Identification
- Summary
Rucaparib is a poly (ADP-ribose) polymerase (PARP) inhibitor used to treat recurrent ovarian and prostate cancers in previously treated adults.
- Brand Names
- Rubraca
- Generic Name
- Rucaparib
- DrugBank Accession Number
- DB12332
- Background
Rucaparib is an anticancer drug and poly (ADP-ribose) polymerase (PARP) inhibitor. PARP is an enzyme that plays an essential role in DNA repair.1 Rucaparib is proposed to work in several PARP-dependent and PARP-independent mechanisms of action; however, it causes a unique effect of synthetic lethality. By targeting the genetically-mutated cancer cells that lack a DNA repair mechanism, rucaparib causes cancer cell death and reduces tumour growth.1,2
Rucaparib was granted FDA Breakthrough Therapy designation in April 2015 1 and accelerated approval in December 2016.4 The drug was later approved by the European Commission in May 2018.7 It is currently used to treat recurrent ovarian and prostate cancer in adults.6,7
- Type
- Small Molecule
- Groups
- Approved, Investigational
- Structure
Structure for Rucaparib (DB12332)
- Weight
- Average: 323.371
Monoisotopic: 323.143390375 - Chemical Formula
- C19H18FN3O
- Synonyms
- Rucaparib
- External IDs
- AG-14447
Pharmacology
- Indication
Rucaparib is indicated for the maintenance treatment of adult patients with a deleterious BRCA mutation (germline and/or somatic)- associated recurrent epithelial ovarian, fallopian tube, or primary peritoneal cancer who are in a complete or partial response to platinum-based chemotherapy.8
Under accelerated approval by the FDA, rucaparib is also indicated for the treatment of adult patients with a deleterious 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.8
Reduce drug development failure ratesBuild, train, & validate machine-learning modelswith evidence-based and structured datasets.Build, train, & validate predictive machine-learning models with structured datasets.- Associated Conditions
- Associated Therapies
- Contraindications & Blackbox Warnings
Avoid life-threatening adverse drug eventsImprove clinical decision support with information on contraindications & blackbox warnings, population restrictions, harmful risks, & more.Avoid life-threatening adverse drug events & improve clinical decision support.- Pharmacodynamics
Rucaparib is an anticancer agent that exerts cytotoxic effects against cancer cells. It works by inhibiting poly (ADP-ribose) polymerase (PARP), an enzyme that plays a role in DNA repair. Rucaparib inhibits PARP-1, PARP-2, and PARP-3. It also interacts with PARP-4, PARP-10, PARP-12, PARP-15, and PARP-16, but to a lesser extent.1 In mice, rucaparib accumulated and was retained in tumours, inhibiting PARP enzymes for seven days.4
Rucaparib decreases tumour growth in tumour cell lines with deficiencies in BRCA1/2 and other DNA repair genes.6 In addition to PARP inhibition, rucaparib demonstrated PARP-independent cytotoxic mechanisms in cancer cells. When co-administered with other chemotherapeutic agents, rucaparib contributed to synergistic or additive effects in vitro and in vivo. There is evidence that rucaparib can sensitize cancer cells to chemotherapy. Rucaparib can also cause vasodilation, which may increase tumour perfusion and enhance the accumulation of cytotoxic drugs in cancer cells.4
- Mechanism of action
PARPs play a role in DNA repair by activating DNA damage response pathways, such as base excision repair, and facilitating DNA repair. PARPs were evaluated as novel anticancer therapeutic targets after discovering that PARP-1 inhibitors reduce tumour growth in BRCA-deficient cancers.1 BRCA1 and BRCA2 are tumour suppressor genes involved in various cellular processes related to cell growth and death, including DNA repair.3 More specifically, BRCA1 and BRCA2 are involved in homologous recombination (HR) DNA repair. Cancer cells with a deleterious BRCA mutation are HR-deficient, resulting in unregulated and aberrant cell repair and growth.1
Rucaparib inhibits PARP1, PARP2, and PARP3.6 Inhibiting PARP traps the enzyme on damaged DNA, halting the repair process and forming toxic PARP–DNA complexes. Alternatively, other DNA repair processes such as error-prone nonhomologous end joining (NHEJ) or alternative end-joining pathways can be initiated, leading to mutations or chromosomal change.2 Further DNA damage can trigger cancer cell apoptosis and cell death.6
Typically, inhibition of PARP converts single-strand breaks in DNA to double-strand breaks at replication forks. HR DNA repair pathways repair double-strand breaks; however, HR-deficient cancer cells lack this repair mechanism. Because HR-deficient cancer cells are more vulnerable to unsalvageable DNA damage, rucaparib-induced PARP inhibition leads to synthetic lethality. In this phenomenon, two non-lethal defects (HR deficiency and PARP inhibition) combine and cause cell death.1,2
Target Actions Organism APoly [ADP-ribose] polymerase 1 inhibitorHumans APoly [ADP-ribose] polymerase 2 inhibitorHumans APoly [ADP-ribose] polymerase 3 inhibitorHumans - Absorption
Rucaparib exhibits a linear pharmacokinetic profile over the dose range from 240 mg to 840 mg twice daily. The mean (coefficient of variation [CV]) steady-state rucaparib Cmax is 1940 ng/mL (54%) and AUC0-12h is 16900 h x ng/mL (54%) at the approved recommended dosage. The mean AUC accumulation ratio is 3.5 to 6.2 fold. The median Tmax at the steady state is 1.9 hours, with a range of 0 to 5.98 hours at the approved recommended dosage. The mean absolute bioavailability is 36%, with a range of 30 to 45%.6
A high-fat meal increased Cmax and AUC0-24h by 20% and 38%, respectively. The Tmax was delayed by 2.5 hours.6
- Volume of distribution
The mean (coefficient of variation) apparent volume of distribution is 2300 L (21%).6
- Protein binding
Rucaparib is 70% bound to human plasma proteins in vitro. Rucaparib preferentially distributed to red blood cells with a blood-to-plasma concentration ratio of 1.8.6
- Metabolism
In vitro, rucaparib is primarily metabolized by CYP2D6 and, to a lesser extent, by CYP1A2 and CYP3A4. In addition to CYP-based oxidation, rucaparib also undergoes N-demethylation, N-methylation, and glucuronidation.6 In one study, seven metabolites of rucaparib were identified in plasma, urine, and feces.5
Hover over products below to view reaction partners
- Route of elimination
Following a single oral dose of radiolabeled rucaparib, unchanged rucaparib accounted for 64% of the radioactivity. Rucaparib accounted for 45% and 95% of radioactivity in urine and feces, respectively.6
- Half-life
The mean (coefficient of variation) terminal elimination half-life is 26 (39%) hours.6
- Clearance
The mean (coefficient of variation) apparent total clearance at steady state is 44.2 L/h (45%).6
- Adverse Effects
Improve decision support & research outcomesWith structured adverse effects data, including: blackbox warnings, adverse reactions, warning & precautions, & incidence rates.Improve decision support & research outcomes with our structured adverse effects data.- Toxicity
There is no information regarding the LD50 and overdose of rucaparib.
- Pathways
- Not Available
- Pharmacogenomic Effects/ADRs
- Not Available
Interactions
- Drug Interactions
- This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
Drug Interaction Integrate drug-drug
interactions in your softwareAbametapir The serum concentration of Rucaparib can be increased when it is combined with Abametapir. Abatacept The metabolism of Rucaparib can be increased when combined with Abatacept. Abemaciclib The metabolism of Abemaciclib can be decreased when combined with Rucaparib. Abiraterone The serum concentration of Rucaparib can be increased when it is combined with Abiraterone. Abrocitinib The metabolism of Abrocitinib can be decreased when combined with Rucaparib. Acalabrutinib The metabolism of Acalabrutinib can be decreased when combined with Rucaparib. Acebutolol The metabolism of Acebutolol can be decreased when combined with Rucaparib. Acenocoumarol The metabolism of Acenocoumarol can be decreased when combined with Rucaparib. Acetaminophen The metabolism of Acetaminophen can be decreased when combined with Rucaparib. Acetohexamide The metabolism of Acetohexamide can be decreased when combined with Rucaparib. 
Identify potential medication risksEasily compare up to 40 drugs with our drug interaction checker.Get severity rating, description, and management advice.Learn more - Food Interactions
- Exercise caution with grapefruit products. Rucaparib is primarily metabolized through CYP2D6 but is also metabolized by CYP3A4 and CYP1A2. Grapefruit inhibits CYP3A4 metabolism, which may increase rucaparib serum levels.
- Exercise caution with St. John's Wort. Rucaparib is primarily metabolized through CYP2D6 but is also metabolized by CYP3A4 and CYP1A2. St. John's Wort induces CYP3A4 metabolism, which may reduce rucaparib serum levels.
- Take with or without food. A high-fat meals increases drug exposure but not to a clinically significant extent.
Products
Drug product information from 10+ global regionsOur datasets provide approved product information including:dosage, form, labeller, route of administration, and marketing period.Access drug product information from over 10 global regions.- Product Ingredients
Ingredient UNII CAS InChI Key Rucaparib camsylate 41AX9SJ8KO 1859053-21-6 INBJJAFXHQQSRW-STOWLHSFSA-N Rucaparib phosphate H3M9955244 459868-92-9 FCCGJTKEKXUBFZ-UHFFFAOYSA-N - Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Rubraca Tablet, film coated 300 mg Oral Clovis Oncology Ireland Limited 2020-12-16 Not applicable EU 
Rubraca Tablet, film coated 200 mg Oral Clovis Oncology Ireland Limited 2020-12-16 Not applicable EU Rubraca Tablet, film coated 200 mg/1 Oral Clovis Oncology, Inc. 2016-12-19 Not applicable US 
Rubraca Tablet, film coated 250 mg Oral Clovis Oncology Ireland Limited 2020-12-16 Not applicable EU Rubraca Tablet, film coated 250 mg/1 Oral Clovis Oncology, Inc. 2017-05-01 Not applicable US Rubraca Tablet, film coated 300 mg/1 Oral Clovis Oncology, Inc. 2016-12-19 Not applicable US
Categories
- ATC Codes
- L01XK03 — Rucaparib
- Drug Categories
- Antineoplastic Agents
- Antineoplastic and Immunomodulating Agents
- BCRP/ABCG2 Inhibitors
- BCRP/ABCG2 Substrates
- Cytochrome P-450 CYP1A2 Inducers
- Cytochrome P-450 CYP1A2 Inducers (moderate)
- Cytochrome P-450 CYP1A2 Inhibitors
- Cytochrome P-450 CYP1A2 Inhibitors (weak)
- Cytochrome P-450 CYP1A2 Substrates
- Cytochrome P-450 CYP1A2 Substrates with a Narrow Therapeutic Index
- Cytochrome P-450 CYP2C19 Inhibitors
- Cytochrome P-450 CYP2C19 Inhibitors (weak)
- Cytochrome P-450 CYP2C8 Inhibitors
- Cytochrome P-450 CYP2C8 Inhibitors (weak)
- Cytochrome P-450 CYP2C9 Inhibitors
- Cytochrome P-450 CYP2C9 Inhibitors (strength unknown)
- Cytochrome P-450 CYP2D6 Inhibitors
- Cytochrome P-450 CYP2D6 Inhibitors (moderate)
- Cytochrome P-450 CYP2D6 Substrates
- Cytochrome P-450 CYP2D6 Substrates with a Narrow Therapeutic Index
- Cytochrome P-450 CYP3A Inhibitors
- Cytochrome P-450 CYP3A Substrates
- Cytochrome P-450 CYP3A4 Inhibitors
- Cytochrome P-450 CYP3A4 Inhibitors (weak)
- Cytochrome P-450 CYP3A4 Substrates
- Cytochrome P-450 CYP3A4 Substrates with a Narrow Therapeutic Index
- Cytochrome P-450 CYP3A5 Inhibitors
- Cytochrome P-450 CYP3A5 Inhibitors (strength unknown)
- Cytochrome P-450 CYP3A7 Inhibitors
- Cytochrome P-450 CYP3A7 Inhibitors (strength unknown)
- Cytochrome P-450 Enzyme Inducers
- Cytochrome P-450 Enzyme Inhibitors
- Cytochrome P-450 Substrates
- Enzyme Inhibitors
- Heterocyclic Compounds, Fused-Ring
- MATE 1 Inhibitors
- MATE 2 Inhibitors
- MATE inhibitors
- Narrow Therapeutic Index Drugs
- OAT1/SLC22A6 inhibitors
- OAT3/SLC22A8 Inhibitors
- OATP1B1/SLCO1B1 Inhibitors
- OATP1B3 inhibitors
- OCT1 inhibitors
- P-glycoprotein inhibitors
- P-glycoprotein substrates
- P-glycoprotein substrates with a Narrow Therapeutic Index
- Poly (ADP-ribose) polymerase (PARP) inhibitors
- Poly(ADP-ribose) Polymerase Inhibitors
- UGT1A1 Inhibitors
- Chemical TaxonomyProvided by Classyfire
- Description
- This compound belongs to the class of organic compounds known as 2-phenylindoles. These are indoles substituted at the 2-position with a phenyl group.
- Kingdom
- Organic compounds
- Super Class
- Organoheterocyclic compounds
- Class
- Indoles and derivatives
- Sub Class
- Indoles
- Direct Parent
- 2-phenylindoles
- Alternative Parents
- Phenylpyrroles / Benzazepines / 3-alkylindoles / Phenylmethylamines / Benzylamines / Aralkylamines / Azepines / Aryl fluorides / Heteroaromatic compounds / Secondary carboxylic acid amides show 9 more
- Substituents
- 2-phenylindole / 2-phenylpyrrole / 3-alkylindole / Amine / Amino acid or derivatives / Aralkylamine / Aromatic heteropolycyclic compound / Aryl fluoride / Aryl halide / Azacycle show 24 more
- Molecular Framework
- Aromatic heteropolycyclic compounds
- External Descriptors
- Not Available
- Affected organisms
- Humans and other mammals
Chemical Identifiers
- UNII
- 8237F3U7EH
- CAS number
- 283173-50-2
- InChI Key
- HMABYWSNWIZPAG-UHFFFAOYSA-N
- InChI
- InChI=1S/C19H18FN3O/c1-21-10-11-2-4-12(5-3-11)18-14-6-7-22-19(24)15-8-13(20)9-16(23-18)17(14)15/h2-5,8-9,21,23H,6-7,10H2,1H3,(H,22,24)
- IUPAC Name
- 6-fluoro-2-{4-[(methylamino)methyl]phenyl}-3,10-diazatricyclo[6.4.1.0^{4,13}]trideca-1,4,6,8(13)-tetraen-9-one
- SMILES
- CNCC1=CC=C(C=C1)C1=C2CCNC(=O)C3=C2C(N1)=CC(F)=C3
References
- General References
- Jenner ZB, Sood AK, Coleman RL: Evaluation of rucaparib and companion diagnostics in the PARP inhibitor landscape for recurrent ovarian cancer therapy. Future Oncol. 2016 Jun;12(12):1439-56. doi: 10.2217/fon-2016-0002. Epub 2016 Apr 18. [Article]
- Dockery LE, Gunderson CC, Moore KN: Rucaparib: the past, present, and future of a newly approved PARP inhibitor for ovarian cancer. Onco Targets Ther. 2017 Jun 19;10:3029-3037. doi: 10.2147/OTT.S114714. eCollection 2017. [Article]
- Varol U, Kucukzeybek Y, Alacacioglu A, Somali I, Altun Z, Aktas S, Oktay Tarhan M: BRCA genes: BRCA 1 and BRCA 2. J BUON. 2018 Jul-Aug;23(4):862-866. [Article]
- Syed YY: Rucaparib: First Global Approval. Drugs. 2017 Apr;77(5):585-592. doi: 10.1007/s40265-017-0716-2. [Article]
- Liao M, Watkins S, Nash E, Isaacson J, Etter J, Beltman J, Fan R, Shen L, Mutlib A, Kemeny V, Papai Z, van Tilburg P, Xiao JJ: Evaluation of absorption, distribution, metabolism, and excretion of [(14)C]-rucaparib, a poly(ADP-ribose) polymerase inhibitor, in patients with advanced solid tumors. Invest New Drugs. 2020 Jun;38(3):765-775. doi: 10.1007/s10637-019-00815-2. Epub 2019 Jun 27. [Article]
- FDA Approved Drug Products: RUBRACA (rucaparib) tablets, for oral use (June 2022) [Link]
- EMA Approved Drug Products: Rubraca (rucaparib) Oral Tablets [Link]
- FDA Approved Drug Products: RUBRACA (rucaparib) tablets, for oral use (December 2022) [Link]
- External Links
- Human Metabolome Database
- HMDB0257361
- KEGG Drug
- D10079
- PubChem Compound
- 9931954
- PubChem Substance
- 347828593
- ChemSpider
- 8107584
- BindingDB
- 50446130
- 1862579
- ChEBI
- 134689
- ChEMBL
- CHEMBL1173055
- ZINC
- ZINC000000025958
- PharmGKB
- PA166163418
- PDBe Ligand
- RPB
- Wikipedia
- Rucaparib
- PDB Entries
- 4bjc / 4rv6 / 6vkk
Clinical Trials
- Clinical Trials
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage Forms
Form Route Strength Tablet, film coated Oral 200 MG Tablet, film coated Oral 200 mg/1 Tablet, film coated Oral 250 MG Tablet, film coated Oral 250 mg/1 Tablet, film coated Oral 300 mg/1 Tablet, film coated Oral 300 MG - Prices
- Not Available
- Patents
Patent Number Pediatric Extension Approved Expires (estimated) Region US8859562 No 2014-10-14 2031-08-04 US US8143241 No 2012-03-27 2027-08-12 US US6495541 No 2002-12-17 2020-01-10 US US8754072 No 2014-06-17 2031-02-10 US US9045487 No 2015-06-02 2031-02-10 US US8071579 No 2011-12-06 2027-08-12 US US7531530 No 2009-05-12 2024-07-23 US US7351701 No 2008-04-01 2024-07-23 US US9861638 No 2018-01-09 2031-02-10 US US9987285 No 2018-06-05 2035-08-17 US US10130636 No 2018-11-20 2035-08-17 US US10278974 No 2019-05-07 2031-02-10 US
Properties
- State
- Solid
- Experimental Properties
Property Value Source water solubility 1 mg/mL https://www.accessdata.fda.gov/drugsatfda_docs/label/2022/209115s011lbl.pdf - Predicted Properties
Property Value Source Water Solubility 0.0114 mg/mL ALOGPS logP 2.39 ALOGPS logP 2.45 Chemaxon logS -4.4 ALOGPS pKa (Strongest Acidic) 13.16 Chemaxon pKa (Strongest Basic) 9.32 Chemaxon Physiological Charge 1 Chemaxon Hydrogen Acceptor Count 2 Chemaxon Hydrogen Donor Count 3 Chemaxon Polar Surface Area 56.92 Å2 Chemaxon Rotatable Bond Count 3 Chemaxon Refractivity 92.91 m3·mol-1 Chemaxon Polarizability 35.19 Å3 Chemaxon Number of Rings 4 Chemaxon Bioavailability 1 Chemaxon Rule of Five Yes Chemaxon Ghose Filter Yes Chemaxon Veber's Rule No Chemaxon MDDR-like Rule No Chemaxon - Predicted ADMET Features
- Not Available
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
Spectrum Spectrum Type Splash Key Predicted MS/MS Spectrum - 10V, Positive (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 20V, Positive (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 40V, Positive (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 10V, Negative (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 20V, Negative (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 40V, Negative (Annotated) Predicted LC-MS/MS Not Available
Targets
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Use our structured and evidence-based datasets to unlock newinsights and accelerate drug research.
Use our structured and evidence-based datasets to unlock new insights and accelerate drug research.
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Inhibitor
- General Function
- Zinc ion binding
- Specific Function
- Involved in the base excision repair (BER) pathway, by catalyzing the poly(ADP-ribosyl)ation of a limited number of acceptor proteins involved in chromatin architecture and in DNA metabolism. This ...
- Gene Name
- PARP1
- Uniprot ID
- P09874
- Uniprot Name
- Poly [ADP-ribose] polymerase 1
- Molecular Weight
- 113082.945 Da
References
- Dockery LE, Gunderson CC, Moore KN: Rucaparib: the past, present, and future of a newly approved PARP inhibitor for ovarian cancer. Onco Targets Ther. 2017 Jun 19;10:3029-3037. doi: 10.2147/OTT.S114714. eCollection 2017. [Article]
- Jenner ZB, Sood AK, Coleman RL: Evaluation of rucaparib and companion diagnostics in the PARP inhibitor landscape for recurrent ovarian cancer therapy. Future Oncol. 2016 Jun;12(12):1439-56. doi: 10.2217/fon-2016-0002. Epub 2016 Apr 18. [Article]
- FDA Approved Drug Products: RUBRACA (rucaparib) tablets, for oral use (June 2022) [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Inhibitor
- General Function
- Nad+ adp-ribosyltransferase activity
- Specific Function
- Involved in the base excision repair (BER) pathway, by catalyzing the poly(ADP-ribosyl)ation of a limited number of acceptor proteins involved in chromatin architecture and in DNA metabolism. This ...
- Gene Name
- PARP2
- Uniprot ID
- Q9UGN5
- Uniprot Name
- Poly [ADP-ribose] polymerase 2
- Molecular Weight
- 66205.31 Da
References
- Dockery LE, Gunderson CC, Moore KN: Rucaparib: the past, present, and future of a newly approved PARP inhibitor for ovarian cancer. Onco Targets Ther. 2017 Jun 19;10:3029-3037. doi: 10.2147/OTT.S114714. eCollection 2017. [Article]
- Jenner ZB, Sood AK, Coleman RL: Evaluation of rucaparib and companion diagnostics in the PARP inhibitor landscape for recurrent ovarian cancer therapy. Future Oncol. 2016 Jun;12(12):1439-56. doi: 10.2217/fon-2016-0002. Epub 2016 Apr 18. [Article]
- FDA Approved Drug Products: RUBRACA (rucaparib) tablets, for oral use (June 2022) [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Inhibitor
- General Function
- Nad+ adp-ribosyltransferase activity
- Specific Function
- Involved in the base excision repair (BER) pathway, by catalyzing the poly(ADP-ribosyl)ation of a limited number of acceptor proteins involved in chromatin architecture and in DNA metabolism. This ...
- Gene Name
- PARP3
- Uniprot ID
- Q9Y6F1
- Uniprot Name
- Poly [ADP-ribose] polymerase 3
- Molecular Weight
- 60069.7 Da
References
- Dockery LE, Gunderson CC, Moore KN: Rucaparib: the past, present, and future of a newly approved PARP inhibitor for ovarian cancer. Onco Targets Ther. 2017 Jun 19;10:3029-3037. doi: 10.2147/OTT.S114714. eCollection 2017. [Article]
- Jenner ZB, Sood AK, Coleman RL: Evaluation of rucaparib and companion diagnostics in the PARP inhibitor landscape for recurrent ovarian cancer therapy. Future Oncol. 2016 Jun;12(12):1439-56. doi: 10.2217/fon-2016-0002. Epub 2016 Apr 18. [Article]
- FDA Approved Drug Products: RUBRACA (rucaparib) tablets, for oral use (June 2022) [Link]
Enzymes
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- SubstrateInhibitor
- General Function
- Steroid hydroxylase activity
- Specific Function
- Responsible for the metabolism of many drugs and environmental chemicals that it oxidizes. It is involved in the metabolism of drugs such as antiarrhythmics, adrenoceptor antagonists, and tricyclic...
- Gene Name
- CYP2D6
- Uniprot ID
- P10635
- Uniprot Name
- Cytochrome P450 2D6
- Molecular Weight
- 55768.94 Da
References
- FDA Approved Drug Products: RUBRACA (rucaparib) tablets, for oral use (June 2022) [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- SubstrateInhibitorInducer
- Curator comments
- Inhibition of the enzyme is reversible.
- General Function
- Oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygen
- Specific Function
- Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
- Gene Name
- CYP1A2
- Uniprot ID
- P05177
- Uniprot Name
- Cytochrome P450 1A2
- Molecular Weight
- 58293.76 Da
References
- Dockery LE, Gunderson CC, Moore KN: Rucaparib: the past, present, and future of a newly approved PARP inhibitor for ovarian cancer. Onco Targets Ther. 2017 Jun 19;10:3029-3037. doi: 10.2147/OTT.S114714. eCollection 2017. [Article]
- Liao M, Jaw-Tsai S, Beltman J, Simmons AD, Harding TC, Xiao JJ: Evaluation of in vitro absorption, distribution, metabolism, and excretion and assessment of drug-drug interaction of rucaparib, an orally potent poly(ADP-ribose) polymerase inhibitor. Xenobiotica. 2020 Sep;50(9):1032-1042. doi: 10.1080/00498254.2020.1737759. Epub 2020 Mar 18. [Article]
- Xiao JJ, Nowak D, Ramlau R, Tomaszewska-Kiecana M, Wysocki PJ, Isaacson J, Beltman J, Nash E, Kaczanowski R, Arold G, Watkins S: Evaluation of Drug-Drug Interactions of Rucaparib and CYP1A2, CYP2C9, CYP2C19, CYP3A, and P-gp Substrates in Patients With an Advanced Solid Tumor. Clin Transl Sci. 2019 Jan;12(1):58-65. doi: 10.1111/cts.12600. Epub 2018 Dec 20. [Article]
- Rucaparib - Drug Summary Prescribers Digital Reference [Link]
- FDA Approved Drug Products: RUBRACA (rucaparib) tablets, for oral use (June 2022) [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- SubstrateInhibitor
- General Function
- Vitamin d3 25-hydroxylase activity
- Specific Function
- Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation react...
- Gene Name
- CYP3A4
- Uniprot ID
- P08684
- Uniprot Name
- Cytochrome P450 3A4
- Molecular Weight
- 57342.67 Da
References
- Xiao JJ, Nowak D, Ramlau R, Tomaszewska-Kiecana M, Wysocki PJ, Isaacson J, Beltman J, Nash E, Kaczanowski R, Arold G, Watkins S: Evaluation of Drug-Drug Interactions of Rucaparib and CYP1A2, CYP2C9, CYP2C19, CYP3A, and P-gp Substrates in Patients With an Advanced Solid Tumor. Clin Transl Sci. 2019 Jan;12(1):58-65. doi: 10.1111/cts.12600. Epub 2018 Dec 20. [Article]
- FDA Approved Drug Products: RUBRACA (rucaparib) tablets, for oral use (June 2022) [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Inhibitor
- Curator comments
- Inhibition is reversible.
- General Function
- Oxygen binding
- Specific Function
- Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
- Gene Name
- CYP3A5
- Uniprot ID
- P20815
- Uniprot Name
- Cytochrome P450 3A5
- Molecular Weight
- 57108.065 Da
References
- Liao M, Jaw-Tsai S, Beltman J, Simmons AD, Harding TC, Xiao JJ: Evaluation of in vitro absorption, distribution, metabolism, and excretion and assessment of drug-drug interaction of rucaparib, an orally potent poly(ADP-ribose) polymerase inhibitor. Xenobiotica. 2020 Sep;50(9):1032-1042. doi: 10.1080/00498254.2020.1737759. Epub 2020 Mar 18. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Inhibitor
- Curator comments
- Inhibition is reversible.
- General Function
- Oxygen binding
- Specific Function
- Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
- Gene Name
- CYP3A7
- Uniprot ID
- P24462
- Uniprot Name
- Cytochrome P450 3A7
- Molecular Weight
- 57525.03 Da
References
- Liao M, Jaw-Tsai S, Beltman J, Simmons AD, Harding TC, Xiao JJ: Evaluation of in vitro absorption, distribution, metabolism, and excretion and assessment of drug-drug interaction of rucaparib, an orally potent poly(ADP-ribose) polymerase inhibitor. Xenobiotica. 2020 Sep;50(9):1032-1042. doi: 10.1080/00498254.2020.1737759. Epub 2020 Mar 18. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Inhibitor
- Curator comments
- Inhibition is reversible.
- General Function
- Monooxygenase activity
- Specific Function
- Exhibits low testosterone 6-beta-hydroxylase activity.
- Gene Name
- CYP3A43
- Uniprot ID
- Q9HB55
- Uniprot Name
- Cytochrome P450 3A43
- Molecular Weight
- 57669.21 Da
References
- Liao M, Jaw-Tsai S, Beltman J, Simmons AD, Harding TC, Xiao JJ: Evaluation of in vitro absorption, distribution, metabolism, and excretion and assessment of drug-drug interaction of rucaparib, an orally potent poly(ADP-ribose) polymerase inhibitor. Xenobiotica. 2020 Sep;50(9):1032-1042. doi: 10.1080/00498254.2020.1737759. Epub 2020 Mar 18. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Inhibitor
- General Function
- Steroid hydroxylase activity
- Specific Function
- Responsible for the metabolism of a number of therapeutic agents such as the anticonvulsant drug S-mephenytoin, omeprazole, proguanil, certain barbiturates, diazepam, propranolol, citalopram and im...
- Gene Name
- CYP2C19
- Uniprot ID
- P33261
- Uniprot Name
- Cytochrome P450 2C19
- Molecular Weight
- 55930.545 Da
References
- Liao M, Jaw-Tsai S, Beltman J, Simmons AD, Harding TC, Xiao JJ: Evaluation of in vitro absorption, distribution, metabolism, and excretion and assessment of drug-drug interaction of rucaparib, an orally potent poly(ADP-ribose) polymerase inhibitor. Xenobiotica. 2020 Sep;50(9):1032-1042. doi: 10.1080/00498254.2020.1737759. Epub 2020 Mar 18. [Article]
- Xiao JJ, Nowak D, Ramlau R, Tomaszewska-Kiecana M, Wysocki PJ, Isaacson J, Beltman J, Nash E, Kaczanowski R, Arold G, Watkins S: Evaluation of Drug-Drug Interactions of Rucaparib and CYP1A2, CYP2C9, CYP2C19, CYP3A, and P-gp Substrates in Patients With an Advanced Solid Tumor. Clin Transl Sci. 2019 Jan;12(1):58-65. doi: 10.1111/cts.12600. Epub 2018 Dec 20. [Article]
- FDA Approved Drug Products: RUBRACA (rucaparib) tablets, for oral use (June 2022) [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Inhibitor
- Curator comments
- Inhibition is reversible.
- General Function
- Steroid hydroxylase activity
- Specific Function
- Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
- Gene Name
- CYP2C9
- Uniprot ID
- P11712
- Uniprot Name
- Cytochrome P450 2C9
- Molecular Weight
- 55627.365 Da
References
- Liao M, Jaw-Tsai S, Beltman J, Simmons AD, Harding TC, Xiao JJ: Evaluation of in vitro absorption, distribution, metabolism, and excretion and assessment of drug-drug interaction of rucaparib, an orally potent poly(ADP-ribose) polymerase inhibitor. Xenobiotica. 2020 Sep;50(9):1032-1042. doi: 10.1080/00498254.2020.1737759. Epub 2020 Mar 18. [Article]
- Xiao JJ, Nowak D, Ramlau R, Tomaszewska-Kiecana M, Wysocki PJ, Isaacson J, Beltman J, Nash E, Kaczanowski R, Arold G, Watkins S: Evaluation of Drug-Drug Interactions of Rucaparib and CYP1A2, CYP2C9, CYP2C19, CYP3A, and P-gp Substrates in Patients With an Advanced Solid Tumor. Clin Transl Sci. 2019 Jan;12(1):58-65. doi: 10.1111/cts.12600. Epub 2018 Dec 20. [Article]
- DailyMed Label: RUBRACA (rucaparib) oral tablet, film coated [Link]
- EMA Reports [Link]
- Rubraca [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Inhibitor
- General Function
- Steroid hydroxylase activity
- Specific Function
- Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
- Gene Name
- CYP2C8
- Uniprot ID
- P10632
- Uniprot Name
- Cytochrome P450 2C8
- Molecular Weight
- 55824.275 Da
References
- FDA Approved Drug Products: RUBRACA (rucaparib) tablets, for oral use (June 2022) [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Inhibitor
- General Function
- Steroid binding
- Specific Function
- UDPGT is of major importance in the conjugation and subsequent elimination of potentially toxic xenobiotics and endogenous compounds. This isoform glucuronidates bilirubin IX-alpha to form both the...
- Gene Name
- UGT1A1
- Uniprot ID
- P22309
- Uniprot Name
- UDP-glucuronosyltransferase 1-1
- Molecular Weight
- 59590.91 Da
References
- FDA Approved Drug Products: RUBRACA (rucaparib) tablets, for oral use (June 2022) [Link]
Transporters
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- SubstrateInhibitor
- General Function
- Xenobiotic-transporting atpase activity
- Specific Function
- Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells.
- Gene Name
- ABCB1
- Uniprot ID
- P08183
- Uniprot Name
- Multidrug resistance protein 1
- Molecular Weight
- 141477.255 Da
References
- FDA Approved Drug Products: RUBRACA (rucaparib) tablets, for oral use (June 2022) [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- SubstrateInhibitor
- General Function
- Xenobiotic-transporting atpase activity
- Specific Function
- High-capacity urate exporter functioning in both renal and extrarenal urate excretion. Plays a role in porphyrin homeostasis as it is able to mediates the export of protoporhyrin IX (PPIX) both fro...
- Gene Name
- ABCG2
- Uniprot ID
- Q9UNQ0
- Uniprot Name
- ATP-binding cassette sub-family G member 2
- Molecular Weight
- 72313.47 Da
References
- FDA Approved Drug Products: RUBRACA (rucaparib) tablets, for oral use (June 2022) [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Inhibitor
- General Function
- Monovalent cation:proton antiporter activity
- Specific Function
- Solute transporter for tetraethylammonium (TEA), 1-methyl-4-phenylpyridinium (MPP), cimetidine, N-methylnicotinamide (NMN), metformin, creatinine, guanidine, procainamide, topotecan, estrone sulfat...
- Gene Name
- SLC47A1
- Uniprot ID
- Q96FL8
- Uniprot Name
- Multidrug and toxin extrusion protein 1
- Molecular Weight
- 61921.585 Da
References
- Kristeleit R, Shapiro GI, Burris HA, Oza AM, LoRusso P, Patel MR, Domchek SM, Balmana J, Drew Y, Chen LM, Safra T, Montes A, Giordano H, Maloney L, Goble S, Isaacson J, Xiao J, Borrow J, Rolfe L, Shapira-Frommer R: A Phase I-II Study of the Oral PARP Inhibitor Rucaparib in Patients with Germline BRCA1/2-Mutated Ovarian Carcinoma or Other Solid Tumors. Clin Cancer Res. 2017 Aug 1;23(15):4095-4106. doi: 10.1158/1078-0432.CCR-16-2796. Epub 2017 Mar 6. [Article]
- FDA Approved Drug Products: RUBRACA (rucaparib) tablets, for oral use (June 2022) [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Inhibitor
- Curator comments
- Rucaparib has been shown to only inhibit the MATE-2K transporter.
- General Function
- Drug transmembrane transporter activity
- Specific Function
- Solute transporter for tetraethylammonium (TEA), 1-methyl-4-phenylpyridinium (MPP), cimetidine, N-methylnicotinamide, metformin, creatinine, guanidine, procainamide, topotecan, estrone sulfate, acy...
- Gene Name
- SLC47A2
- Uniprot ID
- Q86VL8
- Uniprot Name
- Multidrug and toxin extrusion protein 2
- Molecular Weight
- 65083.915 Da
References
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Inhibitor
- General Function
- Secondary active organic cation transmembrane transporter activity
- Specific Function
- Translocates a broad array of organic cations with various structures and molecular weights including the model compounds 1-methyl-4-phenylpyridinium (MPP), tetraethylammonium (TEA), N-1-methylnico...
- Gene Name
- SLC22A1
- Uniprot ID
- O15245
- Uniprot Name
- Solute carrier family 22 member 1
- Molecular Weight
- 61153.345 Da
References
- Jenner ZB, Sood AK, Coleman RL: Evaluation of rucaparib and companion diagnostics in the PARP inhibitor landscape for recurrent ovarian cancer therapy. Future Oncol. 2016 Jun;12(12):1439-56. doi: 10.2217/fon-2016-0002. Epub 2016 Apr 18. [Article]
- Dockery LE, Gunderson CC, Moore KN: Rucaparib: the past, present, and future of a newly approved PARP inhibitor for ovarian cancer. Onco Targets Ther. 2017 Jun 19;10:3029-3037. doi: 10.2147/OTT.S114714. eCollection 2017. [Article]
- FDA Approved Drug Products: RUBRACA (rucaparib) tablets, for oral use (June 2022) [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Inhibitor
- General Function
- Sodium-independent organic anion transmembrane transporter activity
- Specific Function
- Mediates the Na(+)-independent uptake of organic anions such as pravastatin, taurocholate, methotrexate, dehydroepiandrosterone sulfate, 17-beta-glucuronosyl estradiol, estrone sulfate, prostagland...
- Gene Name
- SLCO1B1
- Uniprot ID
- Q9Y6L6
- Uniprot Name
- Solute carrier organic anion transporter family member 1B1
- Molecular Weight
- 76447.99 Da
References
- FDA Approved Drug Products: RUBRACA (rucaparib) tablets, for oral use (June 2022) [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Inhibitor
- General Function
- Sodium-independent organic anion transmembrane transporter activity
- Specific Function
- Mediates the Na(+)-independent uptake of organic anions such as 17-beta-glucuronosyl estradiol, taurocholate, triiodothyronine (T3), leukotriene C4, dehydroepiandrosterone sulfate (DHEAS), methotre...
- Gene Name
- SLCO1B3
- Uniprot ID
- Q9NPD5
- Uniprot Name
- Solute carrier organic anion transporter family member 1B3
- Molecular Weight
- 77402.175 Da
References
- FDA Approved Drug Products: RUBRACA (rucaparib) tablets, for oral use (June 2022) [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Inhibitor
- General Function
- Sodium-independent organic anion transmembrane transporter activity
- Specific Function
- Involved in the renal elimination of endogenous and exogenous organic anions. Functions as organic anion exchanger when the uptake of one molecule of organic anion is coupled with an efflux of one ...
- Gene Name
- SLC22A6
- Uniprot ID
- Q4U2R8
- Uniprot Name
- Solute carrier family 22 member 6
- Molecular Weight
- 61815.78 Da
References
- FDA Approved Drug Products: RUBRACA (rucaparib) tablets, for oral use (June 2022) [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Inhibitor
- General Function
- Sodium-independent organic anion transmembrane transporter activity
- Specific Function
- Plays an important role in the excretion/detoxification of endogenous and exogenous organic anions, especially from the brain and kidney. Involved in the transport basolateral of steviol, fexofenad...
- Gene Name
- SLC22A8
- Uniprot ID
- Q8TCC7
- Uniprot Name
- Solute carrier family 22 member 8
- Molecular Weight
- 59855.585 Da
References
- FDA Approved Drug Products: RUBRACA (rucaparib) tablets, for oral use (June 2022) [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Inhibitor
- General Function
- Atpase activity, coupled to transmembrane movement of substances
- Specific Function
- May be an organic anion pump relevant to cellular detoxification.
- Gene Name
- ABCC4
- Uniprot ID
- O15439
- Uniprot Name
- Multidrug resistance-associated protein 4
- Molecular Weight
- 149525.33 Da
References
- FDA Approved Drug Products: RUBRACA (rucaparib) tablets, for oral use (June 2022) [Link]
Drug created at October 20, 2016 21:59 / Updated at January 13, 2023 10:08