irinotecan

Trade name: Camptosar

Small moleculeapproved

Approved

Jun 14, 1996

Irinotecan is an antineoplastic enzyme inhibitor primarily used in the treatment of colorectal cancer. Irinotecan is sold under the brand name Camptosar among others. CAMPTOSAR is a topoisomerase inhibitor indicated for: • First-line therapy in combination with 5-fluorouracil and leucovorin for patients with metastatic carcinoma of the colon or rectum. • Patients with metastatic carcinoma of the colon or rectum whose disease has recurred or progressed following initial fluorouracil-based therapy. Irinotecan is a derivative of camptothecin. Camptothecins interact specifically with the enzyme topoisomerase I, which relieves torsional strain in DNA by inducing reversible single-strand breaks. Irinotecan and its active metabolite SN-38 bind to the topoisomerase I-DNA complex and prevent religation of these single-strand breaks. Current research suggests that the cytotoxicity of irinotecan is due to double-strand DNA damage produced during DNA synthesis when replication enzymes interact with the ternary complex formed by topoisomerase I, DNA, and either irinotecan or SN-38. Mammalian cells cannot efficiently repair these double-strand breaks. — NCATS

Clinical trial activity

1,733 trials · 775 clinical orgs · 39 marketing orgs

Phase 1
488
Phase 2
1316
Phase 3
264
Phase 4
25

Earliest trial started Nov 1, 1995 (NCT00001495)

Timeline

1990s

  1. Jan 1, 1995

    Earliest Phase 1 Sponsor(trial)

  2. Jan 1, 1996

    Earliest Phase 2 Sponsor(trial)

  3. Jun 14, 1996

    Pharmacia & Upjohn — Earliest FDA Approval

  4. Jun 14, 1996

    Pharmacia & Upjohn — NDA Organization

  5. Jun 14, 1996

    Pfizer — NDA Secondary Org

  6. Jan 1, 1998

    Earliest Phase 3 Sponsor(trial)

2000s

  1. Feb 20, 2008

    Cipla — Marketing Organization

  2. Feb 27, 2008

    Actavis — Marketing Organization

  3. Feb 27, 2008

    Fresenius — Marketing Organization

  4. Feb 27, 2008

    Hospira — Marketing Organization

  5. Feb 27, 2008

    Sandoz — Marketing Organization

  6. Feb 27, 2008

    Novartis — Marketing Organization

  7. Apr 21, 2008

    Sun Pharmaceuticals — Marketing Organization

  8. Oct 31, 2008

    Pliva — Marketing Organization

  9. Oct 31, 2008

    Barr Laboratories — Marketing Organization

  10. Nov 21, 2008

    Accord Research — Marketing Organization

  11. Nov 26, 2008

    Teva — Marketing Organization

  12. Dec 24, 2008

    West-Ward Pharmaceutical — Marketing Organization

  13. Jan 28, 2009

    Zhejiang Hisun Pharmaceutical Co. Ltd. — Marketing Organization

  14. Sep 16, 2009

    Akorn, Inc. — Marketing Organization

  15. Sep 16, 2009

    Epic Pharma Llc — Marketing Organization

2010s

  1. Apr 15, 2010

    Neopharma — Marketing Organization

  2. Apr 15, 2010

    Innogenix — Marketing Organization

  3. Apr 15, 2010

    US Antibiotics — Marketing Organization

  4. Apr 15, 2010

    Picket Pharms — Marketing Organization

  5. Apr 15, 2010

    Chartwell Pharmaceuticals — Marketing Organization

  6. Dec 20, 2010

    Hikma — Marketing Organization

  7. May 13, 2011

    Mustafa Nevzat Pharmaceuticals — Marketing Organization

  8. May 13, 2011

    Zennova — Marketing Organization

  9. May 13, 2011

    PHARMOBEDIENT — Marketing Organization

  10. Dec 16, 2011

    Hengrui Therapeutics, Inc. — Marketing Organization

  11. Dec 16, 2011

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

  12. Feb 14, 2012

    Emcure — Marketing Organization

  13. Oct 22, 2015

    Ipsen — NDA Secondary Org

  14. Oct 22, 2015

    Merrimack Pharmaceuticals — NDA Secondary Org

  15. Oct 22, 2015

    Ipsen — Marketing Organization

  16. May 3, 2016

    Qilu Pharmaceutical Co., Ltd. — Marketing Organization

  17. May 26, 2017

    Ingenus Pharmaceuticals — Marketing Organization

  18. May 26, 2017

    Novast Labs — Marketing Organization

  19. Aug 31, 2017

    Intas Pharmaceuticals Limited — Marketing Organization

  20. Dec 28, 2018

    Shilpa Medicare Ltd. — Marketing Organization

  21. Nov 18, 2019

    Gland Pharma Ltd — Marketing Organization

  22. Nov 18, 2019

    Fosun — Marketing Organization

2020s

  1. Nov 3, 2020

    Eugia Pharma — Marketing Organization

Indications

Studied for

Mechanism of action

Approval history

  • approvedPriority reviewAcceleratedJun 14, 1996

Chemistry & pharmacology

Loading structure…

SMILES

CCc1c2c(nc3ccc(OC(=O)N4CCC(N5CCCCC5)CC4)cc13)-c1cc3c(c(=O)n1C2)COC(=O)[C@]3(O)CC.Cl.O.O.O
Mol. weight
677.19 g/mol
Lipinski Ro5
1 violation(s)
Rule of 3
No
Chirality
Single Stereoisomer
Inorganic
No
Polymer
No
Delivery
Parenteral
Availability
Prescription Only

Oral

No

Parenteral

Yes

Topical

No

Black box warningProdrug

Sources

Also known as

  • 7-ethyl-10-hydroxycamptothecin
  • 7-ethyl-10-hydroxycamptothecin
  • bax2398
  • bax2398
  • biotecan
  • biotecan
  • campto
  • campto
  • campto
  • camptosar
  • camptosar
  • camptosar
  • camptosar
  • camptosar
  • camptothecin-11
  • camptothecin-11
  • camptothecin-11
  • camptothecin-11
  • camptothecine
  • camptothecine
  • (+)-camptothecine
  • (+)-camptothecine
  • cpt 11
  • cpt 11
  • cpt-11
  • cpt-11
  • cpt-11
  • d-camptothecin
  • d-camptothecin
  • ezn-2208
  • ezn-2208
  • folfiri
  • folfiri
  • folfirinox
  • irinotecan
  • irinotecan
  • irinotecan
  • irinotecan
  • irinotecan
  • irinotecan
  • irinotecan
  • irinotecan
  • irinotecan
  • irinotecan hcl
  • irinotecan hcl
  • irinotecan hcl
  • irinotecan hydrochloride
  • irinotecan hydrochloride
  • irinotecan hydrochloride
  • irinotecan hydrochloride
  • irinotecan hydrochloride
  • irinotecan hydrochloride hydrate
  • irinotecan hydrochloride hydrate
  • irinotecan hydrochloride hydrate
  • irinotecan hydrochloride trihydrate
  • irinotecan hydrochloride trihydrate
  • irinotecan hydrochloride trihydrate
  • irinotecan liposome
  • irinotecan liposome injection
  • irinotecan liposome injection
  • irinotecan liposome injection
  • irinotecan liposome injection
  • irinotecan liposome injection
  • irinotecan sucrosofate
  • irinotecan sucrosofate
  • irinotecan sucrosofate
  • irrinotecan
  • liposomal cpt-11
  • liposomal irinotecan
  • mm-398
  • mm-398
  • mm-398
  • nanoliposomal irinotecan
  • nk012 compound
  • onivyde
  • pep02
  • pep02
  • pep-02
  • pep-02
  • pep02 compound
  • (s)-camptothecin
  • (s)-camptothecin
  • (s)-(+)-camptothecin
  • (s)-(+)-camptothecin
  • sn 38
  • sn-38
  • sn-38
  • sn-38
  • sn 38 11
  • sn-38-11
  • sn38 cpd
  • u-101440e
  • u-101440e
  • u-101440e

Clinical trials

NCT IDPhaseStart dateSponsor(s)
NCT07271355Phase 3Jul 1, 2026City of Hope National Medical Center, National Cancer Institute (NCI)
NCT07283705Phase 2May 18, 2026Bristol-Myers Squibb, University of Texas at Houston
NCT07221357Phase 2/Phase 3 (Phase 3)Mar 4, 2026Biontech, Bristol-Myers Squibb
NCT06998940Phase 3Jan 6, 2026National Cancer Institute (NCI), SWOG Cancer Research Network
NCT07004413Phase 3Jan 1, 2026Humboldt University
NCT07141771Phase 1/Phase 2 (Phase 2)Dec 31, 2025Chinese Academy of Medical Sciences
NCT07255404Phase 2Dec 31, 2025Biontech, Bristol-Myers Squibb
NCT07150403Phase 2Dec 31, 2025Federation Francophone de Cancerologie Digestive
NCT07229846Phase 2Dec 31, 2025Harbin Medical University
NCT07155200Phase 1/Phase 2 (Phase 2)Dec 31, 2025Biosplice Therapeutics, Washington University in St. Louis
NCT07238283Phase 3Dec 31, 2025Hengrui Therapeutics, Inc.
NCT07277842Phase 3Dec 29, 2025Sun Yat-Sen University
NCT07258147Phase 2Dec 25, 2025Sichuan University
NCT07235202Phase 1/Phase 2 (Phase 2)Dec 22, 2025Government of China
NCT07284134Phase 3Dec 20, 2025Shanghai Junshi Bioscience Co.,Ltd.
NCT07214298Phase 1/Phase 2 (Phase 2)Dec 1, 2025State University of New York, Buffalo
NCT07033689Early Phase 1 (Phase 1)Dec 1, 2025SONIRE Therapeutics Inc., Stanford University
NCT07030283Phase 1Dec 1, 2025University of Colorado, Denver
NCT07094893Phase 4Nov 15, 2025Gruppo Oncologico del Nord-Ovest, Merck Serono
NCT07085338Phase 2Nov 10, 2025St. Jude Children's Hospital
Showing 20 of 1,733 trials
Page 1 / 87

Organizations

Research & Development (775)

OrganizationOrg typeTrialsAs lead sponsorPhasesEarliest year
National Cancer Institute (NCI)Government28312151995
Fudan UniversityAcademic/Hospital706052008
Sun Yat-Sen UniversityAcademic/Hospital625342011
PfizerFor profit542042001
Chinese Academy of Medical SciencesAcademic/Hospital482852009
RocheFor profit481742001
Cornell UniversityAcademic/Hospital402931997
Harvard UniversityAcademic/Hospital352331998
University of Texas at HoustonAcademic/Hospital352531997
AmgenFor profit341332002
SanofiFor profit341032000
GenentechFor profit31832003
Bristol-Myers SquibbFor profit301332001
MerckFor profit271632004
Zhejiang UniversityAcademic/Hospital262232009
Federation Francophone de Cancerologie DigestiveAcademic/Hospital252021998
Peking UniversityAcademic/Hospital252152009
Mayo ClinicAcademic/Hospital24431997
Jiao Tong UniversityAcademic/Hospital221452009
IpsenFor profit20432015
775 organizations
Page 1 / 39

Marketing (48)

OrganizationOrg typeRelationshipDate
Accord ResearchFor profitMKTGNov 21, 2008
ActavisFor profitMKTGFeb 27, 2008
Akorn, Inc.For profitMKTGSep 16, 2009
Barr LaboratoriesFor profitMKTGOct 31, 2008
Chartwell PharmaceuticalsFor profitMKTGApr 15, 2010
CiplaFor profitMKTGFeb 20, 2008
EmcureFor profitMKTGFeb 14, 2012
Epic Pharma LlcFor profitMKTGSep 16, 2009
Eugia PharmaFor profitMKTGNov 3, 2020
FosunFor profitMKTGNov 18, 2019
FreseniusFor profitMKTGFeb 27, 2008
Gland Pharma LtdFor profitMKTGNov 18, 2019
Gland Pharma LtdFor profitSYNNov 18, 2019
Hengrui Therapeutics, Inc.For profitMKTGDec 16, 2011
Hengrui Therapeutics, Inc.For profitSYNDec 16, 2011
HikmaFor profitMKTGDec 20, 2010
HikmaFor profitSYNDec 24, 2008
HospiraFor profitMKTGFeb 27, 2008
Ingenus PharmaceuticalsFor profitMKTGMay 26, 2017
InnogenixFor profitMKTGApr 15, 2010
Intas Pharmaceuticals LimitedFor profitMKTGAug 31, 2017
IpsenFor profitNDA2Oct 22, 2015
IpsenFor profitMKTGOct 22, 2015
Jiangsu Wuzhong Pharmaceutical Group Co., Ltd.For profitMKTGDec 16, 2011
Merrimack PharmaceuticalsFor profitNDA2Oct 22, 2015
Mustafa Nevzat PharmaceuticalsFor profitMKTGMay 13, 2011
NeopharmaFor profitMKTGApr 15, 2010
NovartisFor profitMKTGFeb 27, 2008
Novast LabsFor profitMKTGMay 26, 2017
PHARMOBEDIENTFor profitMKTGMay 13, 2011
PfizerFor profitNDA2Jun 14, 1996
Pharmacia & UpjohnFor profitNDAJun 14, 1996
Picket PharmsFor profitMKTGApr 15, 2010
PlivaFor profitMKTGOct 31, 2008
Qilu Pharmaceutical Co., Ltd.For profitSYNMay 3, 2016
Qilu Pharmaceutical Co., Ltd.For profitMKTGMay 3, 2016
Qilu Pharmaceutical Co., Ltd.For profitMKTGMay 3, 2016
SandozFor profitMKTGFeb 27, 2008
SandozFor profitSYNNov 12, 2009
Shilpa Medicare Ltd.For profitMKTGDec 28, 2018
Shilpa Medicare Ltd.For profitMKTGDec 28, 2018
Sun PharmaceuticalsFor profitMKTGApr 21, 2008
TevaFor profitSYNFeb 27, 2008
TevaFor profitMKTGNov 26, 2008
US AntibioticsFor profitMKTGApr 15, 2010
West-Ward PharmaceuticalFor profitMKTGDec 24, 2008
ZennovaFor profitMKTGMay 13, 2011
Zhejiang Hisun Pharmaceutical Co. Ltd.For profitMKTGJan 28, 2009