Difference between revisions of "Ribociclib (Kisqali)"
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==General information== | ==General information== | ||
| − | Class/mechanism: Cyclin-dependent kinase (CDK) 4 and 6 inhibitor. Ribociclib inhibits DNA synthesis and cancer cell growth by blocking activity of the cyclin D-CDK4/6 complex which regulates cell cycle progression and cellular proliferation by phosphorylating the retinoblastoma protein (pRb). Inhibiting pRb phosphorylation has been observed to lead to cell cycle arrest in the G1 phase.<ref name="insert">[https://www.pharma.us.novartis.com/sites/www.pharma.us.novartis.com/files/kisqali.pdf Ribociclib (Kisqali) package insert]</ref><ref>[[ | + | Class/mechanism: Cyclin-dependent kinase (CDK) 4 and 6 inhibitor. Ribociclib inhibits DNA synthesis and cancer cell growth by blocking activity of the cyclin D-CDK4/6 complex which regulates cell cycle progression and cellular proliferation by phosphorylating the retinoblastoma protein (pRb). Inhibiting pRb phosphorylation has been observed to lead to cell cycle arrest in the G1 phase.<ref name="insert">[https://www.pharma.us.novartis.com/sites/www.pharma.us.novartis.com/files/kisqali.pdf Ribociclib (Kisqali) package insert]</ref><ref>[[:File:Ribociclib.pdf | Ribociclib (Kisqali) package insert (locally hosted backup)]]</ref><ref>[https://www.us.kisqali.com/ Kisqali manufacturer's website]</ref> |
<br>Route: PO | <br>Route: PO | ||
<br>Extravasation: n/a | <br>Extravasation: n/a | ||
| Line 11: | Line 11: | ||
==History of changes in FDA indication== | ==History of changes in FDA indication== | ||
| − | * | + | *2017-03-13: [https://www.fda.gov/Drugs/InformationOnDrugs/ApprovedDrugs/ucm546438.htm Initial FDA approval] in combination with an [[:Category:Aromatase inhibitors|aromatase inhibitor]] as initial endocrine-based therapy for the treatment of postmenopausal women with [[Biomarkers#HR|hormone receptor (HR)]]-[[Biomarkers#Expression|positive]], [[Biomarkers#HER2|human epidermal growth factor receptor 2 (HER2)]]-[[Biomarkers#Normal_expression|negative]] advanced or metastatic [[breast cancer]]. ''(Based on MONALEESA-2 and MONALEESA-3)'' |
| + | *2018-07-18: FDA approval expanded in combination with an [[:Category:Aromatase inhibitors|aromatase inhibitor]] for pre/perimenopausal women with [[Biomarkers#HR|HR]]-[[Biomarkers#Expression|positive]], [[Biomarkers#HER2|HER2]]-[[Biomarkers#Normal_expression|negative]] advanced or metastatic [[breast cancer]], as initial endocrine-based therapy. ''(No longer limited to postmenopausal women; based on MONALEESA-7)'' | ||
| + | ==History of changes in EMA indication== | ||
| + | *2017-08-22: Initial authorization | ||
| + | ==History of changes in Health Canada indication== | ||
| + | *2018-06-18: Initial notice of compliance in combination with letrozole for treatment of postmenopausal women with hormone receptor (HR)-positive, human epidermal growth factor receptor 2 (HER2)-negative advanced or metastatic [[breast cancer]] as an initial endocrine-based therapy. | ||
| + | *2020-02-07: Expanded indication (details unavailable) | ||
| + | *2023-02-10: Expanded indication (details unavailable) | ||
==Also known as== | ==Also known as== | ||
| − | *'''Code names:''' | + | *'''Code names:''' LEE-011 |
| − | *'''Brand | + | *'''Brand names:''' Kisqali, Kryxana |
==References== | ==References== | ||
<references/> | <references/> | ||
| − | [[Category: | + | [[Category:Drugs]] |
[[Category:Oral medications]] | [[Category:Oral medications]] | ||
[[Category:Protein expression-specific medications]] | [[Category:Protein expression-specific medications]] | ||
| − | [[Category: | + | [[Category:CDK4 inhibitors]] |
| − | [[Category: | + | [[Category:CDK6 inhibitors]] |
| − | |||
[[Category:Breast cancer medications]] | [[Category:Breast cancer medications]] | ||
| − | [[Category: | + | [[Category:FDA approved in 2017]] |
| + | [[Category:EMA approved in 2018]] | ||
| + | [[Category:Health Canada approved in 2018]] | ||
Latest revision as of 13:04, 8 September 2023
General information
Class/mechanism: Cyclin-dependent kinase (CDK) 4 and 6 inhibitor. Ribociclib inhibits DNA synthesis and cancer cell growth by blocking activity of the cyclin D-CDK4/6 complex which regulates cell cycle progression and cellular proliferation by phosphorylating the retinoblastoma protein (pRb). Inhibiting pRb phosphorylation has been observed to lead to cell cycle arrest in the G1 phase.[1][2][3]
Route: PO
Extravasation: n/a
Diseases for which it is used
Patient drug information
History of changes in FDA indication
- 2017-03-13: Initial FDA approval in combination with an aromatase inhibitor as initial endocrine-based therapy for the treatment of postmenopausal women with hormone receptor (HR)-positive, human epidermal growth factor receptor 2 (HER2)-negative advanced or metastatic breast cancer. (Based on MONALEESA-2 and MONALEESA-3)
- 2018-07-18: FDA approval expanded in combination with an aromatase inhibitor for pre/perimenopausal women with HR-positive, HER2-negative advanced or metastatic breast cancer, as initial endocrine-based therapy. (No longer limited to postmenopausal women; based on MONALEESA-7)
History of changes in EMA indication
- 2017-08-22: Initial authorization
History of changes in Health Canada indication
- 2018-06-18: Initial notice of compliance in combination with letrozole for treatment of postmenopausal women with hormone receptor (HR)-positive, human epidermal growth factor receptor 2 (HER2)-negative advanced or metastatic breast cancer as an initial endocrine-based therapy.
- 2020-02-07: Expanded indication (details unavailable)
- 2023-02-10: Expanded indication (details unavailable)
Also known as
- Code names: LEE-011
- Brand names: Kisqali, Kryxana