Niraparib tosylate

Details

Stereochemistry	ABSOLUTE
Molecular Formula	C19H20N4O.C7H8O3S.H2O
Molecular Weight	510.605
Optical Activity	UNSPECIFIED
Defined Stereocenters	1 / 1
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

O.CC1=CC=C(C=C1)S(O)(=O)=O.NC(=O)C2=CC=CC3=CN(N=C23)C4=CC=C(C=C4)[C@@H]5CCCNC5

InChI

InChIKey=ACNPUCQQZDAPJH-FMOMHUKBSA-N

InChI=1S/C19H20N4O.C7H8O3S.H2O/c20-19(24)17-5-1-3-15-12-23(22-18(15)17)16-8-6-13(7-9-16)14-4-2-10-21-11-14;1-6-2-4-7(5-3-6)11(8,9)10;/h1,3,5-9,12,14,21H,2,4,10-11H2,(H2,20,24);2-5H,1H3,(H,8,9,10);1H2/t14-;;/m1../s1

HIDE SMILES / InChI

Molecular Formula	C7H8O3S
Molecular Weight	172.202
Charge	0
Count

Stereochemistry	ACHIRAL
Additional Stereochemistry	No
Defined Stereocenters	0 / 0
E/Z Centers	0
Optical Activity	NONE

Molecular Formula	H2O
Molecular Weight	18.0153
Charge	0
Count

Stereochemistry	ACHIRAL
Additional Stereochemistry	No
Defined Stereocenters	0 / 0
E/Z Centers	0
Optical Activity	NONE

Molecular Formula	C19H20N4O
Molecular Weight	320.3883
Charge	0
Count

Stereochemistry	ABSOLUTE
Additional Stereochemistry	No
Defined Stereocenters	1 / 1
E/Z Centers	0
Optical Activity	UNSPECIFIED

Description
Sources: http://adisinsight.springer.com/drugs/800028881
Curator's Comment: Description was created based on several sources, including https://www.ncbi.nlm.nih.gov/pubmed/19873981 | https://www.ncbi.nlm.nih.gov/pubmed/25761096

Niraparib (MK-4827) displays excellent PARP 1 and 2 inhibition. Inhibition of PARP in the context of defects in other DNA repair mechanisms provide a tumor specific way to kill cancer cells. Niraparib is in development with TESARO, under licence from Merck & Co, for the treatment of cancers (ovarian, fallopian tube and peritoneal cancer, breast cancer, prostate cancer and Ewing's sarcoma). Niraparib was characterized in a number of preclinical models before moving to phase I clinical trials, where it showed excellent human pharmacokinetics suitable for once a day oral dosing, achieved its pharmacodynamic target for PARP inhibition, and had promising activity in cancer patients. It is currently being tested in phase 3 clinical trials as maintenance therapy in ovarian cancer and as a treatment for breast cancer.

CNS Activity

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
Poly [ADP-ribose] polymerase-1 23 Target ID: CHEMBL3105 Sources: https://www.ncbi.nlm.nih.gov/pubmed/19873981	Inhibitor 8504		3.8 nM [IC50]
Poly [ADP-ribose] polymerase 2 16 Target ID: CHEMBL5366 Sources: https://www.ncbi.nlm.nih.gov/pubmed/19873981	Inhibitor 8504		2.1 nM [IC50]

Conditions

Condition	Modality	Highest Phase	Product
epithelial ovarian cancer 4 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/208447lbl.pdf	Primary	Approved 8583	ZEJULA Approved Use ZEJULA is a poly(ADP-ribose) polymerase (PARP) inhibitor indicated 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. Launch Date 2017
Ovarian cancer 160 Sources: http://adisinsight.springer.com/drugs/800028881	Primary	Phase III 665	Unknown Approved Use Unknown
Breast cancer 432 Sources: http://adisinsight.springer.com/drugs/800028881	Primary	Phase III 665	Unknown Approved Use Unknown
Fallopian tube cancer 17 Sources: http://adisinsight.springer.com/drugs/800028881	Primary	Phase III 665	Unknown Approved Use Unknown
Peritoneal cancer 11 Sources: http://adisinsight.springer.com/drugs/800028881	Primary	Phase III 665	Unknown Approved Use Unknown

C_max

Value	Dose	Co-administered	Analyte	Population
804 ng/mL DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/208447s014lbl.pdf	300 mg single, oral dose: 300 mg route of administration: Oral experiment type: SINGLE co-administered:		NIRAPARIB plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
803.7 ng/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/29322231	300 mg single, oral dose: 300 mg route of administration: Oral experiment type: SINGLE co-administered:		NIRAPARIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED

AUC

Value	Dose	Co-administered	Analyte	Population
29016.1 ng × h/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/29322231	300 mg single, oral dose: 300 mg route of administration: Oral experiment type: SINGLE co-administered:		NIRAPARIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED

T_1/2

Value	Dose	Co-administered	Analyte	Population
50.5 h EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/29322231	300 mg single, oral dose: 300 mg route of administration: Oral experiment type: SINGLE co-administered:		NIRAPARIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED

F_unbound

Value	Dose	Co-administered	Analyte	Population
17% DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/208447s014lbl.pdf	300 mg single, oral dose: 300 mg route of administration: Oral experiment type: SINGLE co-administered:		NIRAPARIB plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED

Overview

CYP3A4	CYP2C9	CYP2D6	hERG
inducer 1087	inhibitor 2438	substrate 1388 inhibitor 2507	inhibitor 2217

OverviewOther

Other Inhibitor	Other Substrate	Other Inducer
OCT1 620 BCRP 910 OATP1B1 1079 OATP1B3 961 OAT1 725 OAT3 747 OCT2 779 BSEP 550 CYP1A 70 CYP2B6 926 CYP2C8 1057 CYP2C19 2057 CYP3A4/5 296 P-gp 1741 MATE1 415 MATE2 267	BCRP 697 P-gp 2052 CYP1A2 1197 CYP3A4/5 91 UGT 219 OATP1B1 503 OATP1B3 435 OCT1 393 OAT1 395 OAT3 391 OCT2 434 BSEP 63 MATE1 182 MATE2 98	CYP1A2 832

Drug as perpetrator

Target	Modality	Activity	Metabolite
BCRP 985	inhibitor 4027 Sources: https://www.ema.europa.eu/en/documents/assessment-report/zejula-epar-public-assessment-report_en.pdf#page=42 Page: -	no	M1 13
BSEP 554	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/208447Orig1s000MultidisciplineR.pdf#page=90 Page: 90.0	no
BSEP 554	inhibitor 4027 Sources: https://www.ema.europa.eu/en/documents/assessment-report/zejula-epar-public-assessment-report_en.pdf#page=42 Page: -	no	M1 13
CYP1A 122	inhibitor 4027 Sources: https://www.ema.europa.eu/en/documents/assessment-report/zejula-epar-public-assessment-report_en.pdf#page=42 Page: -	no
CYP1A 122	inhibitor 4027 Sources: https://www.ema.europa.eu/en/documents/assessment-report/zejula-epar-public-assessment-report_en.pdf#page=42 Page: -	no	M1 13
CYP1A2 2333	inducer 1966 Sources: https://www.ema.europa.eu/en/documents/assessment-report/zejula-epar-public-assessment-report_en.pdf#page=42 Page: -	no	M1 13
CYP2B6 1160	inhibitor 4027 Sources: https://www.ema.europa.eu/en/documents/assessment-report/zejula-epar-public-assessment-report_en.pdf#page=42 Page: -	no
CYP2B6 1160	inhibitor 4027 Sources: https://www.ema.europa.eu/en/documents/assessment-report/zejula-epar-public-assessment-report_en.pdf#page=42 Page: -	no	M1 13
CYP2C19 2141	inhibitor 4027 Sources: https://www.ema.europa.eu/en/documents/assessment-report/zejula-epar-public-assessment-report_en.pdf#page=42 Page: -	no
CYP2C19 2141	inhibitor 4027 Sources: https://www.ema.europa.eu/en/documents/assessment-report/zejula-epar-public-assessment-report_en.pdf#page=42 Page: -	no	M1 13
CYP2C8 1117	inhibitor 4027 Sources: https://www.ema.europa.eu/en/documents/assessment-report/zejula-epar-public-assessment-report_en.pdf#page=42 Page: -	no
CYP2C8 1117	inhibitor 4027 Sources: https://www.ema.europa.eu/en/documents/assessment-report/zejula-epar-public-assessment-report_en.pdf#page=42 Page: -	no	M1 13
CYP2C9 2497	inhibitor 4027 Sources: https://www.ema.europa.eu/en/documents/assessment-report/zejula-epar-public-assessment-report_en.pdf#page=42 Page: -	no
CYP2C9 2497	inhibitor 4027 Sources: https://www.ema.europa.eu/en/documents/assessment-report/zejula-epar-public-assessment-report_en.pdf#page=42 Page: -	no	M1 13
CYP2D6 2546	inhibitor 4027 Sources: https://www.ema.europa.eu/en/documents/assessment-report/zejula-epar-public-assessment-report_en.pdf#page=42 Page: -	no
CYP2D6 2546	inhibitor 4027 Sources: https://www.ema.europa.eu/en/documents/assessment-report/zejula-epar-public-assessment-report_en.pdf#page=42 Page: -	no	M1 13
CYP3A4 2633	inducer 1966 Sources: https://www.ema.europa.eu/en/documents/assessment-report/zejula-epar-public-assessment-report_en.pdf#page=42 Page: -	no
CYP3A4 2633	inducer 1966 Sources: https://www.ema.europa.eu/en/documents/assessment-report/zejula-epar-public-assessment-report_en.pdf#page=42 Page: -	no	M1 13
CYP3A4/5 357	inhibitor 4027 Sources: https://www.ema.europa.eu/en/documents/assessment-report/zejula-epar-public-assessment-report_en.pdf#page=42 Page: -	no
CYP3A4/5 357	inhibitor 4027 Sources: https://www.ema.europa.eu/en/documents/assessment-report/zejula-epar-public-assessment-report_en.pdf#page=42 Page: -	no	M1 13
MATE1 416	inhibitor 4027 Sources: https://www.ema.europa.eu/en/documents/assessment-report/zejula-epar-public-assessment-report_en.pdf#page=42 Page: -	no	M1 13
MATE2 267	inhibitor 4027 Sources: https://www.ema.europa.eu/en/documents/assessment-report/zejula-epar-public-assessment-report_en.pdf#page=42 Page: -	no	M1 13
OAT1 730	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/208447Orig1s000MultidisciplineR.pdf#page=90 Page: 90.0	no
OAT1 730	inhibitor 4027 Sources: https://www.ema.europa.eu/en/documents/assessment-report/zejula-epar-public-assessment-report_en.pdf#page=42 Page: -	no	M1 13
OAT3 749	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/208447Orig1s000MultidisciplineR.pdf#page=90 Page: 90.0	no
OAT3 749	inhibitor 4027 Sources: https://www.ema.europa.eu/en/documents/assessment-report/zejula-epar-public-assessment-report_en.pdf#page=42 Page: -	no	M1 13
OATP1B1 1095	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/208447Orig1s000MultidisciplineR.pdf#page=90 Page: 90.0	no
OATP1B1 1095	inhibitor 4027 Sources: https://www.ema.europa.eu/en/documents/assessment-report/zejula-epar-public-assessment-report_en.pdf#page=42 Page: -	no	M1 13
OATP1B3 970	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/208447Orig1s000MultidisciplineR.pdf#page=90 Page: 90.0	no
OATP1B3 970	inhibitor 4027 Sources: https://www.ema.europa.eu/en/documents/assessment-report/zejula-epar-public-assessment-report_en.pdf#page=42 Page: -	no	M1 13
OCT2 782	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/208447Orig1s000MultidisciplineR.pdf#page=90 Page: 90.0	no
OCT2 782	inhibitor 4027 Sources: https://www.ema.europa.eu/en/documents/assessment-report/zejula-epar-public-assessment-report_en.pdf#page=42 Page: -	no	M1 13
P-gp 1932	inhibitor 4027 Sources: https://www.ema.europa.eu/en/documents/assessment-report/zejula-epar-public-assessment-report_en.pdf#page=42 Page: -	no	M1 13
P-gp 1932	inhibitor 4027 Sources: https://www.ema.europa.eu/en/documents/assessment-report/zejula-epar-public-assessment-report_en.pdf#page=42 Page: -	weak [Inhibition 161 uM]
CYP1A2 2333	inducer 1966 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/208447Orig1s000MultidisciplineR.pdf#page=72 Page: 72.0	weak
OCT1 656	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/208447Orig1s000MultidisciplineR.pdf#page=72 Page: 72.0	weak
BCRP 985	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/208447Orig1s000MultidisciplineR.pdf#page=81 Page: 81.0	yes [IC50 1.21 uM]
MATE1 416	inhibitor 4027 Sources: https://www.ema.europa.eu/en/documents/assessment-report/zejula-epar-public-assessment-report_en.pdf#page=42 Page: -	yes [Inhibition 0.18 uM]
MATE2 267	inhibitor 4027 Sources: https://www.ema.europa.eu/en/documents/assessment-report/zejula-epar-public-assessment-report_en.pdf#page=42 Page: -	yes [Inhibition <0.14 uM]

Drug as victim

Target	Modality	Activity	Metabolite
BCRP 697	substrate 4014 Sources: https://www.ema.europa.eu/en/documents/assessment-report/zejula-epar-public-assessment-report_en.pdf#page=43 Page: -	no	M1 18
BSEP 63	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/208447Orig1s000MultidisciplineR.pdf#page=90 Page: 90.0	no
BSEP 63	substrate 4014 Sources: https://www.ema.europa.eu/en/documents/assessment-report/zejula-epar-public-assessment-report_en.pdf#page=42 Page: -	no	M1 18
MATE1 182	substrate 4014 Sources: https://www.ema.europa.eu/en/documents/assessment-report/zejula-epar-public-assessment-report_en.pdf#page=43 Page: -	no
MATE2 98	substrate 4014 Sources: https://www.ema.europa.eu/en/documents/assessment-report/zejula-epar-public-assessment-report_en.pdf#page=43 Page: -	no
OAT1 395	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/208447Orig1s000MultidisciplineR.pdf#page=90 Page: 90.0	no
OAT1 395	substrate 4014 Sources: https://www.ema.europa.eu/en/documents/assessment-report/zejula-epar-public-assessment-report_en.pdf#page=42 Page: -	no	M1 18
OAT3 391	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/208447Orig1s000MultidisciplineR.pdf#page=90 Page: 90.0	no
OAT3 391	substrate 4014 Sources: https://www.ema.europa.eu/en/documents/assessment-report/zejula-epar-public-assessment-report_en.pdf#page=42 Page: -	no	M1 18
OATP1B1 503	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/208447Orig1s000MultidisciplineR.pdf#page=90 Page: 90.0	no
OATP1B1 503	substrate 4014 Sources: https://www.ema.europa.eu/en/documents/assessment-report/zejula-epar-public-assessment-report_en.pdf#page=43 Page: -	no	M1 18
OATP1B3 435	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/208447Orig1s000MultidisciplineR.pdf#page=90 Page: 90.0	no
OATP1B3 435	substrate 4014 Sources: https://www.ema.europa.eu/en/documents/assessment-report/zejula-epar-public-assessment-report_en.pdf#page=43 Page: -	no	M1 18
OCT1 393	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/208447Orig1s000MultidisciplineR.pdf#page=90 Page: 90.0	no
OCT1 393	substrate 4014 Sources: https://www.ema.europa.eu/en/documents/assessment-report/zejula-epar-public-assessment-report_en.pdf#page=43 Page: -	no	M1 18
OCT2 434	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/208447Orig1s000MultidisciplineR.pdf#page=90 Page: 90.0	no
OCT2 434	substrate 4014 Sources: https://www.ema.europa.eu/en/documents/assessment-report/zejula-epar-public-assessment-report_en.pdf#page=42 Page: -	no	M1 18
P-gp 2052	substrate 4014 Sources: https://www.ema.europa.eu/en/documents/assessment-report/zejula-epar-public-assessment-report_en.pdf#page=43 Page: -	no	M1 18
BCRP 697	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/208447Orig1s000MultidisciplineR.pdf#page=72 Page: 72.0	yes
CYP1A2 1197	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/208447Orig1s000MultidisciplineR.pdf#page=89 Page: 89.0	yes
CYP2D6 1388	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/208447Orig1s000MultidisciplineR.pdf#page=89 Page: 89.0	yes
CYP3A4/5 91	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/208447Orig1s000MultidisciplineR.pdf#page=89 Page: 89.0	yes
MATE1 182	substrate 4014 Sources: https://www.ema.europa.eu/en/documents/assessment-report/zejula-epar-public-assessment-report_en.pdf#page=43 Page: -	yes	M1 18
MATE2 98	substrate 4014 Sources: https://www.ema.europa.eu/en/documents/assessment-report/zejula-epar-public-assessment-report_en.pdf#page=43 Page: -	yes	M1 18
P-gp 2052	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/208447Orig1s000MultidisciplineR.pdf#page=72 Page: 72.0	yes
UGT 219	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/208447Orig1s000MultidisciplineR.pdf#page=89 Page: 89.0	yes

Tox targets

Target	Modality	Activity	Metabolite	Clinical evidence
hERG 2263	inhibitor 2237 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/208447Orig1s000MultidisciplineR.pdf#page=30 Page: 30.0

Sourcing

Vendor/Aggregator	ID	URL
AA Blocks	AA0038X2	https://www.aablocks.com/goods/Goods/detail?id=AA0038X2
Aaron Chemicals	AR0039OU	http://www.aaronchem.com/1038915-60-4
abcr GmbH	AB435856	http://www.abcr.com/shop/en/AB435856
AbMole Bioscience	M2215	http://www.abmole.com/products/mk-4827.html
Achemo Scientific Limited	AC-86985	http://www.achemo.com/search/?Keyword= 1038915-60-4
Achemtek	0102-029640	http://www.achemtek.com/1038915-60-4
Adooq BioScience	A11026	https://www.adooq.com/mk-4827.html
Adooq BioScience	MK-4827	http://www.adooq.com/mk-4827.html
AK Scientific, Inc. (AKSCI)	0919AA	http://www.aksci.com/item_detail.php?cat=0919AA
Ambinter	Amb22388574	http://www.ambinter.com/reference/22388574
Angene	AGN-PC-0OSO5V	http://www.angenechemical.com/productshow/AGN-PC-0OSO5V.html
Anward	ANW-62065	http://www.anward.com/pro_result/48516
ApexBio Technology	A3617	http://www.apexbt.com/mk-9380.html
Aurum Pharmatech LLC	W-5696	http://www.Aurumpharmatech.com/Product/ProductDetails/W_5696
Axon MedChem	2928	https://www.axonmedchem.com/product/2928
BioCrick	BCC1761	http://www.biocrick.com/MK-4827-BCC1761.html
BLD Pharm	BD234046	http://www.bldpharm.com/products/1038915-60-4.html
Chem Scene	CS-0780	http://www.chemscene.com/1038915-60-4.html
Chemspace	CSSB00015193672	https://chem-space.com/CSSB00015193672
CSNpharm	CSN13146	https://www.csnpharm.com/products/mk-4827.html
DAOGE BIOPHARMA	DG21-13343	https://www.daogechem.com/product/1038915-60-4.html
eNovation Chemicals	D388300	http://www.enovationchem.com/productDetails.asp?productID=D388300
Excenen	EX-A290	http://www.excenen.com/searchresultlist.php?id=1038915-60-4
iChemical	EBD2206766	http://www.ichemical.com/products/1038915-60-4.html?utm_source=PubChem&utm_medium=website&utm_campaign=product%20catalogs
Lab Network	LN01331029	https://labnetwork.com/frontend-app/p/#!/moleculedetails/LN01331029
Matrix Scientific	153552	https://www.matrixscientific.com/153552.html
MedChem Express	HY-10619	https://www.medchemexpress.com/MK-4827.html
Smolecule	S537248	http://www.smolecule.com/products/s537248
Smolecule	S746643	https://www.smolecule.com/products/s746643
Synblock Inc	SB16547	http://www.synblock.com/product/1038915-60-4.html
Tenova Pharmaceuticals Inc	T31004	https://www.tenovapharma.com/Niraparib
THE BioTek	bt-277148	https://www.thebiotek.com/product/inhibitors/bt-277148
Yuhao Chemical	YH65274	http://www.chemyuhao.com/1038915-60-4.html

PubMed

Title	Date	PubMed
The Role of PARP Inhibitors in the Treatment of Gynecologic Malignancies.	2013-10-01	24098868
Trapping of PARP1 and PARP2 by Clinical PARP Inhibitors.	2012-11-01	23118055
Discovery of 2-{4-[(3S)-piperidin-3-yl]phenyl}-2H-indazole-7-carboxamide (MK-4827): a novel oral poly(ADP-ribose)polymerase (PARP) inhibitor efficacious in BRCA-1 and -2 mutant tumors.	2009-11-26	19873981
Inhibition of poly(ADP-ribose) polymerase in tumors from BRCA mutation carriers.	2009-07-09	19553641
Targeting the DNA repair defect in BRCA mutant cells as a therapeutic strategy.	2005-04-14	15829967
Specific killing of BRCA2-deficient tumours with inhibitors of poly(ADP-ribose) polymerase.	2005-04-14	15829966

Patents

Sample Use Guides

In Vivo Use Guide

Niraparib (PO, 110-210 mg) successfully inhibited poly(ADP-ribose) polymerase (PARP) during a phase I trial in patients with BRCA-deficient or sporadic cancers associated with homologous recombination repair defects. Niraparib (PO, 30-210 mg) was well tolerated during a phase I trial in patients with BRCA-deficient or sporadic cancers associated with homologous recombination repair defects. Maximum tolerated dose (MTD) of niraparib in patients with advanced solid tumours was 300 mg.

Route of Administration: Oral

In Vitro Use Guide

Niraparib (MK-4827) inhibited proliferation of cancer cells with mutant BRCA-1 and BRCA-2 with CC(50) in the 10-100 nM range.

Substance Class	Chemical Created by `admin` on `Mon Mar 31 22:33:35 GMT 2025` Edited by `admin` on `Mon Mar 31 22:33:35 GMT 2025`
Record UNII	195Q483UZD
Record Status	`Validated (UNII)`
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Name

Type

Language

Niraparib tosylate monohydrate

Preferred Name

English

Niraparib tosylate

Official Name

English

ZEJULA

Brand Name

English

(S)-2-[4-(Piperidin-3-yl)phenyl]-2H-indazole-7-carboxamide 4-methylbenzenesulfonate hydrate

Systematic Name

English

GSK3985771

Code

English

NIRAPARIB TOSYLATE [USAN]

Common Name

English

GSK-3985771

Code

English

AKEEGA COMPONENT NIRAPARIB TOSYLATE

Brand Name

English

2H-Indazole-7-carboxamide, 2-[4-(3S)-3-piperidinylphenyl]-, 4-methylbenzenesulfonate, hydrate (1:1:1)

Systematic Name

English

MK-4827 TOSYLATE MONOHYDRATE

Code

English

NIRAPARIB TOSILATE HYDRATE

Common Name

English

NIRAPARIB TOSYLATE MONOHYDRATE [MI]

Common Name

English

NIRAPARIB TOSILATE HYDRATE [JAN]

Common Name

English

Niraparib tosylate monohydrate [WHO-DD]

Common Name

English

Classification Tree Code System Code

NCI_THESAURUS

C62554