How long does it take for Enasidenib to be effective after long-term use?

According to the clinical instructions for Enasidenib, the recommended dose is 100 mg orally once a day, with or without food, until disease progression or unacceptable toxicity. For patients without disease progression or unacceptable toxicity, treat for at least 6 months to allow time for clinical response. For some patients, significant improvement may be seen within a few weeks of starting the drug; for other patients, it may take longer to see the effects of treatment.

The peak plasma concentration (Cmax) after a single 100 mg dose is 1.4 μg/ml [Coefficient of variation (CV%) is 50%] , and the steady-state peak plasma concentration (Cmax) after a daily 100 mg dose is 13.1 μg/ml (CV%) is 45%. The area under the concentration-time curve (AUC) of ensidipine increased approximately dose-proportionally from 50 mg (0.5 times the approved recommended dose) to 450 mg (4.5 times the approved recommended dose) daily. Steady-state plasma levels are achieved within 29 days after once-daily dosing. When administered once daily, the absolute bioavailability of ensidipine with an accumulation of approximately 10-fold and an oral dose of 100 mg is approximately 57%. After a single oral dose, the median time to Cmax (Tmax) is 4 hours.

Encidipine research medicine is not currently on the market in China, so it cannot be included in medical insurance. The price of ensidipine plain medicine when it is launched overseas is very high, and the price of each box may be around 30,000 yuan (the price may fluctuate due to the exchange rate). Currently, there are cheaper generic ensidipine drugs produced by other pharmaceutical companies overseas. For example, the price of Specification50mg*30 tablets produced by a Laos pharmaceutical factory may be more than 2,000 yuan per box (the price may fluctuate due to the exchange rate). Its pharmaceutical ingredients are basically the same as those of the original drugs sold abroad.