Phase 1 Concentration‐QTc and Cardiac Safety Analysis of the MDM2 Antagonist KRT‐232 in Patients With Advanced Solid Tumors, Multiple Myeloma, or Acute Myeloid Leukemia

Metastatic Melanoma Patient–Derived Xenografts Respond to MDM2 Inhibition as a Single Agent or in Combination with BRAF/MEK Inhibition

(2020) Rebecca L. Shattuck-Brandt et al.   CLINICAL CANCER RESEARCH

KRT-232, a first-in-class, murine double minute 2 inhibitor (MDM2i), for TP53 wild-type (p53WT) Merkel cell carcinoma (MCC) after anti–PD-1/L1 immunotherapy.

(2020) Michael K.K. Wong et al.   JOURNAL OF CLINICAL ONCOLOGY

MDM2 inhibition: an important step forward in cancer therapy

(2020) Marina Konopleva et al.   LEUKEMIA

Phase 1 study of the MDM2 inhibitor AMG 232 in patients with advanced P53 wild-type solid tumors or multiple myeloma

(2019) W. Larry Gluck et al.   INVESTIGATIONAL NEW DRUGS

Concentration-QTc (C-QTc) Analysis of the MDM2 Inhibitor KRT-232 (formerly AMG 232) in Subjects with Advanced Solid Tumors, Multiple Myeloma, or Acute Myeloid Leukemia

(2019) Adekemi Taylor et al.   BLOOD

A Randomized, Open-Label, Multicenter, Phase 2 Study to Evaluate the Efficacy, Safety, and Pharmacokinetics of KRT-232 Compared with Ruxolitinib in Patients with Phlebotomy-Dependent Polycythemia Vera

(2019) Jason Gotlib et al.   BLOOD

An Open-Label, Phase 2 Study of KRT-232, a First-in-Class, Oral Small Molecule Inhibitor of MDM2, for the Treatment of Patients with Myelofibrosis (MF) Who Have Previously Received Treatment with a JAK Inhibitor

(2019) Regina Garcia-Delgado et al.   BLOOD

Phase 1 summary of plasma concentration–QTc analysis for idasanutlin, an MDM2 antagonist, in patients with advanced solid tumors and AML

(2018) Steven Blotner et al.   CANCER CHEMOTHERAPY AND PHARMACOLOGY

Scientific white paper on concentration-QTc modeling

(2017) Christine Garnett et al.   JOURNAL OF PHARMACOKINETICS AND PHARMACODYNAMICS

The MDM2 Inhibitor AMG 232 Demonstrates Robust Antitumor Efficacy and Potentiates the Activity of p53-Inducing Cytotoxic Agents

(2015) J. Canon et al.   MOLECULAR CANCER THERAPEUTICS

Pharmacokinetics and metabolism of AMG 232, a novel orally bioavailable inhibitor of the MDM2–p53 interaction, in rats, dogs and monkeys:in vitro–in vivocorrelation

(2015) Qiuping Ye et al.   XENOBIOTICA

Discovery of AMG 232, a Potent, Selective, and Orally Bioavailable MDM2–p53 Inhibitor in Clinical Development

(2014) Daqing Sun et al.   JOURNAL OF MEDICINAL CHEMISTRY