repotrectinib

Repotrectinib is the third pan-solid tumor therapy after larotinib and entrectinib, providing new good news for patients with ROS1-positive NSCLC.

1. Drug name

1. Generic name: Repotrectinib (Repotrectinib)

2. Trade name: AUGTYRO™

2. Indications

It is used to treat adults with locally advanced or metastatic ROS1-positive non-small cell lung cancer (NSCLC).

3. Specifications and properties of

1. Capsules: 40mg/capsule.

2. Characteristics: capsule.

IV. Main ingredient

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

2. Excipients: microcrystalline cellulose, sodium lauryl sulfate, croscarmellose sodium, colloidal silica (tablet core); gelatin, titanium dioxide (capsule shell); shellac, FD&C Blue No. 2 aluminum lake (printing ink).

5. Usage and dosage

1. Recommended dose :

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

Maintenance dose: After 14 days, increase to 160mg twice a day (about 12 hours apart), with or without food.

2. Missing a dose or vomiting : Skip the dose and take the next dose at the originally planned time.

VI. Dose adjustment

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

Intolerable grade 2 or 3: suspend the medication, and reduce the dose after returning to ≤ grade 1.

Level 4: Permanent discontinuation.

2. Interstitial lung disease/pneumonia : Suspend if suspected, permanently discontinue if confirmed.

3. Hepatotoxicity (ALT/AST>3 times ULN with elevated bilirubin): Permanent discontinuation.

7. Medication precautions

1. Medication time : Take it at a fixed time every day, and there is no significant interaction with food.

2. Taking in capsules: Swallow the capsule whole and do not open, chew or dissolve it.

3. Drug interactions :

Avoid the combined use of strong/moderate CYP3A inhibitors (such as ketoconazole) or inducers (such as rifampicin).

Avoid combined use with P-gp inhibitors (such as cyclosporine) or hormonal contraceptives.

8. Use of in special groups

Pregnant women: may cause fetal malformation, so non-hormonal contraceptive measures need to be used until 2 months after the last dose.

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

Hepatic insufficiency : Moderate to severe patients need to adjust the dose.

Children : Safety has not been established.

9. Adverse reactions

1. Common (≥20%) : dizziness (64%), dysgeusia (50%), peripheral neuropathy (47%), constipation (37%), dyspnea (30%).

2. Serious adverse reactions :

Interstitial lung disease (2.9%), liver toxicity (ALT increased by 35%), fracture (2.3%).

10. Contraindications

There are no clear contraindications (according to the instructions).

11. Drug interactions

1. CYP3A4 substrate : Reprotinib can reduce its plasma concentration (such as midazolam AUC decreased by 69%).

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

12. Storage method

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