Difference between revisions of "Selinexor (Xpovio)"
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− | =Mechanism of action= | + | ==Mechanism of action== |
− | From [ | + | From [https://www.cancer.gov/publications/dictionaries/cancer-drug?cdrid=734824 NCI Drug Dictionary]: An orally available, small molecule inhibitor of CRM1 (chromosome region maintenance 1 protein, exportin 1 or XPO1), with potential antineoplastic activity. Selinexor modifies the essential CRM1-cargo binding residue cysteine-528, thereby irreversibly inactivating CRM1-mediated nuclear export of cargo proteins such as tumor suppressor proteins (TSPs), including p53, p21, BRCA1/2, pRB, FOXO, and other growth regulatory proteins. As a result, this agent, via the approach of selective inhibition of nuclear export (SINE), restores endogenous tumor suppressing processes to selectively eliminate tumor cells while sparing normal cells. |
− | [[ | + | ==Diseases for which it is established== |
− | [[Category: | + | *[[Multiple myeloma]] |
− | [[Category:Oral | + | ==Diseases for which it is used== |
+ | *[[Diffuse large B-cell lymphoma]] | ||
+ | *[[Transformed lymphoma]] | ||
+ | |||
+ | ==History of changes in FDA indication== | ||
+ | ===[[Diffuse large B-cell lymphoma]]=== | ||
+ | *2020-06-22: Granted accelerated approval for adult patients with relapsed or refractory [[Diffuse large B-cell lymphoma|diffuse large B-cell lymphoma (DLBCL), not otherwise specified]], including [[Transformed lymphoma|DLBCL arising from follicular lymphoma]], after at least 2 lines of systemic therapy. ''(New disease entity; based on SADAL)'' | ||
+ | |||
+ | ===[[Multiple myeloma]]=== | ||
+ | *2019-07-03: Granted accelerated approval in combination with dexamethasone for adult patients with relapsed or refractory [[multiple myeloma]] (RRMM) who have received at least four prior therapies and whose disease is refractory to at least two proteasome inhibitors, at least two immunomodulatory agents, and an anti-CD38 monoclonal antibody. ''(Based on STORM)'' | ||
+ | **2020-12-18: Full approval in combination with bortezomib and dexamethasone for the treatment of adult patients with [[multiple myeloma]] who have received at least one prior therapy. ''(Based on BOSTON)'' | ||
+ | ==History of changes in EMA indication== | ||
+ | *2021-03-26: Initial authorization as Nexpovio | ||
+ | ==Also known as== | ||
+ | *'''Code name:''' KPT-330 | ||
+ | *'''Brand name:''' Nexpovio, Xpovio | ||
+ | |||
+ | [[Category:Drugs]] | ||
+ | [[Category:Oral medications]] | ||
[[Category:XPO1 inhibitors]] | [[Category:XPO1 inhibitors]] | ||
− | [[Category: | + | [[Category:Diffuse large B-cell lymphoma medications]] |
+ | [[Category:Multiple myeloma medications]] | ||
+ | [[Category:Transformed lymphoma medications]] | ||
+ | |||
+ | [[Category:FDA approved in 2019]] | ||
+ | [[Category:EMA approved in 2021]] |
Latest revision as of 20:20, 27 June 2024
Mechanism of action
From NCI Drug Dictionary: An orally available, small molecule inhibitor of CRM1 (chromosome region maintenance 1 protein, exportin 1 or XPO1), with potential antineoplastic activity. Selinexor modifies the essential CRM1-cargo binding residue cysteine-528, thereby irreversibly inactivating CRM1-mediated nuclear export of cargo proteins such as tumor suppressor proteins (TSPs), including p53, p21, BRCA1/2, pRB, FOXO, and other growth regulatory proteins. As a result, this agent, via the approach of selective inhibition of nuclear export (SINE), restores endogenous tumor suppressing processes to selectively eliminate tumor cells while sparing normal cells.
Diseases for which it is established
Diseases for which it is used
History of changes in FDA indication
Diffuse large B-cell lymphoma
- 2020-06-22: Granted accelerated approval for adult patients with relapsed or refractory diffuse large B-cell lymphoma (DLBCL), not otherwise specified, including DLBCL arising from follicular lymphoma, after at least 2 lines of systemic therapy. (New disease entity; based on SADAL)
Multiple myeloma
- 2019-07-03: Granted accelerated approval in combination with dexamethasone for adult patients with relapsed or refractory multiple myeloma (RRMM) who have received at least four prior therapies and whose disease is refractory to at least two proteasome inhibitors, at least two immunomodulatory agents, and an anti-CD38 monoclonal antibody. (Based on STORM)
- 2020-12-18: Full approval in combination with bortezomib and dexamethasone for the treatment of adult patients with multiple myeloma who have received at least one prior therapy. (Based on BOSTON)
History of changes in EMA indication
- 2021-03-26: Initial authorization as Nexpovio
Also known as
- Code name: KPT-330
- Brand name: Nexpovio, Xpovio