Details of the Drug

General Information of Drug (ID: DM9PVX8)

Drug Name
Rucaparib
Synonyms
RUCAPARIB; 283173-50-2; Rubraca; AG-14447; UNII-8237F3U7EH; 8237F3U7EH; AK317822; 8-Fluoro-1,3,4,5-tetrahydro-2-[4-[(methylamino)methyl]phenyl]-6H-pyrrolo[4,3,2-ef][2]benzazepin-6-one; 8-FLUORO-2-(4-((METHYLAMINO)METHYL)PHENYL)-4,5-DIHYDRO-1H-AZEPINO[5,4,3-CD]INDOL-6(3H)-ONE; 6H-Pyrrolo[4,3,2-ef][2]benzazepin-6-one,8-fluoro-1,3,4,5-tetrahydro-2-[4-[(methylamino)methyl]phenyl]-; 8-fluoro-2-(4-methylaminomethyl-phenyl)-1,3,4,5-tetrahydro-azepino[5,4,3-cd]indol-6-one
Indication
Disease Entry ICD 11 Status REF
Ovarian cancer 2C73 Approved [1]
Drug Type
Small molecular drug
Structure
3D MOL 2D MOL
#Ro5 Violations (Lipinski): 0 Molecular Weight (mw) 323.4
Logarithm of the Partition Coefficient (xlogp) 2.5
Rotatable Bond Count (rotbonds) 3
Hydrogen Bond Donor Count (hbonddonor) 3
Hydrogen Bond Acceptor Count (hbondacc) 3
ADMET Property
Absorption AUC
The area under the plot of plasma concentration (AUC) of drug is 16900 mcgh/L []
Absorption Cmax
The maximum plasma concentration (Cmax) of drug is 1940 mcg/L []
Absorption Tmax
The time to maximum plasma concentration (Tmax) is 1.9 h []
Bioavailability
The bioavailability of drug is 36% []
Clearance
The clearance of drug is 15.3-79.2 L/h []
Half-life
The concentration or amount of drug in body reduced by one-half in 17 - 19 hours []
Metabolism
The drug is metabolized via the CYP2D6 and to a lesser extent by CYP1A2 and CYP3A4 []
Vd
The volume of distribution (Vd) of drug is 113-262 L []
Chemical Identifiers
Formula
C19H18FN3O
IUPAC Name
6-fluoro-2-[4-(methylaminomethyl)phenyl]-3,10-diazatricyclo[6.4.1.04,13]trideca-1,4,6,8(13)-tetraen-9-one
Canonical SMILES
CNCC1=CC=C(C=C1)C2=C3CCNC(=O)C4=C3C(=CC(=C4)F)N2
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)
InChIKey
HMABYWSNWIZPAG-UHFFFAOYSA-N
Cross-matching ID
PubChem CID
9931954
ChEBI ID
CHEBI:94311
CAS Number
283173-50-2
DrugBank ID
DB12332
TTD ID
D01SHZ
INTEDE ID
DR1449
ACDINA ID
D00609
Combinatorial Drugs (CBD) Click to Jump to the Detailed CBD Information of This Drug

Molecular Interaction Atlas of This Drug


Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
Poly [ADP-ribose] polymerase (PARP) TTEBCY8 NOUNIPROTAC Modulator [1]

Drug-Metabolizing Enzyme (DME)
DME Name DME ID UniProt ID MOA REF
Cytochrome P450 3A4 (CYP3A4) DE4LYSA CP3A4_HUMAN Substrate []
Cytochrome P450 2D6 (CYP2D6)
Main DME 		DECB0K3 CP2D6_HUMAN Substrate []
Cytochrome P450 1A2 (CYP1A2) DEJGDUW CP1A2_HUMAN Substrate [2]
Molecular Interaction Atlas (MIA) Jump to Detail Molecular Interaction Atlas of This Drug

Drug-Drug Interaction (DDI) Information of This Drug

Coadministration of a Drug Treating the Disease Different from Rucaparib (Comorbidity)
DDI Drug Name DDI Drug ID Severity Mechanism Comorbidity REF
Ivosidenib DM8S6T7 Major Increased risk of prolong QT interval by the combination of Rucaparib and Ivosidenib. Acute myeloid leukaemia [2A60] [3]
Oliceridine DM6MDCF Moderate Increased risk of prolong QT interval by the combination of Rucaparib and Oliceridine. Acute pain [MG31] [4]
Levalbuterol DM5YBO1 Moderate Increased risk of prolong QT interval by the combination of Rucaparib and Levalbuterol. Asthma [CA23] [5]
Troleandomycin DMUZNIG Moderate Decreased metabolism of Rucaparib caused by Troleandomycin mediated inhibition of CYP450 enzyme. Bacterial infection [1A00-1C4Z] [6]
Ag-221 DMS0ZBI Moderate Decreased clearance of Rucaparib due to the transporter inhibition by Ag-221. BCR-ABL1-negative chronic myeloid leukaemia [2A41] [7]
Pexidartinib DMS2J0Z Major Decreased metabolism of Rucaparib caused by Pexidartinib mediated inhibition of CYP450 enzyme. Bone/articular cartilage neoplasm [2F7B] [8]
Tazemetostat DMWP1BH Moderate Increased metabolism of Rucaparib caused by Tazemetostat mediated induction of CYP450 enzyme. Follicular lymphoma [2A80] [9]
Ripretinib DM958QB Moderate Decreased metabolism of Rucaparib caused by Ripretinib mediated inhibition of CYP450 enzyme. Gastrointestinal stromal tumour [2B5B] [7]
Avapritinib DMK2GZX Moderate Decreased metabolism of Rucaparib caused by Avapritinib mediated inhibition of CYP450 enzyme. Gastrointestinal stromal tumour [2B5B] [10]
Berotralstat DMWA2DZ Major Decreased clearance of Rucaparib due to the transporter inhibition by Berotralstat. Innate/adaptive immunodeficiency [4A00] [11]
Pemigatinib DM819JF Moderate Decreased metabolism of Rucaparib caused by Pemigatinib mediated inhibition of CYP450 enzyme. Liver cancer [2C12] [10]
Lurbinectedin DMEFRTZ Moderate Decreased metabolism of Rucaparib caused by Lurbinectedin mediated inhibition of CYP450 enzyme. Lung cancer [2C25] [12]
Pralsetinib DMWU0I2 Moderate Decreased metabolism of Rucaparib caused by Pralsetinib mediated inhibition of CYP450 enzyme. Lung cancer [2C25] [13]
Selpercatinib DMZR15V Moderate Decreased metabolism of Rucaparib caused by Selpercatinib mediated inhibition of CYP450 enzyme. Lung cancer [2C25] [10]
Ubrogepant DM749I3 Moderate Decreased metabolism of Rucaparib caused by Ubrogepant mediated inhibition of CYP450 enzyme. Migraine [8A80] [14]
Rimegepant DMHOAUG Moderate Decreased clearance of Rucaparib due to the transporter inhibition by Rimegepant. Migraine [8A80] [15]
Siponimod DM2R86O Major Additive immunosuppressive effects by the combination of Rucaparib and Siponimod. Multiple sclerosis [8A40] [7]
Ozanimod DMT6AM2 Major Increased risk of ventricular arrhythmias by the combination of Rucaparib and Ozanimod. Multiple sclerosis [8A40] [16]
Fedratinib DM4ZBK6 Moderate Decreased metabolism of Rucaparib caused by Fedratinib mediated inhibition of CYP450 enzyme. Myeloproliferative neoplasm [2A20] [10]
Macimorelin DMQYJIR Major Increased risk of prolong QT interval by the combination of Rucaparib and Macimorelin. Pituitary gland disorder [5A60-5A61] [17]
Lefamulin DME6G97 Moderate Decreased metabolism of Rucaparib caused by Lefamulin mediated inhibition of CYP450 enzyme. Pneumonia [CA40] [18]
Darolutamide DMV7YFT Moderate Decreased clearance of Rucaparib due to the transporter inhibition by Darolutamide. Prostate cancer [2C82] [19]
Voxelotor DMCS6M5 Moderate Decreased metabolism of Rucaparib caused by Voxelotor mediated inhibition of CYP450 enzyme. Sickle-cell disorder [3A51] [20]
Tedizolid DMG2SKR Moderate Decreased clearance of Rucaparib due to the transporter inhibition by Tedizolid. Skin and skin-structure infection [1F28-1G0Z] [10]
Larotrectinib DM26CQR Moderate Decreased clearance of Rucaparib due to the transporter inhibition by Larotrectinib. Solid tumour/cancer [2A00-2F9Z] [7]
Lusutrombopag DMH6IKO Moderate Decreased clearance of Rucaparib due to the transporter inhibition by Lusutrombopag. Thrombocytopenia [3B64] [6]
⏷ Show the Full List of 26 DDI Information of This Drug

Drug Inactive Ingredient(s) (DIG) and Formulation(s) of This Drug

DIG
DIG Name DIG ID PubChem CID Functional Classification
FD&C blue no. 1 E00263 19700 Colorant
FD&C blue no. 2 E00446 2723854 Colorant
Ferric hydroxide oxide yellow E00539 23320441 Colorant
Magnesium stearate E00208 11177 lubricant
Polyethylene glycol 4000 E00654 Not Available Coating agent; Diluent; Ointment base; Plasticizing agent; Solvent; Suppository base; lubricant
Polyvinyl alcohol E00666 Not Available Coating agent; Emulsion stabilizing agent; Film/Membrane-forming agent
Silicon dioxide E00670 Not Available Anticaking agent; Opacifying agent; Viscosity-controlling agent
Talc E00520 16211421 Anticaking agent; Diluent; Glidant; lubricant
Titanium dioxide E00322 26042 Coating agent; Colorant; Opacifying agent
Acid blue 9 aluminum lake E00583 56841154 Colorant
Colcothar yellow E00436 518696 Colorant
Hydrophobic colloidal silica E00285 24261 Anticaking agent; Emulsion stabilizing agent; Glidant; Suspending agent; Viscosity-controlling agent
Cellulose microcrystalline E00698 Not Available Adsorbent; Suspending agent; Diluent
⏷ Show the Full List of 13 Pharmaceutical Excipients of This Drug
Pharmaceutical Formulation
Formulation Name Drug Dosage Dosage Form Route
Rucaparib 200 mg tablet 200 mg Oral Tablet Oral
Rucaparib Camsylate eq 200mg base tablet eq 200mg base Tablet Oral
Rucaparib Camsylate eq 300mg base tablet eq 300mg base Tablet Oral
Rucaparib Camsylate eq 250mg base tablet eq 250mg base Tablet Oral
Rucaparib 300 mg tablet 300 mg Oral Tablet Oral
Rucaparib 250 mg tablet 250 mg Oral Tablet Oral
Jump to Detail Pharmaceutical Formulation Page of This Drug

References

1 2016 FDA drug approvals. Nat Rev Drug Discov. 2017 Feb 2;16(2):73-76.
2 Rucaparib: the past, present, and future of a newly approved PARP inhibitor for ovarian cancer. Onco Targets Ther. 2017 Jun 19;10:3029-3037.
3 Product Information. Tibsovo (ivosidenib). Agios Pharmaceuticals, Cambridge, MA.
4 Canadian Pharmacists Association.
5 Product Information. Arcapta Neohaler (indacaterol). Novartis Pharmaceuticals, East Hanover, NJ.
6 EMA. European Medicines Agency. European Union "EMA - List of medicines under additional monitoring.".
7 Cerner Multum, Inc. "Australian Product Information.".
8 Product Information. Turalio (pexidartinib). Daiichi Sankyo, Inc., Parsippany, NJ.
9 Product Information. Tazverik (tazemetostat). Epizyme, Inc, Cambridge, MA.
10 Cerner Multum, Inc. "UK Summary of Product Characteristics.".
11 Product Information. Orladeyo (berotralstat). BioCryst Pharmaceuticals Inc, Durham, NC.
12 Product Information. Zepzelca (lurbinectedin). Jazz Pharmaceuticals, Palo Alto, CA.
13 Product Information. Gavreto (pralsetinib). Blueprint Medicines Corporation, Cambridge, MA.
14 Product Information. Ubrelvy (ubrogepant). Allergan Inc, Irvine, CA.
15 Product Information. Nurtec ODT (rimegepant). Biohaven Pharmaceuticals, New Haven, CT.
16 Product Information. Zeposia (ozanimod). Celgene Corporation, Summit, NJ.
17 Product Information. Macrilen (macimorelin). Aeterna Zentaris, Charleston, SC.
18 Product Information. Xenleta (lefamulin). Nabriva Therapeutics US, Inc., King of Prussia, PA.
19 Product Information. Nubeqa (darolutamide). Bayer HealthCare Pharmaceuticals Inc., Whippany, NJ.
20 Product Information. Oxbryta (voxelotor). Global Blood Therapeutics, Inc., South San Francisco, CA.