|
gptkbp:instance_of
|
gptkb:Atom
|
|
gptkbp:administered_by
|
oral tablet
|
|
gptkbp:bioavailability
|
moderate
|
|
gptkbp:can_be_used_to
|
treatment of tumors
|
|
gptkbp:casnumber
|
548472-68-0
|
|
gptkbp:chemical_formula
|
C16 H18 N4 O3 S
|
|
gptkbp:class
|
piperazine derivative
|
|
gptkbp:clinical_trial
|
ongoing
Phase I
various hospitals
|
|
gptkbp:collaborations
|
academic institutions
pharmaceutical companies
|
|
gptkbp:composed_by
|
multi-step synthesis
|
|
gptkbp:discovered_by
|
gptkb:Boehringer_Ingelheim
|
|
gptkbp:dissolved
|
soluble in DMSO
slightly soluble in water
|
|
gptkbp:drug_interactions
|
may interact with CYP450
|
|
gptkbp:excretion
|
urine
|
|
gptkbp:first_described_by
|
gptkb:2004
|
|
gptkbp:formulation
|
capsule form
tablet form
|
|
https://www.w3.org/2000/01/rdf-schema#label
|
nutlin-3b
|
|
gptkbp:invention
|
gptkb:Boehringer_Ingelheim
2024
|
|
gptkbp:knockouts
|
high affinity for MDM2
|
|
gptkbp:market_position
|
not commercially available
|
|
gptkbp:mechanism_of_action
|
inhibits MDM2-p53 interaction
|
|
gptkbp:metabolism
|
liver
|
|
gptkbp:publication
|
clinical trial results
review articles
numerous peer-reviewed articles
mechanistic studies
|
|
gptkbp:related_to
|
gptkb:p53
|
|
gptkbp:research
|
inhibits tumor growth
induces apoptosis
enhances chemosensitivity
increases p53 activity
promotes cell cycle arrest
|
|
gptkbp:research_areas
|
oncology
|
|
gptkbp:route_of_administration
|
oral
|
|
gptkbp:safety_features
|
generally well tolerated
|
|
gptkbp:side_effect
|
gptkb:anemia
fatigue
headache
nausea
diarrhea
insomnia
thrombocytopenia
neutropenia
|
|
gptkbp:targets
|
gptkb:MDM2
gptkb:Oncology
gptkb:Kaposi's_sarcoma
gptkb:neuroblastoma
|
|
gptkbp:used_in
|
cancer therapy
|
|
gptkbp:bfsParent
|
gptkb:nutlin-3
|
|
gptkbp:bfsLayer
|
6
|