rucaparib 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definition	Drug id	CAS RN
poly-ADP-ribose polymerase inhibitors	5203	283173-50-2

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: rucaparib rucaparib camsylate AG-14447 rucaparib phosphate AG-14699 AG014699 PF01367338 PF-1367338-BW CO-338 rubraca rucaparib camphorsulfonate	Rucaparib is an inhibitor of poly (ADP-ribose) polymerase (PARP) enzymes, including PARP-1, PARP-2, and PARP-3, which play a role in DNA repair. In vitro studies have shown that rucaparib-induced cytotoxicity may involve inhibition of PARP enzymatic activity and increased formation of PARP-DNA complexes resulting in DNA damage, apoptosis, and cell death. Increased rucaparib-induced cytotoxicity was observed in tumor cell lines with deficiencies in BRCA1/2 and other DNA repair genes. Rucaparib has been shown to decrease tumor growth in mouse xenograft models of human cancer with or without deficiencies in BRCA. Molecular weight: 323.37 Formula: C19H18FN3O CLOGP: 3.01 LIPINSKI: 0 HAC: 4 HDO: 3 TPSA: 56.92 ALOGS: -4.45 ROTB: 3 Status: ONP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

rucaparib
rucaparib camsylate
AG-14447
rucaparib phosphate
AG-14699
AG014699
PF01367338
PF-1367338-BW
CO-338
rubraca
rucaparib camphorsulfonate

Rucaparib is an inhibitor of poly (ADP-ribose) polymerase (PARP) enzymes, including PARP-1, PARP-2, and PARP-3, which play a role in DNA repair. In vitro studies have shown that rucaparib-induced cytotoxicity may involve inhibition of PARP enzymatic activity and increased formation of PARP-DNA complexes resulting in DNA damage, apoptosis, and cell death. Increased rucaparib-induced cytotoxicity was observed in tumor cell lines with deficiencies in BRCA1/2 and other DNA repair genes. Rucaparib has been shown to decrease tumor growth in mouse xenograft models of human cancer with or without deficiencies in BRCA.

Molecular weight: 323.37
Formula: C19H18FN3O
CLOGP: 3.01
LIPINSKI: 0
HAC: 4
HDO: 3
TPSA: 56.92
ALOGS: -4.45
ROTB: 3

Status: ONP

Legend:
OFP - off patent
OFM - off market
ONP - on patent

Drug dosage:

None

ADMET properties:

Property	Value	Reference
Vd (Volume of distribution)	3.28 L/kg	Lombardo F, Berellini G, Obach RS
CL (Clearance)	4.31 mL/min/kg	Lombardo F, Berellini G, Obach RS
t_half (Half-life)	16.60 hours	Lombardo F, Berellini G, Obach RS
S (Water solubility)	1 mg/mL	Bocci G, Oprea TI, Benet LZ
BDDCS (Biopharmaceutical Drug Disposition Classification System)	2	Bocci G, Oprea TI, Benet LZ

Approvals:

Date	Agency	Company	Orphan
May 24, 2018	EMA	Clovis Oncology UK Limited
Dec. 19, 2016	FDA	Clovis Oncology, Inc.

FDA Adverse Event Reporting System (Female)

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Malignant neoplasm progression	1699.83	36.15	725	20134	81396	63386767
Carbohydrate antigen 125 increased	1524.86	36.15	315	20544	2501	63465662
Fatigue	1283.91	36.15	1500	19359	886528	62581635
Nausea	1189.67	36.15	1417	19442	853054	62615109
Dysgeusia	880.74	36.15	387	20472	46323	63421840
Product dose omission issue	713.55	36.15	599	20260	233714	63234449
Tumour marker increased	531.86	36.15	150	20709	4765	63463398
Adverse event	461.22	36.15	283	20576	67276	63400887
Decreased appetite	428.72	36.15	467	20392	250585	63217578
Constipation	418.51	36.15	438	20421	224505	63243658
Taste disorder	374.34	36.15	148	20711	13514	63454649
Underdose	371.55	36.15	181	20678	27275	63440888
Platelet count decreased	352.26	36.15	297	20562	115825	63352338
Accidental underdose	304.36	36.15	67	20792	736	63467427
Ovarian cancer recurrent	288.60	36.15	67	20792	950	63467213
Full blood count abnormal	226.75	36.15	137	20722	31580	63436583
Photosensitivity reaction	212.25	36.15	102	20757	14892	63453271
Prescribed underdose	196.27	36.15	122	20737	29567	63438596
Red blood cell count decreased	181.81	36.15	131	20728	40514	63427649
Renal function test abnormal	164.33	36.15	57	20802	3596	63464567
Vomiting	158.88	36.15	472	20387	559145	62909018
Anaemia	155.52	36.15	315	20544	293115	63175048
Sunburn	154.98	36.15	51	20808	2737	63465426
Asthenia	150.54	36.15	365	20494	383239	63084924
Blood creatinine increased	148.49	36.15	163	20696	87681	63380482
Drug ineffective	127.71	36.15	95	20764	1044670	62423493
Haemoglobin decreased	126.08	36.15	194	20665	145291	63322872
Condition aggravated	118.19	36.15	3	20856	402214	63065949
Therapy partial responder	108.39	36.15	58	20801	10600	63457563
Liver function test increased	107.69	36.15	88	20771	32723	63435440
Blood magnesium decreased	107.35	36.15	62	20797	13136	63455027
Abdominal pain upper	102.56	36.15	216	20643	206228	63261935
Abdominal distension	102.35	36.15	134	20725	86481	63381682
White blood cell count decreased	90.31	36.15	163	20696	138941	63329222
Laboratory test abnormal	90.04	36.15	73	20786	26839	63441324
Abdominal pain	88.09	36.15	253	20606	293203	63174960
Neuropathy peripheral	79.96	36.15	138	20721	113529	63354634
Flatulence	79.68	36.15	76	20783	34626	63433537
Drug hypersensitivity	79.29	36.15	6	20853	310681	63157482
Intentional underdose	71.84	36.15	26	20833	1856	63466307
Diarrhoea	71.32	36.15	439	20420	714927	62753236
Drug interaction	59.66	36.15	4	20855	229127	63239036
Early satiety	54.47	36.15	18	20841	978	63467185
Swelling	54.38	36.15	12	20847	275366	63192797
Dyspepsia	51.89	36.15	108	20751	102088	63366075
Pneumonia	49.94	36.15	46	20813	456721	63011442
Arthropathy	48.92	36.15	9	20850	234783	63233380
Joint swelling	46.32	36.15	25	20834	327641	63140522
Intestinal obstruction	41.52	36.15	51	20808	30848	63437315
General physical health deterioration	41.35	36.15	8	20851	201394	63266769
Discomfort	40.57	36.15	4	20855	167370	63300793
Fall	37.78	36.15	44	20815	392290	63075873
Small intestinal obstruction	36.21	36.15	37	20822	18300	63449863

FDA Adverse Event Reporting System (Male)

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Malignant neoplasm progression	48.41	40.36	22	360	88024	34868525
Product use in unapproved indication	45.28	40.36	23	359	117476	34839073

FDA Adverse Event Reporting System (Geriatric)

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Carbohydrate antigen 125 increased	941.67	36.76	180	12860	2004	79729344
Fatigue	937.82	36.76	934	12106	928793	78802555
Nausea	762.01	36.76	849	12191	956347	78775001
Dysgeusia	606.35	36.76	257	12783	56920	79674428
Malignant neoplasm progression	490.14	36.76	294	12746	135696	79595652
Product dose omission issue	462.35	36.76	356	12684	247181	79484167
Tumour marker increased	427.47	36.76	106	12934	4166	79727182
Constipation	298.20	36.76	294	12746	282756	79448592
Underdose	295.45	36.76	132	12908	33019	79698329
Decreased appetite	279.01	36.76	310	12730	342108	79389240
Accidental underdose	255.59	36.76	52	12988	810	79730538
Taste disorder	204.23	36.76	82	12958	15741	79715607
Prescribed underdose	196.21	36.76	96	12944	29418	79701930
Adverse event	160.88	36.76	108	12932	60106	79671242
Platelet count decreased	154.17	36.76	174	12866	194490	79536858
Ovarian cancer recurrent	150.83	36.76	30	13010	414	79730934
Vomiting	126.95	36.76	312	12728	665516	79065832
Full blood count abnormal	121.23	36.76	78	12962	40396	79690952
Red blood cell count decreased	116.19	36.76	87	12953	57426	79673922
Photosensitivity reaction	112.00	36.76	59	12981	21068	79710280
Renal function test abnormal	104.94	36.76	37	13003	4961	79726387
Sunburn	102.45	36.76	34	13006	3799	79727549
Anaemia	99.25	36.76	222	12818	444793	79286555
Asthenia	95.39	36.76	238	12802	511451	79219897
Abdominal pain upper	84.84	36.76	140	12900	223679	79507669
Blood magnesium decreased	84.37	36.76	45	12995	16467	79714881
Liver function test increased	79.93	36.76	60	12980	39713	79691635
Haemoglobin decreased	75.01	36.76	132	12908	221987	79509361
Diarrhoea	68.17	36.76	304	12736	880185	78851163
Condition aggravated	66.10	36.76	4	13036	501120	79230228
Abdominal pain	65.01	36.76	174	12866	389395	79341953
Abdominal distension	58.12	36.76	84	12956	119566	79611782
Drug interaction	55.70	36.76	3	13037	415180	79316168
Drug ineffective	54.67	36.76	58	12982	1080855	78650493
White blood cell count decreased	53.59	36.76	104	12936	188184	79543164
Flatulence	51.56	36.76	48	12992	42676	79688672
Blood creatinine increased	50.81	36.76	91	12949	154966	79576382
Abdominal discomfort	49.04	36.76	119	12921	250608	79480740
Intentional underdose	47.79	36.76	17	13023	2337	79729011
Neuropathy peripheral	47.67	36.76	84	12956	141221	79590127
Laboratory test abnormal	44.88	36.76	37	13003	28011	79703337
Therapy partial responder	43.54	36.76	30	13010	17367	79713981
Drug hypersensitivity	37.59	36.76	3	13037	298913	79432435

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
ATC	L01XK03	ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS ANTINEOPLASTIC AGENTS OTHER ANTINEOPLASTIC AGENTS Poly (ADP-ribose) polymerase (PARP) inhibitors
MeSH PA	D000970	Antineoplastic Agents
MeSH PA	D004791	Enzyme Inhibitors
MeSH PA	D000067856	Poly(ADP-ribose) Polymerase Inhibitors
FDA MoA	N0000191622	Poly(ADP-Ribose) Polymerase Inhibitors
FDA EPC	N0000191623	Poly(ADP-Ribose) Polymerase Inhibitor
CHEBI has role	CHEBI:35610	antineoplastic agents
CHEBI has role	CHEBI:62913	PARP

Drug Use | Suggest Off label Use Form| |View source of the data|

Disease	Relation	SNOMED_ID	DOID
Malignant tumor of ovary	indication	363443007	DOID:2394

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	11.08	acidic
pKa2	13.73	acidic
pKa3	9.45	Basic

Orange Book patent data (new drug applications)

Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Patent number	Patent expiration date	Patent use
EQ 200MG BASE	RUBRACA	ZR PHARMA	N209115	Dec. 19, 2016	RX	TABLET	ORAL	7351701	July 23, 2024	A METHOD FOR TREATING EPITHELIAL OVARIAN, FALLOPIAN TUBE, OR PRIMARY PERITONEAL CANCER, WHEREIN THE CANCER IS ASSOCIATED WITH A DELETERIOUS BRCA MUTATION
EQ 200MG BASE	RUBRACA	ZR PHARMA	N209115	Dec. 19, 2016	RX	TABLET	ORAL	7351701	July 23, 2024	A METHOD FOR TREATING METASTATIC CASTRATION-RESISTANT PROSTATE CANCER (MCRPC), WHEREIN THE CANCER IS ASSOCIATED WITH A DELETERIOUS BRCA-MUTATION
EQ 200MG BASE	RUBRACA	ZR PHARMA	N209115	Dec. 19, 2016	RX	TABLET	ORAL	7351701	July 23, 2024	A METHOD FOR TREATING OVARIAN CANCER BY ADMINISTERING RUCAPARIB, WHEREIN THE CANCER IS ASSOCIATED WITH A DELETERIOUS BRCA MUTATION
EQ 200MG BASE	RUBRACA	ZR PHARMA	N209115	Dec. 19, 2016	RX	TABLET	ORAL	7531530	July 23, 2024	A METHOD FOR TREATING EPITHELIAL OVARIAN, FALLOPIAN TUBE, OR PRIMARY PERITONEAL CANCER, WHEREIN THE CANCER IS ASSOCIATED WITH A DELETERIOUS BRCA MUTATION
EQ 200MG BASE	RUBRACA	ZR PHARMA	N209115	Dec. 19, 2016	RX	TABLET	ORAL	7531530	July 23, 2024	A METHOD FOR TREATING METASTATIC CASTRATION-RESISTANT PROSTATE CANCER (MCRPC), WHEREIN THE CANCER IS ASSOCIATED WITH A DELETERIOUS BRCA-MUTATION
EQ 200MG BASE	RUBRACA	ZR PHARMA	N209115	Dec. 19, 2016	RX	TABLET	ORAL	7531530	July 23, 2024	A METHOD FOR TREATING OVARIAN CANCER BY ADMINISTERING RUCAPARIB, WHEREIN THE CANCER IS ASSOCIATED WITH A DELETERIOUS BRCA MUTATION
EQ 250MG BASE	RUBRACA	ZR PHARMA	N209115	May 1, 2017	RX	TABLET	ORAL	7351701	July 23, 2024	A METHOD FOR TREATING EPITHELIAL OVARIAN, FALLOPIAN TUBE, OR PRIMARY PERITONEAL CANCER, WHEREIN THE CANCER IS ASSOCIATED WITH A DELETERIOUS BRCA MUTATION
EQ 250MG BASE	RUBRACA	ZR PHARMA	N209115	May 1, 2017	RX	TABLET	ORAL	7351701	July 23, 2024	A METHOD FOR TREATING METASTATIC CASTRATION-RESISTANT PROSTATE CANCER (MCRPC), WHEREIN THE CANCER IS ASSOCIATED WITH A DELETERIOUS BRCA-MUTATION
EQ 250MG BASE	RUBRACA	ZR PHARMA	N209115	May 1, 2017	RX	TABLET	ORAL	7351701	July 23, 2024	A METHOD FOR TREATING OVARIAN CANCER BY ADMINISTERING RUCAPARIB, WHEREIN THE CANCER IS ASSOCIATED WITH A DELETERIOUS BRCA MUTATION
EQ 250MG BASE	RUBRACA	ZR PHARMA	N209115	May 1, 2017	RX	TABLET	ORAL	7531530	July 23, 2024	A METHOD FOR TREATING EPITHELIAL OVARIAN, FALLOPIAN TUBE, OR PRIMARY PERITONEAL CANCER, WHEREIN THE CANCER IS ASSOCIATED WITH A DELETERIOUS BRCA MUTATION
EQ 250MG BASE	RUBRACA	ZR PHARMA	N209115	May 1, 2017	RX	TABLET	ORAL	7531530	July 23, 2024	A METHOD FOR TREATING METASTATIC CASTRATION-RESISTANT PROSTATE CANCER (MCRPC), WHEREIN THE CANCER IS ASSOCIATED WITH A DELETERIOUS BRCA-MUTATION
EQ 250MG BASE	RUBRACA	ZR PHARMA	N209115	May 1, 2017	RX	TABLET	ORAL	7531530	July 23, 2024	A METHOD FOR TREATING OVARIAN CANCER BY ADMINISTERING RUCAPARIB, WHEREIN THE CANCER IS ASSOCIATED WITH A DELETERIOUS BRCA MUTATION
EQ 300MG BASE	RUBRACA	ZR PHARMA	N209115	Dec. 19, 2016	RX	TABLET	ORAL	7351701	July 23, 2024	A METHOD FOR TREATING EPITHELIAL OVARIAN, FALLOPIAN TUBE, OR PRIMARY PERITONEAL CANCER, WHEREIN THE CANCER IS ASSOCIATED WITH A DELETERIOUS BRCA MUTATION
EQ 300MG BASE	RUBRACA	ZR PHARMA	N209115	Dec. 19, 2016	RX	TABLET	ORAL	7351701	July 23, 2024	A METHOD FOR TREATING METASTATIC CASTRATION-RESISTANT PROSTATE CANCER (MCRPC), WHEREIN THE CANCER IS ASSOCIATED WITH A DELETERIOUS BRCA-MUTATION
EQ 300MG BASE	RUBRACA	ZR PHARMA	N209115	Dec. 19, 2016	RX	TABLET	ORAL	7351701	July 23, 2024	A METHOD FOR TREATING OVARIAN CANCER BY ADMINISTERING RUCAPARIB, WHEREIN THE CANCER IS ASSOCIATED WITH A DELETERIOUS BRCA MUTATION
EQ 300MG BASE	RUBRACA	ZR PHARMA	N209115	Dec. 19, 2016	RX	TABLET	ORAL	7531530	July 23, 2024	A METHOD FOR TREATING EPITHELIAL OVARIAN, FALLOPIAN TUBE, OR PRIMARY PERITONEAL CANCER, WHEREIN THE CANCER IS ASSOCIATED WITH A DELETERIOUS BRCA MUTATION
EQ 300MG BASE	RUBRACA	ZR PHARMA	N209115	Dec. 19, 2016	RX	TABLET	ORAL	7531530	July 23, 2024	A METHOD FOR TREATING METASTATIC CASTRATION-RESISTANT PROSTATE CANCER (MCRPC), WHEREIN THE CANCER IS ASSOCIATED WITH A DELETERIOUS BRCA-MUTATION
EQ 300MG BASE	RUBRACA	ZR PHARMA	N209115	Dec. 19, 2016	RX	TABLET	ORAL	7531530	July 23, 2024	A METHOD FOR TREATING OVARIAN CANCER BY ADMINISTERING RUCAPARIB, WHEREIN THE CANCER IS ASSOCIATED WITH A DELETERIOUS BRCA MUTATION
EQ 200MG BASE	RUBRACA	ZR PHARMA	N209115	Dec. 19, 2016	RX	TABLET	ORAL	8071579	Aug. 12, 2027	A METHOD FOR TREATING EPITHELIAL OVARIAN, FALLOPIAN TUBE, OR PRIMARY PERITONEAL CANCER, WHEREIN THE CANCER IS ASSOCIATED WITH A DELETERIOUS BRCA MUTATION
EQ 200MG BASE	RUBRACA	ZR PHARMA	N209115	Dec. 19, 2016	RX	TABLET	ORAL	8071579	Aug. 12, 2027	A METHOD FOR TREATING METASTATIC CASTRATION-RESISTANT PROSTATE CANCER (MCRPC), WHEREIN THE CANCER IS ASSOCIATED WITH A DELETERIOUS BRCA-MUTATION
EQ 200MG BASE	RUBRACA	ZR PHARMA	N209115	Dec. 19, 2016	RX	TABLET	ORAL	8071579	Aug. 12, 2027	A METHOD FOR TREATING OVARIAN CANCER BY ADMINISTERING RUCAPARIB, WHEREIN THE CANCER IS ASSOCIATED WITH A DELETERIOUS BRCA MUTATION
EQ 200MG BASE	RUBRACA	ZR PHARMA	N209115	Dec. 19, 2016	RX	TABLET	ORAL	8143241	Aug. 12, 2027	A METHOD FOR TREATING EPITHELIAL OVARIAN, FALLOPIAN TUBE, OR PRIMARY PERITONEAL CANCER, WHEREIN THE CANCER IS ASSOCIATED WITH A DELETERIOUS BRCA MUTATION
EQ 200MG BASE	RUBRACA	ZR PHARMA	N209115	Dec. 19, 2016	RX	TABLET	ORAL	8143241	Aug. 12, 2027	A METHOD FOR TREATING METASTATIC CASTRATION-RESISTANT PROSTATE CANCER (MCRPC), WHEREIN THE CANCER IS ASSOCIATED WITH A DELETERIOUS BRCA-MUTATION
EQ 200MG BASE	RUBRACA	ZR PHARMA	N209115	Dec. 19, 2016	RX	TABLET	ORAL	8143241	Aug. 12, 2027	A METHOD FOR TREATING OVARIAN CANCER BY ADMINISTERING RUCAPARIB, WHEREIN THE CANCER IS ASSOCIATED WITH A DELETERIOUS BRCA MUTATION
EQ 250MG BASE	RUBRACA	ZR PHARMA	N209115	May 1, 2017	RX	TABLET	ORAL	8071579	Aug. 12, 2027	A METHOD FOR TREATING EPITHELIAL OVARIAN, FALLOPIAN TUBE, OR PRIMARY PERITONEAL CANCER, WHEREIN THE CANCER IS ASSOCIATED WITH A DELETERIOUS BRCA MUTATION
EQ 250MG BASE	RUBRACA	ZR PHARMA	N209115	May 1, 2017	RX	TABLET	ORAL	8071579	Aug. 12, 2027	A METHOD FOR TREATING METASTATIC CASTRATION-RESISTANT PROSTATE CANCER (MCRPC), WHEREIN THE CANCER IS ASSOCIATED WITH A DELETERIOUS BRCA-MUTATION
EQ 250MG BASE	RUBRACA	ZR PHARMA	N209115	May 1, 2017	RX	TABLET	ORAL	8071579	Aug. 12, 2027	A METHOD FOR TREATING OVARIAN CANCER BY ADMINISTERING RUCAPARIB, WHEREIN THE CANCER IS ASSOCIATED WITH A DELETERIOUS BRCA MUTATION
EQ 250MG BASE	RUBRACA	ZR PHARMA	N209115	May 1, 2017	RX	TABLET	ORAL	8143241	Aug. 12, 2027	A METHOD FOR TREATING EPITHELIAL OVARIAN, FALLOPIAN TUBE, OR PRIMARY PERITONEAL CANCER, WHEREIN THE CANCER IS ASSOCIATED WITH A DELETERIOUS BRCA MUTATION
EQ 250MG BASE	RUBRACA	ZR PHARMA	N209115	May 1, 2017	RX	TABLET	ORAL	8143241	Aug. 12, 2027	A METHOD FOR TREATING METASTATIC CASTRATION-RESISTANT PROSTATE CANCER (MCRPC), WHEREIN THE CANCER IS ASSOCIATED WITH A DELETERIOUS BRCA-MUTATION
EQ 250MG BASE	RUBRACA	ZR PHARMA	N209115	May 1, 2017	RX	TABLET	ORAL	8143241	Aug. 12, 2027	A METHOD FOR TREATING OVARIAN CANCER BY ADMINISTERING RUCAPARIB, WHEREIN THE CANCER IS ASSOCIATED WITH A DELETERIOUS BRCA MUTATION
EQ 300MG BASE	RUBRACA	ZR PHARMA	N209115	Dec. 19, 2016	RX	TABLET	ORAL	8071579	Aug. 12, 2027	A METHOD FOR TREATING EPITHELIAL OVARIAN, FALLOPIAN TUBE, OR PRIMARY PERITONEAL CANCER, WHEREIN THE CANCER IS ASSOCIATED WITH A DELETERIOUS BRCA MUTATION
EQ 300MG BASE	RUBRACA	ZR PHARMA	N209115	Dec. 19, 2016	RX	TABLET	ORAL	8071579	Aug. 12, 2027	A METHOD FOR TREATING METASTATIC CASTRATION-RESISTANT PROSTATE CANCER (MCRPC), WHEREIN THE CANCER IS ASSOCIATED WITH A DELETERIOUS BRCA-MUTATION
EQ 300MG BASE	RUBRACA	ZR PHARMA	N209115	Dec. 19, 2016	RX	TABLET	ORAL	8071579	Aug. 12, 2027	A METHOD FOR TREATING OVARIAN CANCER BY ADMINISTERING RUCAPARIB, WHEREIN THE CANCER IS ASSOCIATED WITH A DELETERIOUS BRCA MUTATION
EQ 300MG BASE	RUBRACA	ZR PHARMA	N209115	Dec. 19, 2016	RX	TABLET	ORAL	8143241	Aug. 12, 2027	A METHOD FOR TREATING EPITHELIAL OVARIAN, FALLOPIAN TUBE, OR PRIMARY PERITONEAL CANCER, WHEREIN THE CANCER IS ASSOCIATED WITH A DELETERIOUS BRCA MUTATION
EQ 300MG BASE	RUBRACA	ZR PHARMA	N209115	Dec. 19, 2016	RX	TABLET	ORAL	8143241	Aug. 12, 2027	A METHOD FOR TREATING METASTATIC CASTRATION-RESISTANT PROSTATE CANCER (MCRPC), WHEREIN THE CANCER IS ASSOCIATED WITH A DELETERIOUS BRCA-MUTATION
EQ 300MG BASE	RUBRACA	ZR PHARMA	N209115	Dec. 19, 2016	RX	TABLET	ORAL	8143241	Aug. 12, 2027	A METHOD FOR TREATING OVARIAN CANCER BY ADMINISTERING RUCAPARIB, WHEREIN THE CANCER IS ASSOCIATED WITH A DELETERIOUS BRCA MUTATION
EQ 200MG BASE	RUBRACA	ZR PHARMA	N209115	Dec. 19, 2016	RX	TABLET	ORAL	9861638	Feb. 10, 2031	A METHOD FOR TREATING EPITHELIAL OVARIAN, FALLOPIAN TUBE, OR PRIMARY PERITONEAL CANCER, WHEREIN THE CANCER IS ASSOCIATED WITH A DELETERIOUS BRCA MUTATION
EQ 200MG BASE	RUBRACA	ZR PHARMA	N209115	Dec. 19, 2016	RX	TABLET	ORAL	9861638	Feb. 10, 2031	A METHOD FOR TREATING OVARIAN CANCER BY ADMINISTERING RUCAPARIB, WHEREIN THE CANCER IS ASSOCIATED WITH A DELETERIOUS BRCA MUTATION
EQ 250MG BASE	RUBRACA	ZR PHARMA	N209115	May 1, 2017	RX	TABLET	ORAL	9861638	Feb. 10, 2031	A METHOD FOR TREATING EPITHELIAL OVARIAN, FALLOPIAN TUBE, OR PRIMARY PERITONEAL CANCER, WHEREIN THE CANCER IS ASSOCIATED WITH A DELETERIOUS BRCA MUTATION
EQ 250MG BASE	RUBRACA	ZR PHARMA	N209115	May 1, 2017	RX	TABLET	ORAL	9861638	Feb. 10, 2031	A METHOD FOR TREATING OVARIAN CANCER BY ADMINISTERING RUCAPARIB, WHEREIN THE CANCER IS ASSOCIATED WITH A DELETERIOUS BRCA MUTATION
EQ 300MG BASE	RUBRACA	ZR PHARMA	N209115	Dec. 19, 2016	RX	TABLET	ORAL	9861638	Feb. 10, 2031	A METHOD FOR TREATING EPITHELIAL OVARIAN, FALLOPIAN TUBE, OR PRIMARY PERITONEAL CANCER, WHEREIN THE CANCER IS ASSOCIATED WITH A DELETERIOUS BRCA MUTATION
EQ 300MG BASE	RUBRACA	ZR PHARMA	N209115	Dec. 19, 2016	RX	TABLET	ORAL	9861638	Feb. 10, 2031	A METHOD FOR TREATING OVARIAN CANCER BY ADMINISTERING RUCAPARIB, WHEREIN THE CANCER IS ASSOCIATED WITH A DELETERIOUS BRCA MUTATION
EQ 200MG BASE	RUBRACA	ZR PHARMA	N209115	Dec. 19, 2016	RX	TABLET	ORAL	8859562	Aug. 4, 2031	A METHOD FOR TREATING EPITHELIAL OVARIAN, FALLOPIAN TUBE, OR PRIMARY PERITONEAL CANCER, WHEREIN THE CANCER IS ASSOCIATED WITH A DELETERIOUS BRCA MUTATION
EQ 200MG BASE	RUBRACA	ZR PHARMA	N209115	Dec. 19, 2016	RX	TABLET	ORAL	8859562	Aug. 4, 2031	A METHOD FOR TREATING METASTATIC CASTRATION-RESISTANT PROSTATE CANCER (MCRPC), WHEREIN THE CANCER IS ASSOCIATED WITH A DELETERIOUS BRCA-MUTATION
EQ 200MG BASE	RUBRACA	ZR PHARMA	N209115	Dec. 19, 2016	RX	TABLET	ORAL	8859562	Aug. 4, 2031	A METHOD FOR TREATING OVARIAN CANCER BY ADMINISTERING RUCAPARIB, WHEREIN THE CANCER IS ASSOCIATED WITH A DELETERIOUS BRCA MUTATION
EQ 250MG BASE	RUBRACA	ZR PHARMA	N209115	May 1, 2017	RX	TABLET	ORAL	8859562	Aug. 4, 2031	A METHOD FOR TREATING EPITHELIAL OVARIAN, FALLOPIAN TUBE, OR PRIMARY PERITONEAL CANCER, WHEREIN THE CANCER IS ASSOCIATED WITH A DELETERIOUS BRCA MUTATION
EQ 250MG BASE	RUBRACA	ZR PHARMA	N209115	May 1, 2017	RX	TABLET	ORAL	8859562	Aug. 4, 2031	A METHOD FOR TREATING METASTATIC CASTRATION-RESISTANT PROSTATE CANCER (MCRPC), WHEREIN THE CANCER IS ASSOCIATED WITH A DELETERIOUS BRCA-MUTATION
EQ 250MG BASE	RUBRACA	ZR PHARMA	N209115	May 1, 2017	RX	TABLET	ORAL	8859562	Aug. 4, 2031	A METHOD FOR TREATING OVARIAN CANCER BY ADMINISTERING RUCAPARIB, WHEREIN THE CANCER IS ASSOCIATED WITH A DELETERIOUS BRCA MUTATION
EQ 300MG BASE	RUBRACA	ZR PHARMA	N209115	Dec. 19, 2016	RX	TABLET	ORAL	8859562	Aug. 4, 2031	A METHOD FOR TREATING EPITHELIAL OVARIAN, FALLOPIAN TUBE, OR PRIMARY PERITONEAL CANCER, WHEREIN THE CANCER IS ASSOCIATED WITH A DELETERIOUS BRCA MUTATION
EQ 300MG BASE	RUBRACA	ZR PHARMA	N209115	Dec. 19, 2016	RX	TABLET	ORAL	8859562	Aug. 4, 2031	A METHOD FOR TREATING METASTATIC CASTRATION-RESISTANT PROSTATE CANCER (MCRPC), WHEREIN THE CANCER IS ASSOCIATED WITH A DELETERIOUS BRCA-MUTATION
EQ 300MG BASE	RUBRACA	ZR PHARMA	N209115	Dec. 19, 2016	RX	TABLET	ORAL	8859562	Aug. 4, 2031	A METHOD FOR TREATING OVARIAN CANCER BY ADMINISTERING RUCAPARIB, WHEREIN THE CANCER IS ASSOCIATED WITH A DELETERIOUS BRCA MUTATION
EQ 200MG BASE	RUBRACA	ZR PHARMA	N209115	Dec. 19, 2016	RX	TABLET	ORAL	10130636	Aug. 17, 2035	A METHOD FOR TREATING EPITHELIAL OVARIAN, FALLOPIAN TUBE, OR PRIMARY PERITONEAL CANCER, WHEREIN THE CANCER IS ASSOCIATED WITH A DELETERIOUS BRCA MUTATION
EQ 200MG BASE	RUBRACA	ZR PHARMA	N209115	Dec. 19, 2016	RX	TABLET	ORAL	10130636	Aug. 17, 2035	A METHOD FOR TREATING METASTATIC CASTRATION-RESISTANT PROSTATE CANCER (MCRPC), WHEREIN THE CANCER IS ASSOCIATED WITH A DELETERIOUS BRCA-MUTATION
EQ 200MG BASE	RUBRACA	ZR PHARMA	N209115	Dec. 19, 2016	RX	TABLET	ORAL	10130636	Aug. 17, 2035	A METHOD FOR TREATING OVARIAN CANCER BY ADMINISTERING RUCAPARIB, WHEREIN THE CANCER IS ASSOCIATED WITH A DELETERIOUS BRCA MUTATION
EQ 200MG BASE	RUBRACA	ZR PHARMA	N209115	Dec. 19, 2016	RX	TABLET	ORAL	10130636	Aug. 17, 2035	MAINTENANCE TREATMENT OF RECURRENT EPITHELIAL OVARIAN, FALLOPIAN TUBE OR PRIMARY PERITONEAL CANCER, WHO ARE IN A COMPLETE OR PARTIAL RESPONSE TO PLATINUM-BASED CHEMOTHERAPY
EQ 250MG BASE	RUBRACA	ZR PHARMA	N209115	May 1, 2017	RX	TABLET	ORAL	10130636	Aug. 17, 2035	A METHOD FOR TREATING EPITHELIAL OVARIAN, FALLOPIAN TUBE, OR PRIMARY PERITONEAL CANCER, WHEREIN THE CANCER IS ASSOCIATED WITH A DELETERIOUS BRCA MUTATION
EQ 250MG BASE	RUBRACA	ZR PHARMA	N209115	May 1, 2017	RX	TABLET	ORAL	10130636	Aug. 17, 2035	A METHOD FOR TREATING METASTATIC CASTRATION-RESISTANT PROSTATE CANCER (MCRPC), WHEREIN THE CANCER IS ASSOCIATED WITH A DELETERIOUS BRCA-MUTATION
EQ 250MG BASE	RUBRACA	ZR PHARMA	N209115	May 1, 2017	RX	TABLET	ORAL	10130636	Aug. 17, 2035	A METHOD FOR TREATING OVARIAN CANCER BY ADMINISTERING RUCAPARIB, WHEREIN THE CANCER IS ASSOCIATED WITH A DELETERIOUS BRCA MUTATION
EQ 250MG BASE	RUBRACA	ZR PHARMA	N209115	May 1, 2017	RX	TABLET	ORAL	10130636	Aug. 17, 2035	MAINTENANCE TREATMENT OF RECURRENT EPITHELIAL OVARIAN, FALLOPIAN TUBE OR PRIMARY PERITONEAL CANCER, WHO ARE IN A COMPLETE OR PARTIAL RESPONSE TO PLATINUM-BASED CHEMOTHERAPY
EQ 300MG BASE	RUBRACA	ZR PHARMA	N209115	Dec. 19, 2016	RX	TABLET	ORAL	10130636	Aug. 17, 2035	A METHOD FOR TREATING EPITHELIAL OVARIAN, FALLOPIAN TUBE, OR PRIMARY PERITONEAL CANCER, WHEREIN THE CANCER IS ASSOCIATED WITH A DELETERIOUS BRCA MUTATION
EQ 300MG BASE	RUBRACA	ZR PHARMA	N209115	Dec. 19, 2016	RX	TABLET	ORAL	10130636	Aug. 17, 2035	A METHOD FOR TREATING METASTATIC CASTRATION-RESISTANT PROSTATE CANCER (MCRPC), WHEREIN THE CANCER IS ASSOCIATED WITH A DELETERIOUS BRCA-MUTATION
EQ 300MG BASE	RUBRACA	ZR PHARMA	N209115	Dec. 19, 2016	RX	TABLET	ORAL	10130636	Aug. 17, 2035	A METHOD FOR TREATING OVARIAN CANCER BY ADMINISTERING RUCAPARIB, WHEREIN THE CANCER IS ASSOCIATED WITH A DELETERIOUS BRCA MUTATION
EQ 300MG BASE	RUBRACA	ZR PHARMA	N209115	Dec. 19, 2016	RX	TABLET	ORAL	10130636	Aug. 17, 2035	MAINTENANCE TREATMENT OF RECURRENT EPITHELIAL OVARIAN, FALLOPIAN TUBE OR PRIMARY PERITONEAL CANCER, WHO ARE IN A COMPLETE OR PARTIAL RESPONSE TO PLATINUM-BASED CHEMOTHERAPY

Orange Book exclusivity data (new drug applications)

Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Exclusivity date	Description
EQ 200MG BASE	RUBRACA	ZR PHARMA	N209115	Dec. 19, 2016	RX	TABLET	ORAL	May 15, 2023	TREATMENT OF ADULT PATIENTS WITH A DELETERIOUS BRCA MUTATION (GERMLINE AND/OR SOMATIC)-ASSOCIATED METASTATIC CASTRATION-RESISTANT PROSTATE CANCER WHO HAVE BEEN TREATED WITH ANDROGEN RECEPTOR-DIRECTED THERAPY AND A TAXANE-BASED CHEMOTHERAPY
EQ 250MG BASE	RUBRACA	ZR PHARMA	N209115	May 1, 2017	RX	TABLET	ORAL	May 15, 2023	TREATMENT OF ADULT PATIENTS WITH A DELETERIOUS BRCA MUTATION (GERMLINE AND/OR SOMATIC)-ASSOCIATED METASTATIC CASTRATION-RESISTANT PROSTATE CANCER WHO HAVE BEEN TREATED WITH ANDROGEN RECEPTOR-DIRECTED THERAPY AND A TAXANE-BASED CHEMOTHERAPY
EQ 300MG BASE	RUBRACA	ZR PHARMA	N209115	Dec. 19, 2016	RX	TABLET	ORAL	May 15, 2023	TREATMENT OF ADULT PATIENTS WITH A DELETERIOUS BRCA MUTATION (GERMLINE AND/OR SOMATIC)-ASSOCIATED METASTATIC CASTRATION-RESISTANT PROSTATE CANCER WHO HAVE BEEN TREATED WITH ANDROGEN RECEPTOR-DIRECTED THERAPY AND A TAXANE-BASED CHEMOTHERAPY
EQ 200MG BASE	RUBRACA	ZR PHARMA	N209115	Dec. 19, 2016	RX	TABLET	ORAL	April 6, 2025	FOR THE MAINTENANCE TREATMENT OF ADULT PATIENTS WITH RECURRENT EPITHELIAL OVARIAN, FALLOPIAN TUBE, OR PRIMARY PERITONEAL CANCER WHO ARE IN A COMPLETE OR PARTIAL RESPONSE TO PLATINUM-BASED CHEMOTHERAPY
EQ 250MG BASE	RUBRACA	ZR PHARMA	N209115	May 1, 2017	RX	TABLET	ORAL	April 6, 2025	FOR THE MAINTENANCE TREATMENT OF ADULT PATIENTS WITH RECURRENT EPITHELIAL OVARIAN, FALLOPIAN TUBE, OR PRIMARY PERITONEAL CANCER WHO ARE IN A COMPLETE OR PARTIAL RESPONSE TO PLATINUM-BASED CHEMOTHERAPY
EQ 300MG BASE	RUBRACA	ZR PHARMA	N209115	Dec. 19, 2016	RX	TABLET	ORAL	April 6, 2025	FOR THE MAINTENANCE TREATMENT OF ADULT PATIENTS WITH RECURRENT EPITHELIAL OVARIAN, FALLOPIAN TUBE, OR PRIMARY PERITONEAL CANCER WHO ARE IN A COMPLETE OR PARTIAL RESPONSE TO PLATINUM-BASED CHEMOTHERAPY

Bioactivity Summary:

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
Poly [ADP-ribose] polymerase 2	Enzyme	Q9UGN5	PARP2_HUMAN	INHIBITOR	IC50	7.55	SCIENTIFIC LITERATURE	DRUG LABEL
Poly [ADP-ribose] polymerase 1	Enzyme	P09874	PARP1_HUMAN	INHIBITOR	IC50	8.50	SCIENTIFIC LITERATURE	DRUG LABEL
Poly [ADP-ribose] polymerase 3	Enzyme	Q9Y6F1	PARP3_HUMAN	INHIBITOR	IC50	6.39	SCIENTIFIC LITERATURE	DRUG LABEL
Poly [ADP-ribose] polymerase 4	Enzyme	Q9UKK3	PARP4_HUMAN	INHIBITOR	IC50	6.08	SCIENTIFIC LITERATURE
Poly [ADP-ribose] polymerase 10	Enzyme	Q53GL7	PAR10_HUMAN	INHIBITOR	IC50	6.25	SCIENTIFIC LITERATURE
Mono [ADP-ribose] polymerase PARP16	Unclassified	Q8N5Y8	PAR16_HUMAN		Kd	5.54	CHEMBL
Poly [ADP-ribose] polymerase 14	Enzyme	Q460N5	PAR14_HUMAN	INHIBITOR	IC50	5.05	SCIENTIFIC LITERATURE
Poly [ADP-ribose] polymerase 15	Enzyme	Q460N3	PAR15_HUMAN	INHIBITOR	IC50	4.49	SCIENTIFIC LITERATURE
Poly [ADP-ribose] polymerase 12	Enzyme	Q9H0J9	PAR12_HUMAN	INHIBITOR	IC50	5.18	SCIENTIFIC LITERATURE
Tankyrase-2	Enzyme	Q9H2K2	TNKS2_HUMAN	INHIBITOR	IC50	6.05	SCIENTIFIC LITERATURE
Tankyrase-1	Enzyme	O95271	TNKS1_HUMAN	INHIBITOR	IC50	6.84	SCIENTIFIC LITERATURE

External reference:

ID	Source
8237F3U7EH	UNII
1859053-21-6	SECONDARY_CAS_RN
459868-92-9	SECONDARY_CAS_RN
4036311	VANDF
C3661315	UMLSCUI
CHEBI:134689	CHEBI
RPB	PDB_CHEM_ID
CHEMBL1173055	ChEMBL_ID
9931954	PUBCHEM_CID
DB12332	DRUGBANK_ID
D10079	KEGG_DRUG
CHEMBL3833368	ChEMBL_ID
CHEMBL2105733	ChEMBL_ID
9471	INN_ID
C520469	MESH_SUPPLEMENTAL_RECORD_UI
7736	IUPHAR_LIGAND_ID
247942	MMSL
32185	MMSL
d08507	MMSL
017056	NDDF
017057	NDDF
1217204001	SNOMEDCT_US
723984009	SNOMEDCT_US
763539004	SNOMEDCT_US
1862578	RXNORM
C531549	MESH_SUPPLEMENTAL_RECORD_UI

Pharmaceutical products:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Rubraca	HUMAN PRESCRIPTION DRUG LABEL	1	69660-201	TABLET, FILM COATED	200 mg	ORAL	NDA	30 sections
Rubraca	HUMAN PRESCRIPTION DRUG LABEL	1	69660-201	TABLET, FILM COATED	200 mg	ORAL	NDA	30 sections
Rubraca	HUMAN PRESCRIPTION DRUG LABEL	1	69660-201	TABLET, FILM COATED	200 mg	ORAL	NDA	30 sections
Rubraca	HUMAN PRESCRIPTION DRUG LABEL	1	69660-202	TABLET, FILM COATED	250 mg	ORAL	NDA	30 sections
Rubraca	HUMAN PRESCRIPTION DRUG LABEL	1	69660-202	TABLET, FILM COATED	250 mg	ORAL	NDA	30 sections
Rubraca	HUMAN PRESCRIPTION DRUG LABEL	1	69660-202	TABLET, FILM COATED	250 mg	ORAL	NDA	30 sections
Rubraca	HUMAN PRESCRIPTION DRUG LABEL	1	69660-203	TABLET, FILM COATED	300 mg	ORAL	NDA	30 sections
Rubraca	HUMAN PRESCRIPTION DRUG LABEL	1	69660-203	TABLET, FILM COATED	300 mg	ORAL	NDA	30 sections
Rubraca	HUMAN PRESCRIPTION DRUG LABEL	1	69660-203	TABLET, FILM COATED	300 mg	ORAL	NDA	30 sections
Rubraca	HUMAN PRESCRIPTION DRUG LABEL	1	82154-0783	TABLET, FILM COATED	200 mg	ORAL	NDA	29 sections
Rubraca	HUMAN PRESCRIPTION DRUG LABEL	1	82154-0784	TABLET, FILM COATED	250 mg	ORAL	NDA	29 sections
Rubraca	HUMAN PRESCRIPTION DRUG LABEL	1	82154-0785	TABLET, FILM COATED	300 mg	ORAL	NDA	29 sections