Osimertinib AXTN-80 Osimertinib 80mg 30 TABLETS Approval No. 03 L 0953/23 Validity Date 22-3-2026

Osimertinib instructions

Product Name: Osimitib

Manufacturer: Alliance Pharmaceuticals

Chinese name: Osimertinib

English Name: Osimertinib

Drug approval number: 03 L 0953/23

【Summary】

Osimertinib is a new type of EGFR-TKI, and its irreversible binding to certain EGFR mutants (T790M, L858R, and exon 19 deletion) is about 9 times lower than that of the wild type. After oral administration of osimertinib, two pharmacologically active metabolites (AZ7550 and AZ5104, accounting for about 10% of the parent compound) were found in plasma, and their inhibitory characteristics were similar to those of osimertinib. The potency of AZ7550 is similar to that of osimertinib, while AZ5104 has stronger activity against EGFR exon 19 deletion and T790M mutations (about 8 times) and wild type (about 15 times). In vitro experiments have shown that at clinical concentrations, osimertinib can also inhibit the activity of HER2, HER3, HER4, ACK1, and BLK.

【Indications】

Osimertinib is indicated for the treatment of adult patients with locally advanced or metastatic non-small cell lung cancer (NSCLC) who have disease progression during or after prior epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKI) treatment and who have been tested positive for EGFR T790M mutation.

【Specification】

80mg/tablet 30 tablets/box

【Storage】

Store at 20°C to 25°C (68°C to 77°F); short-distance transport is permitted at a temperature range of 15 to 30°C (59–86°F).

【Usage and Dosage】

The recommended dose of osimertinib is 80 mg daily until disease progression or unacceptable toxicity.

If you miss a dose of osimertinib, you should take a make-up dose of osimertinib unless the next dose is within 12 hours.

Osimertinib should be taken at the same time each day, with or without food.

Dosage Considerations

The medication may be suspended or reduced based on the safety and tolerability of the individual patient. If a reduction is required, the dose should be reduced to 40 mg once daily.

【Contraindications】

Hypersensitivity to the active ingredients or any of the excipients.

Osimertinib should not be taken with St. John's wort (see [Drug Interactions]).

【Adverse Reactions】

The most common adverse reactions (≥20%) were diarrhea (42%), rash (41%), dry skin (31%), nail toxicity (25%), and fatigue.

【Warnings and Precautions】

1. Interstitial lung disease (ILD)

Severe, life-threatening, or fatal interstitial lung disease (ILD) or ILD-like adverse reactions (such as non-infectious pneumonia) have been observed in patients using osimertinib. Carefully examine patients with acute onset and/or unexplained exacerbation of pulmonary symptoms (dyspnea, cough, fever) to rule out ILD. While looking for the cause of these symptoms, osimertinib should be suspended. If ILD is confirmed, osimertinib should be discontinued and necessary treatment measures should be taken.

2. QTc interval prolongation

QTc interval prolongation has occurred in patients taking osimertinib. QTc interval prolongation may lead to an increased risk of ventricular arrhythmias (e.g., torsade de pointes) or sudden death. If possible, osimertinib should be avoided in patients with congenital long QT syndrome. Patients with congestive heart failure, electrolyte abnormalities, or taking medications known to prolong the QTc interval should undergo regular electrocardiogram (ECG) and electrolyte monitoring. Patients with a QTc interval >500ms on at least two independent ECGs should temporarily withhold osimertinib until the QTc interval is resolved.

3. Changes in myocardial contractility For patients with known cardiovascular risks and conditions that may affect LVEF, cardiac function monitoring, including LVEF measurement at baseline and during medication, should be considered. For patients who experience symptoms and signs related to cardiac events during osimertinib treatment, cardiac monitoring including LVEF measurement should be considered.

4. Effects on the Ability to Drive and Use Machines Osimertinib has no effect or only a slight effect on the ability to drive and use machines.

[Use of osimertinib in pregnant and lactating women]

Contraception for men and women

Women of childbearing age should avoid pregnancy while taking osimertinib. Such patients should continue to use effective contraceptive measures for the following period after completing osimertinib treatment: at least 2 months for women and at least 4 months for men. The risk of decreased exposure to hormonal contraceptives cannot be ruled out after taking osimertinib concomitantly.

Pregnancy

There is no data on the use of osimertinib in pregnant women, or the data are very limited. Animal studies suggest that osimertinib is reproductively toxic (embryo-lethality, embryonic growth retardation, neonatal death). Based on the mechanism of action and preclinical data, osimertinib may cause fetal harm when used by pregnant women. Osimertinib should not be used during pregnancy unless the patient's clinical condition requires treatment with osimertinib.

breast-feeding

It is not known whether osimertinib or its metabolites are excreted in human milk. In addition, there is currently insufficient information to indicate that osimertinib or its metabolites are excreted in animal milk. However, osimertinib and its metabolites have been detected in suckling fetuses and have adverse effects on fetal growth and survival. Therefore, it cannot be ruled out that osimertinib may affect the nursing infant. Therefore, breastfeeding should be discontinued during treatment with osimertinib.

Fertility

There are currently no data on the effects of osimertinib on human fertility. Results from animal studies suggest that osimertinib has effects on the reproductive organs of both females and males and may impair fertility.