motexafin gadolinium

Small moleculeexperimental

Gadobutrol is a second-generation extracellular non-ionic macrocyclic GBCA that is used in patients undergoing diagnostic contrast-enhanced MRI for visualization of pathological lesions in the CNS and all other body regions or for contrast-enhanced magnetic resonance angiography (MRA) to evaluate perfusion and flow-related abnormalities. It is a non-ionic, paramagnetic complex consisting of gadolinium (Gd3+) chelated with the macrocyclic compound dihydroxy-hydroxymethylpropyl-tetraazacyclododecane-triacetic acid (butrol). Gadavist (the trade name of gadobutrol) was approved by FDA in 2011 for intravenous use in diagnostic MRI in adults and children (2 years of age and older) to detect and visualize areas with disrupted blood brain barrier and/or abnormal vascularity of the central nervous system. Application of gadobutrol in humans, up to a dose of 0.5 mmol/kg was shown to be well tolerated. Following intravenous administration, gadobutrol may increase MRI sensitivity for the detection of tumors and inflammatory and demyelinating diseases of the central nervous system which are associated with areas with blood-brain barrier defects due to altered perfusion or an enlarged extracellular space. Gadobutrol is not metabolized. It is eliminated in an unchanged form via the kidneys; extra-renal elimination is negligible. Side effects include headache, nausea, abnormal taste and feeling hot. — NCATS

Clinical trial activity

79 trials · 62 clinical orgs · 0 marketing orgs

Phase 1
34
Phase 2
32
Phase 3
4
Phase 4
4

Earliest trial started Jul 1, 1998 (NCT00003409)

Timeline

1990s

  1. Jan 1, 1998

    Earliest Phase 1 Sponsor(trial)

  2. Jan 1, 1998

    Earliest Phase 3 Sponsor(trial)

2000s

  1. Jan 1, 2001

    Earliest Phase 2 Sponsor(trial)

Indications

Studied for

Mechanism of action

Chemistry & pharmacology

Loading structure…

SMILES

[Gd+3]
Mol. weight
157.25 g/mol
Chirality
Achiral Molecule
Inorganic
Yes
Polymer
No

Oral

No

Parenteral

No

Topical

No

Sources

Also known as

  • api-gp3
  • fp-gp1
  • gadolinium
  • gadolinium
  • gadolinium
  • gadolinium texaphyrin
  • gadolinium texaphyrin
  • gadolinium texaphyrin
  • gadolinium texaphyrin
  • gadolinium texaphyrin complex
  • gd(iii) texaphyrin
  • gd-tex
  • gd-tex
  • gd texaphyrin
  • gd texaphyrin
  • motexafin gadolinium
  • motexafin gadolinium
  • motexafin gadolinium
  • motexafin gadolinium
  • motexafin gadolinium
  • moxtezafin gadolinium
  • pci-0120
  • pci-0120
  • pci-0120
  • xcytrin
  • xcytrin
  • xcytrin

Clinical trials

NCT IDPhaseStart dateSponsor(s)
NCT05692635Phase 2Aug 30, 2023National Cancer Institute (NCI), Wake Forest University
NCT05390021N/AOct 31, 2022Harvard University
NCT04899908Phase 2Sep 15, 2021Harvard University, NH TherAguix SAS
NCT04727242Phase 2Jan 28, 2021Stanford University
NCT04474353Phase 1Nov 30, 2020NovoCure Ltd., Stanford University
NCT04340180Phase 1Jun 30, 2020Bracco, University of Alabama, Birmingham
NCT04264143Phase 1Apr 30, 2020Columbia University, Midatech Pharma
NCT04058132Phase 2Aug 9, 2019Uniformed Services University of the Health Sciences, United States Army
NCT03565367Phase 1Nov 14, 2018Stanford University
NCT03154996Phase 1Jan 18, 2018Columbia University, National Cancer Institute (NCI)
NCT03270059Phase 2Oct 6, 2017Celgene, OHSU Knight Cancer Institute, Oregon Health and Science University
NCT02234375Phase 4Jul 1, 2017Harvard University
NCT03067467Early Phase 1 (Phase 1)May 1, 2017The University of Texas, Dallas
NCT02783768Phase 1Mar 1, 2017Columbia University
NCT02163005Phase 4Dec 1, 2016Harvard University
NCT02390635Phase 1May 1, 2016General Electric, University of Texas at Houston
NCT02826343Early Phase 1 (Phase 1)May 1, 2016National Institutes of Health (NIH), University of Virginia
NCT02530931Phase 4Mar 1, 2016Guerbet, University of Grenoble
NCT02590497N/AMar 1, 2016Ohio State University
NCT02112097Phase 1/Phase 2 (Phase 2)Jan 1, 2016ASIS Corporation, AUTOMATIC SUBDERMAL INJECTOR SYSTEM, INC
Showing 20 of 79 trials
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Organizations

Research & Development (62)

OrganizationOrg typeTrialsAs lead sponsorPhasesEarliest year
National Cancer Institute (NCI)Government24631998
PharmacyclicsFor profit191731998
Stanford UniversityAcademic/Hospital6542007
ASIS CorporationFor profit5512016
Northwestern UniversityAcademic/Hospital5332003
Oregon Health and Science UniversityAcademic/Hospital5422004
AUTOMATIC SUBDERMAL INJECTOR SYSTEM, INCAcademic/Hospital4012016
Harvard UniversityAcademic/Hospital4432016
Columbia UniversityAcademic/Hospital3312017
Ohio State UniversityAcademic/Hospital3121999
University of PennsylvaniaAcademic/Hospital3221999
University of WisconsinAcademic/Hospital3122002
American College of RadiologyAcademic/Hospital2212010
AstellasFor profit2022010
Johns Hopkins UniversityAcademic/Hospital2211999
Mayo ClinicAcademic/Hospital2012004
University of California, Los AngelesAcademic/Hospital2211998
University of PittsburghAcademic/Hospital2111998
University of RochesterAcademic/Hospital2022006
University of South FloridaAcademic/Hospital2011999
62 organizations
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