AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML)

Patrick P. Zarrinkar, Ruwanthi N. Gunawardane, Merryl Cramer, +13

Blood

Phase I Study of Quizartinib Administered Daily to Patients With Relapsed or Refractory Acute Myeloid Leukemia Irrespective of FMS-Like Tyrosine Kinase 3–Internal Tandem Duplication Status

Jörge E. Cortes, Hagop M. Kantarjian, James M. Foran, +8

Journal of Clinical Oncology

Identification of <i>N</i>-(5-<i>tert</i>-Butyl-isoxazol-3-yl)-<i>N</i>′-{4-[7-(2-morpholin-4-yl-ethoxy)imidazo[2,1-<i>b</i>][1,3]benzothiazol-2-yl]phenyl}urea Dihydrochloride (AC220), a Uniquely Potent, Selective, and Efficacious FMS-Like Tyrosine Kinase-3 (FLT3) Inhibitor

Qi Chao, Kelly G. Sprankle, Robert M. Grotzfeld, +10

Journal of Medicinal Chemistry

Drug TargetAml PatientsPharmacotherapyChemical BiologyPharmaceutical Chemistry +18

Discovery of GBT440, an Orally Bioavailable R-State Stabilizer of Sickle Cell Hemoglobin

Brian Metcalf, Chih-Yuan Chuang, Kobina Dufu, +21

ACS Medicinal Chemistry Letters

AC220, a Potent, Selective, Second Generation FLT3 Receptor Tyrosine Kinase (RTK) Inhibitor, in a First-in-Human (FIH) Phase 1 AML Study.

Jörge E. Cortes, James M. Foran, Darejan Ghirdaladze, +14

Blood

Identification of 1-(3-(6,7-Dimethoxyquinazolin-4-yloxy)phenyl)-3-(5-(1,1,1-trifluoro-2-methylpropan-2-yl)isoxazol-3-yl)urea Hydrochloride (CEP-32496), a Highly Potent and Orally Efficacious Inhibitor of V-RAF Murine Sarcoma Viral Oncogene Homologue B1 (BRAF) V600E

Martin W. Rowbottom, Raffaella Faraoni, Qi Chao, +29

Journal of Medicinal Chemistry

Orally Efficacious InhibitorChemoprevention StrategyImmunologySeveral BrafAntiviral Drug +17

CEP-32496: A Novel Orally Active BRAFV600E Inhibitor with Selective Cellular and <i>In Vivo</i> Antitumor Activity

Joyce James, Bruce Ruggeri, Robert C. Armstrong, +20

Molecular Cancer Therapeutics

Tumor BiologyActive Braf InhibitorNovel TherapyBraf GeneMedicine +13

Arylcarboxyamino-substituted diaryl ureas as potent and selective FLT3 inhibitors

Hitesh Patel, Robert M. Grotzfeld, Andiliy Lai, +12

Bioorganic & Medicinal Chemistry Letters

Molecular PharmacologyMedicinal ChemistryMedicinePharmacological AgentPharmacotherapy +5

An open-label, single-dose, phase 1 study of the absorption, metabolism and excretion of quizartinib, a highly selective and potent FLT3 tyrosine kinase inhibitor, in healthy male subjects, for the treatment of acute myeloid leukemia

Madhu Sanga, Joyce James, Joseph Marini, +3

Xenobiotica

A Phase II Open-Label, Ac220 Monotherapy Efficacy Study In Patients with Refractory/Relapsed Flt3-Itd Positive Acute Myeloid Leukemia: Updated Interim Results

Jörge E. Cortes, Alexander E. Perl, Catherine C. Smith, +19

Blood