Statements (94)
| Predicate | Object |
|---|---|
| gptkbp:instance_of |
gptkb:Atom
|
| gptkbp:administered_by |
oral medication
oral tablet |
| gptkbp:animal_studies |
showed efficacy in mice
|
| gptkbp:bioavailability |
high bioavailability
|
| gptkbp:case_types |
p53 wild-type tumors
|
| gptkbp:casnumber |
675576-98-4
|
| gptkbp:chemical_category |
antineoplastic agent
|
| gptkbp:chemical_formula |
C16 H18 N4 O3 S
C16 H18 N2 O3 S |
| gptkbp:chemical_property |
stable at room temperature
|
| gptkbp:class |
piperidine derivative
piperazine derivative |
| gptkbp:clinical_trial |
ongoing
Phase I ongoing trials promising outcomes NCT00420212 NCT00420225 |
| gptkbp:clinical_use |
solid tumors
|
| gptkbp:collaborator |
academic institutions
|
| gptkbp:composed_by |
multi-step synthesis
|
| gptkbp:developed_by |
gptkb:Roche
treatment of tumors with wild-type p53 |
| gptkbp:discovered_by |
gptkb:Novartis
|
| gptkbp:discovery_year |
gptkb:2004
|
| gptkbp:dissolved |
soluble in DMSO
soluble in ethanol poorly soluble in water |
| gptkbp:drug_interactions |
may interact with CYP450 enzymes
|
| gptkbp:excretion |
excreted in urine
|
| gptkbp:field_of_study |
oncology
|
| gptkbp:first_described_by |
gptkb:2004
|
| gptkbp:first_published |
Vassilev et al.
|
| gptkbp:funding |
pharmaceutical companies
|
| https://www.w3.org/2000/01/rdf-schema#label |
Nutlin-3a
|
| gptkbp:in_vitro_studies |
demonstrated efficacy
|
| gptkbp:in_vivo_studies |
showed tumor regression
|
| gptkbp:inhibitor_type |
MDM2 antagonist
|
| gptkbp:initiated_by |
tumor growth
|
| gptkbp:invention |
2024
patented US20060200000 A1 |
| gptkbp:investigates |
gptkb:Oncology
gptkb:Kaposi's_sarcoma gptkb:neuroblastoma |
| gptkbp:knockouts |
high affinity for MDM2
|
| gptkbp:lifespan |
approximately 4 hours
|
| gptkbp:marketed_as |
not commercially available
not marketed |
| gptkbp:mechanism_of_action |
inhibits MDM2
inhibits MDM2-p53 interaction |
| gptkbp:metabolism |
metabolized by liver enzymes
|
| gptkbp:notable_work |
studied in breast cancer
studied in glioblastoma studied in head and neck cancer studied in leukemia studied in lung cancer studied in ovarian cancer studied in pancreatic cancer studied in prostate cancer studied in sarcoma studied in colon cancer |
| gptkbp:pharmacokinetics |
oral bioavailability
|
| gptkbp:potential_use_in |
combination therapy
|
| gptkbp:project |
clinical phase II
|
| gptkbp:promotes |
apoptosis in cancer cells
|
| gptkbp:publication |
numerous studies published
|
| gptkbp:related_to |
p53 tumor suppressor
p53 tumor suppressor protein |
| gptkbp:research |
inhibits tumor growth
potential for combination therapy induces apoptosis in cancer cells enhances chemotherapy efficacy increases p53 activity promotes cell cycle arrest |
| gptkbp:research_areas |
oncology
|
| gptkbp:research_focus |
MDM2-p53 pathway
|
| gptkbp:research_status |
under clinical investigation
|
| gptkbp:safety_features |
generally well tolerated
|
| gptkbp:side_effect |
fatigue
headache nausea diarrhea |
| gptkbp:structure |
contains a thiazole ring
contains a sulfonamide group contains a piperazine ring |
| gptkbp:synergistic_effects_with |
other chemotherapeutics
|
| gptkbp:targets |
gptkb:MDM2
gptkb:MDM2_protein various cancers |
| gptkbp:used_for |
gptkb:cancer_treatment
|
| gptkbp:weight |
334.41 g/mol
302.39 g/mol |