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

Stem definition	Drug id	CAS RN
poly-ADP-ribose polymerase inhibitors	4907	763113-22-0

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: olaparib lynparza AZD2281	Olaparib is an inhibitor of poly (ADP-ribose) polymerase (PARP) enzymes, including PARP1, PARP2, and PARP3. PARP enzymes are involved in normal cellular homeostasis, such as DNA transcription, cell cycle regulation, and DNA repair. Olaparib has been shown to inhibit growth of select tumor cell lines in vitro and decrease tumor growth in mouse xenograft models of human cancer both as monotherapy or following platinum-based chemotherapy. Increased cytotoxicity and anti-tumor activity following treatment with olaparib were noted in cell lines and mouse tumor models with deficiencies in BRCA. In vitro studies have shown that olaparib-induced cytotoxicity may involve inhibition of PARP enzymatic activity and increased formation of PARP-DNA complex, resulting in disruption of cellular homeostasis and cell death. Molecular weight: 434.47 Formula: C24H23FN4O3 CLOGP: 1.07 LIPINSKI: 0 HAC: 7 HDO: 1 TPSA: 82.08 ALOGS: -3.86 ROTB: 4 Status: ONP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

olaparib
lynparza
AZD2281

Olaparib is an inhibitor of poly (ADP-ribose) polymerase (PARP) enzymes, including PARP1, PARP2, and PARP3. PARP enzymes are involved in normal cellular homeostasis, such as DNA transcription, cell cycle regulation, and DNA repair. Olaparib has been shown to inhibit growth of select tumor cell lines in vitro and decrease tumor growth in mouse xenograft models of human cancer both as monotherapy or following platinum-based chemotherapy. Increased cytotoxicity and anti-tumor activity following treatment with olaparib were noted in cell lines and mouse tumor models with deficiencies in BRCA. In vitro studies have shown that olaparib-induced cytotoxicity may involve inhibition of PARP enzymatic activity and increased formation of PARP-DNA complex, resulting in disruption of cellular homeostasis and cell death.

Molecular weight: 434.47
Formula: C24H23FN4O3
CLOGP: 1.07
LIPINSKI: 0
HAC: 7
HDO: 1
TPSA: 82.08
ALOGS: -3.86
ROTB: 4

Status: ONP

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

Drug dosage:

None

ADMET properties:

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Property	Value	Reference
BDDCS (Biopharmaceutical Drug Disposition Classification System)	2	Hosey CM, Chan R, Benet LZ
S (Water solubility)	0.10 mg/mL	Bocci G, Oprea TI, Benet LZ

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Approvals:

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Date	Agency	Company
Dec. 19, 2014	FDA	ASTRAZENECA PHARMS
Jan. 19, 2018	PMDA	AstraZeneca KK
Oct. 23, 2014	EMA

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FDA Adverse Event Reporting System (Female)

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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	1933.07	28.19	655	9599	81466	63397302
Anaemia	1090.88	28.19	640	9614	292790	63185978
Myelodysplastic syndrome	1016.18	28.19	278	9976	16476	63462292
Acute myeloid leukaemia	747.59	28.19	220	10034	16927	63461841
Death	581.53	28.19	479	9775	373902	63104866
Myelosuppression	446.02	28.19	161	10093	23542	63455226
Interstitial lung disease	410.95	28.19	200	10054	61708	63417060
Ovarian cancer recurrent	384.73	28.19	75	10179	942	63477826
Carbohydrate antigen 125 increased	263.18	28.19	66	10188	2750	63476018
Pancytopenia	192.00	28.19	144	10110	96789	63381979

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FDA Adverse Event Reporting System (Male)

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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
Death	439.13	43.04	270	1711	397779	34557171
Malignant neoplasm progression	346.76	43.04	143	1838	87903	34867047
Anaemia	103.27	43.04	93	1888	233242	34721708
Prostatic specific antigen increased	93.27	43.04	34	1947	14646	34940304
Product use issue	83.28	43.04	49	1932	63167	34891783
Off label use	73.41	43.04	103	1878	419421	34535529
Fatigue	69.24	43.04	94	1887	370559	34584391
Product use in unapproved indication	59.99	43.04	51	1930	117448	34837502
Metastases to bone	51.87	43.04	21	1960	11949	34943001

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FDA Adverse Event Reporting System (Geriatric)

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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	1122.87	29.19	459	8627	135531	79599771
Anaemia	940.18	29.19	596	8490	444419	79290883
Myelodysplastic syndrome	708.42	29.19	222	8864	30079	79705223
Acute myeloid leukaemia	617.75	29.19	201	8885	30684	79704618
Death	406.08	29.19	403	8683	566111	79169191
Myelosuppression	313.46	29.19	131	8955	40165	79695137
Ovarian cancer recurrent	267.55	29.19	46	9040	398	79734904
Interstitial lung disease	247.67	29.19	156	8930	112444	79622858
Nausea	188.66	29.19	365	8721	956831	78778471
Neutrophil count decreased	157.52	29.19	110	8976	93849	79641453

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	L01XK01	ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS ANTINEOPLASTIC AGENTS OTHER ANTINEOPLASTIC AGENTS Poly (ADP-ribose) polymerase (PARP) inhibitors
CHEBI has role	CHEBI:35610	antineoplastic agents
CHEBI has role	CHEBI:62913	PARP
CHEBI has role	CHEBI:68495	Type I cell-death inducers
FDA EPC	N0000191623	Poly(ADP-Ribose) Polymerase Inhibitor
FDA MoA	N0000191622	Poly(ADP-Ribose) Polymerase Inhibitors
MeSH PA	D000970	Antineoplastic Agents
MeSH PA	D004791	Enzyme Inhibitors
MeSH PA	D000067856	Poly(ADP-ribose) Polymerase Inhibitors

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

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Disease	Relation	SNOMED_ID	DOID
Epithelial tumor of ovary	indication	237057005	DOID:2152
Malignant tumor of pancreas	indication	363418001
Malignant tumor of ovary	indication	363443007	DOID:2394
Malignant tumor of peritoneum	indication	363492001
Hormone refractory prostate cancer	indication	427492003
Human epidermal growth factor 2 negative carcinoma of breast	indication	431396003
BRCA mutation-positive and HER2-negative breast cancer	indication	767444009

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🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	11.54	acidic

Orange Book patent data (new drug applications)

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Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Patent number	Patent expiration date	Patent use
100MG	LYNPARZA	ASTRAZENECA	N208558	Aug. 17, 2017	RX	TABLET	ORAL	8912187	March 12, 2024	ADJUVANT TREATMENT OF PATIENTS WITH GBRCA-MUTATED HUMAN EPIDERMAL GROWTH FACTOR RECEPTOR 2 (HER2)-NEGATIVE HIGH RISK EARLY BREAST CANCER WHO HAVE BEEN TREATED WITH NEOADJUVANT OR ADJUVANT CHEMOTHERAPY
100MG	LYNPARZA	ASTRAZENECA	N208558	Aug. 17, 2017	RX	TABLET	ORAL	8912187	March 12, 2024	MAINTENANCE TREATMENT OF GBRCA- OR SBRCA-MUTATED ADVANCED EPITHELIAL OVARIAN, FALLOPIAN TUBE OR PRIMARY PERITONEAL CANCER WHO ARE IN A COMPLETE OR PARTIAL RESPONSE TO FIRST-LINE PLATINUM-BASED CHEMOTHERAPY
100MG	LYNPARZA	ASTRAZENECA	N208558	Aug. 17, 2017	RX	TABLET	ORAL	8912187	March 12, 2024	MAINTENANCE TREATMENT OF RECURRENT EPITHELIAL OVARIAN, FALLOPIAN TUBE OR PRIMARY PERITONEAL CANCER, WHO ARE IN A COMPLETE OR PARTIAL RESPONSE TO PLATINUM-BASED CHEMOTHERAPY
100MG	LYNPARZA	ASTRAZENECA	N208558	Aug. 17, 2017	RX	TABLET	ORAL	8912187	March 12, 2024	MAINTENANCE TREATMENT WITH BEVACIZUMAB OF ADV. EPITHELIAL OVARIAN CANCER IN COMPLETE OR PARTIAL RESPONSE TO FIRST-LINE PLATINUM CHEMOTHERAPY AND HOMOLOGOUS RECOMBINATION DEFICIENCY-POSITIVE WITH A DELETERIOUS OR SUSPECTED DELETERIOUS BRCA MUTATION
100MG	LYNPARZA	ASTRAZENECA	N208558	Aug. 17, 2017	RX	TABLET	ORAL	8912187	March 12, 2024	MAINTENANCE TREATMENT WITH BEVACIZUMAB OF ADV. EPITHELIAL OVARIAN CANCER IN COMPLETE OR PARTIAL RESPONSE TO FIRST-LINE PLATINUM CHEMOTHERAPY AND HOMOLOGOUS RECOMBINATION DEFICIENCY-POSITIVE WITH GENOMIC INSTABILITY
100MG	LYNPARZA	ASTRAZENECA	N208558	Aug. 17, 2017	RX	TABLET	ORAL	8912187	March 12, 2024	MAINTENANCE TREATMENT WITH BEVACIZUMAB OF FALLOPIAN TUBE CANCER IN COMPLETE OR PARTIAL RESPONSE TO FIRST-LINE PLATINUM CHEMOTHERAPY AND HOMOLOGOUS RECOMBINATION DEFICIENCY-POSITIVE WITH A DELETERIOUS OR SUSPECTED DELETERIOUS BRCA MUTATION
100MG	LYNPARZA	ASTRAZENECA	N208558	Aug. 17, 2017	RX	TABLET	ORAL	8912187	March 12, 2024	MAINTENANCE TREATMENT WITH BEVACIZUMAB OF FALLOPIAN TUBE CANCER IN COMPLETE OR PARTIAL RESPONSE TO FIRST-LINE PLATINUM CHEMOTHERAPY AND HOMOLOGOUS RECOMBINATION DEFICIENCY-POSITIVE WITH GENOMIC INSTABILITY
100MG	LYNPARZA	ASTRAZENECA	N208558	Aug. 17, 2017	RX	TABLET	ORAL	8912187	March 12, 2024	MAINTENANCE TREATMENT WITH BEVACIZUMAB OF PRIMARY PERITONEAL CANCER IN COMPLETE OR PARTIAL RESPONSE TO FIRST-LINE PLATINUM CHEMOTHERAPY AND HOMOLOGOUS RECOMBINATION DEFICIENCY-POSITIVE WITH A DELETERIOUS OR SUSPECTED DELETERIOUS BRCA MUTATION
100MG	LYNPARZA	ASTRAZENECA	N208558	Aug. 17, 2017	RX	TABLET	ORAL	8912187	March 12, 2024	MAINTENANCE TREATMENT WITH BEVACIZUMAB OF PRIMARY PERITONEAL CANCER IN COMPLETE OR PARTIAL RESPONSE TO FIRST-LINE PLATINUM CHEMOTHERAPY AND HOMOLOGOUS RECOMBINATION DEFICIENCY-POSITIVE WITH GENOMIC INSTABILITY
100MG	LYNPARZA	ASTRAZENECA	N208558	Aug. 17, 2017	RX	TABLET	ORAL	8912187	March 12, 2024	TREATMENT OF HR-NEGATIVE, HER-2 NEGATIVE, GBRCA-MUTATED METASTATIC BREAST CANCER, WHO HAVE BEEN TREATED WITH CHEMOTHERAPY IN THE NEOADJUVANT, ADJUVANT, OR METASTATIC SETTING

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Orange Book exclusivity data (new drug applications)

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Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Exclusivity date	Description
100MG	LYNPARZA	ASTRAZENECA	N208558	Aug. 17, 2017	RX	TABLET	ORAL	May 8, 2023	W/BEVACIZUMAB FOR MAINTENANCE TX OF ADULTS W/ADV. EPITHELIAL OVARIAN, FALLOPIAN TUBE OR PRIMARY PERITONEAL CA IN COMPLETE OR PARTIAL RESPONSE TO FIRST-LINE PLATINUM-BASED CHEMO & CA ASSOCIATED W/ HOMOLOGOUS RECOMBINATION DEFICIENCY POSITIVE STATUS
100MG	LYNPARZA	ASTRAZENECA	N208558	Aug. 17, 2017	RX	TABLET	ORAL	May 19, 2023	TX OF ADULT PTS WITH DELETERIOUS OR SUSPECTED DELETERIOUS GERMLINE OR SOMATIC HOMOLOGOUS RECOMBINATION REPAIR GENE-MUTATED METASTATIC CASTRATION-RESISTANT PROSTATE CANCER WHO HAVE PROGRESSED FOLLOWING PRIOR TREATMENT WITH ENZALUTAMIDE OR ABIRATERONE
100MG	LYNPARZA	ASTRAZENECA	N208558	Aug. 17, 2017	RX	TABLET	ORAL	Aug. 17, 2024	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
100MG	LYNPARZA	ASTRAZENECA	N208558	Aug. 17, 2017	RX	TABLET	ORAL	Aug. 17, 2024	TREATMENT OF ADULT PATIENTS WITH DELETERIOUS OR SUSPECTED DELETERIOUS GERMLINE BRCA-MUTATED ADVANCED OVARIAN CANCER WHO HAVE BEEN TREATED WITH THREE OR MORE PRIOR LINES OF CHEMOTHERAPY
100MG	LYNPARZA	ASTRAZENECA	N208558	Aug. 17, 2017	RX	TABLET	ORAL	March 11, 2025	FOR THE ADJUVANT TREATMENT OF ADULT PATIENTS WITH DELETERIOUS OR SUSPECTED DELETERIOUS GBRCA MUTATED HER2-NEGATIVE HIGH-RISK EARLY BREAST CANCER WHO HAVE PREVIOUSLY BEEN TREATED WITH NEOADJUVANT OR ADJUVANT CHEMOTHERAPY
100MG	LYNPARZA	ASTRAZENECA	N208558	Aug. 17, 2017	RX	TABLET	ORAL	Dec. 19, 2025	MAINTENANCE TREATMENT OF ADULTS WITH DELETERIOUS OR SUSPECTED DELETERIOUS GERMLINE OR SOMATIC BRCA-MUTATED ADVANCED EPITHELIAL OVARIAN, FALLOPIAN TUBE, OR PRIMARY PERITONEAL CANCER IN COMPLETE OR PARTIAL RESPONSE TO FIRST-LINE PLATINUM-BASED CHEMOTHERAPY
100MG	LYNPARZA	ASTRAZENECA	N208558	Aug. 17, 2017	RX	TABLET	ORAL	May 31, 2026	IN COMBINATION WITH ABIRATERONE AND PREDNISONE OR PREDNISOLONE FOR THETREATMENT OF ADULT PATIENTS WITH DELETERIOUS OR SUSPECTED DELETERIOUS BRCA-MUTATED (BRCAM) METASTATIC CASTRATION-RESISTANT PROSTATE CANCER (MCRPC)
100MG	LYNPARZA	ASTRAZENECA	N208558	Aug. 17, 2017	RX	TABLET	ORAL	Dec. 27, 2026	MAINTENANCE TX OF ADULTS W/ DELETERIOUS OR SUSPECTED DELETERIOUS GBRCAM METASTATIC PANCREATIC ADENOCARCINOMA WHOSE DZ HAS NOT PROGRESSED ON >=16WKS OF 1ST LINE PLATINUM BASED CHEMO REGIMEN. SELECT PTS FOR THERAPY BASED ON APPROVED COMPANION DIAGNOSTIC
100MG	LYNPARZA	ASTRAZENECA	N208558	Aug. 17, 2017	RX	TABLET	ORAL	May 8, 2027	W/ BEVACIZUMAB FOR MAINT TX OF ADULTS W/ ADV EPITHELIAL OVARIAN, FALLOPIAN TUBE, OR PRIMARY PERITONEAL CA IN COMPLETE OR PARTIAL RESPONSE TO 1ST LINE PT BASED CHEMO & WHOSE CA IS ASSOC W/ HOMOLOGOUS RECOMB DEF + STATUS DEFINED BY GENOMIC INSTABILITY
150MG	LYNPARZA	ASTRAZENECA	N208558	Aug. 17, 2017	RX	TABLET	ORAL	May 8, 2023	W/BEVACIZUMAB FOR MAINTENANCE TX OF ADULTS W/ADV. EPITHELIAL OVARIAN, FALLOPIAN TUBE OR PRIMARY PERITONEAL CA IN COMPLETE OR PARTIAL RESPONSE TO FIRST-LINE PLATINUM-BASED CHEMO & CA ASSOCIATED W/ HOMOLOGOUS RECOMBINATION DEFICIENCY POSITIVE STATUS

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Bioactivity Summary:

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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	9	SCIENTIFIC LITERATURE	SCIENTIFIC LITERATURE
Poly [ADP-ribose] polymerase 1	Enzyme	P09874	PARP1_HUMAN	INHIBITOR	IC50	8.30	SCIENTIFIC LITERATURE	SCIENTIFIC LITERATURE
Poly [ADP-ribose] polymerase 3	Enzyme	Q9Y6F1	PARP3_HUMAN	INHIBITOR	IC50	7.34	CHEMBL	DRUG LABEL
Poly [ADP-ribose] polymerase 12	Enzyme	Q9H0J9	PAR12_HUMAN		IC50	5	CHEMBL
Poly [ADP-ribose] polymerase 15	Enzyme	Q460N3	PAR15_HUMAN		IC50	4.75	CHEMBL
Tankyrase-2	Enzyme	Q9H2K2	TNKS2_HUMAN		IC50	8.28	CHEMBL
Mono [ADP-ribose] polymerase PARP16	Unclassified	Q8N5Y8	PAR16_HUMAN		IC50	5.29	CHEMBL
Tankyrase-1	Enzyme	O95271	TNKS1_HUMAN		IC50	5.82	SCIENTIFIC LITERATURE
Poly [ADP-ribose] polymerase 6	Unclassified	Q2NL67	PARP6_HUMAN		IC50	5.75	CHEMBL
Poly [ADP-ribose] polymerase 4	Enzyme	Q9UKK3	PARP4_HUMAN		IC50	6.39	CHEMBL

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External reference:

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ID	Source
09L	PDB_CHEM_ID
015824	NDDF
1597582	RXNORM
231537	MMSL
23725625	PUBCHEM_CID
30771	MMSL
4034034	VUID
4034034	VANDF
432162002	SNOMEDCT_US
432885003	SNOMEDCT_US

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Lynparza	HUMAN PRESCRIPTION DRUG LABEL	1	0310-0668	TABLET, FILM COATED	100 mg	ORAL	NDA	26 sections
Lynparza	HUMAN PRESCRIPTION DRUG LABEL	1	0310-0668	TABLET, FILM COATED	100 mg	ORAL	NDA	26 sections
Lynparza	HUMAN PRESCRIPTION DRUG LABEL	1	0310-0668	TABLET, FILM COATED	100 mg	ORAL	NDA	26 sections
Lynparza	HUMAN PRESCRIPTION DRUG LABEL	1	0310-0668	TABLET, FILM COATED	100 mg	ORAL	NDA	26 sections
Lynparza	HUMAN PRESCRIPTION DRUG LABEL	1	0310-0679	TABLET, FILM COATED	150 mg	ORAL	NDA	26 sections
Lynparza	HUMAN PRESCRIPTION DRUG LABEL	1	0310-0679	TABLET, FILM COATED	150 mg	ORAL	NDA	26 sections
Lynparza	HUMAN PRESCRIPTION DRUG LABEL	1	0310-0679	TABLET, FILM COATED	150 mg	ORAL	NDA	26 sections
Lynparza	HUMAN PRESCRIPTION DRUG LABEL	1	0310-0679	TABLET, FILM COATED	150 mg	ORAL	NDA	26 sections

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