Difference between revisions of "Rucaparib (Rubraca)"
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=General information= | =General information= | ||
| − | Class/mechanism: PARP inhibitor. Rucaparib inhibits activity of the poly (ADP-ribose) polymerase (PARP) enzymes--including PARP-1, PARP-2, and PARP-3--and interferes with PARP-mediated DNA repair. PARP inhibitor cytotoxicity is believed to involve formation of PARP-DNA complexes, DNA damage, apotosis, and cell death. This cytotoxicity was observed to have increased cytotoxicity in cells with mutations in BRCA1, BRCA2, and other DNA repair genes.<ref name="insert">[ | + | Class/mechanism: PARP inhibitor. Rucaparib inhibits activity of the poly (ADP-ribose) polymerase (PARP) enzymes--including PARP-1, PARP-2, and PARP-3--and interferes with PARP-mediated DNA repair. PARP inhibitor cytotoxicity is believed to involve formation of PARP-DNA complexes, DNA damage, apotosis, and cell death. This cytotoxicity was observed to have increased cytotoxicity in cells with mutations in BRCA1, BRCA2, and other DNA repair genes.<ref name="insert">[https://clovisoncology.com/media/1094/rubraca-prescribing-info.pdf Rucaparib (Rubraca) package insert]</ref><ref>[[:File:Rucaparib.pdf | Rucaparib (Rubraca) package insert (locally hosted backup)]]</ref><ref>[http://rubraca.com/ Rubraca manufacturer's website]</ref><ref>[https://www.cancer.gov/publications/dictionaries/cancer-drug?cdrid=594405 Rucaparib phosphate at NCI Drug Dictionary]</ref> |
<br>Route: PO | <br>Route: PO | ||
<br>Extravasation: n/a | <br>Extravasation: n/a | ||
| + | |||
| + | *[https://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=7736 IUPHAR/BPS] | ||
For conciseness and simplicity, HemOnc.org currently will focus on treatment regimens and not list information such as: renal/hepatic dose adjustments, metabolism (including CYP450), excretion, monitoring parameters (although this will be considered for checklists), or manufacturer. Instead, for the most current information, please refer to your preferred pharmacopeias such as [http://www.thomsonhc.com/home/dispatch Micromedex], [http://online.lexi.com/ Lexicomp], [http://www.utdol.com/online/content/search.do UpToDate (courtesy of Lexicomp)], or the prescribing information.<ref name="insert" /> | For conciseness and simplicity, HemOnc.org currently will focus on treatment regimens and not list information such as: renal/hepatic dose adjustments, metabolism (including CYP450), excretion, monitoring parameters (although this will be considered for checklists), or manufacturer. Instead, for the most current information, please refer to your preferred pharmacopeias such as [http://www.thomsonhc.com/home/dispatch Micromedex], [http://online.lexi.com/ Lexicomp], [http://www.utdol.com/online/content/search.do UpToDate (courtesy of Lexicomp)], or the prescribing information.<ref name="insert" /> | ||
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==Diseases for which it is used== | ==Diseases for which it is used== | ||
*[[Ovarian cancer]] | *[[Ovarian cancer]] | ||
| + | *[[Prostate cancer]] | ||
==Patient drug information== | ==Patient drug information== | ||
| − | *[ | + | *[https://clovisoncology.com/media/1094/rubraca-prescribing-info.pdf Rucaparib (Rubraca) package insert]<ref name="insert" /> |
==History of changes in FDA indication== | ==History of changes in FDA indication== | ||
| − | *12 | + | ===[[Ovarian cancer]] - '''PARTIALLY WITHDRAWN'''=== |
| − | * | + | *2016-12-19: [http://www.fda.gov/Drugs/InformationOnDrugs/ApprovedDrugs/ucm533891.htm Granted accelerated approval] for treatment of patients with deleterious [[Biomarkers#BRCA|BRCA]] [[Biomarkers#Mutation|mutation]] ([[Biomarkers#germline|germline]] and/or [[Biomarkers#Somatic|somatic]]) associated advanced [[ovarian cancer]] who have been treated with two or more chemotherapies. ''(Based on Study 10 and ARIEL2)'' |
| + | **2022-06-10: Manufacturer has requested withdrawal of accelerated approval. ''(Based on ARIEL4)'' | ||
| + | *2018-04-06: Full approval for the maintenance treatment of recurrent [[Ovarian cancer|epithelial ovarian, fallopian tube, or primary peritoneal cancer]] who are in a complete or partial response to [[Regimen_classes#Platinum-based_regimen|platinum-based chemotherapy]]. ''(Indication expanded to maintenance therapy; based on ARIEL3)'' | ||
| + | |||
| + | ===[[Prostate cancer]]=== | ||
| + | *2020-05-15: Granted accelerated approval for patients with [[Biomarkers#BRCA|BRCA]] [[Biomarkers#Mutation|mutation]] ([[Biomarkers#germline|germline]] and/or [[Biomarkers#Somatic|somatic]])-associated metastatic castration-resistant [[prostate cancer]] (mCRPC) who have been treated with [[Regimen_classes#Androgen_receptor-directed_therapy|androgen receptor-directed therapy]] and a [[Regimen_classes#Taxane-based_regimen|taxane-based chemotherapy]]. ''(New disease entity; based on TRITON2)'' | ||
| + | |||
| + | ==History of changes in EMA indication== | ||
| + | *2018-05-23: Rubraca is indicated as monotherapy treatment of adult patients with platinum sensitive, relapsed or progressive, BRCA mutated (germline and/or somatic), [[Ovarian cancer|high-grade epithelial ovarian, fallopian tube, or primary peritoneal cancer]], who have been treated with two or more prior lines of platinum based chemotherapy, and who are unable to tolerate further platinum based chemotherapy. | ||
| + | **2023-04-24: Indication withdrawn | ||
| + | *Uncertain date: Rubraca is indicated as monotherapy for the maintenance treatment of adult patients with platinum-sensitive relapsed [[Ovarian cancer|high-grade epithelial ovarian, fallopian tube, or primary peritoneal cancer]] who are in response (complete or partial) to platinum-based chemotherapy. | ||
| + | *2023-10-12: CHMP approved new indication as monotherapy for the maintenance treatment of adult patients with advanced (FIGO Stages III and IV) [[Ovarian cancer|high-grade epithelial ovarian, fallopian tube, or primary peritoneal cancer]] who are in response (complete or partial) following completion of first-line platinum-based chemotherapy. | ||
==Also known as== | ==Also known as== | ||
| − | *'''Code names:''' CO-338, AG-014699, PF-0136738 | + | *'''Code names:''' CO-338, AG-14447, AG-014699, PF-0136738 |
*'''Brand name:''' Rubraca | *'''Brand name:''' Rubraca | ||
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[[Category:Mutation-specific medications]] | [[Category:Mutation-specific medications]] | ||
| − | [[Category: | + | [[Category:PARP1 inhibitors]] |
| − | |||
[[Category:Ovarian cancer medications]] | [[Category:Ovarian cancer medications]] | ||
| − | [[Category: | + | [[Category:Prostate cancer medications]] |
| + | |||
| + | [[Category:FDA approved in 2016]] | ||
| + | [[Category:EMA approved in 2018]] | ||
Latest revision as of 11:46, 9 April 2024
General information
Class/mechanism: PARP inhibitor. Rucaparib inhibits activity of the poly (ADP-ribose) polymerase (PARP) enzymes--including PARP-1, PARP-2, and PARP-3--and interferes with PARP-mediated DNA repair. PARP inhibitor cytotoxicity is believed to involve formation of PARP-DNA complexes, DNA damage, apotosis, and cell death. This cytotoxicity was observed to have increased cytotoxicity in cells with mutations in BRCA1, BRCA2, and other DNA repair genes.[1][2][3][4]
Route: PO
Extravasation: n/a
For conciseness and simplicity, HemOnc.org currently will focus on treatment regimens and not list information such as: renal/hepatic dose adjustments, metabolism (including CYP450), excretion, monitoring parameters (although this will be considered for checklists), or manufacturer. Instead, for the most current information, please refer to your preferred pharmacopeias such as Micromedex, Lexicomp, UpToDate (courtesy of Lexicomp), or the prescribing information.[1]
Diseases for which it is used
Patient drug information
History of changes in FDA indication
Ovarian cancer - PARTIALLY WITHDRAWN
- 2016-12-19: Granted accelerated approval for treatment of patients with deleterious BRCA mutation (germline and/or somatic) associated advanced ovarian cancer who have been treated with two or more chemotherapies. (Based on Study 10 and ARIEL2)
- 2022-06-10: Manufacturer has requested withdrawal of accelerated approval. (Based on ARIEL4)
- 2018-04-06: Full approval for the maintenance treatment of recurrent epithelial ovarian, fallopian tube, or primary peritoneal cancer who are in a complete or partial response to platinum-based chemotherapy. (Indication expanded to maintenance therapy; based on ARIEL3)
Prostate cancer
- 2020-05-15: Granted accelerated approval for patients with BRCA mutation (germline and/or somatic)-associated metastatic castration-resistant prostate cancer (mCRPC) who have been treated with androgen receptor-directed therapy and a taxane-based chemotherapy. (New disease entity; based on TRITON2)
History of changes in EMA indication
- 2018-05-23: Rubraca is indicated as monotherapy treatment of adult patients with platinum sensitive, relapsed or progressive, BRCA mutated (germline and/or somatic), high-grade epithelial ovarian, fallopian tube, or primary peritoneal cancer, who have been treated with two or more prior lines of platinum based chemotherapy, and who are unable to tolerate further platinum based chemotherapy.
- 2023-04-24: Indication withdrawn
- Uncertain date: Rubraca is indicated as monotherapy for the maintenance treatment of adult patients with platinum-sensitive relapsed high-grade epithelial ovarian, fallopian tube, or primary peritoneal cancer who are in response (complete or partial) to platinum-based chemotherapy.
- 2023-10-12: CHMP approved new indication as monotherapy for the maintenance treatment of adult patients with advanced (FIGO Stages III and IV) high-grade epithelial ovarian, fallopian tube, or primary peritoneal cancer who are in response (complete or partial) following completion of first-line platinum-based chemotherapy.
Also known as
- Code names: CO-338, AG-14447, AG-014699, PF-0136738
- Brand name: Rubraca