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cytarabine

Trade name: cytosar-u

Small moleculeapproved

Approved

Jun 17, 1969

Cytarabine is a pyrimidine nucleoside analog. Cytarabine or cytosine arabinoside (Cytosar-U or Depocyt) is a chemotherapy agent used mainly in the treatment of cancers of white blood cells such as acute myeloid leukemia (AML) and non-Hodgkin lymphoma. It also has antiviral and immunosuppressant properties. Cytarabine is an antimetabolite antineoplastic agent that inhibits the synthesis of DNA. It is a cell cycle phase-specific, affecting cells only during the S phase of cell division. Intracellularly, cytarabine is converted into cytarabine-5-triphosphate (ara-CTP), which is the active metabolite. The mechanism of action is not completely understood, but it appears that ara-CTP acts primarily through inhibition of DNA polymerase. Incorporation into DNA and RNA may also contribute to cytarabine cytotoxicity. Cytarabine is cytotoxic to a wide variety of proliferating mammalian cells in culture.The drug has a short plasma half-life, low stability and limited bioavailability. Overdosing of patients with continuous infusions may lead to side effects. Thus, various prodrug strategies and delivery systems have been explored extensively to enhance the half-life, stability and delivery of cytarabine. Alternative, delivery systems of cytarabine have emerged for the treatment of different cancers. The liposomal-cytarabine formulation has been approved for the treatment of lymphomatous meningitis. — NCATS

Clinical trial activity

1,353 trials · 618 clinical orgs · 15 marketing orgs

Phase 1
391
Phase 2
966
Phase 3
289
Phase 4
47

Earliest trial started Nov 1, 1986 (NCT01324063)

Timeline

1960s

  1. Jun 17, 1969

    Earliest FDA Approval

  2. Jun 17, 1969

    Teva — NDA Secondary Org

1980s

  1. Jan 1, 1986

    Earliest Phase 3 Sponsor(trial)

  2. Jan 1, 1987

    Earliest Phase 2 Sponsor(trial)

  3. Aug 2, 1989

    West-Ward Pharmaceutical — Marketing Organization

  4. Aug 2, 1989

    Hikma — Marketing Organization

1990s

  1. Jun 4, 1990

    Hospira — Marketing Organization

  2. Jan 1, 1995

    Earliest Phase 1 Sponsor(trial)

  3. Dec 30, 1998

    Teva — First NDA Organization

  4. Dec 30, 1998

    Teva — NDA Organization

  5. Dec 30, 1998

    Teva — Marketing Organization

  6. Apr 1, 1999

    Pacira Pharmaceuticals — NDA Secondary Org

2000s

  1. Jan 15, 2004

    Fresenius — Marketing Organization

2010s

  1. Dec 13, 2011

    Rising Pharmaceuticals — Marketing Organization

  2. Dec 13, 2011

    Mylan — Marketing Organization

  3. Aug 3, 2017

    Celator Pharmaceuticals — Marketing Organization

  4. Aug 3, 2017

    Jazz Pharmaceuticals — NDA Secondary Org

  5. Nov 9, 2017

    Eu Yan Sang — Marketing Organization

  6. Nov 9, 2017

    Meitheal — Marketing Organization

  7. Dec 23, 2019

    Gland Pharma Ltd — Marketing Organization

  8. Dec 23, 2019

    Fosun — Marketing Organization

Indications

Approved for

Studied for

Mechanism of action

Combination products

  • vyxeos

    with daunorubicin

    Also known as cytarabine and daunorubicin

Approval history

  • approvedPriority reviewJun 17, 1969

Chemistry & pharmacology

Loading structure…

SMILES

Nc1ccn([C@@H]2O[C@H](CO)[C@@H](O)[C@@H]2O)c(=O)n1
Mol. weight
243.22 g/mol
Lipinski Ro5
Pass
Rule of 3
No
Chirality
Single Stereoisomer
Inorganic
No
Polymer
No
Delivery
Parenteral
Availability
Prescription Only

Oral

No

Parenteral

Yes

Topical

No

Black box warning

Sources

Also known as

  • 1-.beta.-d-arabinofuranosyl-4-amino-2(1h)pyrimidinone
  • 1-beta-d-arabinofuranosyl-4-amino-2(1h)pyrimidinone
  • 1-.beta.-d-arabinofuranosylcytosine
  • 1-beta-d-arabinofuranosylcytosine
  • 1-beta-d-arabinofuranosylcytosine
  • 1-beta-d-arabinofuranosylcytosine
  • 1.beta.-d-arabinofuranosylcytosine
  • 2(1h)-pyrimidinone, 4-amino-1-beta-d-arabinofuranosyl-
  • 2(1h)-pyrimidinone, 4-amino-1.beta.-d-arabinofuranosyl-
  • 4-amino-1-beta-d-arabinofuranosyl-2(1h)-pyrimidinone
  • 4-amino-1-beta-d-arabinofuranosyl-2(1h)-pyrimidinone
  • alexan
  • alexan
  • alexan
  • alexan 100
  • arabine
  • arabinocytosine
  • arabinofuranosylcytosine
  • arabinoside c
  • arabinosylcytosine
  • arabinosyl cytosine
  • arabinosyl cytosine
  • ara-c
  • ara-c
  • ara-cell
  • aracytidine
  • aracytidine
  • ara-cytidine
  • ara-cytidine
  • aracytin
  • aracytine
  • aracytine
  • astarabine
  • .beta.-cytosine arabinoside
  • beta-cytosine arabinoside
  • chx-3311
  • citarabina
  • citarabina
  • cpx-351
  • cpx-351
  • cyclocide
  • cytarabin
  • cytarabine
  • cytarabine
  • cytarabine
  • cytarabine
  • cytarabine
  • cytarabine
  • cytarabine
  • cytarabine
  • cytarabine
  • cytarabine
  • cytarabine hcl
  • cytarabine hcl
  • cytarabine hcl
  • cytarabine hydrochloride
  • cytarabine hydrochloride
  • cytarabine hydrochloride
  • cytarabine hydrochloride
  • cytarabine hydrochloride
  • cytarabine hydrochloride
  • cytarabine liposome
  • cytarabinoside
  • cytarabinum
  • cytarabinum
  • cytarabinum
  • cytarbel
  • cytosar
  • cytosar
  • cytosar
  • cytosar-u
  • cytosar-u
  • cytosine-1-beta-d-arabinofuranoside
  • cytosine-1-beta-d-arabinofuranoside
  • cytosine arabinoside
  • cytosine arabinoside
  • cytosine arabinoside
  • cytosine arabinoside hcl
  • cytosine arabinoside hcl
  • cytosine-.beta.-arabinoside
  • cytosine-beta-arabinoside
  • cytosine beta-d-arabinofuranoside
  • cytosine-β-d-arabinofuranoside
  • cytosine-β-d-arabinofuranoside
  • depocyt
  • depocyt
  • depocyte
  • depocyte
  • erpalfa
  • liposomal ara-c
  • liposomal cytarabine
  • mk-8242
  • mk-8242
  • starasid
  • tarabine pfs
  • tarabine pfs
  • tarabine pfs
  • u 19920
  • u-19920
  • u-19920
  • u-19920
  • u-19920a
  • u-19920a
  • udicil
  • wr-28453

Clinical trials

NCT IDPhaseStart dateSponsor(s)
NCT07175415Phase 1/Phase 2 (Phase 2)Oct 1, 2026AbbVie, AstraZeneca, Humboldt University, Princess Maxima Center for Pediatric Oncology
NCT07227584Phase 2Apr 30, 2026Harvard University
NCT07072585Phase 2/Phase 3 (Phase 3)Mar 30, 2026National Cancer Institute (NCI)
NCT07294677Phase 1/Phase 2 (Phase 2)Mar 17, 2026University of Chicago
NCT07153796Phase 2Feb 28, 2026Amgen, University of Texas at Houston
NCT07022678Phase 3Jan 20, 2026National Cancer Institute (NCI)
NCT06930352Phase 2Jan 10, 2026Kura Oncology, Inc., Ohio State University
NCT07223814Phase 3Dec 31, 2025German-Austrian Acute Myeloid Leukemia Study Group, HOVON - Dutch Haemato-Oncology Association
NCT07255872Phase 2/Phase 3 (Phase 3)Dec 31, 2025Baili Pharmaceutical Group
NCT07228273Phase 2Dec 24, 2025OHSU Knight Cancer Institute, Oregon Health and Science University
NCT07304739Phase 2Dec 22, 2025Tianjin Medical University
NCT07301138Phase 2Dec 15, 2025Jiao Tong University
NCT06770257Phase 2Dec 10, 2025China Academy of Chinese Medical Sciences, CSPC Zhongnuo Pharmaceutical (Shijiazhuang) Co., Ltd.
NCT07052994Phase 1Dec 1, 2025University of Texas at Houston
NCT07053020Phase 1/Phase 2 (Phase 2)Dec 1, 2025University of Texas at Houston
NCT07214779Phase 3Dec 1, 2025ENGOT Foundation, GOG Foundation, Inc., Incyte
NCT07230626Phase 3Nov 20, 2025Shijiazhuang Pharma Group (CSPC)
NCT06917911Phase 2Nov 20, 2025National Cancer Institute (NCI)
NCT07059975Early Phase 1 (Phase 1)Oct 22, 2025Baylor University
NCT06918431Phase 2Oct 10, 2025City of Hope National Medical Center, National Cancer Institute (NCI)
Showing 20 of 1,353 trials
Page 1 / 68

Organizations

Research & Development (618)

OrganizationOrg typeTrialsAs lead sponsorPhasesEarliest year
National Cancer Institute (NCI)Government37016041987
University of Texas at HoustonAcademic/Hospital11810341993
University of WashingtonAcademic/Hospital524341994
St. Jude Children's HospitalAcademic/Hospital393651993
Cornell UniversityAcademic/Hospital363241990
Harvard UniversityAcademic/Hospital363131993
Jiao Tong UniversityAcademic/Hospital312252010
Jazz PharmaceuticalsFor profit27442009
NovartisFor profit26631996
People's Liberation Army of ChinaGovernment251352004
PETHEMA FoundationAcademic/Hospital252551996
Chinese Academy of Medical SciencesAcademic/Hospital231852010
Soochow UniversityAcademic/Hospital232032014
University of Southern CaliforniaAcademic/Hospital221822002
Ohio State UniversityAcademic/Hospital211021999
PfizerFor profit20732000
Southwest Oncology GroupAcademic/Hospital201521994
European Organisation for Research and Treatment of CancerAcademic/Hospital191721986
AbbVieFor profit17332015
Zhejiang UniversityAcademic/Hospital171242020
618 organizations
Page 1 / 31

Marketing (20)

OrganizationOrg typeRelationshipDate
Athenex, Inc.For profitMKTG—
Celator PharmaceuticalsFor profitMKTGAug 3, 2017
Eu Yan SangFor profitMKTGNov 9, 2017
FosunFor profitMKTGDec 23, 2019
FreseniusFor profitMKTGJan 15, 2004
Gland Pharma LtdFor profitMKTGDec 23, 2019
HikmaFor profitSYNAug 2, 1989
HikmaFor profitMKTGAug 2, 1989
HospiraFor profitMKTGJun 4, 1990
Jazz PharmaceuticalsFor profitNDA2Aug 3, 2017
MeithealFor profitMKTGNov 9, 2017
MylanFor profitMKTGDec 13, 2011
Pacira PharmaceuticalsFor profitNDA2Apr 1, 1999
Rising PharmaceuticalsFor profitMKTGDec 13, 2011
Rising PharmaceuticalsFor profitSYNDec 13, 2011
TevaFor profitNDA2Jun 17, 1969
TevaFor profitSYNDec 30, 1998
TevaFor profitNDADec 30, 1998
TevaFor profitMKTGDec 30, 1998
West-Ward PharmaceuticalFor profitMKTGAug 2, 1989