AXIMED

AXIMED

Axitinib 5mg
Net Qty- 28 Tablets
Self-Life- 2 Years

Aximed (Axitinib 5mg) is an oral targeted therapy used primarily in the treatment of advanced kidney cancer. It belongs to the class of tyrosine kinase inhibitors (TKIs) and works by blocking the blood supply that tumors need to grow.

USE

✅ Aximed (Axitinib) is primarily used to treat advanced kidney cancer. It works by blocking specific proteins that help cancer cells grow new blood vessels (angiogenesis).

🔹 Main Indications

1. Advanced Renal Cell Carcinoma (RCC)

  • Approved for patients with advanced or metastatic RCC, especially:
    • After failure of one prior systemic therapy, such as sunitinib, sorafenib, or immunotherapy.
    • Can be used alone or in combination with checkpoint inhibitors:
      • Axitinib + Pembrolizumab (Keytruda)
      • Axitinib + Avelumab (Bavencio)

These combinations are now first-line options for many patients with metastatic RCC.

2. Off-label / Investigational Uses (in clinical trials)

  • Other solid tumors (e.g., thyroid cancer, hepatocellular carcinoma) — ongoing trials are exploring Axitinib’s role in these.
  • Combinations with other targeted therapies or immunotherapies.

📌 Summary

ConditionUse
Advanced RCC (2nd line)Monotherapy after prior systemic therapy
Advanced RCC (1st line)In combination with immunotherapy
Other cancersInvestigational, in clinical trial settings

Key Benefits

🌟 Aximed (Axitinib) is a powerful targeted therapy that works by blocking blood vessel growth in tumors. It is mainly used to treat advanced renal cell carcinoma (RCC) and has shown strong benefits, especially in patients who have failed previous treatments or in combination with immunotherapy.

✅ Delays Cancer Progression

  • Improves Progression-Free Survival (PFS) in advanced RCC patients.
  • Shown to slow tumor growth and delay worsening of disease.

✅ Effective in Combination Therapies

  • When combined with pembrolizumab or avelumab, it:
    • Significantly increases overall survival (OS)
    • Improves tumor response rates
  • Now considered a first-line treatment option in many patients with metastatic RCC.

✅ Targets Tumor Blood Supply

  • Axitinib inhibits VEGF receptors (VEGFR-1, 2, and 3), blocking angiogenesis (formation of blood vessels that feed tumors).
  • This helps starve the tumor and limit its growth and spread.

✅ Oral Administration

  • Convenient oral tablet form—taken at home.
  • Helps reduce hospital visits compared to IV treatments.

✅ Well Studied in RCC

Demonstrated effectiveness in several major clinical trials like:

  • AXIS trial (as second-line therapy)
  • JAVELIN Renal 101 (in combo with Avelumab)
  • KEYNOTE-426 (in combo with Pembrolizumab)

✅ Tolerable and Adjustable

  • Dosing can be adjusted based on side effects.
  • Patients can often continue therapy long term if tolerated.

✅ Provides Options After Treatment Failure

Offers continued hope for patients whose disease progressed on other therapies like sunitinib or immunotherapy.

Mechanism
of Action

🧬 Aximed (Axitinib) is a tyrosine kinase inhibitor (TKI) that primarily targets the vascular endothelial growth factor receptors (VEGFR), which are involved in the formation of new blood vessels (angiogenesis). By blocking these receptors, Axitinib helps to inhibit the tumor’s ability to grow and spread through the blood vessels.

Here’s how Axitinib works in detail:

🔹 VEGFR Inhibition

  • VEGF (Vascular Endothelial Growth Factor) is a key protein involved in the formation of new blood vessels (angiogenesis), which tumors need to grow and spread.
  • Axitinib specifically blocks VEGFR-1, VEGFR-2, and VEGFR-3, which are receptors on the surface of endothelial cells (cells lining blood vessels).
  • Blocking VEGFRs prevents the tumor from forming new blood vessels, starving the tumor and limiting its growth and ability to metastasize.

🔹 Inhibition of Angiogenesis

  • Tumors rely on angiogenesis to supply them with oxygen and nutrients through the blood vessels.
  • By inhibiting VEGFRs, Axitinib prevents angiogenesis, essentially cutting off the blood supply to the tumor, causing it to shrink or stop growing.

🔹 Impact on Other Signaling Pathways

  • Axitinib also affects other pathways involved in tumor cell proliferation and metastasis.
  • Although its main target is VEGFR, Axitinib may also influence other tyrosine kinases involved in cancer cell growth and survival, leading to further inhibition of tumor progression.

🔹 Selective and Potent

  • Axitinib is a potent inhibitor of VEGFR, meaning it is effective at lower doses compared to other TKIs.
  • It is considered more selective for VEGFR than other tyrosine kinase inhibitors like sunitinib and sorafenib, making it a more targeted approach in blocking angiogenesis.

💡 Summary of Action:

  • Blocks VEGFR-1, VEGFR-2, and VEGFR-3
  • Inhibits angiogenesis (new blood vessel formation)
  • Limits tumor growth and metastasis

Dosage and Administration

💊 Aximed (Axitinib) is typically administered orally in the form of tablets. The dosage may be adjusted based on the patient’s response and tolerance to the medication.

🔹 Recommended Dosage

  • Initial Dose:

5 mg orally twice a day (morning and evening).

  • Adjustments:
    • The dose can be increased to 7 mg twice daily or 10 mg twice daily based on tolerance and the patient’s side effect profile.
    • If side effects are severe, the dose can be reduced. The minimum dose should not go below 2 mg twice a day.

🔹 Administration Guidelines

  • Take orally with or without food.
  • Swallow the tablets whole—do not crush, chew, or split them.
  • Take at the same time every day to help remember the dose.

🔹 Dose Modifications for Toxicity

If the patient experiences significant side effects, such as hypertension, diarrhea, fatigue, or neutropenia, the dose may need to be adjusted:

  • Severe toxicity:
    • Temporarily interrupt treatment until symptoms improve.
    • Reduce dose after the patient recovers.
  • Hypertension:
    • Monitor regularly—control hypertension with antihypertensive agents before continuing therapy.

🔹 Renal Impairment

  • Mild to Moderate Renal Impairment (CrCl 30-89 mL/min):

No dosage adjustment needed.

  • Severe Renal Impairment (CrCl <30 mL/min):

Use with caution—dosage adjustments may be necessary depending on the patient’s tolerance.

🔹 Hepatic Impairment

  • Mild Hepatic Impairment (Child-Pugh Class A):

No adjustment needed.

  • Moderate Hepatic Impairment (Child-Pugh Class B):

Start at a lower dose, typically 2 mg twice a day.

  • Severe Hepatic Impairment (Child-Pugh Class C):

Avoid using Axitinib unless the potential benefits outweigh the risks.

🔹 Missed Dose

If a dose is missed, take it as soon as remembered unless it is almost time for the next dose.

  • Do not double dose to make up for a missed dose.

📋 Summary of Dosing

  • Initial dose: 5 mg twice a day
  • Titration: Increase to 7 mg or 10 mg twice a day as tolerated
  • Dose reductions: In case of significant side effects, reduce dose or temporarily discontinue.

Common Side Effects

⚠️ Aximed (Axitinib), like many targeted cancer therapies, can cause side effects due to its action on blood vessels and other cell signaling pathways. Most side effects are manageable, especially with early detection and supportive care.

Here’s a breakdown of the most commonly reported side effects:

🔹 Hypertension (High Blood Pressure)

  • Most common side effect
  • May occur early in treatment
  • Requires regular blood pressure monitoring
  • Often managed with antihypertensive medications

🔹 Diarrhea

  • Frequently reported; can be mild to severe
  • Important to stay hydrated
  • Antidiarrheal medications (e.g., loperamide) may be needed

🔹 Fatigue

  • Persistent tiredness or weakness
  • Often improves with rest and energy-conservation strategies

🔹 Dysphonia (Voice Changes)

  • Hoarseness or voice becoming softer/deeper
  • Usually not harmful but can be bothersome

🔹 Hand-Foot Syndrome (Palmar-Plantar Erythrodysesthesia)

  • Redness, swelling, or pain on the palms or soles
  • Preventative measures: avoid friction, heat, and harsh soaps

🔹 Decreased Appetite / Weight Loss

  • May impact nutrition and energy
  • Nutritional support and high-calorie meals can help

🔹 Nausea and Vomiting

  • Usually mild
  • Can be managed with anti-nausea medications if needed

🔹 Hypothyroidism

  • Axitinib can lower thyroid hormone levels
  • Requires monitoring of TSH and possible thyroid hormone replacement

🔹 Stomatitis / Mouth Sores

  • Painful ulcers in the mouth
  • Soft diet, good oral hygiene, and mouth rinses can help

🔹 Proteinuria (Protein in the Urine)

  • Can indicate kidney effects
  • Routine urine testing is recommended during treatment

📋 Other Possible Side Effects:

  • Rash or skin dryness
  • Constipation
  • Cough
  • Elevated liver enzymes (monitor with blood tests)

🧪 When to Call Your Doctor

  • Seek medical advice if you experience:
  • Severe diarrhea
  • Uncontrolled high blood pressure
  • Signs of blood clots (e.g., chest pain, leg swelling)
  • Persistent fatigue or bleeding

Monitoring

🔍 Proper monitoring is crucial for ensuring treatment safety and effectiveness during Aximed (Axitinib) therapy. Here’s a comprehensive list of what clinicians typically monitor during treatment:

📌 Blood Pressure

  • Frequency: At baseline, then weekly for the first few weeks, and regularly thereafter.
  • Why: Axitinib commonly causes hypertension, which may appear early in treatment.
  • Management: May require antihypertensives; dose adjustments may be needed if BP is uncontrolled.

📌 Thyroid Function (TSH)

  • Frequency: At baseline, then periodically during treatment.
  • Why: Hypothyroidism is common and may develop during therapy.
  • Management: Treated with thyroid hormone replacement if needed.

📌 Renal Function / Urinalysis

  • Frequency: At baseline, then periodically.
  • Why: Axitinib can cause proteinuria and affect kidney function.
  • Tests: Serum creatinine, urine protein.

📌 Liver Function Tests (LFTs)

  • Frequency: Baseline and periodic monitoring.
  • Why: Liver enzyme elevations and hepatotoxicity can occur.
  • Tests: ALT, AST, bilirubin.

📌 Complete Blood Count (CBC)

  • Frequency: At baseline, then regularly during treatment.
  • Why: To detect anemia, neutropenia, or thrombocytopenia.

📌 Electrolytes

  • Frequency: Periodic.
  • Why: Diarrhea and reduced appetite can cause electrolyte imbalances.

📌 ECG (if indicated)

  • Why: In patients with a history of heart disease or on other QT-prolonging drugs.
  • Not required for all but may be done based on risk factors.

📌 Weight and Nutritional Status

  • Frequency: Ongoing.
  • Why: Weight loss and reduced appetite are common.
  • Action: May need nutritionist support if weight loss is significant.

📝 Summary Table

ParameterFrequencyPurpose
Blood PressureBaseline, weekly, ongoingDetect/manage hypertension
Thyroid Function (TSH)Baseline, periodicMonitor for hypothyroidism
Liver Function TestsBaseline, periodicDetect hepatotoxicity
Renal Function / UrinalysisBaseline, periodicDetect proteinuria/kidney issues
CBCBaseline, periodicMonitor for cytopenias
ElectrolytesPeriodicDetect imbalances
Weight & NutritionOngoingAssess for weight loss/malnutrition

Precautions

⚠️ Aximed (Axitinib) is a potent cancer therapy, and while effective, it requires careful use and monitoring to reduce the risk of serious side effects. Below are key precautions that patients and healthcare providers should be aware of:

🔹 Hypertension

  • Common and can be severe.
  • Monitor blood pressure frequently, especially early in treatment.
  • Initiate or adjust antihypertensive therapy as needed.
  • Interrupt or reduce Axitinib if blood pressure is not controlled.

🔹 Arterial and Venous Thromboembolic Events

  • Includes myocardial infarction, stroke, deep vein thrombosis (DVT), and pulmonary embolism (PE).
  • Use with caution in patients with a history of cardiovascular disease.
  • Discontinue if serious clotting events occur.

🔹 Hemorrhagic Events

  • Bleeding (e.g., gastrointestinal or cerebral) may occur.
  • Not recommended in patients with recent hemorrhage or active bleeding.
  • Caution in patients on anticoagulants.

🔹 Gastrointestinal Perforation or Fistula

  • Rare but potentially fatal.
  • Caution in patients with history of GI disorders, such as ulcers or diverticulitis.

🔹 Impaired Wound Healing

  • Discontinue Axitinib at least 2 days before major surgery.
  • Resume only after adequate wound healing has occurred.

🔹 Thyroid Dysfunction

  • Hypothyroidism is common.
  • Monitor TSH levels before and during treatment.
  • Treat with thyroid hormone replacement if needed.

🔹 Proteinuria

  • Monitor for protein in the urine periodically.
  • Consider dose reduction or interruption if proteinuria is severe.

🔹 Hepatotoxicity

  • Elevated liver enzymes (ALT, AST) can occur.
  • Monitor LFTs regularly.
  • Discontinue in case of severe liver impairment.

🔹 Pregnancy and Breastfeeding

  • Contraindicated during pregnancy – may cause fetal harm.
  • Use effective contraception during treatment and for at least 1 week after the last dose.
  • Avoid breastfeeding during treatment and for 2 weeks after the last dose.

🔹 Use in Renal or Hepatic Impairment

  • No adjustment needed for mild-to-moderate renal impairment.
  • Reduce dose in moderate hepatic impairment (Child-Pugh B).
  • Avoid in severe hepatic impairment unless benefits outweigh risks.

Drug Interactions

💊 Aximed (Axitinib) is metabolized mainly by the liver enzyme CYP3A4, so its blood levels can be significantly altered by drugs that affect this pathway. Some interactions can increase toxicity, while others can reduce effectiveness.

🔹 CYP3A4 Inhibitors – Can Increase Axitinib Levels

These drugs slow down the metabolism of Axitinib, leading to higher blood levels and a greater risk of side effects.

Common examples:

  • Ketoconazole
  • Itraconazole
  • Clarithromycin
  • Ritonavir
  • Grapefruit juice (natural CYP3A4 inhibitor)

⚠️ What to do:

  • Avoid if possible, or reduce Axitinib dose under close monitoring.

🔹 CYP3A4 Inducers – Can Decrease Axitinib Levels

These drugs speed up the metabolism of Axitinib, potentially making it less effective.

Common examples:

  • Rifampin
  • Carbamazepine
  • Phenytoin
  • St. John’s Wort

⚠️ What to do:

  • Avoid use; they may make Axitinib ineffective.
  • Consider alternative medications or adjust Axitinib dose if absolutely necessary.

🔹 Antihypertensive Drugs

  • Axitinib may raise blood pressure; patients are often on antihypertensives.
  • Monitor BP closely when starting or adjusting either therapy.
  • No direct pharmacokinetic interaction, but therapeutic interaction is important.

🔹 Anticoagulants and Antiplatelets

  • Increased risk of bleeding when used with:
    • Warfarin
    • DOACs (e.g., apixaban, rivaroxaban)
    • Aspirin / Clopidogrel
  • Monitor closely for signs of bleeding; use caution if combined.

🔹 Other TKIs or VEGF Inhibitors

  • Co-administration with other angiogenesis inhibitors (e.g., bevacizumab) may increase toxicity (e.g., hypertension, bleeding, proteinuria).
  • Avoid combining unless in a controlled clinical setting.

🔹 Immunotherapy Agents (Checkpoint Inhibitors)

  • Pembrolizumab, Avelumab, and others are often used in combination.
  • No significant pharmacokinetic interaction, but monitor for additive toxicity (e.g., fatigue, liver enzymes, diarrhea).

✅ Patient Advice

  • Always inform your doctor about all medications, supplements, or herbal products.
  • Avoid grapefruit juice and St. John’s Wort.
  • Be alert for signs of toxicity when starting new medications.

Clinical Effectiveness

✅ Aximed (Axitinib) is a highly selective tyrosine kinase inhibitor (TKI) that targets vascular endothelial growth factor receptors (VEGFR-1, -2, and -3), making it effective in tumors that rely heavily on angiogenesis (blood vessel formation).

🔬 Indications and Tumor Types

Axitinib has shown proven clinical benefits in:

  • Advanced renal cell carcinoma (RCC) – especially after failure of one prior systemic therapy.
  • Being studied or used in combination for other cancers, such as:
    • Hepatocellular carcinoma (HCC)
    • Thyroid cancer
    • Non-small cell lung cancer (NSCLC) (in clinical trials)

📊 Key Clinical Trials

🔹 AXIS Trial (Phase III)

  • Compared Axitinib vs. Sorafenib in metastatic RCC after one prior therapy.
  • Results:
    • Progression-Free Survival (PFS):
    • Axitinib: 6.7 months vs. Sorafenib: 4.7 months
    • Objective Response Rate (ORR):
    • Axitinib: 19% vs. Sorafenib: 9%
    • Conclusion: Axitinib significantly improved PFS and tumor response in pre-treated RCC.

🔹 JAVELIN Renal 101 (Combo: Avelumab + Axitinib)

  • First-line treatment for advanced RCC.
  • PFS benefit: The combination significantly improved PFS over sunitinib (13.8 vs. 8.4 months).
  • Implication: Axitinib is now widely used in combination immunotherapy regimens.

📈 Summary of Effectiveness

OutcomeFindings with Axitinib
Progression-Free SurvivalImproved vs. comparator TKIs
Tumor ResponseHigher response rate (especially in RCC)
Overall SurvivalModestly improved, especially in combos
Combination BenefitExcellent synergy with immunotherapy

💡 Clinical Relevance

  • Axitinib offers a targeted approach with manageable toxicity.
  • Particularly beneficial for patients resistant to first-line VEGF inhibitors.
  • As part of combo therapy, it’s becoming a standard first-line option in advanced RCC.

Tips for Patients

💡 Aximed (Axitinib) is an effective oral cancer medication, but proper use and awareness can significantly improve both treatment success and quality of life. Here are key tips to help patients navigate their therapy safely:

📋 Take Your Medication Correctly

  • Take Axitinib twice a day, approximately 12 hours apart.
  • Swallow the tablet whole with water; do not crush, chew, or split.
  • Can be taken with or without food.
  • If you miss a dose, take it as soon as you remember unless it’s less than 6 hours before your next dose — do not double up.

🍊 Avoid Grapefruit Products

  • Grapefruit juice can raise Axitinib levels and increase side effects.
  • Check with your doctor before taking any new foods or supplements.

💓 Monitor Your Blood Pressure

  • Axitinib can cause or worsen high blood pressure.
  • Check BP at home regularly, especially when starting.
  • Report any headaches, dizziness, or chest discomfort.

💧 Stay Hydrated & Manage Diarrhea

  • Drink plenty of fluids to avoid dehydration.
  • Keep anti-diarrheal medicine (like loperamide) handy in case of loose stools.
  • Report persistent diarrhea to your doctor — it can become serious.

🦶 Watch for Hand-Foot Syndrome

  • Look for redness, tenderness, or peeling on palms/soles.
  • Moisturize daily, avoid hot water, and wear soft shoes.
  • Tell your care team early — dose adjustments may help.

🧪 Keep Up with Lab Tests

  • Regular blood tests are needed to monitor:
    • Liver and kidney function
    • Thyroid levels
    • Protein in urine
  • Never skip scheduled appointments or bloodwork.

🛌 Rest When Needed

  • Fatigue is common — listen to your body.
  • Balance light activity with rest, and ask for support when needed.

🚫 Pregnancy & Breastfeeding Warning

  • Do not use if pregnant or breastfeeding – may harm the baby.
  • Use effective birth control during treatment and for at least 1 week after the last dose.

🩸 Report Concerning Symptoms Immediately

  • Unusual bleeding or bruising
  • Chest pain, shortness of breath
  • Severe abdominal pain or black stools
  • Vision changes, voice hoarseness

📞 Communicate with Your Healthcare Team

  • Always report side effects, even if they seem minor.
  • Don’t hesitate to ask for help managing symptoms or adjusting your routine.