Difference between revisions of "Rucaparib (Rubraca)"

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(Created page with "=General information= From the [https://www.cancer.gov/publications/dictionaries/cancer-drug?cdrid=594405 NCI Drug Dictionary]: A tricyclic indole poly(ADP-Ribose) polymerase...")
 
(FDA approval)
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=General information=
 
=General information=
From the [https://www.cancer.gov/publications/dictionaries/cancer-drug?cdrid=594405 NCI Drug Dictionary]: A tricyclic indole poly(ADP-Ribose) polymerase (PARP1) inhibitor with potential chemosensitizing, radiosensitizing, and antineoplastic activities. Rucaparib selectively binds to PARP1 and inhibits PARP1-mediated DNA repair, thereby enhancing the accumulation of DNA strand breaks and promoting genomic instability and apoptosis. This may enhance the cytotoxicity of DNA-damaging agents and reverse tumor cell resistance to chemotherapy and radiation therapy.
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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">[http://clovisoncology.com/files/rubraca-prescribing-info.pdf Rucaparib (Rubraca) package insert]</ref><ref>[[Media: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
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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" />
  
 
==Diseases for which it is used==
 
==Diseases for which it is used==
 
*[[Ovarian cancer]]
 
*[[Ovarian cancer]]
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==Patient drug information==
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*[http://clovisoncology.com/files/rubraca-prescribing-info.pdf Rucaparib (Rubraca) package insert]<ref name="insert" />
  
 
==History of changes in FDA indication==
 
==History of changes in FDA indication==
*12/19/2016: FDA 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."
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*12/19/2016: [http://www.fda.gov/Drugs/InformationOnDrugs/ApprovedDrugs/ucm533891.htm FDA 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."
  
 
==Also known as==
 
==Also known as==
CO-338, AG-014699, PF-0136738
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CO-338, AG-014699, PF-0136738, PARP-1 inhibitor AG014699, PARP1 inhibitor PF-01367338, Rucaparib phosphate
  
 
[[Category:Drug index]]
 
[[Category:Drug index]]
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[[Category:Ovarian cancer medications]]
 
[[Category:Ovarian cancer medications]]
 
 
[[Category:Drugs FDA approved in 2016]]
 
[[Category:Drugs FDA approved in 2016]]

Revision as of 13:12, 20 December 2016

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

Also known as

CO-338, AG-014699, PF-0136738, PARP-1 inhibitor AG014699, PARP1 inhibitor PF-01367338, Rucaparib phosphate