Scientific Presentations & Publications

TH-302 Research

  • Mechanistic Studies of the Potentiation of Hypoxia-Targeted Drug TH-302 by Co-treatment with Checkpoint Kinase (Chk1) Inhibitors. Meng et al. 2013 AACR Annual Meeting, April 2013. Poster doc.

  • Response Biomarkers for the Hypoxia-Targeted Drug TH-302: Imaging, Plasma, and Tissue. Sun et al. 2013 AACR Annual Meeting, April 2013. Poster doc.

Hypoxia Activated Prodrug (HAP) TH-302

  • TH-302 + gemcitabine (G+T) vs gemcitabine (G) in patients with previously untreated advanced pancreatic cancer. Ryan et al. 2013 Gastrointestinal Cancers Symposium, January 2013. Poster doc.

  • Leukemia Microenvironment and Pathologic Hypoxia: Sensitivity to Hypoxia-Activated Cytotoxin TH-302. Benito et al. 2012 ASH Annual Meeting, December 2012. Poster doc.

  • Activity of the Hypoxia-Activated Prodrug, TH-302, in Human Acute Myeloid Leukemia Models. Poortwood et al. 2012 ASH Annual Meeting, December 2012. Poster doc.

  • TH-302 Maintenance Following TH-302 Plus Doxorubicin Induction: The Results pf a Phase 2 Study of TH-302 in Combination with Doxorubicin in Soft Tissue Sarcoma. Ganjoo et al. Connective Tissue Oncology Society (CTOS) 2012 Meeting, November 2012. PDF doc.

  • A dual phase I/II study of TH-302 and bevacizumab in resectable recurrent glioblastoma following single-agent bevacizumab failure. Zuniga et al. European Society for Medical Oncology (ESMO) 2012 Congress, September 2012. PDF doc.

  • TH-302 Plus Gemcitabine vs. Gemcitabine in Patients with Untreated Advanced Pancreatic Adenocarcinoma. Borad et al. European Society for Medical Oncology (ESMO) 2012 Congress, September 2012. Threshold Pharmaceuticals, Inc. PDF doc.

  • Preclinical Evaluation of Antitumor Efficacy of the Hypoxia-Activated Prodrug TH-302 and Sunitinib in Neuroblastoma Mouse Models. Kumar et al. Advances In Neuroblastoma Research (ANR) Conference, June 2012. PDF doc.

  • Hypoxia-Activated Prodrug TH-302 in Combination with Gemcitabine for the Treatment of Pancreatic Adenocarcinoma: Preclinical and Clinical Studies. Hart et al. American Association for Cancer Research (AACR) Pancreatic Cancer: Progress and Challenges, June 2012. Poster PDF.

  • Randomized phase III, multicenter, open-label study comparing TH-302 in combination with doxorubicin versus doxorubicin alone in subjects with locally advanced unresectable or metastatic soft tissue sarcoma. Chawla et al. American Society for Clinical Oncology (ASCO) Annual Meeting, June 2012. Poster PDF.

  • Phase I study of TH-302, a hypoxia-activated cytotoxic prodrug, in subjects with advanced leukemias. Thomas et al. American Society for Clinical Oncology (ASCO) Annual Meeting, June 2012. Poster PDF.

  • Enhancement of hypoxia-activated prodrug TH-302 activity by Chk1 inhibition. Meng et al. AACR Annual Meeting, April 2012. Poster PDF.

  • Randomized phase II study of the efficacy and safety of gemcitabine + TH-302 (G+T) vs gemcitabine (G) alone in previously untreated patients with advanced pancreatic cancer. Borad et al. AACR Annual Meeting, April 2012. Presentation PDF.

  • Combination treatment with hypoxia-activated prodrug TH-302 and the mTOR inhibitor everolimus results in enhanced antitumor efficacy in preclinical models. Sun et al. AACR Annual Meeting, April 2012. Poster PDF.

  • Hypoxia activated pro-drug TH-302 induces hypoxia-dependent anti-leukemia activity in vitro and in vivo. Benito et al. AACR Annual Meeting, April 2012. Poster PDF.

  • Selective tumor hypoxia targeting by hypoxia-activated prodrug TH-302 inhibits tumor growth in preclinical models of cancer. Sun et al. Clinical Cancer Research, December 2011. PubMed page.

  • Molecular and cellular pharmacology of the hypoxia-activated prodrug TH-302. Meng et al. Molecular Cancer Therapeutics, December 2011. PubMed page.

  • Resolution of Cullen's sign in patient with metastatic melanoma responding to hypoxia-activated prodrug TH-302. Weiss et al. Dermatology Reports 3: 128-129, 2011. PDF doc.

  • A phase 2 study of TH-302 in combination with doxorubicin in advanced soft tissue sarcoma. Chawla et al. Connective Tissue Oncology Society (CTOS) Annual Meeting, October 2011. PDF doc.

  • Metabolism, pharmacokinetics and excretion of a novel hypoxia activated cytotoxic prodrug, TH-302, in rats. Jung et al. Xenobiotica. October 2011. PubMed page.

  • Pharmacokinetics of TH-302: a hypoxically activated prodrug of bromo-isophosphoramide mustard in mice, rats, dogs and monkeys. Jung et al. Cancer Chemotherapy and Pharmacology. October 2011. PubMed page.

  • Randomized phase II study of the efficacy and safety of gemcitabine + TH-302 vs gemcitabine alone in previously untreated patients with advanced pancreatic cancer. Borad et al. American Society for Clinical Oncology (ASCO) Annual Meeting, June 2011. PDF doc.

  • A phase 2 dose expansion of TH-302 in combination with doxorubicin in advanced soft tissue sarcoma. Cranmer et al. American Society for Clinical Oncology (ASCO) Annual Meeting, June 2011. PDF doc.

  • A phase I study of the safety and pharmacokinetics of the hypoxia-activated prodrug TH-302 in combination with doxorubicin in patients with advanced soft tissue sarcoma. Ganjoo et al. Oncology 80: 50-56, 2011. PubMed page.

  • Phase 1 study of the safety, tolerability, and pharmacokinetics of TH-302, a hypoxia-activated prodrug, in patients with advanced solid malignancies. Weiss et al. Clinical Cancer Research 17: 2997-3004, 2011. PubMed page.

  • Combination of TH-302 and bortezomib has synergistic activity in multiple myeloma. Hu et al. 13th International Myeloma Workshop, May 2011. PDF doc.

  • Hypoxia-dependent in vivo activity of the hypoxia-activated prodrug (HAP) TH-302. Sun et al. American Association for Cancer Research (AACR) Annual Meeting, April 2011. PDF doc.

  • Hypoxia-activated prodrug TH-302 enhances antitumor activity of antiangiogenics in preclinical models. Sun et al. American Association for Cancer Research (AACR) Annual Meeting, April 2011. PDF doc.

  • TH-302, a tumor selective hypoxia-activated prodrug, complements the clinical benefits of gemcitabine in first line pancreatic cancer. Borad et al. ASCO Gastrointestinal Cancers Symposium, January 2011. PDF doc.

  • Targeting the multiple myeloma hypoxic niche with TH-302, a hypoxia-activated prodrug. Hu et al. Blood 116: 1524-1527, 2010. PubMed page.

  • TH-302, a tumor selective hypoxia-activated prodrug, complements and enhances chemotherapy treatment with gemcitabine, docetaxel, pemetrexed and doxorubicin. Hart et al. EORTC-NCI-AACR Symposium on Molecular Targets and Cancer Therapeutics, November 2010. PDF doc.

  • Phase 1/2 Study of TH-302 combined with doxorubicin in soft tissue sarcoma. Chawla et al. 16th Annual Connective Tissue Oncology Society (CTOS) Meeting, November 2010. PDF doc.

  • Complete phase 1B study of TH-302 in combination with gemcitabine, docetaxel or pemetrexed. Borad et al. European Society for Medical Oncology (ESMO) Annual Meeting, October 2010. PDF doc.

  • Hypoxia-dependent antitumor activity of TH-302, a hypoxia-activated prodrug, in preclinical pancreatic xenograft models. Sun et al. American Association for Cancer Research (AACR) Translational Cancer Medicine Meeting, July 2010. PDF doc.

  • Antiangiogenic-induced increase in tumor hypoxia in RCC and NSCLC human tumor xenografts and its selective targeting by the hypoxia-activated prodrug TH-302: A model for clinical exploration? Hart et al. American Association for Cancer Research (AACR) Translational Cancer Medicine Meeting, July 2010. PDF doc.

  • Phase 1/2 study of the hypoxia-activated prodrug TH-302 combined with doxorubicin in soft tissue sarcoma. Cranmer et al. American Society of Clinical Oncology (ASCO) Annual Meeting, June 2010. PDF doc.

  • NADPH-cytochrome P450 reductase-mediated reduction of TH-302, a hypoxia-activated prodrug. Meng et al. American Association for Cancer Research (AACR) Annual Meeting, April 2010. PDF doc.

  • TH-302, a tumor selective hypoxia-activated prodrug, in gastrointestinal cancers. Borad et al. ASCO Gastrointestinal Cancers Symposium, January 2010. PDF doc.

  • Hypoxia activated prodrug TH-302 for the treatment of multiple myeloma. Hu et al. American Society for Hematology (ASH) Annual Meeting, December, 2009. PDF doc.

  • Bench to bedside experience with TH-302: a tumor-selective hypoxia-activated prodrug as a promising treatment for prostate cancer. Hart et al. AACR-NCI-EORTC Symposium on Molecular Targets and Cancer Therapeutics, November, 2009. PDF doc.

  • Phase 1/2 study of TH-302 with doxorubicin in soft tissue sarcoma (STS): preliminary results. Ganjoo et al. Connective Tissue Oncology Society (CTOS), November 2009. PDF doc.

  • 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. PDF doc.

  • A 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. PDF doc.

  • 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. PDF doc.

  • Targeting pathophysiological hypoxia in cancer with the hypoxia-activated prodrug (HAP) TH-302. Hart et al. New York Academy of Sciences (NYAS) Conference on Hypoxia, March 2009. PDF doc.

  • A first-in-man phase 1 study of TH-302, a hypoxia-activated cytotoxic prodrug (HAP). Weiss et al. European Organisation for Research and Treatment of Cancer (EORTC) Annual Meeting, October 2008. PDF doc.

  • Potent and highly selective hypoxia-activated achiral phosphoramidate mustards as anticancer drugs. Duan et al. Journal of Medicinal Chemistry, 51: 2412-2420, 2008. PubMed page.

  • Efficacy of the hypoxia-activated prodrug TH-302 in a preclinical model of prostate cancer metastasis. Hart et al. Joint Metastasis Research Society (MRS) and American Association for Cancer Research (AACR) Conference on Metastasis, August, 2008. PDF doc.

  • Anti-cancer activity of hypoxia activated prodrug, TH-302 in H460 non-small cell lung carcinoma metastatic model. Sun et al. Joint Metastasis Research Society (MRS) and American Association for Cancer Research (AACR) Conference on Metastasis, August, 2008. PDF doc.

  • Plasma pharmacokinetics, oral bioavailability, and interspecies scaling of the hypoxically activated prodrug, TH-302, in mice, rats, dogs and monkeys. Jung et al. American Association for Cancer Research (AACR) Annual Meeting, April 2008. PDF doc.

  • In vitro activity profile of the novel hypoxia-activated cytotoxic prodrug TH-302. Hart et al. American Association for Cancer Research (AACR) Annual Meeting, April 2008. PDF doc.

  • Discovery of TH-302: an achiral hypoxia-activated cytotoxic prodrug. Hart et al. American Society of Clinical Oncology (ASCO) Annual Meeting, June 2007. PDF doc.

General HAP Research

  • Aminocamptothecins: their synthesis, preclinical activity, and potential use for cancer treatment. Duan et al. Journal of Medicinal Chemistry, 54: 1715-1723, 2011. PubMed page.

  • Aminocamptothecin: synthesis, preclinical activity, and potential use for cancer treatment. Duan et al. American Association for Cancer Research (AACR) Annual Meeting, April, 2010. PDF doc.

  • A novel class of tubulin inhibitors that exhibit potent antiproliferation and in vitro vessel-disrupting activity. Meng et al. Cancer Chemotherapy and Pharmacology, 61: 953-963, 2008. PubMed page.

  • 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. PDF doc.

  • Potent anti-tubulin tumor cell cytotoxins based on 3-aroyl indazoles. Duan et al. Journal of Medicinal Chemistry, 50: 1001-1006, 2007. PubMed page.

  • 3-aroyl indazoles: their synthesis and potential use for cancer treatment. Duan et al. American Association for Cancer Research (AACR) Annual Meeting, April 2007.