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

Side Effects

Side effects of Tazemetostat :

Mode of Action

Enhancer of zeste homolog 2 (EZH2) inhibitor Misregulated EZH2 enzyme activity results in poorly regulated genes that control cell proliferation