG monitoring may be required if you have a heart condition or are taking other medications that affect heart rhythm.

✅ Eye Irritation

  • Precaution: Inform your doctor if you have a history of eye problems.
  • Reason: Gefitinib can cause eye irritation or dry eyes.
  • Action: Use artificial tears or consult your doctor for eye care.

5. General Precautions

✅ Regular Monitoring

  • Precaution: Frequent monitoring is necessary for liver function, lung health, and blood counts.
  • Reason: To detect side effects early and adjust treatment as needed.
  • Action: Schedule regular checkups with your doctor.

✅ Avoid Concomitant Chemotherapy

  • Precaution: Avoid chemotherapy during Gefitinib treatment unless specifically directed by your doctor.
  • Reason: Combining therapies may increase the risk of side effects.
  • Action: Always discuss treatment plans with your healthcare team.

Key Takeaways

✔ Monitor for lung issues (ILD), liver toxicity, and skin problems.
✔ Avoid drugs that interact with Gefitinib, including acid reducers, grapefruit juice, and certain antibiotics.
✔ Use contraception, and avoid breastfeeding during treatment.
✔ Stay hydrated, and report any severe side effects immediately.

Drug Interactions

Gefimed (Gefitinib 250mg) can interact with other drugs, affecting its effectiveness or increasing the risk of side effects. Below are the key drug interactions to be aware of:

 

1. CYP3A4 Inhibitors (Increase Gefitinib Levels – Risk of Toxicity)

Gefitinib is metabolized by the CYP3A4 enzyme, so drugs that inhibit this enzyme can increase its levels in the body, leading to an increased risk of side effects.

Examples of CYP3A4 Inhibitors:

  • Antifungals: Ketoconazole, Itraconazole
  • Antibiotics: Clarithromycin, Erythromycin
  • HIV Medications: Ritonavir, Saquinavir
  • Antidepressants: Fluoxetine, Paroxetine
  • Other: Grapefruit juice (which also inhibits CYP3A4)

✅ Solution: Dose adjustment or more frequent monitoring may be necessary if you need to take these medications.

2. CYP3A4 Inducers (Reduce Gefitinib Levels – Risk of Treatment Failure)

CYP3A4 inducers can reduce Gefitinib levels, making it less effective in treating cancer.

Examples of CYP3A4 Inducers:

  • Anticonvulsants: Phenytoin, Carbamazepine, Phenobarbital
  • Antituberculosis Drugs: Rifampin, Rifabutin
  • Herbal Products: St. John’s Wort
  • Other: Barbiturates, some other HIV medications

✅ Solution: If possible, avoid these drugs or ask your doctor about alternative therapies. If you must take these drugs, your doctor may adjust the dose of Gefitinib.

3. Antacids, Proton Pump Inhibitors (PPIs), and H2 Blockers (Reduce Gefitinib Absorption)

These drugs reduce stomach acid, which can impair the absorption of Gefitinib, reducing its effectiveness.

Examples:

  • Antacids: Aluminum hydroxide, Magnesium hydroxide
  • H2 Blockers: Ranitidine, Famotidine
  • PPIs: Omeprazole, Esomeprazole

✅ Solution: Avoid taking antacids or acid reducers at the same time as Gefitinib. If needed, take antacids at least 2 hours before or after Gefitinib.

4. Warfarin (Blood Thinner) and Other Anticoagulants

Gefitinib can increase the effect of blood thinners, which increases the risk of bleeding.

Example: Warfarin

✅ Solution: If you take warfarin, your doctor may need to monitor your INR (International Normalized Ratio) more closely and adjust the dose of your blood thinner accordingly.

5. Chemotherapy and Other Cancer Drugs

  • Concurrent chemotherapy with Gefitinib is generally not recommended unless directed by your doctor.
  • Other EGFR inhibitors (like Erlotinib, Afatinib) should not be used together with Gefitinib, as it could increase toxicity without improving effectiveness.

✅ Solution: Always inform your doctor of all medications you are taking, including cancer treatments.

6. Drugs Affecting the QT Interval

Gefitinib can prolong the QT interval on the electrocardiogram (ECG), so taking it with drugs that also prolong the QT interval may increase the risk of heart problems.

Examples of QT-prolonging drugs:

  • Antiarrhythmic drugs: Amiodarone, Sotalol
  • Antipsychotics: Haloperidol
  • Antibiotics: Moxifloxacin

✅ Solution: If you are on any of these medications, ECG monitoring is advised.

Key Takeaways

 

❌ Avoid drugs that inhibit or induce CYP3A4, such as certain antifungals, antibiotics, and antiepileptic drugs.
❌ Avoid antacids or PPIs close to the time you take Gefitinib.
⚠ Be cautious with blood thinners and QT-prolonging drugs.
✔ Inform your doctor about all medications, including over-the-counter drugs and supplements.

Clinical Effectiveness

Gefimed (Gefitinib 250mg) is a tyrosine kinase inhibitor (TKI) primarily used in the treatment of EGFR-mutant non-small cell lung cancer (NSCLC). It has shown significant clinical effectiveness in patients with EGFR-positive mutations. Here’s a summary of its effectiveness:

 

1. Effectiveness in Non-Small Cell Lung Cancer (NSCLC)

Gefitinib is approved for first-line treatment of advanced or metastatic NSCLC in patients whose tumors have activating EGFR mutations (Exon 19 deletions or Exon 21 L858R mutation).

✅ Key Clinical Trials

  • IDEAL 1 & 2 Trials (2003):
    • Overall response rate (ORR): 43-46% in patients with EGFR mutations.
    • Progression-free survival (PFS): 9.2 to 11 months, significantly better than chemotherapy options (4-5 months).
    • Patients with Exon 19 deletions or L858R mutations saw better outcomes than those without these mutations.
  • IPASS Trial (2009):
    • First-line treatment trial for Asian patients with EGFR mutations.
    • Gefitinib showed superior progression-free survival (PFS) over chemotherapy.
    • PFS was 9.5 months for Gefitinib vs. 6.3 months for standard chemotherapy (carboplatin and paclitaxel).

2. Comparison with Chemotherapy

Gefitinib has better efficacy in EGFR-positive patients when compared to standard chemotherapy (e.g., carboplatin and paclitaxel).

  • Gefitinib’s response rate in EGFR-mutant NSCLC patients is higher, and it has fewer side effects like nausea, vomiting, and hair loss, which are common with chemotherapy.

✅ Key Findings:

  • Improved Quality of Life (QoL): Patients treated with Gefitinib have reported fewer side effects, leading to better quality of life compared to chemotherapy.
  • Faster Response Time: Gefitinib produces rapid responses compared to chemotherapy in EGFR-mutated tumors.

3. Resistance and Limitations

  • T790M Mutation Resistance:
    • One limitation of Gefitinib is the development of the T790M mutation in some patients, which causes resistance to EGFR TKIs.
    • This mutation often occurs after initial success with Gefitinib, leading to disease progression.
    • Alternatives: Osimertinib, a third-generation TKI, has been shown to be more effective in treating T790M-resistant NSCLC.

4. Effectiveness in Other Cancers

While Gefitinib is most commonly used for NSCLC, it has shown some limited activity in other cancers where EGFR plays a role (e.g., head and neck cancers), though it is not FDA-approved for those indications.

Key Takeaways

 

✔ Highly effective in EGFR-mutant NSCLC, especially in first-line therapy.
✔ Better PFS and quality of life compared to chemotherapy in EGFR-positive patients.
✔ Resistance due to the T790M mutation can occur after some time, which limits long-term effectiveness.
✔ Not effective for EGFR-negative patients.

Tips for Patients

If you are taking Gefimed (Gefitinib 250mg) for EGFR-mutated non-small cell lung cancer (NSCLC), following these tips can help maximize effectiveness and minimize side effects:

1. How to Take Gefitinib Properly

✔ Take it at the same time each day to maintain stable drug levels.
✔ Take with or without food (food does not affect absorption).
✔ Swallow the tablet whole with a glass of water—do not crush, chew, or break it.
✔ If you miss a dose, take it as soon as you remember, but if it’s close to your next dose, skip the missed dose (do not double the dose).

2. Managing Side Effects

✅ Skin Rash & Dry Skin

  • Skin rash is a common side effect.
  • Use moisturizers to prevent dryness.
  • Avoid sun exposure and use sunscreen to protect your skin from sunburn.
  • If the rash is severe, consult your doctor for topical treatments or possible dose adjustments.

✅ Diarrhea

  • Stay hydrated and drink plenty of fluids to prevent dehydration.
  • Avoid spicy or greasy foods, which can aggravate diarrhea.
  • Use anti-diarrheal medications (like loperamide) with your doctor’s approval.
  • If diarrhea becomes severe, contact your doctor immediately.

✅ Nausea & Vomiting

  • Take with food to reduce nausea.
  • Eat small, frequent meals throughout the day.
  • If nausea persists, your doctor may prescribe anti-nausea medications.

3. Regular Monitoring

✔ Liver Function Tests: Gefitinib can cause liver toxicity, so monitor liver enzymes regularly (especially in the first few months).
✔ Lung Function Monitoring: Be aware of any breathing issues like cough or shortness of breath.
✔ Skin Checks: Regularly check for skin rashes or dryness.
✔ Eye Care: If you experience eye irritation, consider using artificial tears.

4. Lifestyle Tips

✔ Avoid grapefruit juice, which can increase Gefitinib levels and the risk of side effects.
✔ Quit smoking (if applicable), as smoking can reduce the effectiveness of Gefitinib.
✔ Stay hydrated to manage side effects like diarrhea and prevent dehydration.
✔ Eat a balanced diet rich in fruits, vegetables, and protein to help maintain energy and strength.

5. When to Contact Your Doctor 🚨

❌ Shortness of breath, persistent cough, or fever (possible signs of Interstitial Lung Disease, ILD).
❌ Yellowing of the skin or eyes (sign of liver problems).
❌ Severe diarrhea or dehydration.
❌ Unusual skin rashes, blisters, or sores that do not improve.

Key Takeaways

✔ Take once daily, with or without food.
✔ Monitor liver function, lung health, and skin regularly.
✔ Stay hydrated, avoid grapefruit, and use sun protection.
✔ Report severe side effects like breathing problems or liver issues immediately.