title: PARP inhibitors as antitumor agents: a patent update (2013-2015).
abstract: PARP inhibitors have been extensively explored as antitumor agents and have shown potent efficacy both in vitro and in vivo. They can be used in monotherapy under the synthetic lethality concept or in combination with radiotherapy or chemotherapy, inducing a synergistic effect. Areas covered: This review covers relevant efforts in the development of PARP inhibitors with a particular focus on recently patented PARP inhibitors, combination therapy involving PARP inhibitors, tumor responsiveness to PARP inhibitors as detailed in reports made from 2013 - 2015, and PARP drugs in clinical trials and other novel inhibitors that emerged in 2013 - 2015. Expert opinion: Clinical studies and applications of PARP inhibitors as antitumor agents have gained considerable recognition in the last few years. In addition to FDA-approved olaparib, an increasing number of new inhibitors have been designed and synthesized, some of which are under preclinical or clinical evaluation. Novel inhibitors are still required, especially new scaffold compounds or drugs with improved properties, such as higher selectivity, higher potency and lower toxicity. The development of combination therapies involving PARP inhibitors and the exploration of biomarkers to predict outcomes with PARP inhibitors would expand the applications of these inhibitors, allowing more patients to benefit from this promising class of drugs in the future.
authors.affiliation: a Department of Chemistry , Tsinghua University , Beijing , P. R. China.|b The Ministry-Province Jointly Constructed Base for State Key Lab-Shenzhen Key Laboratory of Chemical Biology, the Graduate School at Shenzhen , Tsinghua University , Shenzhen , P. R. China.
authors.forename: Zigao
authors.initials: Z
authors.lastname: Yuan
authors.affiliation: a Department of Chemistry , Tsinghua University , Beijing , P. R. China.|b The Ministry-Province Jointly Constructed Base for State Key Lab-Shenzhen Key Laboratory of Chemical Biology, the Graduate School at Shenzhen , Tsinghua University , Shenzhen , P. R. China.
authors.forename: Jiwei
authors.initials: J
authors.lastname: Chen
authors.affiliation: a Department of Chemistry , Tsinghua University , Beijing , P. R. China.|b The Ministry-Province Jointly Constructed Base for State Key Lab-Shenzhen Key Laboratory of Chemical Biology, the Graduate School at Shenzhen , Tsinghua University , Shenzhen , P. R. China.
authors.forename: Wenlu
authors.initials: W
authors.lastname: Li
authors.affiliation: a Department of Chemistry , Tsinghua University , Beijing , P. R. China.|b The Ministry-Province Jointly Constructed Base for State Key Lab-Shenzhen Key Laboratory of Chemical Biology, the Graduate School at Shenzhen , Tsinghua University , Shenzhen , P. R. China.
authors.forename: Dan
authors.initials: D
authors.lastname: Li
authors.affiliation: a Department of Chemistry , Tsinghua University , Beijing , P. R. China.|b The Ministry-Province Jointly Constructed Base for State Key Lab-Shenzhen Key Laboratory of Chemical Biology, the Graduate School at Shenzhen , Tsinghua University , Shenzhen , P. R. China.
authors.forename: Changjun
authors.initials: C
authors.lastname: Chen
authors.affiliation: b The Ministry-Province Jointly Constructed Base for State Key Lab-Shenzhen Key Laboratory of Chemical Biology, the Graduate School at Shenzhen , Tsinghua University , Shenzhen , P. R. China.|c National & Local United Engineering Lab for Personalized anti-tumor drugs, the Graduate School at Shenzhen , Tsinghua University , Shenzhen , P. R. China.
authors.forename: Chunmei
authors.initials: C
authors.lastname: Gao
authors.affiliation: b The Ministry-Province Jointly Constructed Base for State Key Lab-Shenzhen Key Laboratory of Chemical Biology, the Graduate School at Shenzhen , Tsinghua University , Shenzhen , P. R. China.|c National & Local United Engineering Lab for Personalized anti-tumor drugs, the Graduate School at Shenzhen , Tsinghua University , Shenzhen , P. R. China.|d School of Medicine , Tsinghua University , Beijing , P. R. China.
authors.forename: Yuyang
authors.initials: Y
authors.lastname: Jiang
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000009:adverse effects / Q000494:pharmacology*; D003131:Combined Modality Therapy; D015195:Drug Design; D006801:Humans; D009369:Neoplasms / Q000188:drug therapy*; D010330:Patents as Topic; D010793:Phthalazines / Q000494:pharmacology; D010879:Piperazines / Q000494:pharmacology; D000067856:Poly(ADP-ribose) Polymerase Inhibitors / Q000009:adverse effects / Q000494:pharmacology*
chemical_list: D000970:Antineoplastic Agents; D010793:Phthalazines; D010879:Piperazines; D000067856:Poly(ADP-ribose) Polymerase Inhibitors; C531550:olaparib
keywords: PARP inhibitors; biomarkers; combination therapy; drug design; synthetic lethality