Getinib250 mg

Getinib is an epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor indicated for:

• First-line treatment (FDA-approved, established use): Metastatic non-small cell lung cancer (NSCLC) whose tumors have EGFR exon 19 deletions or exon 21 (L858R) substitution mutations, as detected by an FDA-approved or validated test. Mutation testing is required before starting Getinib, as efficacy depends on mutation status.
• Guideline-supported use: Continued therapy in patients who have already responded to or are being treated with Getinib for EGFR mutation-positive NSCLC, per oncology treatment guidelines (e.g., NCCN).

Getinib is not indicated for NSCLC without confirmed EGFR exon 19 deletion or exon 21 L858R mutations, as efficacy has not been demonstrated in this setting.

Each film-coated tablet contains Gefitinib 250 mg as the active ingredient, along with pharmaceutically inert excipients such as lactose monohydrate, microcrystalline cellulose, croscarmellose sodium, povidone, sodium lauryl sulfate, magnesium stearate, and a film-coating system.

Getinib is an orally active, small-molecule inhibitor of the epidermal growth factor receptor (EGFR) tyrosine kinase, belonging to the class of targeted anticancer agents used in precision oncology. It is used to treat a genetically-defined subset of non-small cell lung cancer (NSCLC).

Getinib is supplied as a 250 mg film-coated tablet for oral administration, taken once daily.

Getinib belongs to the epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors, a subclass of targeted anticancer (antineoplastic) agents.

Gefitinib reversibly inhibits the kinase activity of wild-type and certain activating mutant forms of the epidermal growth factor receptor (EGFR), including exon 19 deletions and the exon 21 L858R substitution. By blocking EGFR autophosphorylation, Gefitinib interrupts downstream signal transduction pathways (including RAS/RAF/MEK/ERK and PI3K/AKT) that drive tumor cell proliferation, survival, and angiogenesis in EGFR mutation-positive tumors.

Pharmacokinetics: Gefitinib is slowly absorbed after oral administration, with peak plasma concentrations reached in 3-7 hours. Absorption is affected by gastric pH (higher pH reduces absorption). It is extensively metabolized in the liver, primarily by CYP3A4, with a mean terminal half-life of approximately 48 hours. Elimination is predominantly hepatic/fecal, with less than 4% excreted renally.

Getinib tablets should be taken at approximately the same time each day, swallowed whole with water. If a patient cannot swallow tablets, they may be dispersed in non-carbonated water as described in Dosage and Administration, without crushing or chewing.

The following clinically significant interactions have been established with Getinib:

• Strong CYP3A4 inducers (e.g., rifampicin, phenytoin, carbamazepine, St. John's Wort): significantly decrease plasma concentrations of Getinib, potentially reducing efficacy. Avoid concomitant use where possible; if unavoidable, increase the Getinib dose to 500 mg once daily.
• Strong CYP3A4 inhibitors (e.g., itraconazole, ketoconazole, clarithromycin): increase plasma concentrations of Getinib, raising the risk of adverse reactions. Monitor closely for toxicity if co-administered.
• Drugs that increase gastric pH (proton pump inhibitors, H2-receptor antagonists, antacids): reduce absorption and plasma concentrations of Getinib, potentially reducing efficacy. Avoid concomitant proton pump inhibitors where possible; if H2-blockers or antacids are needed, dose Getinib away from these agents (e.g., take Getinib 6 hours before or after an H2-blocker dose).
• Warfarin and other vitamin K antagonists: co-administration has been associated with elevated International Normalized Ratio (INR) and bleeding events; monitor INR/prothrombin time regularly.

The most common adverse reactions (occurring in more than 20% of patients) with Getinib are skin reactions (such as rash, acne, dry skin) and diarrhea.

• Very common: diarrhea, rash, dry skin, nausea, vomiting, elevated liver enzymes (ALT/AST), stomatitis, decreased appetite.
• Common: pruritus, alopecia, conjunctivitis, blepharitis, paronychia, asthenia, fever, peripheral edema, dehydration, epistaxis, hematuria, proteinuria.
• Serious (see Precautions and Warnings for detail): interstitial lung disease, hepatotoxicity/hepatic failure, gastrointestinal perforation, severe or persistent diarrhea, bullous and exfoliative skin conditions, keratitis and corneal erosion, and rare cases of Stevens-Johnson syndrome/toxic epidermal necrolysis.

Pregnancy: Getinib can cause fetal harm based on its mechanism of action and findings in animal reproduction studies. Getinib should be avoided in pregnant women; if used during pregnancy, or if the patient becomes pregnant while taking Getinib, the patient should be informed of the potential risk to the fetus. Females of reproductive potential should use effective contraception during treatment and for a defined period (at least 2 weeks) after the final dose. Getinib should only be used in pregnancy if clearly needed and the potential benefit justifies the potential risk to the fetus; consult a physician.

Lactation: There is no data on the presence of Getinib in human milk or its effects on the breastfed infant. Because of the potential for serious adverse reactions in breastfed infants, women should be advised not to breastfeed during treatment with Getinib and for a period after the final dose; consult a physician.

The following require special caution or monitoring during treatment with Getinib:

• Interstitial lung disease (ILD): ILD, including cases with fatal outcome, has occurred in patients treated with Getinib. Getinib should be interrupted and the patient promptly investigated if new or worsening pulmonary symptoms (dyspnea, cough, fever) occur; Getinib should be permanently discontinued if ILD is confirmed.
• Hepatotoxicity: Elevations in liver transaminases and, rarely, hepatic failure (some fatal) have occurred. Periodic liver function testing is recommended; interrupt Getinib for significant liver enzyme elevation and discontinue permanently if severe hepatic impairment develops.
• Gastrointestinal perforation: Cases of GI perforation, some fatal, have been reported. Permanently discontinue Getinib in patients who develop GI perforation.
• Severe or persistent diarrhea: May require interruption of therapy and, in severe cases, dose reduction or discontinuation, with appropriate antidiarrheal treatment and fluid management.
• Ocular disorders: Corneal erosion, aberrant eyelash growth, and keratitis (a class effect of EGFR inhibitors) can occur; patients with symptoms of keratitis (eye inflammation, watering eyes, light sensitivity, blurred vision, eye pain) should be promptly referred for ophthalmologic evaluation.
• Bullous and exfoliative skin conditions: Discontinue or interrupt Getinib if severe or worsening skin reactions occur.
• Embryo-fetal toxicity: See Pregnancy and Lactation.
• Testing for EGFR exon 19 deletion or exon 21 L858R mutation status is required prior to initiating Getinib, as efficacy depends on mutation status.

There is no specific antidote for Getinib overdose. In case of suspected overdose, seek immediate medical attention or contact emergency services/a poison control center. Management should be supportive, including close observation for adverse reactions such as diarrhea and skin reactions, with appropriate symptomatic treatment as directed by a physician.

Store at room temperature (below 30°C), away from light and moisture. Keep out of reach of children.

Pediatric use: Safety and efficacy of Getinib have not been established in pediatric patients.

Geriatric use: No overall differences in safety or effectiveness have been observed between elderly and younger patients; no dose adjustment is required based on age alone, though age-related organ function decline should be considered.

Renal impairment: No dosage adjustment required (see Dosage and Administration).

Hepatic impairment: Close monitoring required in mild-to-moderate impairment; permanently discontinue in severe impairment (see Dosage and Administration).

Females and males of reproductive potential: Verify pregnancy status before starting Getinib; advise effective contraception during and after treatment (see Pregnancy and Lactation).

Getinib is continued once daily until disease progression or unacceptable toxicity occurs, as determined by the treating oncologist. There is no fixed maximum duration; treatment duration is individualized based on tumor response and tolerability, with regular clinical and radiological monitoring.

Epidermal Growth Factor Receptor (EGFR) Tyrosine Kinase Inhibitor; Targeted Antineoplastic Agent

Gefitinib selectively and reversibly binds to the intracellular tyrosine kinase domain of the epidermal growth factor receptor (EGFR), including tumors harboring activating EGFR exon 19 deletion or exon 21 L858R substitution mutations. By inhibiting autophosphorylation of EGFR, Gefitinib blocks downstream oncogenic signaling cascades responsible for tumor cell proliferation, survival, invasion, and angiogenesis, leading to inhibition of tumor growth in EGFR mutation-positive non-small cell lung cancer.

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The safety and efficacy of Getinib have not been established in pediatric patients. Getinib is not indicated for use in children or adolescents, and no pediatric dosing recommendations exist.