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temozolomide

Trade name: temodar

Small moleculeapprovedOrphan Drug FDA

Approved

Aug 11, 1999

NEO 212 is novel DNA alkylating agent exhibiting superior activity against breast cancer cells in vitro and intracranial triple-negative tumor growth in vivo. NEO212 is a conjugate of temozolomide (TMZ,) with the natural product perillyl alcohol (POH). NEO 212 causes DNA damage and cell death much more efficiently than TMZ because linkage with POH increased it's biological half-life and thus provided greater opportunity for placement of cytotoxic DNA lesions. — NCATS

Clinical trial activity

921 trials · 541 clinical orgs · 25 marketing orgs

Phase 1
364
Phase 2
655
Phase 3
98
Phase 4
6

Earliest trial started Jul 1, 1997 (NCT00003062)

Timeline

1990s

  1. Jan 1, 1997

    Earliest Phase 2 Sponsor(trial)

  2. Jan 1, 1998

    Earliest Phase 1 Sponsor(trial)

  3. Oct 5, 1998

    Orphan Drug Designation

  4. Jan 1, 1999

    Earliest Phase 3 Sponsor(trial)

  5. Aug 11, 1999

    Schering-Plough — Earliest FDA Approval

  6. Aug 11, 1999

    Merck — NDA Secondary Org

  7. Aug 11, 1999

    Schering-Plough — NDA Organization

2010s

  1. Mar 1, 2010

    Barr Laboratories — Marketing Organization

  2. Mar 1, 2010

    Heritage Pharma — Marketing Organization

  3. Feb 12, 2014

    Sun Pharmaceuticals — Marketing Organization

  4. May 8, 2015

    Amneal Pharmaceuticals — Marketing Organization

  5. Feb 10, 2016

    Lannett Company, Inc. — Marketing Organization

  6. Feb 10, 2016

    Opko — Marketing Organization

  7. Apr 12, 2016

    IDT Australia Ltd. — Marketing Organization

  8. Apr 12, 2016

    Chartwell Pharmaceuticals — Marketing Organization

  9. Apr 27, 2016

    Rising Pharmaceuticals — Marketing Organization

  10. Apr 27, 2016

    ANDA Repository — Marketing Organization

  11. Jun 29, 2016

    Mylan — Marketing Organization

  12. Jun 29, 2016

    EXTROVIS — Marketing Organization

  13. Jul 13, 2016

    Amerigen Pharmaceuticals — Marketing Organization

  14. Jul 13, 2016

    Ani Pharmaceuticals — Marketing Organization

  15. Nov 23, 2016

    Chemi SpA — Marketing Organization

  16. Nov 23, 2016

    Italfarmaco — Marketing Organization

  17. Feb 27, 2017

    Accord Research — Marketing Organization

  18. Apr 18, 2017

    Teva — Marketing Organization

  19. Apr 26, 2017

    Deva Holding A.S. — Marketing Organization

  20. Jul 31, 2017

    Zydus Discovery DMCC — Marketing Organization

  21. Jul 5, 2018

    Apotex — Marketing Organization

2020s

  1. Nov 23, 2021

    Nivagen Pharmaceuticals Inc. — Marketing Organization

  2. Aug 23, 2024

    Hetero Labs Ltd — Marketing Organization

Indications

Approved for

Studied for

Mechanism of action

  • DNAINHIBITOR

    DNA inhibitor

Approval history

  • approvedPriority reviewAcceleratedAug 11, 1999

Chemistry & pharmacology

Loading structure…

SMILES

CN1N=NC2=C(N=CN2C1=O)C(N)=O
Mol. weight
194.1508 g/mol
Lipinski Ro5
Pass
Rule of 3
No
Chirality
Achiral Molecule
Inorganic
No
Polymer
No
Delivery
Oral, Parenteral
Availability
Prescription Only

Oral

Yes

Parenteral

Yes

Topical

No

Black box warningProdrug

Sources

Also known as

  • 3,4-dihydro-3-methyl-4-oxoimidazo(5,1-d)-1,2,3,5-tetrazine-8-carboxamide
  • 3,4-dihydro-3-methyl-4-oxoimidazo(5,1-d)-1,2,3,5-tetrazine-8-carboxamide
  • 3,4-dihydro-3-methyl-4-oxoimidazo(5,1-d)-as-tetrazine-8-carboxamide
  • 3,4-dihydro-3-methyl-4-oxoimidazo(5,1-d)-as-tetrazine-8-carboxamide
  • 3-methyl-4-oxo-3,4-dihydroimidazo(5,1-d)(1,2,3,5)tetrazine-8-carboxamide
  • 3-methyl-4-oxo-3,4-dihydroimidazo(5,1-d)(1,2,3,5)tetrazine-8-carboxamide
  • 8-carbamoyl-3-methylimidazo(5,1-d)-1,2,3,5-tetrazin-4(3h)-one
  • 8-carbamoyl-3-methylimidazo(5,1-d)-1,2,3,5-tetrazin-4(3h)-one
  • 8-carbamoyl-3-methylimidazo(5,1-d)-1,2,3,5-tetrazin-4(3h)-one
  • brn 5547136
  • brn 5547136
  • ccrg 81045
  • ccrg 81045
  • ccrg 81045
  • ccrg-81045
  • ccrg-81045
  • ccrg-81045
  • ccrg-81045
  • ccris 8996
  • ccris 8996
  • m-39831
  • m-39831
  • m & b 39831
  • m & b 39831
  • m & b 39831
  • m&b 39831
  • m&b-39831
  • m&b-39831
  • m&b-39831
  • mb 39831
  • mb 39831
  • methazolastone
  • methazolastone
  • methazolastone
  • methazolastone
  • methazolastone
  • nsc 362856
  • nsc 362856
  • nsc 362856
  • nsc-362856
  • sch 52365
  • sch 52365
  • sch-52365
  • sch-52365
  • temodal
  • temodal
  • temodal
  • temodal
  • temodal
  • temodal
  • temodar
  • temodar
  • temodar
  • temodar
  • temodar
  • temomedac
  • temomedac
  • temomedac
  • temomedac
  • temomedac
  • temomedac
  • temozolamide
  • temozolamide
  • temozolamide
  • temozolodida
  • temozolodida
  • temozololmide
  • temozolomid
  • temozolomid
  • temozolomida
  • temozolomida
  • temozolomide
  • temozolomide
  • temozolomide
  • temozolomide
  • temozolomide
  • temozolomide
  • temozolomide
  • temozolomide
  • temozolomide
  • temozolomide
  • temozolomide
  • témozolomide
  • témozolomide
  • temozolomidum
  • temozolomidum
  • tmz
  • tmz
  • tmz-bioshuttle

Clinical trials

NCT IDPhaseStart dateSponsor(s)
NCT07297212Phase 2Jan 31, 2026Biontech, Bristol-Myers Squibb
NCT07120984Phase 2Jan 30, 2026Philogen S.p.A.
NCT07141771Phase 1/Phase 2 (Phase 2)Dec 31, 2025Chinese Academy of Medical Sciences
NCT07310784Phase 2Dec 16, 2025Government of China
NCT07195591Phase 3Nov 30, 2025GT Medical Technologies, Inc.
NCT06991101Phase 2Nov 30, 2025Baptist Health, Incyte
NCT07104032Phase 3Nov 30, 2025Deciphera Pharmaceuticals LLC, Ono Pharmaceuticals
NCT07085338Phase 2Nov 10, 2025St. Jude Children's Hospital
NCT07015242Phase 2Nov 6, 2025Bristol-Myers Squibb
NCT07243470Phase 1/Phase 2 (Phase 2)Nov 4, 2025Amgen, Centre Leon Berard, National Cancer Institute, France
NCT07156019Phase 2Oct 31, 2025Chinese Academy of Medical Sciences
NCT07194044Phase 1Oct 31, 2025National Pediatric Cancer Foundation, University of South Florida
NCT07223034Phase 1Oct 27, 2025Memorial Sloan-Kettering Cancer Center, Novartis
NCT06995872Phase 1Oct 21, 2025National Cancer Institute (NCI)
NCT07215910Phase 3Oct 20, 2025National Cancer Institute (NCI)
NCT06942039Early Phase 1 (Phase 1)Sep 30, 2025C17 Council
NCT07191431N/ASep 22, 2025Jiao Tong University
NCT07138001Phase 2Aug 31, 2025Capital Medical University, Government of China
NCT06931626Phase 1Aug 15, 2025Nerviano Medical Sciences
NCT07025226Early Phase 1 (Phase 1)Aug 12, 2025Mayo Clinic
Showing 20 of 921 trials
Page 1 / 47

Organizations

Research & Development (541)

OrganizationOrg typeTrialsAs lead sponsorPhasesEarliest year
National Cancer Institute (NCI)Government2189241997
Duke UniversityAcademic/Hospital433331997
University of Texas at HoustonAcademic/Hospital393131998
Schering-PloughFor profit34022000
Harvard UniversityAcademic/Hospital312242001
MerckFor profit311842000
Cornell UniversityAcademic/Hospital271831999
GenentechFor profit25122004
European Organisation for Research and Treatment of CancerAcademic/Hospital231731997
University of California, San FranciscoAcademic/Hospital221341998
Chinese Academy of Medical SciencesAcademic/Hospital211832011
Johns Hopkins UniversityAcademic/Hospital211632002
Mayo ClinicAcademic/Hospital201152000
Radiation Therapy Oncology GroupAcademic/Hospital16822000
Sun Yat-Sen UniversityAcademic/Hospital161532007
Bristol-Myers SquibbFor profit15432008
NRG OncologyAcademic/Hospital15432000
Capital Medical UniversityAcademic/Hospital14752012
Northwestern UniversityAcademic/Hospital141121998
PfizerFor profit13431999
541 organizations
Page 1 / 28

Marketing (31)

OrganizationOrg typeRelationshipDate
ANDA RepositoryFor profitMKTGApr 27, 2016
Accord ResearchFor profitMKTGFeb 27, 2017
Amerigen PharmaceuticalsFor profitMKTGJul 13, 2016
Amneal PharmaceuticalsFor profitMKTGMay 8, 2015
Ani PharmaceuticalsFor profitSYNJul 13, 2016
Ani PharmaceuticalsFor profitMKTGJul 13, 2016
ApotexFor profitMKTGJul 5, 2018
ApotexFor profitSYNJul 5, 2018
Barr LaboratoriesFor profitMKTGMar 1, 2010
Chartwell PharmaceuticalsFor profitMKTGApr 12, 2016
Chartwell PharmaceuticalsFor profitSYNFeb 10, 2016
Chemi SpAFor profitMKTGNov 23, 2016
Deva Holding A.S.For profitMKTGApr 26, 2017
EXTROVISFor profitMKTGJun 29, 2016
Heritage PharmaFor profitMKTGMar 1, 2010
Hetero Labs LtdFor profitMKTGAug 23, 2024
IDT Australia Ltd.For profitMKTGApr 12, 2016
ItalfarmacoFor profitMKTGNov 23, 2016
Lannett Company, Inc.For profitMKTGFeb 10, 2016
MerckFor profitNDA2Aug 11, 1999
MylanFor profitMKTGJun 29, 2016
MylanFor profitSYNJun 29, 2016
Nivagen Pharmaceuticals Inc.For profitMKTGNov 23, 2021
OpkoFor profitMKTGFeb 10, 2016
Rising PharmaceuticalsFor profitMKTGApr 27, 2016
Rising PharmaceuticalsFor profitSYNApr 27, 2016
Schering-PloughFor profitNDAAug 11, 1999
Sun PharmaceuticalsFor profitMKTGFeb 12, 2014
Sun PharmaceuticalsFor profitSYNFeb 12, 2014
TevaFor profitMKTGApr 18, 2017
Zydus Discovery DMCCFor profitMKTGJul 31, 2017