glasdegib   Click here for help

GtoPdb Ligand ID: 8201

Synonyms: Daurismo® | PF 04449913 | PF-04449913
Approved drug
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].
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2D Structure
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Physico-chemical Properties
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Hydrogen bond acceptors 6
Hydrogen bond donors 3
Rotatable bonds 5
Topological polar surface area 96.84
Molecular weight 374.19
XLogP 2.15
No. Lipinski's rules broken 0
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Canonical SMILES N#Cc1ccc(cc1)NC(=O)NC1CCN(C(C1)c1nc2c([nH]1)cccc2)C
Isomeric SMILES N#Cc1ccc(cc1)NC(=O)N[C@@H]1CCN([C@H](C1)c1nc2c([nH]1)cccc2)C
InChI InChI=1S/C21H22N6O/c1-27-11-10-16(24-21(28)23-15-8-6-14(13-22)7-9-15)12-19(27)20-25-17-4-2-3-5-18(17)26-20/h2-9,16,19H,10-12H2,1H3,(H,25,26)(H2,23,24,28)/t16-,19-/m1/s1
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Summary of Clinical Use Click here for help
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'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