Repotrectinib is the third pan solid tumor therapy after La Rotinib and Entrotinib, providing new hope for ROS1 positive NSCLC patients.

1、 Drug name

1. Common name: Repotrectinib

2. Product Name: AUGTYRO ™

2、 Indications

Used for the treatment of locally advanced or metastatic ROS1 positive non-small cell lung cancer (NSCLC) in adults.

3、 Specifications and characteristics

1. Capsules: 40mg/capsule

2. Appearance: Capsule.

4、 Main components

1. Active ingredient: Riptinib (ROS1/TRK kinase inhibitor)

2. Accessories: Microcrystalline cellulose, sodium dodecyl sulfate, cross-linked carboxymethyl cellulose sodium, colloidal silica (core); Gelatin, titanium dioxide (capsule shell); Cordyceps, FD&C Blue No.2 Aluminum Lake (Printing Ink).

5、 Usage and dosage

1. Recommended dosage:

Initial dose: 160mg orally, once daily, for 14 consecutive days.

Maintenance dose: Increase to 160mg twice daily (with an interval of about 12 hours) after 14 days, with or without meals.

2. Omission or vomiting: skip this dose and take the next dose at the original scheduled time.

6、 Dose adjustment

1. Central nervous system reactions (such as dizziness, ataxia):

Intolerable grade 2 or 3: Suspend medication and reduce dosage after returning to ≤ grade 1.

Level 4: Permanent discontinuation of medication.

2. Interstitial lung disease/pneumonia: If suspected, medication will be temporarily suspended; if diagnosed, medication will be permanently discontinued.

3. Hepatotoxicity (ALT/AST>3 times ULN with elevated bilirubin): permanently discontinued.

7、 Medication precautions

1. Medication time: taken daily at a fixed time without significant interaction with food.

2. Capsule administration: Swallow the whole capsule, do not open, chew or dissolve.

3. Drug interactions:

Avoid using strong/medium acting CYP3A inhibitors (such as ketoconazole) or inducers (such as rifampicin) in combination.

Avoid using P-gp inhibitors (such as cyclosporine) or hormonal contraceptives in combination.

8、 Medication for special populations

Pregnant women: May cause fetal malformation, non hormonal contraceptive measures should be used until 2 months after the last dose.

Breastfeeding period: Breastfeeding is prohibited during the treatment period and within 10 days after the last dose.

Liver dysfunction: Moderate to severe patients need to adjust the dosage.

Children: Safety has not been established.

9、 Adverse reactions

1. Common (≥ 20%): Dizziness (64%), taste disorders (50%), peripheral neuropathy (47%), constipation (37%), and difficulty breathing (30%).

2. Serious adverse reactions:

Interstitial lung disease (2.9%), hepatotoxicity (ALT elevation of 35%), and fractures (2.3%).

10、 Contraindications

No clear contraindications (according to the instructions).

11、 Drug interactions

1. CYP3A4 substrate: Riptinib reduces its blood drug concentration (such as a 69% decrease in AUC of midazolam).

2. Gastric acid regulator: Avoid using it in combination with proton pump inhibitors.

12、 Storage method

Store at 20 ° C-25 ° C and allow short-term exposure to 15 ° C-30 ° C.

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