Difference between revisions of "Tazemetostat (Tazverik)"
Jump to navigation
Jump to search
(added package insert) |
|||
| Line 1: | Line 1: | ||
==Mechanism of action== | ==Mechanism of action== | ||
| − | From the [https://www.cancer.gov/publications/dictionaries/cancer-drug/def/tazemetostat NCI Drug Dictionary]: An orally available, small molecule selective and S-adenosyl methionine (SAM) competitive inhibitor of histone methyl transferase EZH2, with potential antineoplastic activity. Upon oral administration, E7438 selectively inhibits the activity of both wild-type and mutated forms of EZH2. Inhibition of EZH2 specifically prevents the methylation of histone H3 lysine 27 (H3K27). This decrease in histone methylation alters gene expression patterns associated with cancer pathways and results in decreased tumor cell proliferation in EZH2 mutated cancer cells. | + | From the [https://www.cancer.gov/publications/dictionaries/cancer-drug/def/tazemetostat NCI Drug Dictionary]: An orally available, small molecule selective and S-adenosyl methionine (SAM) competitive inhibitor of histone methyl transferase EZH2, with potential antineoplastic activity. Upon oral administration, E7438 selectively inhibits the activity of both wild-type and mutated forms of EZH2. Inhibition of EZH2 specifically prevents the methylation of histone H3 lysine 27 (H3K27). This decrease in histone methylation alters gene expression patterns associated with cancer pathways and results in decreased tumor cell proliferation in EZH2 mutated cancer cells.<ref name="insert">[https://www.tazverik.com/Content/pdf/prescribing-information.pdf Tazemetostat (Tazverik) package insert]</ref><ref>[[:File:Tazemetostat.pdf | Tazemetostat (Tazverik) package insert (locally hosted backup)]]</ref><ref>[https://www.tazverik.com/ Tazverik manufacturer's website]</ref> |
==Diseases for which it is used== | ==Diseases for which it is used== | ||
*[[Epithelioid sarcoma]] | *[[Epithelioid sarcoma]] | ||
*[[Follicular lymphoma]] | *[[Follicular lymphoma]] | ||
| + | |||
| + | ==Patient drug information== | ||
| + | *[https://www.tazverik.com/Content/pdf/prescribing-information.pdf Tazemetostat (Tazverik) package insert]<ref name="insert"></ref> | ||
| + | *[http://chemocare.com/chemotherapy/drug-info/tazemetostat.aspx Tazemetostat (Tazverik) patient drug information (Chemocare)]<ref>[http://chemocare.com/chemotherapy/drug-info/tazemetostat.aspx Tazemetostat (Tazverik) patient drug information (Chemocare)]</ref> | ||
| + | *[http://www.uptodate.com/contents/tazemetostat-patient-drug-information Tazemetostat (Tazverik) patient drug information (UpToDate)]<ref>[http://www.uptodate.com/contents/tazemetostat-patient-drug-information Tazemetostat (Tazverik) patient drug information (UpToDate)]</ref> | ||
==History of changes in FDA indication== | ==History of changes in FDA indication== | ||
| Line 17: | Line 22: | ||
*'''Code names:''' E7438, EPZ6438 | *'''Code names:''' E7438, EPZ6438 | ||
*'''Brand name:''' Tazverik | *'''Brand name:''' Tazverik | ||
| + | |||
| + | ==References== | ||
| + | <references/> | ||
[[Category:Drugs]] | [[Category:Drugs]] | ||
Revision as of 08:10, 23 November 2021
Mechanism of action
From the NCI Drug Dictionary: An orally available, small molecule selective and S-adenosyl methionine (SAM) competitive inhibitor of histone methyl transferase EZH2, with potential antineoplastic activity. Upon oral administration, E7438 selectively inhibits the activity of both wild-type and mutated forms of EZH2. Inhibition of EZH2 specifically prevents the methylation of histone H3 lysine 27 (H3K27). This decrease in histone methylation alters gene expression patterns associated with cancer pathways and results in decreased tumor cell proliferation in EZH2 mutated cancer cells.[1][2][3]
Diseases for which it is used
Patient drug information
- Tazemetostat (Tazverik) package insert[1]
- Tazemetostat (Tazverik) patient drug information (Chemocare)[4]
- Tazemetostat (Tazverik) patient drug information (UpToDate)[5]
History of changes in FDA indication
Epithelioid sarcoma
- 1/23/2020: Granted accelerated approval for adults and pediatric patients aged 16 years and older with metastatic or locally advanced epithelioid sarcoma not eligible for complete resection. (Based on EZH-202)
Follicular lymphoma
- 6/17/2020: Granted accelerated approval for adult patients with relapsed or refractory (R/R) follicular lymphoma (FL) whose tumors are positive for an EZH2 mutation as detected by an FDA-approved test and who have received at least 2 prior systemic therapies. (Based on E7438-G000-101)
- 6/17/2020: Granted accelerated approval for adult patients with R/R FL who have no satisfactory alternative treatment options. (Based on E7438-G000-101)
Also known as
- Code names: E7438, EPZ6438
- Brand name: Tazverik