Fulvenat — Fulvestrant Injection 250 mg/vial Cold chain · Storage +2…+8 °C

Fulvenat is supplied as a clear, viscous oily solution for intramuscular injection. Each single-dose vial contains:

• Active Ingredient: Fulvestrant — 250 mg per 5 mL of solution.
• Excipient Core: Ethanol 96%, benzyl alcohol, benzyl benzoate, and castor oil (blended to maintain compound solubility and ensure controlled sustained release from the muscle depot).

Pharmacodynamics: Fulvestrant is a reversible, competitive estrogen receptor (ER) antagonist with an affinity comparable to estradiol. It blocks ER signaling pathways and downregulates ER protein levels in tumor cells without exhibiting partial agonist activity. This leads to complete blockade of estrogen-driven gene transcription and tumor growth suppression.

Pharmacokinetics: Following intramuscular administration, fulvestrant is slowly absorbed from the injection depot site, attaining peak plasma concentration (Cmax) within 5 to 7 days. Sustained therapeutic levels are maintained throughout the 28-day dosing interval. It is extensively metabolized in the liver via CYP3A4 enzymes and excreted predominantly in feces (greater than 90%), with less than 1% eliminated by the kidneys.

Fulvenat 250 mg is clinically indicated for postmenopausal women under the following conditions:

• 🔹 Metastatic Breast Cancer: Treatment of estrogen-receptor-positive (ER+) locally advanced or metastatic breast cancer in postmenopausal women with disease relapse on or after adjuvant antiestrogen therapy.
• 🔹 First-Line Endocrine Therapy: Monotherapy for postmenopausal women with ER-positive locally advanced or metastatic breast cancer not previously treated with endocrine therapy.

Fulvenat is intended strictly for deep intramuscular administration into the gluteal area. The injection should be administered slowly over 1 to 2 minutes:

• Standard Dosing: The recommended dose is 500 mg (two 250 mg/5 mL vials). Administered as two consecutive 5 mL injections, one into each gluteal muscle (left and right).
• Dosing Schedule: Recommended as a loading dose regimen on Days 1, 15, and 29, followed by maintenance dosing of 500 mg once every 28 days thereafter.
• Special Populations: Dose adjustments are not required for patients with mild to moderate renal or hepatic impairment. Caution and clinical monitoring are advised in severe cases.

The administration of Fulvenat is strictly contraindicated in the following cases:

• ⛔ Hypersensitivity: Known allergy or severe hypersensitivity to fulvestrant, castor oil, or any excipient in the formulation.
• ⛔ Pregnancy and Lactation: Strictly contraindicated during pregnancy and breastfeeding due to potential fetal harm and developmental toxicity.
• ⛔ Severe Hepatic Impairment: Not recommended for use in patients with severe hepatic impairment (Child-Pugh Class C) due to lack of safety data.

Fulvestrant undergoes hepatic metabolism involving CYP3A4 pathways, but clinical drug interaction potential remains low:

• ⚠️ CYP3A4 Inhibitors and Inducers: Co-administration with CYP3A4 inhibitors or inducers does not require dose adjustments of fulvestrant, as clearance changes are not clinically significant.
• ⚠️ Anticoagulant Therapy: Due to intramuscular route of administration, exercise caution when administering to patients with bleeding diatheses, thrombocytopenia, or those receiving anticoagulant medications to avoid deep tissue hematomas.

Fulvenat is specified for postmenopausal female patients:

• Contraceptive Measures: Females of reproductive potential (if postmenopausal status is unconfirmed) must use effective contraception during treatment and for at least 2 years after receiving the final dose of Fulvenat. Discontinue immediately if pregnancy occurs.

Common and potential adverse reactions associated with Fulvenat therapy include:

• 🔴 Injection Site Reactions: Localized pain, inflammation, induration, hematoma, or erythema at the gluteal injection site.
• 🟡 Gastrointestinal and Hepatic: Nausea, vomiting, diarrhea, loss of appetite, and elevated hepatic enzymes (ALT, AST, ALP).
• 🟠 Systemic and Vascular: Hot flashes, fatigue, asthenia, headache, skin rash, and musculoskeletal pain (arthralgia, myalgia).

Accidental acute overdose in humans is rare due to controlled intramuscular administration by healthcare professionals:

• Symptoms: Exceeding recommended doses may exacerbate known pharmacological side effect profiles.
• Management: No specific antidote exists. In case of overdose, supportive and symptomatic treatment should be provided.

Storage parameter requirements to preserve formulation integrity:

• 🌡️ Temperature Controls: Store and transport refrigerated at 2 °C to 8 °C. Do not freeze. Keep the vial in the original outer carton to protect from direct light exposure.
• 👶 Safety Precautions: Keep out of the reach and sight of children. Do not use solution if cracked or containing visible particulate matter.
• ⏳ Shelf Life: 2 years. Do not use past the expiration date printed on the package.

Authentic Fulvenat 250 mg/vial manufactured by Natco Pharma Ltd. features multi-level anti-counterfeiting elements:

• 🛡️ Security Hologram (Natco Hologram): A reflective holographic security seal with micro-engraved NATCO text is placed on the top opening flap seam of the carton as a tamper-evident mechanism.
• 🔒 Packaging Identity: High-quality white matte outer box. The lower right portion features two prominent intersecting geometric bands in purple and magenta (pink) tones over a gray accent. The official blue-and-red oval NATCO logo is printed on the bottom left.
• 🔍 Typography and Branding: The brand name "Fulvenat" is printed in a stylized purple typeface with a long-descender "f" and a registered trademark symbol ®. Descriptive text like "Fulvestrant Injection", "250 mg/vial", "For Intramuscular use only", and "Single dose vial" are clearly rendered in black font.
• 🔢 Factory Production Stamp: The side panel displays factory-stamped details including Batch Number (Batch No.), Manufacturing Date (Mfg. Date), Expiration Date (Exp. Date), and Maximum Retail Price (M.R.P.). All stamped data must correspond exactly to the inner glass vial label.