In March 2017, it was approved by the National Medical Products Administration (NMPA) of China, becoming the first targeted drug approved for EGFRT790M mutation positive NSCLC patients in China. Axitinib has been included in the national medical insurance catalog.

1、 Basic information of drugs

1. Drug name: Axitinib (TAGRASSO)

2. Main ingredients: Axitinib (existing in the form of Axitinib mesylate salt)

3. Specifications and characteristics:

80mg: Tablets.

2、 Indications, usage and dosage

1. Indications: Used for the treatment of metastatic non-small cell lung cancer (NSCLC) patients confirmed by FDA approved testing to be positive for EGFRT790M mutation, and these patients experience disease progression after EGFRTKI treatment.

2. Usage and dosage:

(1) Recommended dosage: 80mg orally, once daily.

(2) Medication requirements: Can be taken with food or on an empty stomach.

(3) Dysphagia treatment: Put the pill into about 50mL of non carbonated water and stir until completely dispersed before taking it immediately or administering it through a nasogastric tube.

3、 Dose Adjustment Guidelines

1. Interstitial lung disease/pneumonia: permanently discontinue medication after diagnosis.

2. QTc interval prolongation:

QTc>500ms (at least 2 independent electrocardiograms): Suspend administration until QTc<481ms or return to baseline level and switch to 40mg once daily.

3. Symptoms of life-threatening arrhythmia: permanent discontinuation of medication.

4. Cardiomyopathy:

Asymptomatic LVEF decrease ≥ 10% and<50%: Suspend medication for up to 4 weeks, resume medication after returning to baseline, and permanently discontinue medication if not restored.

Symptomatic heart failure: permanent discontinuation of medication.

Other grade 3 or above adverse reactions: Suspend medication for up to 3 weeks. If the condition improves to grade 0-2, 80mg or 40mg once daily can be restored. If there is no improvement, the medication will be permanently discontinued.

4、 Key precautions

Omission treatment: Do not supplement the missed dose, take the next dose according to the original plan.

5、 Safety warnings and adverse reactions

1. Serious adverse reactions:

(1) Interstitial lung disease/pneumonia (incidence 3.3%, with 0.5% fatal).

(2) QTc interval prolongation (0.2% of patients had QTc>500ms, and 2.7% of patients had an increase of>60ms from baseline).

(3) Cardiomyopathy (with an incidence rate of 1.4%, of which 0.2% is fatal).

(4) Embryo fetal toxicity (animal experiments show teratogenic risk).

2. Common adverse reactions (incidence ≥ 25%):

Diarrhea (42%), rash (41%), dry skin (31%), and nail toxicity (25%).

6、 Medication for special populations

1. Pregnant women: Prohibited, may cause fetal damage.

2. Breastfeeding period: Breastfeeding is prohibited during the medication period and within 2 weeks after the last administration.

3. Population of childbearing age:

Women: Effective contraceptive measures should be taken during treatment and 6 weeks after the last dose.

Men: Effective contraceptive measures should be taken during the treatment period and 4 months after the last dose.

4. Liver and kidney dysfunction: Mild to moderate liver and kidney dysfunction requires dose adjustment, while severe liver and kidney dysfunction requires recommended dose adjustment.

7、 Drug interactions

1. Strong CYP3A inhibitors (such as clarithromycin): Avoid co administration and closely monitor toxicity reactions if no alternative is available.

2. Strong CYP3A inducers (such as rifampicin): Avoid co administration as it may lower the blood concentration of osimertinib.

3. Narrow therapeutic window drugs: Avoid co administration with sensitive substrates of CYP3A, BCRP, or CYP1A2 (such as fentanyl, cyclosporine).

8、 Storage and production information

Storage conditions: Store at room temperature of 25 ℃ (77 ℉), allowing short-term fluctuations of 15-30 ℃ (59-86 ℉).

Osimertinibinformation