Rucaparib

Poly(ADP-Ribose) Polymerase Inhibitor — ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS

Key facts

Rucaparib is an onp drug in the Poly(ADP-Ribose) Polymerase Inhibitor class catalogued in DrugCentral. It was first approved by the FDA in 2016. Its mechanism of action is classified as Poly(ADP-Ribose) Polymerase Inhibitors. DrugCentral lists 17 molecular targets, including POLA1, PARP1 and PARP2. Recorded indications include Malignant tumor of ovary.

• Approval status: onp (first approved 2016 by the FDA).
• Drug class: Poly(ADP-Ribose) Polymerase Inhibitor.
• Mechanism of action: Poly(ADP-Ribose) Polymerase Inhibitors.
• Molecular targets: POLA1, PARP1, PARP2 and TNKS (17 listed in DrugCentral).
• Indications: Malignant tumor of ovary.
• ATC code: L01XK03 (Poly (ADP-ribose) polymerase (PARP) inhibitors).
• Molecular formula: C19H18FN3O; molecular weight 323.37 g/mol.

Indications & contraindications

Drug–disease relationships curated by DrugCentral (OMOP / SNOMED concepts).

Indications (1)

• Malignant tumor of ovary

Mechanism & targets

• Mechanism of action (MoA): Poly(ADP-Ribose) Polymerase Inhibitors
• Established pharmacologic class: Poly(ADP-Ribose) Polymerase Inhibitor

Molecular targets (17)

Target	Gene	Action	Activity
DNA polymerase alpha catalytic subunit	POLA1	unknown	IC50 9.40
Poly [ADP-ribose] polymerase 1	PARP1	inhibitor	IC50 8.50
Poly [ADP-ribose] polymerase 2	PARP2	inhibitor	IC50 7.55
Tankyrase-1	TNKS	inhibitor	IC50 6.84
Cyclin-dependent kinase 16	CDK16	unknown	IC50 6.42
Poly [ADP-ribose] polymerase 3	PARP3	inhibitor	IC50 6.39
Serine/threonine-protein kinase pim-3	PIM3	unknown	IC50 6.36
Poly [ADP-ribose] polymerase 10	PARP10	inhibitor	IC50 6.25
Dual specificity tyrosine-phosphorylation-regulated kinase 1B	DYRK1B	unknown	IC50 6.13
Poly [ADP-ribose] polymerase 4	PARP4	inhibitor	IC50 6.08
Tankyrase-2	TNKS2	inhibitor	IC50 6.05
Dual specificity tyrosine-phosphorylation-regulated kinase 1A	DYRK1A	unknown	IC50 5.63
Mono [ADP-ribose] polymerase PARP16	PARP16	unknown	Kd 5.54
Poly [ADP-ribose] polymerase 9	PARP9	unknown	Kd 5.51
Poly [ADP-ribose] polymerase 12	PARP12	inhibitor	IC50 5.18
Poly [ADP-ribose] polymerase 14	PARP14	inhibitor	IC50 5.05
Poly [ADP-ribose] polymerase 15	PARP15	inhibitor	IC50 4.49

Regulatory approvals (2)

Date	Agency	Marketed as	Applicant	Orphan
2018-05-24	EMA	—	Clovis Oncology UK Limited	Yes
2016-12-19	FDA	—	Clovis Oncology, Inc.

ATC classification

ATC code	Therapeutic hierarchy
L01XK03	ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS › ANTINEOPLASTIC AGENTS › OTHER ANTINEOPLASTIC AGENTS › Poly (ADP-ribose) polymerase (PARP) inhibitors

Pharmacogenomics

Drug-label and guideline annotations from PharmGKB and CPIC.

• EMA label: BRCA1, BRCA2 · Testing Required
• EMA label: CYP1A2, CYP2D6 · No Clinical PGx
• FDA label: BRCA1, BRCA2 · Testing Required
• FDA label: CYP1A2, CYP2D6 · No Clinical PGx
• HCSC label

Reported adverse-event signals

Strongest FDA FAERS disproportionality signals (log-likelihood ratio). A signal is a statistical association in spontaneous reports, not proof that the drug causes the event.

MedDRA term	LLR
Malignant neoplasm progression	1720.2
Carbohydrate antigen 125 increased	1718.6
Fatigue	1486.4
Nausea	1408.0
Dysgeusia	927.6
Product dose omission issue	765.9
Tumour marker increased	584.9
Adverse event	496.7
Constipation	449.2
Decreased appetite	404.3
Platelet count decreased	337.8
Ovarian cancer recurrent	305.0

Chemical structure

• Molecular formula: C₁₉H₁₈FN₃O
• Molecular weight: 323.37 g/mol
• CAS number: —
• InChIKey: HMABYWSNWIZPAG-UHFFFAOYSA-N
• PubChem CID: 9931954

CNCC1=CC=C(C=C1)C1=C2CCNC(=O)C3=CC(F)=CC(N1)=C23

Frequently asked questions

Answers are generated from the structured data on this page, not written by hand.

What is Rucaparib used for?

DrugCentral lists the following indications for Rucaparib: Malignant tumor of ovary.

How does Rucaparib work?

Rucaparib is classified as Poly(ADP-Ribose) Polymerase Inhibitors; its molecular targets in DrugCentral include POLA1, PARP1 (inhibitor), PARP2 (inhibitor) and TNKS (inhibitor).

When was Rucaparib first approved?

Rucaparib was first approved by the FDA in 2016.

What drug class does Rucaparib belong to?

Rucaparib is in the Poly(ADP-Ribose) Polymerase Inhibitor class.

What is the chemical formula of Rucaparib?

Rucaparib has the molecular formula C19H18FN3O and a molecular weight of 323.37 g/mol.

Sources

• DrugCentral drug card 5203 — structure, indications, targets, approvals, pharmacologic classes (CC BY-SA 4.0)
• ChEMBL CHEMBL1173055 — compound record and bioactivity
• PubChem CID 9931954 — chemical identifiers
• DrugBank DB12332 — drug record
• FDA UNII 8237F3U7EH — substance identity
• DailyMed: FDA labels for Rucaparib — current prescribing information (label search)
• UniProt P09884 (POLA1) — target protein
• UniProt P09874 (PARP1) — target protein
• UniProt Q9UGN5 (PARP2) — target protein
• UniProt O95271 (TNKS) — target protein
• UniProt Q00536 (CDK16) — target protein
• UniProt Q9Y6F1 (PARP3) — target protein
• FDA Adverse Event Reporting System (openFDA FAERS) — adverse-event signals, as aggregated by DrugCentral
• PharmGKB / CPIC — pharmacogenomic label annotations

How this page is built: methodology · editorial policy & corrections.