Tazemetostat

Tazemetostat is the world's first EZH2 inhibitor developed and launched by EZsolution Biosciences Inc., a Swedish pharmaceutical company based in the United States. The drug specification produced by Lucius is 200mg * 56pills.

EZH2 is an important histone methyltransferase that plays a crucial role in the occurrence and development of tumors.

Tazemetostat is an orally administered small molecule targeted inhibitor that selectively inhibits EZH2 enzyme activity. It has high selectivity and affinity, and can specifically act on EZH2 enzyme, thereby inhibiting its catalytic activity.

1.Main components

Tazemetostat

2.Adapt to the population

Tazemetostat is a Broad-spectrum antitumor agents.

3.Medication for special populations

3.1Pregnancy

Based on findings from animal studies and its mechanism of action, Tazemetostat can cause fetal harm when administered to pregnant women. There are no available data on Tazemetostat use in pregnant women to inform the drug-associated risk. Advise pregnant women of the potential risk to  a fetus.

3.2Lactation

There are no animal or human data on the presence of tazemetostat in human milk or on its effects on the  breastfed child or milk production. Because of the potential risk for serious adverse reactions from Tazemetostat  in the breastfed child, advise women not to breastfeed during treatment with Tazemetostat and for one week after  the final dose.

3.3Females and Males of Reproductive Potential

Females

Advise females of reproductive potential to use effective non-hormonal contraception during treatment with Tazemetostat and for 6 months after the final dose. Tazemetostat can render some hormonal contraceptives  ineffective.  

Males 

Advise males with female partners of reproductive potential to use effective contraception during treatment with  Tazemetostat and for at least 3 months after the final dose.

3.4Pediatric Use

The safety and effectiveness of Tazemetostat have been established in pediatric patients aged 16 years and older (adolescents) with metastatic or locally advanced epithelioid sarcoma. The safety and effectiveness of Tazemetostat in pediatric patients aged less than 16 years have not been  established.

3.5Geriatric Use

Clinical studies of Tazemetostat did not include sufficient numbers of patients with epithelioid sarcoma or relapsed or refractory follicular lymphoma aged 65 and over to determine whether they respond differently from younger subjects.

3.6Renal Impairment

No dose adjustment of Tazemetostat is recommended for patients with mild to severe renal impairment or end  stage renal disease.

3.7Hepatic Impairment

 No dose adjustment of Tazemetostat is recommended for patients with mild hepatic impairment (total bilirubin > 1 to 1.5 times upper limit of normal [ULN] or AST > ULN). Tazemetostat has not been studied in patients  with moderate (total bilirubin > 1.5 to 3 times ULN) or severe (total bilirubin > 3 times ULN) hepatic  impairment.

4.Drug overdose

Drug overdose is not yet clear.

5.Drug storage

Do not store above 30°C (86°F).

6.Pharmacokinetics

The mean absolute oral bioavailability of tazemetostat is approximately 33%. The median time to reach the  peak plasma concentration of tazemetostat is 1 to 2 hours.  

from FDA，2024.08