Difference between revisions of "Selinexor (Xpovio)"
Jump to navigation
Jump to search
m (Jwarner moved page Selinexor (KPT-330) to Selinexor (Xpovio): FDA approval) |
m |
||
| Line 2: | Line 2: | ||
From [http://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. | From [http://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 used== |
| − | + | *[[Multiple myeloma]] | |
| − | * | + | |
| + | ==History of changes in FDA indication== | ||
| + | *7/3/2019: Granted accelerated approval in combination with dexamethasone for adult patients with [[Multiple_myeloma,_relapsed/refractory|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. | ||
[[Category:Drugs]] | [[Category:Drugs]] | ||
| Line 11: | Line 13: | ||
[[Category:XPO1 inhibitors]] | [[Category:XPO1 inhibitors]] | ||
| − | [[Category: | + | [[Category:Multiple myeloma medications]] |
| + | |||
| + | [[Category:FDA approved in 2019]] | ||
Revision as of 18:14, 3 July 2019
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 used
History of changes in FDA indication
- 7/3/2019: 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.