[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 …

Small-molecule inhibitors, immune checkpoint inhibitors, and more: FDA-approved novel therapeutic drugs for solid tumors from 1991 to 2021

Q Wu, W Qian, X Sun, S Jiang - Journal of hematology & oncology, 2022 - Springer
Abstract The United States Food and Drug Administration (US FDA) has always been a
forerunner in drug evaluation and supervision. Over the past 31 years, 1050 drugs …

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 …

Pexidartinib: first approval

YN Lamb - Drugs, 2019 - Springer
Pexidartinib (TURALIO™) is an orally administered small molecule tyrosine kinase inhibitor
with selective activity against the colony-stimulating factor 1 (CSF1) receptor, KIT proto …

Gilteritinib, a FLT3/AXL inhibitor, shows antileukemic activity in mouse models of FLT3 mutated acute myeloid leukemia

M Mori, N Kaneko, Y Ueno, M Yamada… - Investigational new …, 2017 - Springer
Advances in the understanding of the molecular basis for acute myeloid leukemia (AML)
have generated new potential targets for treatment. Fms-like tyrosine kinase 3 (FLT3) is one …

Targeting gatekeeper mutations for kinase drug discovery

Y Zhou, S Xiang, F Yang, X Lu - Journal of medicinal chemistry, 2022 - ACS Publications
Clinically acquired resistance is a major challenge in cancer therapies with small-molecule
kinase inhibitors (SMKIs). Gatekeeper mutations in the ATP-binding pocket of kinases are …

Small molecule inhibitors targeting the cancers

GH Liu, T Chen, X Zhang, XL Ma, HS Shi - MedComm, 2022 - Wiley Online Library
Compared with traditional therapies, targeted therapy has merits in selectivity, efficacy, and
tolerability. Small molecule inhibitors are one of the primary targeted therapies for cancer …

Clinical resistance to crenolanib in acute myeloid leukemia due to diverse molecular mechanisms

H Zhang, S Savage, AR Schultz, D Bottomly… - Nature …, 2019 - nature.com
FLT3 mutations are prevalent in AML patients and confer poor prognosis. Crenolanib, a
potent type I pan-FLT3 inhibitor, is effective against both internal tandem duplications and …

FLT3 D835 mutations confer differential resistance to type II FLT3 inhibitors

CC Smith, K Lin, A Stecula, A Sali, NP Shah - Leukemia, 2015 - nature.com
Activating mutations in FLT3 occur in~ 30% of adult acute myeloid leukemia, primarily
consisting of internal tandem duplication (ITD) mutations (~ 25%) and point mutations in the …