伊瑞可 吉非替尼片, Gefitinib Tablets, Jifeitini Pian, 0.25g*10 Tablets

Drug Name
Gefitinib Tablets
Jifeitini Pian
吉非替尼片

Composition
Each tablet contains gefitinib as the active ingredient.

Description
Brown film-coated tablets, white or off-white in color after removal of the coating.

Indications
This product is indicated as monotherapy for the first-line treatment of locally advanced or metastatic non-small cell lung cancer (NSCLC) with epidermal growth factor receptor (EGFR) gene-sensitive mutations (see Precautions).
Results from two large randomized controlled clinical trials showed that gefitinib in combination with platinum-based chemotherapy as first-line treatment for locally advanced or metastatic NSCLC did not demonstrate clinical benefit. Therefore, such combination regimens are not recommended as first-line therapy.
This product may be used as monotherapy for the treatment of locally advanced or metastatic NSCLC that has failed after at least one prior chemotherapy regimen. This product is not recommended for patients with EGFR wild-type NSCLC.

Dosage and Administration
The recommended dose is 250 mg (1 tablet) once daily, administered orally, with or without food. If a dose is missed, the patient should take it as soon as remembered. If the next dose is due within 12 hours, the missed dose should be skipped. Patients must not double the dose to compensate for a missed dose.
When the entire tablet cannot be administered (e.g., patients who can only swallow liquids), the tablet may be dispersed in water. Place the tablet in half a glass of drinking water (non-carbonated), stir without crushing until fully dispersed (approximately 15 minutes), and drink immediately. Rinse the glass with half a glass of water and drink the rinse. The dispersion may also be administered via a nasogastric tube.

Dosage Adjustment
No dosage adjustment is required based on age, weight, gender, ethnicity, renal function, or moderate-to-severe hepatic impairment due to liver metastases.
If patients experience intolerable diarrhea or skin adverse reactions, treatment may be temporarily suspended (for up to 14 days), after which the daily dose of 250 mg may be resumed (see Adverse Reactions).

Use in Children
No safety and efficacy data are available for gefitinib in pediatric or adolescent patients; therefore, use in this population is not recommended.

Adverse Reactions
The most common (≥20%) adverse drug reactions (ADRs) are diarrhea and skin reactions (including rash, acne, dry skin, and pruritus), typically occurring within the first month of treatment and usually reversible. Severe ADRs (Grade 3 or 4 per NCI CTCAE criteria) occur in approximately 10% of patients. Treatment discontinuation due to ADRs occurs in approximately 3% of patients.

Contraindications
Hypersensitivity to the active substance or any excipient in the product.

Precautions
When considering gefitinib for first-line treatment of advanced or metastatic NSCLC, EGFR mutation testing of tumor tissue is recommended for all patients. If tumor specimens are not evaluable, circulating tumor DNA (ctDNA) from blood (plasma) may be used.
Only validated assays with demonstrated reliability and sensitivity for detecting EGFR mutations in tumor tissue or ctDNA should be used to avoid false-negative or false-positive results.

Use in Pregnancy and Lactation:
Pregnancy: No data are available on gefitinib use in pregnant women. In rats, administration of gefitinib at maternally toxic doses during organogenesis increased the incidence of incomplete ossification. In rabbits, fetal weight reduction was observed. No malformations were noted in rats, and malformations in rabbits were observed only at maternally toxic doses. Women of childbearing potential should be advised to avoid pregnancy during gefitinib treatment.
Lactation: Women should be advised to discontinue breastfeeding during gefitinib treatment. No data are available on gefitinib excretion in human milk. However, in lactating rats, gefitinib and certain metabolites were extensively secreted into milk after oral administration of 5 mg/kg (0.2 times the clinical dose on a body surface area basis). Administration of gefitinib at 20 mg/kg/day (0.7 times the clinical dose on a body surface area basis) during pregnancy and lactation in rats reduced pup survival.

Geriatric Use
No specific studies have been conducted in elderly patients.

Pharmacological Action
Epidermal Growth Factor Receptor (EGFR) is expressed in both normal and tumor cells and plays a critical role in cell growth and differentiation. EGFR mutations (exon 19 deletion and exon 21 L858R mutation) in NSCLC cells promote tumor growth, inhibit apoptosis, increase production of vascular growth factors, and enhance tumor metastasis. Gefitinib is a reversible inhibitor of wild-type and certain mutant EGFRs, inhibiting EGFR tyrosine kinase autophosphorylation and downstream signaling, thereby blocking EGFR-dependent cell proliferation. Gefitinib has greater affinity for mutant EGFRs (exon 19 deletion and exon 21 L858R mutation) than for wild-type EGFRs. At clinically relevant concentrations, gefitinib may also inhibit IGF- and PDGF-mediated signaling; its inhibitory effects on other tyrosine kinases are not well defined.

Storage
Store below 30°C.

Specifications
0.25 g.

Packaging
0.25 g × 10 tablets/box.

Expiration
24 months.