Details of the Drug Therapeutic Target (DTT)

General Information of Drug Therapeutic Target (DTT) (ID: TTEBCY8)

• DTT Name: Poly [ADP-ribose] polymerase (PARP)
• Synonyms: Poly-ADP-ribose polymerase
• Gene Name: PARP
• DTT Type: Successful target; [1]
• UniProt ID: NOUNIPROTAC
• TTD ID: T34867

Molecular Interaction Atlas (MIA) of This DTT

3 Approved Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Olaparib	DM8QB1D	Ovarian cancer	2C73	Approved	[1]
Rucaparib	DM9PVX8	Ovarian cancer	2C73	Approved	[2]
Talazoparib	DM1KS78	Breast cancer	2C60-2C65	Approved	[3]

13 Clinical Trial Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
ABT-888	DM4HYMS	Breast cancer	2C60-2C65	Phase 3	[4]
BSI-201	DMM0VO3	Solid tumour/cancer	2A00-2F9Z	Phase 3	[5]
INO-1001	DM5L8QT	Brain cancer	2A00	Phase 3	[6]
MK-4827	DMLYGH4	Ovarian cancer	2C73	Phase 3	[4]
Rubraca rucaparib	DM25TMP	Ovarian cancer	2C73	Phase 3	[7]
2X-121	DMX9MSL	Breast cancer	2C60-2C65	Phase 2	[7]
AZD9574	DMKAIR9	Aggressive cancer	2A00-2F9Z	Phase 2	[8]
BGB-290	DMRO6XT	Ovarian cancer	2C73	Phase 2	[7]
BGP-15	DMYDM68	Type-2 diabetes	5A11	Phase 2	[9]
E7016	DMAHGKE	Melanoma	2C30	Phase 2	[4]
CEP-9722	DMY8NUF	Cerebrovascular ischaemia	8B1Z	Phase 1/2	[4]
ABT-767	DMFH3JM	Solid tumour/cancer	2A00-2F9Z	Phase 1	[4]
MP-124	DMQRNTG	Ischemic stroke	8B11.5Z	Phase 1	[10]

15 Patented Agent(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
7-azaindole derivative 9	DMAY4G1	N. A.	N. A.	Patented	[11]
Aza-phenalene-3-ketone derivative 1	DMEUHCD	N. A.	N. A.	Patented	[11]
Dihydrodiazepinocarbazolone derivative 2	DM1R0FJ	N. A.	N. A.	Patented	[11]
Dihydropyrido phthalazinone derivative 3	DMMFBI3	N. A.	N. A.	Patented	[11]
Dihydropyrido phthalazinone derivative 4	DMWEJ6U	N. A.	N. A.	Patented	[11]
Phthalazine derivative 1	DMZPHN5	N. A.	N. A.	Patented	[11]
Phthalazine derivative 2	DMODTSC	N. A.	N. A.	Patented	[11]
PMID27841036-Compound-23	DMY9WHZ	N. A.	N. A.	Patented	[11]
PMID27841036-Compound-24	DM9VMJ3	N. A.	N. A.	Patented	[11]
PMID27841036-Compound-36	DMHIV2L	N. A.	N. A.	Patented	[11]
PMID27841036-Compound-38	DM1KJAQ	N. A.	N. A.	Patented	[11]
PMID27841036-Compound-V	DM3FAIS	N. A.	N. A.	Patented	[11]
PMID27841036-Compound-XI	DM1HPY7	N. A.	N. A.	Patented	[11]
PMID27841036-Compound-XVII	DM9K5BZ	N. A.	N. A.	Patented	[11]
Tetra/penta-cyclic pyridophthalazinone derivative 1	DMS3YPJ	N. A.	N. A.	Patented	[11]

1 Discontinued Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
ONO-2231	DM8KN2M	Cerebrovascular ischaemia	8B1Z	Discontinued in Phase 1	[12]

References

• [1] 2014 FDA drug approvals. Nat Rev Drug Discov. 2015 Feb;14(2):77-81.
• [2] 2016 FDA drug approvals. Nat Rev Drug Discov. 2017 Feb 2;16(2):73-76.
• [3] 2018 FDA drug approvals.Nat Rev Drug Discov. 2019 Feb;18(2):85-89.
• [4] Interpreting expression profiles of cancers by genome-wide survey of breadth of expression in normal tissues. Genomics 2005 Aug;86(2):127-41.
• [5] Failure of iniparib to inhibit poly(ADP-Ribose) polymerase in vitro. Clin Cancer Res. 2012 Mar 15;18(6):1655-62.
• [6] Therapeutic injection of PARP inhibitor INO-1001 preserves cardiac function in porcine myocardial ischemia and reperfusion without reducing infarct size. Shock. 2010 May;33(5):507-12.
• [7] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
• [8] Clinical pipeline report, company report or official report of AstraZeneca
• [9] BGP-15, a PARP-inhibitor, prevents imatinib-induced cardiotoxicity by activating Akt and suppressing JNK and p38 MAP kinases. Mol Cell Biochem. 2012 Jun;365(1-2):129-37.
• [10] Company report (Mitsubishi Tanabe Pharma)
• [11] PARP inhibitors as antitumor agents: a patent update (2013-2015).Expert Opin Ther Pat. 2017 Mar;27(3):363-382.
• [12] Company report (ONO PHARMACEUTICAL)