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]

Affected Organisms

Humans and other mammals

ATC Code

L01XK03: Rucaparib

L01XK: Poly (ADP-ribose) polymerase (PARP) inhibitors

L01X: OTHER ANTINEOPLASTIC AGENTS

L01: ANTINEOPLASTIC AGENTS

L: ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS

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)

Hydrogen Bond Donor Count (hbonddonor)

Hydrogen Bond Acceptor Count (hbondacc)

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: CHEMBL1173055
CAS Number: 283173-50-2
UNII: 8237F3U7EH
DrugBank ID: DB12332
TTD ID: D01SHZ
INTEDE ID: DR1449
ACDINA ID: D00609

Drug-Molecule Activity Atlas (DMA)^NEW

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Drug Pharmacogenomic Perturbation (DPP)^NEW

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Drug ADMET Endpoint Profile (DAE)^NEW

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Combinatorial Drugs (CBD)

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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)

MIA Detail

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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]


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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

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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.