Pralsetinib

pralsetinib, as a novel selective RET inhibitor, provides a new treatment option for various cancer patients caused by RET gene mutations. Its high selectivity and specificity enable drugs to inhibit cancer cell proliferation while minimizing their impact on normal cells, thereby improving the safety and effectiveness of treatment.

Pralsetinib has good overall safety, but may also cause some adverse reactions such as rash, difficulty breathing, fatigue, loss of appetite, etc. These reactions are mostly tolerable and relieved after discontinuation or dose adjustment.

1.Main components

Pralsetinib

2.Adapt to the population

pralsetinib is suitable for FDA approved testing that confirms the presence of RET fusion positive in metastatic non-small cell lung cancer (NSCLC), as well as advanced or metastatic thyroid cancer with RET fusion positive that requires systemic treatment and is difficult to treat with radioactive iodine (if radioactive iodine is applicable).

3.Medication for special populations

3.1Pregnant women and lactation period

Pregnant women taking this medication may cause damage to the fetus, and it is necessary to inform them of the potential risks to the fetus. It is recommended that lactating women do not breastfeed during the treatment period and for one week after the last dose.

3.2Patients with reproductive ability

It is recommended that women with reproductive ability take effective non hormonal contraceptives during the treatment period of Pralsetinib and within 2 weeks after the last dose; It is recommended that male patients with female partners with reproductive ability take effective contraceptive measures during the treatment period of Pralsetinib and within one week after the last dose.

3.3Geriatric Use

There is no significant difference, use under the guidance of a doctor.

3.4Pediatric Use

The safety and efficacy have been confirmed in children aged 12 and above with RET fusion positive thyroid cancer, and children need to use it under the guidance of a doctor.

3.5Patients with liver dysfunction

Mild liver function impairment patients do not require dose adjustment and have not been studied in patients with moderate to severe liver function impairment.

4.Drug overdose

Drug overdose is not yet clear.

5.Drug storage

Pralsetinib should be stored at room temperature of 20-25 ° C and should be kept away from moisture.

6.Pharmacokinetics

The median time (Tmax) to reach peak concentration after a single dose of Pralsetinib 60mg to 600mg is 2 to 4 hours. The average (± standard deviation) plasma elimination half-life (T ^ 2) of a single dose of Pralsetinib is 15.7 hours (9.8), and the multiple doses of Pralsetinib are 20 hours.

from FDA，2024.03