Introduction
Repotrex 40 mg (Repotrectinib) is a next-generation, potent tyrosine kinase inhibitor (TKI) designed for precision oncology. Manufactured by Everest Pharmaceuticals Ltd. and supplied globally by Onco Solution, Repotrex is specifically engineered to target ROS1 and NTRK gene fusions. This medication is a life-saving therapy for patients with locally advanced or metastatic non-small cell lung cancer (NSCLC) and other solid tumors that have become resistant to earlier-generation inhibitors. Its unique molecular structure allows it to cross the blood-brain barrier, making it highly effective against brain metastases.
Indications
Repotrex 40 mg (Repotrectinib) is indicated for:
- ROS1-Positive NSCLC: Treatment of adult patients with locally advanced or metastatic ROS1-positive non-small cell lung cancer.
- NTRK-Positive Solid Tumors: Treatment of adult and pediatric patients (12 years and older) with solid tumors that have a Neurotrophic Tyrosine Receptor Kinase (NTRK) gene fusion, are metastatic, or where surgical removal is likely to result in severe complications.
Pharmacology
Repotrectinib, the active ingredient in Repotrex, is an inhibitor of proto-oncogene tyrosine-protein kinase ROS1 and tropomyosin receptor tyrosine kinases (TRKs) TRKA, TRKB, and TRKC. It works by binding to the ATP-binding site of the kinase, preventing the activation of downstream signaling pathways (like MAPK/ERK) that drive uncontrolled cell proliferation. Unlike older inhibitors, Repotrectinib is a “compact” macrocycle, allowing it to bypass common gatekeeper mutations (such as ROS1 G2032R) that cause drug resistance.
Dosage & Administration
Oral Administration for Adults and Pediatrics (12+):
- Initial Phase (Step-up Dosing): 160 mg (four 40 mg capsules) orally once daily for the first 14 days.
- Maintenance Phase: If the initial dose is well-tolerated, increase to 160 mg (four 40 mg capsules) twice daily.
- Administration: Swallow capsules whole with or without food. Do not open, crush, or chew.
- Missed Dose: If a dose is missed, take it as soon as remembered unless it is within 6 hours of the next dose.
Drug Interactions
- Strong/Moderate CYP3A Inhibitors: May increase Repotrectinib levels, increasing toxicity risk. Avoid co-administration.
- Strong/Moderate CYP3A Inducers: May decrease Repotrectinib levels, reducing clinical efficacy.
- Hormonal Contraceptives: Repotrex may render birth control pills or patches ineffective. Use non-hormonal methods.
- Grapefruit Products: Avoid grapefruit juice/products as they may interfere with drug metabolism.
Contraindications
- Hypersensitivity: Known hypersensitivity to Repotrectinib or any component of the capsule shell.
- Pregnancy: Categorized as a risk to fetal development.
Side Effects
Patients receiving Repotrex 40 mg may experience:
- Neurological: Dizziness (most common), ataxia, cognitive impairment (memory loss/confusion), and changes in taste (dysgeusia).
- Gastrointestinal: Constipation, nausea, and dry mouth.
- Respiratory: Dyspnea (shortness of breath) and cough.
- General: Fatigue, muscular weakness, and peripheral neuropathy (tingling/numbness).
- Metabolic: Increased blood uric acid levels (hyperuricemia).
Pregnancy & Lactation
- Pregnancy: Can cause fetal harm. Females of reproductive potential should use effective non-hormonal contraception during treatment and for 2 months after the last dose.
- Lactation: Advise patients not to breastfeed during treatment and for 10 days after the final dose.
Precautions & Warnings
- CNS Effects: Can cause significant dizziness and cognitive issues; patients should avoid driving if these symptoms occur.
- Interstitial Lung Disease (ILD): Monitor for new or worsening respiratory symptoms. Discontinue immediately if ILD/Pneumonitis is confirmed.
- Hepatotoxicity: Monitor liver function tests (ALT/AST) every 2 weeks during the first month.
- Myalgia & CPK: Monitor Creatine Phosphokinase (CPK) levels if the patient reports unexplained muscle pain or weakness.
Use in Special Populations
- Hepatic Impairment: No adjustment needed for mild impairment. Not recommended for moderate to severe liver disease.
- Pediatrics: Safety and efficacy are established for NTRK-positive tumors in children aged 12 and older.
Overdose Effects
Overdose may lead to severe CNS toxicity, dizziness, or gastrointestinal distress. Treatment is supportive, and patients should be monitored closely by an oncology team.
Storage
- Intact Capsules: Store at 20°C to 25°C (68°F to 77°F); excursions permitted between 15°C and 30°C.
- Handling: Keep in the original container to protect from light and moisture.
Supplier Information
Onco Solution is a leading global supplier of advanced oncology medications. We are committed to providing access to cutting-edge treatments like Repotrex 40 mg to patients and healthcare providers globally. Visit www.oncosolution.com for more information.
Manufacturer Information
Repotrex 40 mg is manufactured by Everest Pharmaceuticals Ltd., a premier pharmaceutical company in Bangladesh known for its expertise in manufacturing high-quality, targeted cancer therapies and specialty medicines.
