Endofree 2.5 mg is a nonsteroidal aromatase inhibitor designed for the first-line treatment of advanced or metastatic breast cancer in postmenopausal women, particularly in patients with hormone receptor-positive tumors or unknown receptor status. By selectively inhibiting estrogen biosynthesis, Endofree deprives estrogen-dependent breast cancer cells of the growth stimulus necessary for tumor progression. Its targeted mechanism allows for effective hormone therapy without significantly affecting adrenal corticosteroids, mineralocorticoids, or thyroid hormones.

রেজিস্টার্ড চিকিৎসকের পরামর্শ অনুযায়ী ঔষধ সেবন করুন

Therapeutic Class

Hormonal Chemotherapy

Indications

Endofree 2.5 mg is indicated for:

• Advanced or metastatic breast cancer in postmenopausal women

• Hormone receptor-positive or receptor status unknown cases

It is used as a first-line therapy and continued until tumor progression is observed.

Pharmacology

Endofree 2.5 mg is a potent aromatase inhibitor that blocks the conversion of androgens to estrogens by competitively binding to the heme group of the cytochrome P450 subunit of the aromatase enzyme. This leads to a significant reduction of serum estrone, estradiol, and estrone sulfate levels.

• Selective Action: Inhibits gonadal steroidogenesis without affecting adrenal steroid production

• Effect on Tumor Growth: Suppresses estrogen-dependent tumor growth

• Pharmacokinetics:

  • Rapid and complete absorption; absolute bioavailability ~99.9%

  • Plasma protein binding ~60%, mainly to albumin

  • Terminal elimination half-life ~2 days

  • Steady-state plasma levels reached in 2–6 weeks

Dosage & Administration

• Recommended Dose: 2.5 mg orally once daily, with or without food

• Duration: Continue until tumor progression

• Special Populations:

  • Elderly: No dose adjustment required

  • Mild to moderate hepatic impairment: No adjustment needed

  • Severe hepatic dysfunction: Dose reduced by 50% (2.5 mg every other day)

  • Renal impairment: No adjustment needed if creatinine clearance ≥10 ml/min

Drug Interactions

• Minimal clinically significant interactions observed with cimetidine or warfarin

• No notable effect on adrenal corticosteroid or thyroid hormone synthesis

  রেজিস্টার্ড চিকিৎসকের পরামর্শ অনুযায়ী ঔষধ সেবন করুন

Contraindications

• Known hypersensitivity to Endofree or other aromatase inhibitors

• Pregnancy and lactation

• Pre-menopausal women

• Severe hepatic dysfunction

Side Effects

Most adverse events are mild to moderate and reflect estrogen deprivation:

• Common: Hot flushes, musculoskeletal pain, arthralgia, fatigue, nausea, headache

• Less common: Dyspnea, peripheral edema, vomiting, chest pain, viral infections, dizziness, weight increase, pruritus

• Generally tolerable and rarely require treatment discontinuation

Precautions & Warnings

• Caution in patients with moderate hepatic dysfunction

• May cause fatigue and dizziness, affecting ability to operate machinery

• Dialysis: Endofree may be removed due to weak plasma protein binding

Overdose

• No specific antidote available

• Supportive care and monitoring recommended

• Gastric lavage or dialysis may be considered in severe cases

Pregnancy & Lactation

• Category D: Use is contraindicated during pregnancy

• Excretion in human milk unknown; nursing not recommended

Mode of Action

Endofree 2.5 mg inhibits aromatase, the enzyme converting adrenal androgens into estrogens. Suppression of estrogen levels reduces stimulation of estrogen-dependent breast cancer cells, limiting tumor growth. It does not significantly alter androgen levels or adrenal steroid synthesis.

• Achieves 78–95% reduction in estradiol, estrone, and estrone sulfate

• Maximum suppression occurs within 48–78 hours

• Provides highly selective and potent estrogen blockade in postmenopausal women

Storage

• Store below 30°C, away from light and moisture

• Keep out of reach of children.