An update on the nitrogen heterocycle compositions and properties of US FDA-approved pharmaceuticals (2013–2023)

CM Marshall, JG Federice, CN Bell… - Journal of Medicinal …, 2024 - ACS Publications
This Perspective is a continuation of our analysis of US FDA-approved small-molecule drugs
(1938–2012) containing nitrogen heterocycles. In this study we report drug structure and …

[HTML][HTML] Small molecules in targeted cancer therapy: advances, challenges, and future perspectives

L Zhong, Y Li, L Xiong, W Wang, M Wu… - Signal transduction and …, 2021 - nature.com
Due to the advantages in efficacy and safety compared with traditional chemotherapy drugs,
targeted therapeutic drugs have become mainstream cancer treatments. Since the first …

Quizartinib plus chemotherapy in newly diagnosed patients with FLT3-internal-tandem-duplication-positive acute myeloid leukaemia (QuANTUM-First): a randomised …

HP Erba, P Montesinos, HJ Kim, E Patkowska… - The Lancet, 2023 - thelancet.com
Background Patients with acute myeloid leukaemia (AML) positive for internal tandem
duplication (ITD) mutations of FLT3 have poor outcomes. Quizartinib, an oral, highly potent …

Targeting FLT3 mutations in AML: review of current knowledge and evidence

N Daver, RF Schlenk, NH Russell, MJ Levis - Leukemia, 2019 - nature.com
Genomic investigations of acute myeloid leukemia (AML) have demonstrated that several
genes are recurrently mutated, leading to new genomic classifications, predictive …

Proteolysis-targeting chimeras as therapeutics and tools for biological discovery

GM Burslem, CM Crews - Cell, 2020 - cell.com
New biological tools provide new techniques to probe fundamental biological processes.
Here we describe the burgeoning field of proteolysis-targeting chimeras (PROTACs), which …

Quizartinib versus salvage chemotherapy in relapsed or refractory FLT3-ITD acute myeloid leukaemia (QuANTUM-R): a multicentre, randomised, controlled, open …

JE Cortes, S Khaled, G Martinelli, AE Perl… - The Lancet …, 2019 - thelancet.com
Background Patients with relapsed or refractory FLT3 internal tandem duplication (FLT3-
ITD)-positive acute myeloid leukaemia have a poor prognosis, including high frequency of …

Clonal selection with RAS pathway activation mediates secondary clinical resistance to selective FLT3 inhibition in acute myeloid leukemia

CM McMahon, T Ferng, J Canaani, ES Wang… - Cancer discovery, 2019 - AACR
Gilteritinib is a potent and selective FLT3 kinase inhibitor with single-agent clinical efficacy in
relapsed/refractory FLT3-mutated acute myeloid leukemia (AML). In this context, however …

PROTAC'ing oncoproteins: targeted protein degradation for cancer therapy

JM Kelm, DS Pandey, E Malin, H Kansou, S Arora… - Molecular Cancer, 2023 - Springer
Molecularly targeted cancer therapies substantially improve patient outcomes, although the
durability of their effectiveness can be limited. Resistance to these therapies is often related …

A review of FLT3 inhibitors in acute myeloid leukemia

JC Zhao, S Agarwal, H Ahmad, K Amin, JP Bewersdorf… - Blood reviews, 2022 - Elsevier
FLT3 mutations are the most common genetic aberrations found in acute myeloid leukemia
(AML) and associated with poor prognosis. Since the discovery of FLT3 mutations and their …

FLT3 Mutations in Acute Myeloid Leukemia: Key Concepts and Emerging Controversies

VE Kennedy, CC Smith - Frontiers in Oncology, 2020 - frontiersin.org
The FLT3 receptor is overexpressed on the majority of acute myeloid leukemia (AML) blasts.
Mutations in FLT3 are the most common genetic alteration in AML, identified in …