Threshold Pharmaceuticals - Scientific Publications



Hypoxia Activated Prodrugs Initial Clinical Observations Regarding TH-302, a Tumor Selective Hypoxia-Activated Prodrug in Metastatic Melanoma, Curd et al., Perspectives in Melanoma XIII Conference, October 2009. Multi-arm Phase IB study of TH-302 in combination with gemcitabine, docetaxel or pemetrexed, Borad et al., Joint 15th Congress of the European CanCer Organisation (ECCO) and the 34th Congress of the European Society for Medical Oncology (ESMO), September 2009. Final results of a phase I study of TH-302, a hypoxia-activated cytotoxic prodrug (HAP), Bendell et al., American Society of Clinical Oncology (ASCO) Annual Meeting, June 2009. TH-302, a novel hypoxia-activated prodrug, shows superior efficacy and less toxicity than ifosfamide (IFOS) in metastatic and ectopic human lung carcinoma models, Ahluwalia et al., American Association for Cancer Research (AACR) Annual Meeting, April 2009. TH-302 pharmacological activity in 3D multicellular tumor spheroid models, Meng et al., American Association for Cancer Research (AACR) Annual Meeting, April 2009. Preclinical dose sequence and regimen optimization of the hypoxia-activated prodrug TH-302, Sun et al., American Association for Cancer Research (AACR) Annual Meeting, April 2009. Complementary Chemotherapies with TH-302, a Novel Hypoxia-Activated Prodrug: Optimization of Dosing Regimens and Schedules for Study in Phase 1/2 with Docetaxel, Gemcitabine, Pemetrexed, and Doxorubicin, J.Sun et al., BioSymposia: Hypoxia, Ischemia and Inflammation, November 2008. A First-in-Man Phase 1 Study of TH-302, A Hypoxia-Activated Cytotoxic Prodrug (HAP), G.Weiss et al., European Organisation for Research and Treatment of Cancer (EORTC) Annual Meeting, October 2008. Efficacy of the Hypoxia-Activated Prodrug TH-302 in a Preclinical Model of Prostate Cancer Metastasis, C.Hart et al., American Association for Cancer Research (AACR) Centennial Meeting, August 2008. Anti-cancer activity of Hypoxia-Activated Prodrug, TH-302 in H460 non-small cell lung carcinoma metastatic, J.Sun et al., American Association for Cancer Research (AACR) Centennial Meeting, August 2008. Targeting Tumor Hypoxia with TH-302 and Complementary Chemotherapy, J.Curd et al., American Association for Cancer Research (AACR) Conference on Translational Medicine, July 2008. Potent and Highly Selective Hypoxia-Activated Achiral Phosphoramidate Mustards as Anticancer Drugs, J. Duan et al., Journal of Medicinal Chemistry, 51: 2412-2420, 2008. In vitro activity profile of the novel hypoxia-activated cytotoxic prodrug, TH-302, C.Hart et al., American Association for Cancer Research (AACR) Annual Meeting, April 2008. Plasma pharmacokinetics, oral bioavailability, and interspecies scaling of the hypoxically activated prodrug, TH-302, in mice, rats, dogs and monkeys, D.Jung et al., American Association for Cancer Research (AACR) Annual Meeting, April 2008. Anti-cancer activity of TH-1011, a novel Hypoxia-activated prodrug, is related to tumor vessel disruption, J.Sun et al., American Association for Cancer Research (AACR) Annual Meeting, April 2008. Discovery of TH-302: an achiral hypoxia-activated cytotoxic prodrug, C. Hart et al., American Society of Clinical Oncology (ASCO) Annual Meeting, June 2007. in vivo anti-cancer activity of a hypoxia activated prodrug, TH-302, J. Wang et al., American Association for Cancer Research (AACR) Annual Meeting, April 2007. A cell-based screening platform for hypoxia-activated prodrugs, J.W. Evans et al., American Association for Cancer Research (AACR) Annual Meeting, April 2006. Glufosfamide A Phase 1 dose-escalation trial of glufosfamide in combination with gemcitabine in solid tumors including pancreatic adenocarcinoma, E.G. Chiorean et al., Cancer Chemother Pharmacol (2008) 61:1019-1026 Preliminary Efficacy and Safety Results of Glufosfamide (GLU) in Relapsed Soft Tissue Sarcoma: Results of a Phase 2 Trial, G.D’Amato et al., American Society of Clinical Oncology (ASCO) Annual Meeting, June 2008. Glufosfamide (GLU) in metastatic pancreatic adenocarcinoma previously treated with gemcitabine: results of a phase III trial (TH-CR-302), V.K. Langmuir et al., European Cancer Conference (ECCO) Annual Meeting, September 2007. Glufosfamide (GLU) plus gemcitabine (GEM) in pancreatic adenocarcinoma: results of a phase 2 trial (TH-CR-301), E.G. Chiorean et al., European Cancer Conference (ECCO) Annual Meeting, September 2007. Glufosfamide administered using a 1-hour infusion given as first-line treatment for advanced pancreatic cancer. A phase II trial of the EORTC-new drug development group, E. Briasoulis et al., European Journal of Cancer, 39: 2334-2340, 2003. Phase I trial of 6-hour infusion of glufosfamide, a new alkylating agent with potentially enhanced selectivity for tumors that overexpress transmembrane glucose transporters: a study of the European Organization for Research and Treatment of Cancer Early Clinical Studies Group, E. Briasoulis et al., Journal of Clinical Oncology 18: 3535-3544, 2000. 2-Deoxyglucose (2-DG) Glycolytic inhibition with 2-Deoxy-glucose in patients with lung and head and neck cancers, L.E. Raez et al., ASCO 2006. Research Antiproliferative activity of 3-bromopyruvate is not due to selective inhibition of glycolysis, F.Meng et al., American Association for Cancer Research (AACR) Annual Meeting, April 2008. A novel class of tubulin inhibitors that exhibit potent antiproliferation and in vitro vessel-disrupting activity, F. Meng et al., Cancer Chemotherapy and Pharmacology, 61: 953-963, 2008. Potent anti-tubulin tumor cell cytotoxins based on 3-aroyl indazoles, J. Duan et al., Journal of Medicinal Chemistry, 50: 1001-1006, 2007. 3-aroyl indazoles: their synthesis and potential use for cancer treatment, J.Duan et al., American Association for Cancer Research (AACR) Annual Meeting, April 2007. ARC-111 inhibits hypoxia-mediated hypoxia-inducible factor-1α accumulation, F. Meng et al., Anti-Cancer Drugs, 18: 435-445, 2007. Final results of a phase I study of TH-302, a hypoxia-activated cytotoxic prodrug (HAP), Bendell et al., American Society of Clinical Oncology (ASCO) Annual Meeting, June 2009. TH-302, a novel hypoxia-activated prodrug, shows superior efficacy and less toxicity than ifosfamide (IFOS) in metastatic and ectopic human lung carcinoma models, Ahluwalia et al., American Association for Cancer Research (AACR) Annual Meeting, April 2009. TH-302 pharmacological activity in 3D multicellular tumor spheroid models, Meng et al., American Association for Cancer Research (AACR) Annual Meeting, April 2009. Preclinical dose sequence and regimen optimization of the hypoxia-activated prodrug TH-302, Sun et al., American Association for Cancer Research (AACR) Annual Meeting, April 2009. Complementary Chemotherapies with TH-302, a Novel Hypoxia-Activated Prodrug: Optimization of Dosing Regimens and Schedules for Study in Phase 1/2 with Docetaxel, Gemcitabine, Pemetrexed, and Doxorubicin, J.Sun et al., BioSymposia: Hypoxia, Ischemia and Inflammation, November 2008. A First-in-Man Phase 1 Study of TH-302, A Hypoxia-Activated Cytotoxic Prodrug (HAP), G.Weiss et al., European Organisation for Research and Treatment of Cancer (EORTC) Annual Meeting, October 2008. Efficacy of the Hypoxia-Activated Prodrug TH-302 in a Preclinical Model of Prostate Cancer Metastasis, C.Hart et al., American Association for Cancer Research (AACR) Centennial Meeting, August 2008. Anti-cancer activity of Hypoxia-Activated Prodrug, TH-302 in H460 non-small cell lung carcinoma metastatic, J.Sun et al., American Association for Cancer Research (AACR) Centennial Meeting, August 2008. Targeting Tumor Hypoxia with TH-302 and Complementary Chemotherapy, J.Curd et al., American Association for Cancer Research (AACR) Conference on Translational Medicine, July 2008. Potent and Highly Selective Hypoxia-Activated Achiral Phosphoramidate Mustards as Anticancer Drugs, J. Duan et al., Journal of Medicinal Chemistry, 51: 2412-2420, 2008. In vitro activity profile of the novel hypoxia-activated cytotoxic prodrug, TH-302, C.Hart et al., American Association for Cancer Research (AACR) Annual Meeting, April 2008. Plasma pharmacokinetics, oral bioavailability, and interspecies scaling of the hypoxically activated prodrug, TH-302, in mice, rats, dogs and monkeys, D.Jung et al., American Association for Cancer Research (AACR) Annual Meeting, April 2008. Anti-cancer activity of TH-1011, a novel Hypoxia-activated prodrug, is related to tumor vessel disruption, J.Sun et al., American Association for Cancer Research (AACR) Annual Meeting, April 2008. Discovery of TH-302: an achiral hypoxia-activated cytotoxic prodrug, C. Hart et al., American Society of Clinical Oncology (ASCO) Annual Meeting, June 2007. in vivo anti-cancer activity of a hypoxia activated prodrug, TH-302, J. Wang et al., American Association for Cancer Research (AACR) Annual Meeting, April 2007. A cell-based screening platform for hypoxia-activated prodrugs, J.W. Evans et al., American Association for Cancer Research (AACR) Annual Meeting, April 2006. Glufosfamide A Phase 1 dose-escalation trial of glufosfamide in combination with gemcitabine in solid tumors including pancreatic adenocarcinoma, E.G. Chiorean et al., Cancer Chemother Pharmacol (2008) 61:1019-1026 Preliminary Efficacy and Safety Results of Glufosfamide (GLU) in Relapsed Soft Tissue Sarcoma: Results of a Phase 2 Trial, G.D’Amato et al., American Society of Clinical Oncology (ASCO) Annual Meeting, June 2008. Glufosfamide (GLU) in metastatic pancreatic adenocarcinoma previously treated with gemcitabine: results of a phase III trial (TH-CR-302), V.K. Langmuir et al., European Cancer Conference (ECCO) Annual Meeting, September 2007. Glufosfamide (GLU) plus gemcitabine (GEM) in pancreatic adenocarcinoma: results of a phase 2 trial (TH-CR-301), E.G. Chiorean et al., European Cancer Conference (ECCO) Annual Meeting, September 2007. Glufosfamide administered using a 1-hour infusion given as first-line treatment for advanced pancreatic cancer. A phase II trial of the EORTC-new drug development group, E. Briasoulis et al., European Journal of Cancer, 39: 2334-2340, 2003. Phase I trial of 6-hour infusion of glufosfamide, a new alkylating agent with potentially enhanced selectivity for tumors that overexpress transmembrane glucose transporters: a study of the European Organization for Research and Treatment of Cancer Early Clinical Studies Group, E. Briasoulis et al., Journal of Clinical Oncology 18: 3535-3544, 2000. 2-Deoxyglucose (2-DG) Glycolytic inhibition with 2-Deoxy-glucose in patients with lung and head and neck cancers, L.E. Raez et al., ASCO 2006. Research Antiproliferative activity of 3-bromopyruvate is not due to selective inhibition of glycolysis, F.Meng et al., American Association for Cancer Research (AACR) Annual Meeting, April 2008. A novel class of tubulin inhibitors that exhibit potent antiproliferation and in vitro vessel-disrupting activity, F. Meng et al., Cancer Chemotherapy and Pharmacology, 61: 953-963, 2008. Potent anti-tubulin tumor cell cytotoxins based on 3-aroyl indazoles, J. Duan et al., Journal of Medicinal Chemistry, 50: 1001-1006, 2007. 3-aroyl indazoles: their synthesis and potential use for cancer treatment, J.Duan et al., American Association for Cancer Research (AACR) Annual Meeting, April 2007. ARC-111 inhibits hypoxia-mediated hypoxia-inducible factor-1α accumulation, F. Meng et al., Anti-Cancer Drugs, 18: 435-445, 2007.