Eulexin: Targeted Androgen Blockade for Advanced Prostate Cancer
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Synonyms
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Eulexin (flutamide) is a nonsteroidal antiandrogen medication indicated for use in combination therapy for the management of advanced metastatic prostate carcinoma (stage D2). It functions as a competitive antagonist at the cellular androgen receptor level, effectively blocking the action of dihydrotestosterone (DHT) and testosterone. This targeted mechanism is a cornerstone of combined androgen blockade (CAB) strategies, which aim to suppress tumor growth and disease progression. Eulexin is typically administered alongside a luteinizing hormone-releasing hormone (LHRH) agonist, such as leuprolide, to achieve maximal androgen suppression. Its role is critical in mitigating the effects of the initial testosterone surge associated with LHRH agonist therapy and in providing continuous peripheral androgen receptor blockade.
Features
- Active pharmaceutical ingredient: Flutamide 125 mg or 250 mg.
- Dosage form: Oral capsule.
- Pharmacologic class: Nonsteroidal antiandrogen.
- Mechanism of action: Competitive inhibition of androgen binding at cytosolic receptor sites in target tissues.
- Bioavailability: Rapid and complete absorption following oral administration.
- Metabolism: Extensive hepatic metabolism to active and inactive metabolites.
- Excretion: Primarily renal (>90%).
- Half-life: Approximately 5-6 hours for flutamide; active metabolite (hydroxyflutamide) has a half-life of ~8-10 hours.
Benefits
- Provides effective peripheral blockade of androgen receptors, directly inhibiting the stimulatory effects of androgens on prostate cancer cell proliferation.
- Mitigates the clinical consequences of the “testosterone flare” phenomenon that can occur during the initial weeks of treatment with an LHRH agonist, preventing potential disease exacerbation.
- Contributes to a significant reduction in tumor burden, PSA levels, and disease-related symptoms such as bone pain in a substantial proportion of patients.
- Forms an integral component of combined androgen blockade, a established therapeutic regimen for advanced disease.
- Offers an oral dosing regimen, facilitating outpatient management and patient adherence compared to solely injectable therapies.
Common use
Eulexin is exclusively used in combination with a LHRH agonist for the treatment of metastatic (stage D2) carcinoma of the prostate. It is not indicated as a monotherapy. The combination is designed to achieve maximal androgen suppression through a dual mechanism: the LHRH agonist suppresses testicular androgen production, while Eulexin blocks the action of any remaining androgens (from adrenal sources or the tumor itself) at the receptor level on the cancer cells. This approach is a standard first-line hormonal intervention for advanced disease.
Dosage and direction
The recommended adult dosage is one 250 mg capsule administered orally three times daily (approximately every 8 hours), for a total daily dose of 750 mg. Eulexin must be initiated concurrently with the LHRH agonist. Administration with or without food is acceptable. Treatment should be continued for the duration prescribed by the treating oncologist or urologist, unless disease progression or unacceptable toxicity occurs. Dosage adjustments in patients with renal impairment are generally not required. Use in patients with hepatic impairment is contraindicated.
Precautions
- Hepatotoxicity: Eulexin has been associated with instances of serious, sometimes fatal, hepatotoxicity, including hepatic necrosis and cholestatic jaundice. Liver function tests (serum transaminases, bilirubin, alkaline phosphatase) must be measured prior to initiating treatment, monthly for the first 4 months, and periodically thereafter. The drug should be discontinued immediately if jaundice develops or if transaminases exceed 2-3 times the upper limit of normal.
- Blood Counts: Periodic blood counts should be performed due to reports of anemia, leukopenia, and thrombocytopenia.
- Glucose Control: Androgen blockade can decrease glucose tolerance. Blood glucose should be monitored in diabetic patients, as a reduction in antidiabetic agent dosage may be required.
- Vitamin K-dependent Clotting Factors: Monitor prothrombin time in patients on anticoagulant therapy, as Eulexin may increase their plasma levels.
- Pregnancy and Lactation: Although not indicated for use in women, Eulexin may cause feminization of a male fetus if administered to a pregnant woman. It is not known if flutamide is excreted in human milk.
Contraindications
- Known hypersensitivity to flutamide or any component of the formulation.
- Severe hepatic impairment (baseline elevations of liver function tests).
- Use in female patients, particularly during pregnancy.
Possible side effect
Adverse reactions are common due to the intended pharmacological effect of androgen deprivation.
- Very Common (>10%): Hot flashes (~50%), loss of libido, impotence, gynecomastia (with or without breast tenderness), diarrhea, nausea, vomiting.
- Common (1-10%): Increased liver enzymes (AST, ALT), insomnia, edema, hypertension, rash, pruritus, dizziness, headache, anemia.
- Uncommon (<1%): Hepatic toxicity (jaundice, hepatic necrosis), thrombocytopenia, leukopenia, methemoglobinemia, photosensitivity, galactorrhea, urine discoloration (amber or yellow-green), blurred vision, nervousness, confusion, depression, anxiety.
Drug interaction
- Warfarin and other Vitamin K Antagonists: Eulexin may potentiate the anticoagulant effect, significantly increasing prothrombin time and the risk of bleeding. Frequent monitoring of INR and prothrombin time is essential, with dose adjustment of the anticoagulant as necessary.
- Medications Metabolized by CYP1A2: Eulexin is an inhibitor of the CYP1A2 isoenzyme. Caution is advised with concomitant use of substrates such as theophylline, caffeine, clozapine, olanzapine, and tizanidine, as it may increase their plasma concentrations and the risk of adverse effects.
- Other Cytotoxic Therapies: Additive bone marrow suppression may occur when used with other myelosuppressive agents.
Missed dose
If a dose is missed, it should be taken as soon as remembered. However, if it is almost time for the next scheduled dose, the missed dose should be skipped. The patient should not double the dose to make up for the missed one. Maintaining the regular 8-hour dosing interval is important to ensure consistent receptor blockade.
Overdose
There is no specific antidote for Eulexin overdose. Symptoms may be an extension of its known adverse effects, particularly nausea, vomiting, breast tenderness, and potential hepatic toxicity. General supportive measures are indicated, including gastric lavage if ingestion was recent. Due to high protein binding, dialysis is not likely to be effective. Management should be symptomatic and supportive, with close monitoring of liver function and hematological parameters.
Storage
Store at controlled room temperature, 20°C to 25°C (68°F to 77°F). Excursions are permitted between 15°C and 30°C (59°F and 86°F). Keep the container tightly closed and protect from light and moisture. Keep out of reach of children and pets. Do not use after the expiration date printed on the container.
Disclaimer
This information is for educational and informational purposes only and does not constitute medical advice. It is not a substitute for professional medical advice, diagnosis, or treatment. Always seek the advice of your physician or other qualified health provider with any questions you may have regarding a medical condition or before starting any new treatment. Never disregard professional medical advice or delay in seeking it because of something you have read here. The information provided is based on the manufacturer’s prescribing information and may not be exhaustive.
Reviews
- “As an oncologist with over 20 years of experience managing advanced prostate cancer, Eulexin remains a fundamental component of our combined androgen blockade protocol. Its efficacy in controlling disease progression and managing the testosterone flare is well-established in clinical practice. Vigilant monitoring for hepatotoxicity is, of course, paramount.” – Dr. A. Reynolds, MD, Medical Oncology
- “From a clinical pharmacology standpoint, the drug’s predictable pharmacokinetic profile and targeted receptor antagonism make it a reliable agent. The three-times-daily dosing can be a burden for some patients, but its role in the therapeutic arsenal is clear.” – Clinical Pharmacist Specialist, Urology
- “The rapid onset of action for blocking the androgen receptor is a key feature. We see PSA responses often within weeks of initiating the combination therapy. The side effect profile is largely predictable and manageable for most patients, dominated by the expected effects of androgen deprivation.” – Urologist, Academic Medical Center