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zarnestra

Small moleculeexperimental

Tipifarnib is a farnesyltransferase inhibitor. Farnesyltransferase inhibitors block the activity of the farnesyltransferase enzyme by inhibiting prenylation of the CAAX tail motif, which ultimately prevents Ras from binding to the membrane, rendering it inactive. — Wikipedia

Clinical trial activity

89 trials · 46 clinical orgs · 0 marketing orgs

Phase 1
36
Phase 2
63
Phase 3
4
Phase 4
0

Earliest trial started Oct 1, 1998 (NCT00003707)

Timeline

1990s

  1. Jan 1, 1998

    Earliest Phase 1 Sponsor(trial)

  2. Jan 1, 1999

    Earliest Phase 2 Sponsor(trial)

  3. Jan 1, 1999

    Earliest Phase 3 Sponsor(trial)

Indications

Studied for

Mechanism of action

Chemistry & pharmacology

Loading structure…

SMILES

Cn1cncc1[C@@](N)(c1ccc(Cl)cc1)c1ccc2c(c1)c(-c1cccc(Cl)c1)cc(=O)n2C
Mol. weight
489.41 g/mol
Lipinski Ro5
1 violation(s)
Rule of 3
No
Chirality
Single Stereoisomer
Inorganic
No
Polymer
No

Oral

No

Parenteral

No

Topical

No

Sources

Also known as

  • 2 (1h))-quinolinone,6-(amino(4-chlorophenyl)(1-methyl-1h-imidazol-5-yl)methyl)-4-(3-chlorophenyl)-1-methyl-,(+)-
  • r11577
  • r-11577
  • r-11577
  • r115777
  • r115777
  • r115777
  • r 115777
  • r-115777
  • r-115777
  • r-115777
  • (r)-6-(amino(4-chlorophenyl)(1-methyl-1h-imidazol-5-yl)methyl)-4-(3-chlorophenyl)-1-methyl-2(1h)-quinolinone
  • tipifarnib
  • tipifarnib
  • tipifarnib
  • tipifarnib
  • tipifarnib
  • zarnestra
  • zarnestra
  • zarnestra
  • zarnestra

Clinical trials

NCT IDPhaseStart dateSponsor(s)
NCT06540963Phase 2Nov 1, 2024Beat Childhood Cancer, Pennsylvania State University
NCT05693090Phase 1Feb 1, 2023Kura Oncology, Inc.
NCT04997902Phase 1/Phase 2 (Phase 2)Nov 30, 2021Kura Oncology, Inc.
NCT04865159Phase 1May 6, 2021Kura Oncology, Inc., NEXT Oncology
NCT04284774Phase 2Mar 20, 2020National Cancer Institute (NCI)
NCT03719690Phase 2Nov 5, 2018Kura Oncology, Inc.
NCT03496766Phase 2May 7, 2018Spanish Lung Cancer Group, Universidad Complutense de Madrid
NCT02807272Phase 2Oct 1, 2016Kura Oncology, Inc.
NCT02779777Phase 2May 1, 2016Kura Oncology, Inc.
NCT02535650Phase 2Nov 12, 2015Sungkyunkwan University
NCT02464228Phase 2Sep 1, 2015Kura Oncology, Inc.
NCT02383927Phase 2Mar 1, 2015Kura Oncology, Inc.
NCT01361464Phase 2May 1, 2011National Cancer Institute (NCI), University of South Florida
NCT00602771Phase 2Jan 1, 2008Johns Hopkins University, National Cancer Institute (NCI)
NCT00281957Phase 2Aug 1, 2007National Cancer Institute (NCI), Southwest Oncology Group
NCT00847223Phase 2Jun 1, 2007The Lymphoma Study Association
NCT00101153Phase 1Apr 1, 2007National Cancer Institute (NCI), University of Toronto
NCT00470301Phase 1/Phase 2 (Phase 2)Apr 1, 2007National Cancer Institute (NCI), Yeshiva University
NCT00510939Phase 2Mar 1, 2007Johnson and Johnson, University of Bologna
NCT00972712Phase 1Dec 1, 2006Emory University, Millennium Pharmaceuticals, Ortho Biotech, Inc.
Showing 20 of 89 trials
Page 1 / 5

Organizations

Research & Development (46)

OrganizationOrg typeTrialsAs lead sponsorPhasesEarliest year
National Cancer Institute (NCI)Government624231998
Johnson and JohnsonFor profit11631999
Kura Oncology, Inc.For profit9932015
University of Texas at HoustonAcademic/Hospital8221998
Mayo ClinicAcademic/Hospital6122002
University of South FloridaAcademic/Hospital6322000
Johns Hopkins UniversityAcademic/Hospital5021999
Southwest Oncology GroupAcademic/Hospital4212000
University of PennsylvaniaAcademic/Hospital3222001
Yeshiva UniversityAcademic/Hospital3012003
City of Hope National Medical CenterAcademic/Hospital2112001
Millennium PharmaceuticalsFor profit2022005
National Institutes of Health (NIH)Government2122001
New York UniversityAcademic/Hospital2221999
Stanford UniversityAcademic/Hospital2112000
Temple UniversityAcademic/Hospital2112000
University of Texas, San AntonioAcademic/Hospital2221998
University of TorontoAcademic/Hospital2222002
University of ToulouseAcademic/Hospital2212003
Beat Childhood CancerAcademic/Hospital1012024
46 organizations
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