Table 1.
Overview of hypoxia prodrugs in clinical trials (Update 2/2016, Clinicaltrials.gov). Abbreviation: * -trial included biological or imaging study with FAZA and or evaluation biomarkers; AML-Acute Myeloid Leukemia; ALL-Acute Lymphoblastic Leukemia; CML-Chronic Myeloid Leukemia; CLL-Chronic Lymphoblastic leukemia; 5-FU-5-Fluorouracil; GCSF-Granulocyte Colony Stimulating Factor ; GIST-Gastrointestinal Stromal Tumors; HCC-Hepatocellular Carcinoma; MDS-Myelodysplastic Syndrome; MM-Multiple Myeloma; NHL- Non-Hodgkin Lymphoma; NSCLC-Non-Small Cell Lung Cancer; pNET- Pancreatic Neuroendocrine Tumors; RCC-Renal Cell Carcinoma; RT-Radiotherapy; SCCHN-Squamous Cell Carcinoma of Head and Neck; SCLC-Small Cell Lung Cancer; SLL-Small Lymphocytic Leukemia; TACE- Transcatheter Arterial Chemoembolization; TAE- Transcatheter arterial Embolization; TURB-Transurethral Resection of the Bladder: NR- not recruiting: NYR- not yet recruiting: *** Polychemotherapy: Vincristine+ Irinotecan+ Cyclophosphamide+ Doxorubicin+ Ifosfamide+ Etoposide+ GCSF
| DRUG | INDICATION | PHASE | TREATMENT | TRIAL | STATUS |
|---|---|---|---|---|---|
| TH-302 | Pancreatic Ca | I–III | TH-302 +/− Gemcitabine | NCT01746979, NCT01144455, NCT01833546 | completed |
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| Soft Tissue Sarcoma | I/II–III | TH-302 +/− Doxorubicin | NCT01440088, NCT00742963 | completed | |
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| Biliary Tract Ca | II | TH-302 Monotherapy | NCT02433639 | recruiting | |
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| Glioblastoma | II | TH-302 + Bevacizumab | NCT02342379 | recruiting | |
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| High Grade Glioma | II | TH-302 MonotherapyàBevacizumab | NCT01403610 | completed | |
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| MM | II | TH-302 +/− Dexamethasone +/− Bortezomib/Pomalidomide | NCT01522872 | active, NR | |
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| Melanoma | II* | TH-302 Monotherapy | NCT01864538* | active, NR | |
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| Solid Tumors | I–I/II | TH-302 + Gemcitabine/Docetaxel/Pemetrexed TH-302 + Pazopanib TH-302 Monotherapy |
NCT00743379, NCT00495144, NCT02020226, NCT01485042, NCT01833546, NCT02076230* |
completed active, NR |
|
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| RCC, GIST, pNET | I I* II |
TH-302 + Sunitinib TH-302 [14C] TH-302 + Sunitinib |
NCT01381822 NCT02076230 NCT02402062 |
active completed active, NR |
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| HCC | I | TH-302 + Doxorubicin (TACE) | NCT01721941 | NYR | |
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| AML, ALL, CML, MDS | I | TH-302 Monotherapy | NCT01149915 | completed | |
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| TIRAPAZAMINE | SCLC | II* I |
Tirapazamine + Cisplatin, Etoposide, RT Tirapazamine +/− Cisplatin+ Etoposide+ RT |
NCT00066742 NCT00006487 |
completed |
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| NSCLC | III I |
Tirapazamine +/− Carboplatin+Paclitaxel Tirapazamine + Carboplatin, Paclitaxel, RT |
NCT00006484 NCT00033410 |
completed | |
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| Cervical Ca Ovarian Ca Peritoneal Cavity Ca |
III II I |
Tirapazamine +/− Cisplatin, RT Tirapazamine + Cisplatin Tirapazamine + Cisplatin, RT |
NCT00262821 NCT00003369 NCT00098995 NCT00020696 |
completed | |
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| HCC | I | Tirapazamine (TAE) | NCT02174549 | recruiting | |
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| SCCHN | II, III | Tirapazamine +/− Cisplatin, 5-FU, RT | NCT00002774, NCT00174837 | completed | |
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| Childhood Solid Tumor | I | Tirapazamine + Cyclophosphamide+ GCSF | NCT00003288 | completed | |
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| Head and Neck Tumor | III | Tirapazamine +/− Cisplatin, RT | NCT00094081 | completed | |
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| Childhood Rhabdomyosarcoma | II* | Tirapazamine + Polychemotherapy *** | NCT00025363 | completed | |
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| TH-4000 | NSCLC Recurrent/Metastatic SCCHN |
II | TH-4000 Monotherapy | NCT02454842 NCT02449681 |
active, active, NR |
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| EO9 | Bladder Cancer | I–III | EO9 Monotherapy | NCT01373398, NCT00598806, NCT00141531 NCT01469221 |
completed active, NR |
| III | EO9 Monotherapy pre TURB | NCT00461591 NCT02563561 |
completed active, NR |
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