Leveraging an Open Science Drug Discovery Model to Develop CNS-Penetrant ALK2 Inhibitors for the Treatment of Diffuse Intrinsic Pontine Glioma
David Smil, Jong Fu Wong, Eleanor P. Williams, R.J. Adamson, Alison Howarth, David McLeod, Ahmed Mamai, Soyoung Kim, Brian J. Wilson, Taira Kiyota, Ahmed Aman, Julie Owen, Gennady Poda, Kurumi Y. Horiuchi, Ekaterina Kuznetsova, Haiching Ma, J. Hamblin, Sue Cramp, Owen G Roberts, A.M. Edwards, David Uehling, Rima Al‐awar, Alex N. Bullock, Jeff A. O’Meara, Methvin Isaac
Abstract
pharmacokinetic (PK) properties and tolerability mark these inhibitors as advanced preclinical compounds suitable for further development and evaluation in orthotopic models of DIPG.
Topics & Concepts
ChemistryDrug discoveryPharmacologyPharmacokineticsActivin receptorPenetrant (biochemical)Blood–brain barrierTolerabilityCancer researchKinaseMedicineCentral nervous systemInternal medicineAdverse effectBiochemistryOrganic chemistryGlioma Diagnosis and TreatmentNeuroblastoma Research and TreatmentsManagement of metastatic bone disease