Erlonat 100 — Erlotinib 100 mg

Erlonat 100 is manufactured in the form of film-coated tablets for oral use, containing a strictly calibrated dose of components:

• Active Compound: Erlotinib hydrochloride — equivalent to 100 mg of free base erlotinib in each tablet.
• Excipients: Lactose monohydrate, microcrystalline cellulose, sodium starch glycolate, magnesium stearate, sodium lauryl sulfate; film-coating components: hypromellose, titanium dioxide, macrogol.
• Appearance: Round, film-coated tablets contained in a plastic bottle containing 30 tablets, packed in an original cardboard box.

Pharmacodynamics: Erlotinib is a potent inhibitor of HER1/EGFR growth factor receptor tyrosine kinase. It effectively suppresses ligand-induced receptor phosphorylation, blocking the further transmission of cascade signals responsible for the proliferation, angiogenesis, and metastasis of malignancies.

Pharmacokinetics: Following oral administration, erlotinib is well absorbed, achieving a bioavailability of approximately 59% (food intake significantly increases this index). Peak plasma concentration is reached within 4 hours. Plasma protein binding is about 95%. It is metabolized in the liver predominantly via the CYP3A4 isoenzyme. The elimination half-life is about 36 hours, excreted mainly as metabolites in feces.

Erlonat 100 is used strictly as prescribed by a specialized professional (oncologist) for the therapy of the following conditions:

• 🔹 Non-Small Cell Lung Cancer (NSCLC): Locally advanced or metastatic lung cancer with activating EGFR mutations as first-line therapy, as well as for maintenance treatment or upon progression following chemotherapy.
• 🔹 Pancreatic Cancer: Locally advanced, unresectable, or metastatic pancreatic cancer as first-line therapy (in combination with gemcitabine).

Dose calculation and monitoring of therapy are carried out by medical personnel based on the patient's diagnosis. Alteration of treatment regimens without an oncologist is strictly prohibited:

• Recommended Dosage: In non-small cell lung cancer, the standard daily dose is 150 mg. In pancreatic cancer, the drug is prescribed at 100 mg daily in combination with gemcitabine.
• Method of Administration: Tablets are taken orally whole, at least 1 hour before or 2 hours after meals, swallowed with a sufficient amount of water. Tablets must not be broken or chewed.
• Dosing Regimen: The medication is taken once daily at the same fixed time. Upon development of toxicity, the dose is stepped down by 50 mg.
• Duration of Treatment: Therapy is continued long-term as long as clinical benefit is maintained or until signs of unacceptable toxicity and disease progression occur.

The use of Erlonat 100 tablets is strictly prohibited in the presence of the following contraindications or physiological conditions:

• ⛔ Hypersensitivity: Individual intolerance to erlotinib or any excipient component of the tablet.
• ⛔ Pregnancy and Lactation: The drug possesses embryotoxic and teratogenic potential, capable of causing fetal death; breastfeeding must be discontinued during treatment.
• ⛔ Severe Hepatic and Renal Impairment: Severe organ insufficiency (due to the lack of sufficient clinical experience in this patient population).
• ⛔ Pediatric Patients: Contraindicated in patients under 18 years of age, as the safety and efficacy profiles for children have not been established.

Erlotinib is actively metabolized by the hepatic cytochrome P450 system, leading to significant drug interactions:

• ❌ CYP3A4 Inhibitors: Ketoconazole, clarithromycin, and grapefruit juice slow down erlotinib metabolism, sharply increasing its concentration and systemic toxicity.
• ❌ CYP3A4 Inducers: Rifampicin, phenytoin, carbamazepine, and St. John's wort preparations accelerate erlotinib degradation, substantially decreasing its therapeutic efficacy.
• ⚠️ Gastric pH-Altering Drugs: Proton pump inhibitors (omeprazole) and antacids reduce the solubility and absorption of erlotinib. They should be taken with a time interval.

The drug possesses a pronounced toxic effect on the developing embryo and poses a hazard to the female reproductive system:

• Risks to the Fetus: Erlotinib therapy during pregnancy may lead to spontaneous abortion or severe fetal developmental anomalies. Pregnancy is strictly contraindicated in women of childbearing potential.
• Contraception for Women and Men: Patients of both sexes must utilize reliable barrier or hormonal methods of contraception throughout the course of treatment and for at least 1–2 months following the last dose.
• Testing: Prior to initiating the therapy course, the treating physician must completely rule out pregnancy using a highly sensitive laboratory test.

Therapy with Erlonat 100 is frequently accompanied by the development of characteristic adverse reactions requiring medical monitoring:

• 🟢 Dermatological Manifestations (Very Common): Skin rash (acneiform dermatitis), pruritus, dry skin, fissures, alopecia, paronychia (inflammation of the nail fold).
• 🟡 Gastrointestinal Tract: Diarrhea (can lead to dehydration), nausea, vomiting, stomatitis, anorexia, abdominal pain.
• 🟡 Respiratory System: Cough, dyspnea; in rare cases, development of severe interstitial lung disease (ILD) may occur.
• 🟠 Laboratory Parameters: Elevated bilirubin levels, transient increase in liver transaminase activity (ALT, AST).
• ⚠️ Urgent Medical Attention: Upon sudden onset or worsening of cough, dyspnea, fever, or development of severe persistent diarrhea, a doctor must be contacted immediately.

Ingestion of doses significantly exceeding therapeutic ones results in a sharp amplification of dose-dependent adverse effects:

• Main Manifestations: Overdose presents with severe persistent diarrhea, pronounced generalized skin rashes, and a substantial transient increase in liver transaminases.
• First Aid: Urgent discontinuation of the drug, administration of sorbents, and immediate admission to a specialized medical hospital.
• Treatment: No specific antidote to erlotinib exists. Symptomatic measures aimed at stopping diarrhea and restoring fluid-electrolyte balance are performed.

Adherence to the regulated storage conditions of the tablets ensures the preservation of its medicinal properties and compositional stability:

• 🌡️ Temperature Regimen: Store in a dry, dark, moisture-protected place in the original packaging at a temperature strictly not exceeding 30°C.
• 📦 Environmental Protection: Protect from direct sunlight and high humidity; tablets must remain inside the tightly closed factory bottle.
• 👶 Accessibility: The medication is a potent substance and must be stored in a secure location, completely excluding access by children or pets.
• ⏳ Special Instructions: Do not use the drug after the expiration date. Disposal of unused tablets must be carried out strictly in accordance with medical waste regulations.