thiotepa
Approved
Mar 9, 1959
N,N’N’-triethylenethiophosphoramide (ThioTEPA) is a cancer chemotherapeutic member of the alkylating agent group, now in use for over 50 years. It is a stable derivative of N,N’,N’’- triethylenephosphoramide (TEPA). The radiomimetic action of thiotepa is believed to occur through the release of ethylenimine radicals which, like irradiation, disrupt the bonds of DNA. One of the principal bond disruptions is initiated by alkylation of guanine at the N-7 position, which severs the linkage between the purine base and the sugar and liberates alkylated guanines. Thiotepa has been used in the palliation of a wide variety of neoplastic diseases. The more consistent results have been seen in: adenocarcinoma of the breast, adenocarcinoma of the ovary, superficial papillary carcinoma of the urinary bladder and for controlling intracavitary effusions secondary to diffuse or localized neoplastic diseases of various serosal cavities. — NCATS
Clinical trial activity
247 trials · 150 clinical orgs · 18 marketing orgs
Earliest trial started Feb 1, 1990 (NCT00002471)
Timeline
1950s
- Mar 9, 1959
Earliest FDA Approval
- Mar 9, 1959
Immunex — NDA Secondary Org
1990s
2000s
- Apr 2, 2001
West-Ward Pharmaceutical — Marketing Organization
- Apr 20, 2001
Teva — Marketing Organization
- Sep 20, 2001
Fresenius — Marketing Organization
2010s
- Jan 26, 2017
Adienne SA — NDA Secondary Org
- May 4, 2018
Dr. Reddy's Laboratories — Marketing Organization
- May 4, 2018
Hengrui Therapeutics, Inc. — Marketing Organization
- May 4, 2018
Jiangsu Wuzhong Pharmaceutical Group Co., Ltd. — Marketing Organization
2020s
- Jan 10, 2020
STI Pharma, LLC — Marketing Organization
- Jan 10, 2020
PENN LIFE — Marketing Organization
- Mar 4, 2020
MSN Laboratories — Marketing Organization
- Mar 8, 2021
Gland Pharma Ltd — Marketing Organization
- Mar 8, 2021
Fosun — Marketing Organization
- Dec 8, 2021
Beloteca Inc — Marketing Organization
- Sep 5, 2023
Hikma — Marketing Organization
- Dec 26, 2023
Meitheal — Marketing Organization
- Jun 25, 2024
SHORLA — Marketing Organization
Indications
Approved for
Studied for
- Adrenoleukodystrophy · Phase 1/Phase 2
- Agammaglobulinemia · Phase 2
- Allografts · Phase 2
- Anemia · Phase 4
- Anemia, Aplastic · Phase 2
- Anemia, Diamond-Blackfan · Phase 1/Phase 2
- Anemia, Hemolytic · Phase 1/Phase 2
- Anemia, Refractory · Phase 2
- Anemia, Sickle Cell · Phase 2
- Arthritis, Juvenile · Phase 2
- Arthritis, Rheumatoid · Phase 2
- Autoimmune Lymphoproliferative Syndrome · Phase 2
- beta-Thalassemia · Phase 1/Phase 2
- Bone Marrow Cells · Phase 2
- Bone Marrow Failure Disorders · Phase 1/Phase 2
- Brain Neoplasms · Phase 3
- Breast Neoplasms · Phase 3
- Breast Neoplasms, Male · Phase 2
- Burkitt Lymphoma · Phase 2
- Carcinoma, Embryonal · Phase 2
- Central Nervous System Diseases · Phase 2
- Central Nervous System Neoplasms · Phase 3
- Chediak-Higashi Syndrome · Phase 2/Phase 3
- Chordoma · Phase 1
- Choriocarcinoma · Phase 2
- Choroid Plexus Neoplasms · Phase 1
- Common Variable Immunodeficiency · Phase 2
- Congenital Bone Marrow Failure Syndromes · Phase 2
- Desmoplastic Small Round Cell Tumor · Phase 2
- DiGeorge Syndrome · Phase 2
- Drug-Related Side Effects and Adverse Reactions · Phase 2
- Drug Therapy · Phase 2
- Ependymoma · Phase 2/Phase 3
- Fallopian Tube Neoplasms · Phase 1/Phase 2
- Ganglioneuroblastoma · Phase 3
- Glioblastoma · Phase 2
- Glioma · Phase 1
- Graft vs Host Disease · Phase 4
- Granulomatous Disease, Chronic · Phase 2
- Hair · Phase 2/Phase 3
- Hamartoma · Phase 1/Phase 2
- Head and Neck Neoplasms · Phase 2
- Hematologic Diseases · Phase 2/Phase 3
- Hematologic Neoplasms · Phase 2
- Hematopoietic Stem Cell Transplantation · Phase 2
- Hemoglobinopathies · Phase 2
- Hemoglobinuria, Paroxysmal · Phase 3
- Histiocytosis · Phase 2
- Histiocytosis, Langerhans-Cell · Phase 2/Phase 3
- HIV Infections · Phase 2
- Hodgkin Disease · Phase 2
- Hypertension, Pulmonary · Phase 2
- Idiopathic Pulmonary Fibrosis · Phase 1/Phase 2
- Immune System Diseases · Phase 2/Phase 3
- Immunoglobulin M · Phase 2
- Immunotherapy · Phase 3
- Inflammation · Phase 2
- Inflammatory Breast Neoplasms · Phase 2
- Intestinal Neoplasms · Phase 2
- Intraocular Lymphoma · Phase 2
- Kidney Neoplasms · Phase 2
- Leukemia · Phase 4
- Leukemia, Biphenotypic, Acute · Phase 2
- Leukemia, Hairy Cell · Phase 2
- Leukemia, Large Granular Lymphocytic · Phase 2
- Leukemia, Lymphocytic, Chronic, B-Cell · Phase 2
- Leukemia, Lymphoid · Phase 2
- Leukemia-Lymphoma, Adult T-Cell · Phase 2
- Leukemia, Mast-Cell · Phase 2
- Leukemia, Megakaryoblastic, Acute · Phase 2
- Leukemia, Monocytic, Acute · Phase 2
- Leukemia, Myelogenous, Chronic, BCR-ABL Positive · Phase 3
- Leukemia, Myeloid · Phase 2
- Leukemia, Myeloid, Acute · Phase 3
- Leukemia, Myeloid, Chronic, Atypical, BCR-ABL Negative · Phase 2
- Leukemia, Myeloid, Chronic-Phase · Phase 2
- Leukemia, Myelomonocytic, Chronic · Phase 2
- Leukemia, Myelomonocytic, Juvenile · Phase 3
- Liver Neoplasms · Phase 2
- Lung Diseases, Interstitial · Phase 2
- Lymphocytes · Phase 2
- Lymphohistiocytosis, Hemophagocytic · Phase 2/Phase 3
- Lymphoma · Phase 4
- Lymphoma, B-Cell · Phase 2
- Lymphoma, B-Cell, Marginal Zone · Phase 2
- Lymphoma, Follicular · Phase 2
- Lymphoma, Large B-Cell, Diffuse · Phase 3
- Lymphoma, Large-Cell, Anaplastic · Phase 2
- Lymphoma, Large-Cell, Immunoblastic · Phase 2/Phase 3
- Lymphoma, Mantle-Cell · Phase 2
- Lymphoma, Non-Hodgkin · Phase 3
- Lymphoma, T-Cell · Phase 2
- Lymphoma, T-Cell, Peripheral · Phase 2
- Lymphomatoid Granulomatosis · Phase 2
- Lymphoproliferative Disorders · Phase 2/Phase 3
- Mannosidase Deficiency Diseases · Phase 1/Phase 2
- Medulloblastoma · Phase 4
- Metabolic Diseases · Phase 2
- Mucopolysaccharidosis I · Phase 1/Phase 2
- Multiple Myeloma · Phase 4
- Mycoses · Phase 2
- Myelodysplastic-Myeloproliferative Diseases · Phase 2/Phase 3
- Myelodysplastic Syndromes · Phase 4
- Myeloproliferative Disorders · Phase 2/Phase 3
- Neoplasm Metastasis · Phase 2
- Neoplasms · Phase 2/Phase 3
- Neoplasms, Germ Cell and Embryonal · Phase 4
- Neoplasms, Neuroepithelial · Early Phase 1
- Nerve Sheath Neoplasms · Phase 2
- Neuroblastoma · Phase 3
- Neuroectodermal Tumors · Phase 3
- Neuroectodermal Tumors, Primitive · Phase 2
- Neutropenia · Phase 1/Phase 2
- Osteosarcoma · Phase 2
- Ovarian Neoplasms · Phase 2
- Pediatrics · Phase 1
- Pinealoma · Early Phase 1
- Plasmacytoma · Phase 2
- Polycythemia Vera · Phase 2
- Precursor B-Cell Lymphoblastic Leukemia-Lymphoma · Phase 3
- Precursor Cell Lymphoblastic Leukemia-Lymphoma · Phase 3
- Primary Immunodeficiency Diseases · Phase 2
- Primary Myelofibrosis · Phase 2
- Pulmonary Disease, Chronic Obstructive · Phase 1/Phase 2
- Retinoblastoma · Phase 3
- Rhabdoid Tumor · Phase 3
- Rhabdomyosarcoma · Phase 2
- Sarcoma · Phase 2
- Sarcoma, Ewing · Phase 2
- Sarcoma, Myeloid · Phase 2
- Scleroderma, Diffuse · Phase 2
- Scleroderma, Systemic · Phase 2
- Severe Combined Immunodeficiency · Phase 2
- Sezary Syndrome · Phase 2
- Stem Cell Transplantation · Phase 2
- Teratoma · Phase 2
- Testicular Neoplasms · Phase 2
- Thalassemia · Phase 1/Phase 2
- Thrombocythemia, Essential · Phase 2
- Thrombocytopenia · Phase 2
- Tissue Donors · Phase 2
- Transplantation · Phase 2
- Waldenstrom Macroglobulinemia · Phase 2
- Wiskott-Aldrich Syndrome · Phase 2
Mechanism of action
- DNAINHIBITOR
DNA inhibitor
Approval history
- approvedPriority reviewMar 9, 1959
Chemistry & pharmacology
SMILES
S=P(N1CC1)(N2CC2)N3CC3- Mol. weight
- 189.218 g/mol
- Lipinski Ro5
- Pass
- Rule of 3
- Yes
- Chirality
- Achiral Molecule
- Inorganic
- No
- Polymer
- No
- Delivery
- Parenteral
- Availability
- Prescription Only
Oral
No
Parenteral
Yes
Topical
No
Sources
- WikipediaThiotepa ↗
- NCATS905Z5W3GKH ↗
- ChEMBLCHEMBL671 ↗
Also known as
- oncotepa
- phosphorothioic acid triethylenetriamide
- tepadina
- tespamin
- tespamine
- thiophosphamide
- thioplex
- thioplex
- thioplex
- thiotepa
- thiotepa
- thiotepa
- thiotepa
- thiotepa
- thiotepa
- thiotepa
- thiotepa
- thiotepa
- thiotepa
- thio-tepa
- thio-tepa
- thio-tepa
- thio-tepa
- thio-tepa
- thio-tepa
- triethylenethiophosphoramide
- triethylenethiophosphoramide
- triethylenethiophosphortriamide
Clinical trials
| NCT ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT07257419 | Phase 1 | Dec 31, 2025 | St. Jude Children's Hospital |
| NCT07052370 | Phase 1 | Dec 31, 2025 | St. Jude Children's Hospital |
| NCT07276737 | Phase 2 | Dec 30, 2025 | Jiao Tong University |
| NCT07259161 | Phase 2 | Dec 15, 2025 | China Academy of Chinese Medical Sciences |
| NCT07263425 | Phase 2 | Oct 27, 2025 | Nanjing Medical University |
| NCT06942039 | Early Phase 1 (Phase 1) | Sep 30, 2025 | C17 Council |
| NCT07191431 | N/A | Sep 22, 2025 | Jiao Tong University |
| NCT06869265 | Phase 2 | May 1, 2025 | Peking University |
| NCT06901999 | Phase 2 | Apr 30, 2025 | Jiao Tong University |
| NCT07193654 | Phase 2 | Apr 1, 2025 | Zhejiang University |
| NCT06807606 | Phase 2 | Mar 3, 2025 | University of Texas at Houston |
| NCT06687772 | Phase 2 | Feb 28, 2025 | Washington University in St. Louis |
| NCT06832267 | N/A | Feb 14, 2025 | Chinese Academy of Medical Sciences |
| NCT06646211 | Phase 2 | Jan 1, 2025 | Sun Yat-Sen University |
| NCT06872333 | Phase 2 | Nov 19, 2024 | University of Minnesota |
| NCT06680661 | Phase 2 | Nov 15, 2024 | Case Western Reserve University |
| NCT06252870 | Phase 2 | Jul 18, 2024 | University of Angers, University of Nantes, University of Western Brittany |
| NCT06468267 | Phase 2 | Jul 15, 2024 | Jiao Tong University |
| NCT06543992 | Phase 2 | Jul 13, 2024 | Nanjing Medical University |
| NCT06195891 | Phase 1 | May 24, 2024 | City of Hope National Medical Center, National Cancer Institute (NCI) |
Organizations
Research & Development (150)
Marketing (22)
| Organization | Org type | Relationship | Date |
|---|---|---|---|
| Adienne SA | For profit | NDA2 | Jan 26, 2017 |
| American Cyanamid | For profit | NDA | — |
| Beloteca Inc | For profit | MKTG | Dec 8, 2021 |
| Beloteca Inc | For profit | SYN | Dec 8, 2021 |
| Dr. Reddy's Laboratories | For profit | MKTG | May 4, 2018 |
| Dr. Reddy's Laboratories | For profit | SYN | May 4, 2018 |
| Fosun | For profit | MKTG | Mar 8, 2021 |
| Fresenius | For profit | MKTG | Sep 20, 2001 |
| Gland Pharma Ltd | For profit | MKTG | Mar 8, 2021 |
| Gland Pharma Ltd | For profit | SYN | Mar 8, 2021 |
| Hengrui Therapeutics, Inc. | For profit | MKTG | May 4, 2018 |
| Hengrui Therapeutics, Inc. | For profit | SYN | May 4, 2018 |
| Hikma | For profit | MKTG | Sep 5, 2023 |
| Immunex | For profit | NDA2 | Mar 9, 1959 |
| Jiangsu Wuzhong Pharmaceutical Group Co., Ltd. | For profit | MKTG | May 4, 2018 |
| MSN Laboratories | For profit | MKTG | Mar 4, 2020 |
| Meitheal | For profit | MKTG | Dec 26, 2023 |
| PENN LIFE | For profit | MKTG | Jan 10, 2020 |
| SHORLA | For profit | MKTG | Jun 25, 2024 |
| STI Pharma, LLC | For profit | MKTG | Jan 10, 2020 |
| Teva | For profit | MKTG | Apr 20, 2001 |
| West-Ward Pharmaceutical | For profit | MKTG | Apr 2, 2001 |