Target Information

Target General Infomation
Target ID
T34867
Target Name
Poly ADP ribose polymerase (PARP)
Target Type
Successful
Disease Acute ischemic stroke [ICD9: 434.91; ICD10: I61-I63]
Breast cancer [ICD9: 174, 175; ICD10: C50]
Brain cancer [ICD9: 191, 225.0; ICD10: C71, D33]
Breast cancer; Ovarian cancer [ICD9:174, 175, 183; ICD10: C50, C56]
BRCA-positive ovarian cancer [ICD10: C56]
Breast cancer; Ovarian cancer [ICD9: 174, 175, 183; ICD10: C50, C56]
Cerebrovascular ischaemia; Non-small cell lung cancer [ICD9:434.91; ICD10: I61-I63, C33-C34]
Cerebrovascular ischaemia [ICD9: 434.91; ICD10: I61-I63]
Melanoma [ICD9: 172; ICD10: C43]
Ovarian cancer [ICD9: 183; ICD10: C56]
Psoriatic arthritis [ICD9: 696; ICD10: L40.5, M07]
Solid tumours [ICD9: 140-199, 210-229; ICD10: C00-D48]
Type 2 diabetes [ICD9: 250; ICD10: E11]
BioChemical Class
Transferases (EC:2)
EC Number
EC 2.4.2.30
Drugs and Mode of Action
Drug(s) Olaparib Drug Info Approved Breast cancer; Ovarian cancer [542530], [550296]
Rucaparib Drug Info Approved BRCA-positive ovarian cancer [889440]
ABT-888 Drug Info Phase 3 Breast cancer [524798], [542441]
BMN-673 Drug Info Phase 3 Psoriatic arthritis [524436], [543065]
BSI-201 Drug Info Phase 3 Solid tumours [531781], [543086]
INO-1001 Drug Info Phase 3 Brain cancer [527044], [530857]
Rucaparib Drug Info Phase 3 Breast cancer; Ovarian cancer [524484], [542704]
BGP-15 Drug Info Phase 2 Type 2 diabetes [526305], [531807]
E7016 Drug Info Phase 2 Melanoma [523915]
MK-4827 Drug Info Phase 2 Ovarian cancer [523258], [543030]
CEP-9722 Drug Info Phase 1/2 Cerebrovascular ischaemia; Non-small cell lung cancer [523387]
ABT-767 Drug Info Phase 1 Solid tumours [523443]
MP-124 Drug Info Phase 1 Acute ischemic stroke [531546]
ONO-2231 Drug Info Discontinued in Phase 1 Cerebrovascular ischaemia [548174]
Modulator ABT-767 Drug Info [1572591]
ABT-888 Drug Info [1572591]
BGP-15 Drug Info [526305], [531807]
BMN-673 Drug Info [1572591]
BSI-201 Drug Info [531781]
CEP-9722 Drug Info [1572591]
E7016 Drug Info [1572591]
INO-1001 Drug Info [527044], [530857]
MK-4827 Drug Info [1572591]
MP-124 Drug Info
Olaparib Drug Info [533123]
ONO-2231 Drug Info
Rucaparib Drug Info [889440]
References
Ref 523258ClinicalTrials.gov (NCT01244009) A Study of MK-4827 for the Treatment of Mantle Cell Lymphoma (MK-4827-002). U.S. National Institutes of Health.
Ref 523387ClinicalTrials.gov (NCT01311713) Study to Determine the Maximum Tolerated Dose of the PARP Inhibitor CEP-9722 in Patients With Solid Tumors. U.S. National Institutes of Health.
Ref 523443ClinicalTrials.gov (NCT01339650) Study of ABT-767 in Subjects With Breast Cancer 1 and Breast Cancer 2 (BRCA 1 and BRCA 2) Mutations and Solid Tumors or High Grade Serous Ovarian, Fallopian Tube, or Primary Peritoneal Cancer. U.S. National Institutes of Health.
Ref 523915ClinicalTrials.gov (NCT01605162) Phase 2 Study of the Poly(ADP-Ribose) Polymerase Inhibitor E7016 in Combination With Temozolomide in Subjects With Wild Type BRAF Stage IV or Unresectable Stage III Melanoma. U.S. National Institutes of Health.
Ref 524436ClinicalTrials.gov (NCT01945775) A Study Evaluating Talazoparib (BMN 673), a PARP Inhibitor, in Advanced and/or Metastatic Breast Cancer Patients With BRCA Mutation (EMBRACA Study). U.S. National Institutes of Health.
Ref 524484ClinicalTrials.gov (NCT01968213) A Study of Rucaparib as Switch Maintenance Following Platinum-Based Chemotherapy in Patients With Platinum-Sensitive, High-Grade Serous or Endometrioid Epithelial Ovarian, Primary Peritoneal or Fallopian Tube Cancer. U.S. National Institutes of Health.
Ref 524798ClinicalTrials.gov (NCT02163694) A Phase 3 Randomized, Placebo-controlled Trial of Carboplatin and Paclitaxel With or Without Veliparib (ABT-888) in HER2-negative Metastatic or Locally Advanced Unresectable BRCA-associated Breast Cancer. U.S. National Institutes of Health.
Ref 526305BGP-15 - a novel poly(ADP-ribose) polymerase inhibitor - protects against nephrotoxicity of cisplatin without compromising its antitumor activity. Biochem Pharmacol. 2002 Mar 15;63(6):1099-111.
Ref 527044INO-1001 a novel poly(ADP-ribose) polymerase (PARP) inhibitor improves cardiac and pulmonary function after crystalloid cardioplegia and extracorporal circulation. Shock. 2004 May;21(5):426-32.
Ref 530857Therapeutic 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.
Ref 531546MP-124, a novel poly(ADP-ribose) polymerase-1 (PARP-1) inhibitor, ameliorates ischemic brain damage in a non-human primate model. Brain Res. 2011 Sep 2;1410:122-31.
Ref 531781Failure of iniparib to inhibit poly(ADP-Ribose) polymerase in vitro. Clin Cancer Res. 2012 Mar 15;18(6):1655-62.
Ref 531807BGP-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.
Ref 542441(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7417).
Ref 542530(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7519).
Ref 542704(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7736).
Ref 543030(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 8275).
Ref 543065(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 8313).
Ref 543086(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 8360).
Ref 548174Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800022742)
Ref 550296LYNPARZA? approved by the US food and drug administration for the treatment of advanced ovarian cancer in patients with germline BRCA-mutations
Ref 8894402016 FDA drug approvals. Nat Rev Drug Discov. 2017 Feb 2;16(2):73-76. doi: 10.1038/nrd.2017.14.
Ref
Ref 526305BGP-15 - a novel poly(ADP-ribose) polymerase inhibitor - protects against nephrotoxicity of cisplatin without compromising its antitumor activity. Biochem Pharmacol. 2002 Mar 15;63(6):1099-111.
Ref 527044INO-1001 a novel poly(ADP-ribose) polymerase (PARP) inhibitor improves cardiac and pulmonary function after crystalloid cardioplegia and extracorporal circulation. Shock. 2004 May;21(5):426-32.
Ref 530857Therapeutic 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.
Ref 531781Failure of iniparib to inhibit poly(ADP-Ribose) polymerase in vitro. Clin Cancer Res. 2012 Mar 15;18(6):1655-62.
Ref 531807BGP-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.
Ref 5331232014 FDA drug approvals. Nat Rev Drug Discov. 2015 Feb;14(2):77-81.
Ref 8894402016 FDA drug approvals. Nat Rev Drug Discov. 2017 Feb 2;16(2):73-76. doi: 10.1038/nrd.2017.14.
Ref 1572591Interpreting expression profiles of cancers by genome-wide survey of breadth of expression in normal tissues. Genomics 2005 Aug;86(2):127-41.

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