Synonyms: Daurismo® | PF 04449913 | PF-04449913
glasdegib is an approved drug (FDA (2018), EMA (2020))
Compound class:
Synthetic organic
Comment: Glasdegib is a potent and orally active inhibitor of the hedgehog signalling pathway, that acts as an antagonist of the class frizzled GPCR, smoothened (SMO) [2].
Ligand Activity Visualisation ChartsThese are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts. ✖ |
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No information available. |
Summary of Clinical Use |
Glasdegib (as research code PF-04449913) was evaluated in clinical trials for various hematologic malignancies. Phase 2 results from trial NCT01546038 were published by Cortes et al. in 2018, which indicated that glasdegib plus cytarabine/daunorubicin was well tolerated and achieved 40% complete remission in patients ≥55 years old with newly-diagnosed acute myeloid leukemia (AML) or high-risk myelodysplastic syndromes [1]. Click here to link to ClinicalTrials.gov's full listing of PF-04449913 trials. Following 'Priority Review', the FDA approved glasdegib (in November 2018) as a first-line therapy (in combination with low dose cytarabine chemotherapy) for AML in patients ≥75 years who are too fragile (due to chronic ill health or other comorbidities) to tolerate more intensive and toxic chemotherapy. |
Clinical Trials | |||||
Clinical Trial ID | Title | Type | Source | Comment | References |
NCT01546038 | A Study To Evaluate PF-04449913 With Chemotherapy In Patients With Acute Myeloid Leukemia or Myelodysplastic Syndrome | Phase 2 Interventional | Pfizer |