The mechanism and precautions of Ripotinib

Introduction: Ripotinib (Augtyro) is a tyrosine kinase inhibitor targeting ROS1, TRK and ALK. It effectively binds to the active kinase conformation to avoid spatial interference from various clinical drug-resistant mutations, thereby inhibiting the proliferation of tumor cells. The U.S. Food and Drug Administration has approved the next-generation tyrosine kinase inhibitor reprotinib for the treatment of locally advanced or metastatic ROS1-positive non-small cell lung cancer.

Mechanism of action

has a low molecular weight macrocyclic structure, can target ROS1, TRKA-C and ALK with high selectivity, and has high potency against these targets. It can significantly enhance the activity against intracranial tumors, especially showing good efficacy in patients with ROS1-positive non-small cell lung cancer (NSCLC).

Usage and Dosage

The recommended dose of repotinib is 160 mg, taken orally once a day for 14 days, then increased to 160 mg twice a day, and continued until disease progression or unacceptable toxicity.

Notes

1. Central nervous system adverse reactions: Ripotinib can cause central nervous system adverse reactions such as dizziness, ataxia and cognitive impairment.

2. Liver toxicity: Alanine aminotransferase (ALT) and aspartate aminotransferase (AST) may increase during treatment.

3. Myalgia and elevated creatine phosphokinase: Ripotinib may cause myalgia with or without elevated creatine phosphokinase (CPK).

4. Hyperuricemia: It may cause hyperuricemia, and serum uric acid levels need to be monitored regularly.

5. Bone fracture: Ripotinib may increase the risk of bone fracture.

6. Embryotoxicity: Ripotinib may cause harm to the fetus. It is recommended that women and men of childbearing potential take effective contraceptive measures during treatment.

7. Interstitial lung disease or non-infectious pneumonia: During medication, pay attention to monitor whether the patient develops pulmonary symptoms suggesting new or worsening interstitial lung disease or non-infectious pneumonia. Suspected patients should stop taking Ripotinib immediately. After the diagnosis is confirmed, Ripotinib needs to be permanently stopped.

Common side effects and treatment measures

The most common adverse reactions are dizziness, dysgeusia, peripheral neuropathy, constipation, dyspnea, ataxia, fatigue, cognitive impairment and muscle weakness. You may feel dizzy during treatment, and it is recommended to avoid drinking large amounts of caffeinated beverages, including coffee, tea, and soda, and to avoid sudden movements, such as carefully sitting up from a lying position. If you feel dizzy when you stand up, hold on to a chair or table for balance and stand up slowly.