thiotepa

Small moleculeapproved

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

Phase 1
55
Phase 2
188
Phase 3
32
Phase 4
2

Earliest trial started Feb 1, 1990 (NCT00002471)

Timeline

1950s

  1. Mar 9, 1959

    Earliest FDA Approval

  2. Mar 9, 1959

    Immunex — NDA Secondary Org

1990s

  1. Jan 1, 1990

    Earliest Phase 2 Sponsor(trial)

  2. Jan 1, 1993

    Earliest Phase 3 Sponsor(trial)

  3. Jan 1, 1995

    Earliest Phase 1 Sponsor(trial)

2000s

  1. Apr 2, 2001

    West-Ward Pharmaceutical — Marketing Organization

  2. Apr 20, 2001

    Teva — Marketing Organization

  3. Sep 20, 2001

    Fresenius — Marketing Organization

2010s

  1. Jan 26, 2017

    Adienne SA — NDA Secondary Org

  2. May 4, 2018

    Dr. Reddy's Laboratories — Marketing Organization

  3. May 4, 2018

    Hengrui Therapeutics, Inc. — Marketing Organization

  4. May 4, 2018

    Jiangsu Wuzhong Pharmaceutical Group Co., Ltd. — Marketing Organization

2020s

  1. Jan 10, 2020

    STI Pharma, LLC — Marketing Organization

  2. Jan 10, 2020

    PENN LIFE — Marketing Organization

  3. Mar 4, 2020

    MSN Laboratories — Marketing Organization

  4. Mar 8, 2021

    Gland Pharma Ltd — Marketing Organization

  5. Mar 8, 2021

    Fosun — Marketing Organization

  6. Dec 8, 2021

    Beloteca Inc — Marketing Organization

  7. Sep 5, 2023

    Hikma — Marketing Organization

  8. Dec 26, 2023

    Meitheal — Marketing Organization

  9. Jun 25, 2024

    SHORLA — Marketing Organization

Indications

Studied for

Mechanism of action

  • DNAINHIBITOR

    DNA inhibitor

Approval history

  • approvedPriority reviewMar 9, 1959

Chemistry & pharmacology

Loading structure…

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

Black box warning

Sources

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 IDPhaseStart dateSponsor(s)
NCT07257419Phase 1Dec 31, 2025St. Jude Children's Hospital
NCT07052370Phase 1Dec 31, 2025St. Jude Children's Hospital
NCT07276737Phase 2Dec 30, 2025Jiao Tong University
NCT07259161Phase 2Dec 15, 2025China Academy of Chinese Medical Sciences
NCT07263425Phase 2Oct 27, 2025Nanjing Medical University
NCT06942039Early Phase 1 (Phase 1)Sep 30, 2025C17 Council
NCT07191431N/ASep 22, 2025Jiao Tong University
NCT06869265Phase 2May 1, 2025Peking University
NCT06901999Phase 2Apr 30, 2025Jiao Tong University
NCT07193654Phase 2Apr 1, 2025Zhejiang University
NCT06807606Phase 2Mar 3, 2025University of Texas at Houston
NCT06687772Phase 2Feb 28, 2025Washington University in St. Louis
NCT06832267N/AFeb 14, 2025Chinese Academy of Medical Sciences
NCT06646211Phase 2Jan 1, 2025Sun Yat-Sen University
NCT06872333Phase 2Nov 19, 2024University of Minnesota
NCT06680661Phase 2Nov 15, 2024Case Western Reserve University
NCT06252870Phase 2Jul 18, 2024University of Angers, University of Nantes, University of Western Brittany
NCT06468267Phase 2Jul 15, 2024Jiao Tong University
NCT06543992Phase 2Jul 13, 2024Nanjing Medical University
NCT06195891Phase 1May 24, 2024City of Hope National Medical Center, National Cancer Institute (NCI)
Showing 20 of 247 trials
Page 1 / 13

Organizations

Research & Development (150)

OrganizationOrg typeTrialsAs lead sponsorPhasesEarliest year
National Cancer Institute (NCI)Government751841993
University of WashingtonAcademic/Hospital212131996
St. Jude Children's HospitalAcademic/Hospital181842002
Cornell UniversityAcademic/Hospital171641990
University of Texas at HoustonAcademic/Hospital151531995
University of MinnesotaAcademic/Hospital9841998
Harvard UniversityAcademic/Hospital8422000
Jiao Tong UniversityAcademic/Hospital6622023
National Heart, Lung, and Blood Institute (NHLBI)Government6112003
Herbert Irving Comprehensive Cancer CenterAcademic/Hospital5521996
Netherlands Cancer InstituteAcademic/Hospital5422004
New York UniversityAcademic/Hospital5431994
Northwestern UniversityAcademic/Hospital5321999
University of PittsburghAcademic/Hospital5512012
Institut Gustave RoussyAcademic/Hospital4422002
Memorial Sloan-Kettering Cancer CenterAcademic/Hospital4412004
St. Anna KinderkrebsforschungAcademic/Hospital4412003
State University of New York, BuffaloAcademic/Hospital4431991
Sungkyunkwan UniversityAcademic/Hospital4412008
Sun Yat-Sen UniversityAcademic/Hospital4422021
150 organizations
Page 1 / 8

Marketing (22)

OrganizationOrg typeRelationshipDate
Adienne SAFor profitNDA2Jan 26, 2017
American CyanamidFor profitNDA
Beloteca IncFor profitMKTGDec 8, 2021
Beloteca IncFor profitSYNDec 8, 2021
Dr. Reddy's LaboratoriesFor profitMKTGMay 4, 2018
Dr. Reddy's LaboratoriesFor profitSYNMay 4, 2018
FosunFor profitMKTGMar 8, 2021
FreseniusFor profitMKTGSep 20, 2001
Gland Pharma LtdFor profitMKTGMar 8, 2021
Gland Pharma LtdFor profitSYNMar 8, 2021
Hengrui Therapeutics, Inc.For profitMKTGMay 4, 2018
Hengrui Therapeutics, Inc.For profitSYNMay 4, 2018
HikmaFor profitMKTGSep 5, 2023
ImmunexFor profitNDA2Mar 9, 1959
Jiangsu Wuzhong Pharmaceutical Group Co., Ltd.For profitMKTGMay 4, 2018
MSN LaboratoriesFor profitMKTGMar 4, 2020
MeithealFor profitMKTGDec 26, 2023
PENN LIFEFor profitMKTGJan 10, 2020
SHORLAFor profitMKTGJun 25, 2024
STI Pharma, LLCFor profitMKTGJan 10, 2020
TevaFor profitMKTGApr 20, 2001
West-Ward PharmaceuticalFor profitMKTGApr 2, 2001