[HTML][HTML] Tyrosine kinase inhibitors for solid tumors in the past 20 years (2001–2020)

L Huang, S Jiang, Y Shi - Journal of hematology & oncology, 2020 - Springer
Tyrosine kinases are implicated in tumorigenesis and progression, and have emerged as
major targets for drug discovery. Tyrosine kinase inhibitors (TKIs) inhibit corresponding …

ROS1-dependent cancers—biology, diagnostics and therapeutics

A Drilon, C Jenkins, S Iyer, A Schoenfeld… - Nature reviews Clinical …, 2021 - nature.com
The proto-oncogene ROS1 encodes a receptor tyrosine kinase with an unknown
physiological role in humans. Somatic chromosomal fusions involving ROS1 produce …

Entrectinib in patients with advanced or metastatic NTRK fusion-positive solid tumours: integrated analysis of three phase 1–2 trials

RC Doebele, A Drilon, L Paz-Ares, S Siena… - The Lancet …, 2020 - thelancet.com
Background Entrectinib is a potent inhibitor of tropomyosin receptor kinase (TRK) A, B, and
C, which has been shown to have anti-tumour activity against NTRK gene fusion-positive …

The European MAPPYACTS trial: precision medicine program in pediatric and adolescent patients with recurrent malignancies

P Berlanga, G Pierron, L Lacroix, M Chicard… - Cancer discovery, 2022 - AACR
MAPPYACTS (NCT02613962) is an international prospective precision medicine trial
aiming to define tumor molecular profiles in pediatric patients with recurrent/refractory …

[HTML][HTML] TRK inhibitors in TRK fusion-positive cancers

A Drilon - Annals of Oncology, 2019 - Elsevier
TRK fusions are oncogenic drivers of various adult and paediatric cancers. The first-
generation TRK inhibitors, larotrectinib and entrectinib, were granted landmark, tumour …

Entrectinib: first global approval

ZT Al-Salama, SJ Keam - Drugs, 2019 - Springer
Entrectinib (Rozlytrek®) is an oral selective inhibitor of the tyrosine kinases tropomyosin
receptor kinases (Trk) A/B/C [encoded by the genes neurotrophic tyrosine receptor kinase …

Recent progress in the treatment of cancer in children

E Butler, K Ludwig, HL Pacenta… - CA: a cancer journal …, 2021 - Wiley Online Library
Although significant improvements have been made in the outcomes of children with cancer,
the pace of improvement has slowed in recent years as the limits of therapy intensification …

Updated Integrated Analysis of the Efficacy and Safety of Entrectinib in Patients With NTRK Fusion-Positive Solid Tumors

GD Demetri, F De Braud, A Drilon, S Siena… - Clinical Cancer …, 2022 - AACR
Purpose: Entrectinib potently inhibits tropomyosin receptor kinases (TRKAs)/B/C and ROS1,
and previously induced deep [objective response rate (ORR) 57.4%] and durable [median …

NTRK fusions identified in pediatric tumors: the frequency, fusion partners, and clinical outcome

X Zhao, C Kotch, E Fox, LF Surrey… - JCO precision …, 2021 - ascopubs.org
PURPOSE Neurotrophic tyrosine receptor kinase (NTRK) fusions have been described as
oncogenic drivers in a variety of tumors. However, little is known about the overall frequency …

Histology-agnostic drug development—considering issues beyond the tissue

RC Pestana, S Sen, BP Hobbs, DS Hong - Nature Reviews Clinical …, 2020 - nature.com
With advances in tumour biology and immunology that continue to refine our understanding
of cancer, therapies are now being developed to treat cancers on the basis of specific …