Tazemetostat
Indications
Tazemetostat is used for:
Epithelial Sarcoma
Adult Dose
Epithelial Sarcoma
Indicated for metastatic or locally advanced epithelioid sarcoma not eligible for complete resection
800 mg PO BID; continue until disease progression or unacceptable toxicity
Hepatic impairment
Mild (total bilirubin >1-1.5 times ULN or AST > ULN): No dosage adjustment necessary
Moderate-to-severe (total bilirubin >1.5 times ULN): Not studied
Child Dose
Epithelioid Sarcoma
Indicated for metastatic or locally advanced epithelioid sarcoma not eligible for complete resection in adults and adolescents aged ?16 years
<16 years: Safety and efficacy not established
>16 years: 800 mg PO BID; continue until disease progression or unacceptable toxicity
Renal Dose
Renal impairment
Mild-to-severe or end-stage renal disease: No dosage adjustment necessary
Administration
Take with or without food
Swallow tablets whole
Contra Indications
Precautions
May increase the risk of developing secondary malignancies, including T-cell lymphoblastic lymphoma, myelodysplastic syndrome, and acute myeloid leukemia
Can cause fetal harm; advise patients of potential risk to a fetus and to use effective nonhormonal contraception
Pregnancy-Lactation
Pregnancy
Based on findings from animal studies and its mechanism of action, fetal harm may occur when administered to pregnant women
No data available on use in pregnant women to inform a drug-associated risk
Advise pregnant women of the potential risk to a fetus
Verify pregnancy status of females of reproductive potential before use
Animal data
Administration of tazemetostat to pregnant rats and rabbits during organogenesis resulted in dose-dependent increases in skeletal developmental abnormalities in both species beginning at maternal exposures ~1.5 times the adult human dose at 800 mg BID
Contraception
Females of reproductive potential: Use effective nonhormonal contraception during treatment and for 6 months after the final dose; may render some hormonal contraceptives ineffective
Males with female partners of reproductive potential: Use effective contraception during treatment and for at least 3 months after the final dose
Lactation
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
Owing to the potential risk for serious adverse reactions from tazemetostat in the breastfed child, advise women not to breastfeed during treatment and for 1 week after the final dose
Interactions
Adverse Effects
Side effects of Tazemetostat :
Mechanism of Action
Enhancer of zeste homolog 2 (EZH2) inhibitor
Misregulated EZH2 enzyme activity results in poorly regulated genes that control cell proliferation