Small molecule kinase inhibitor drugs (1995–2021): medical indication, pharmacology, and synthesis

CC Ayala-Aguilera, T Valero… - Journal of Medicinal …, 2021 - ACS Publications
The central role of dysregulated kinase activity in the etiology of progressive disorders,
including cancer, has fostered incremental efforts on drug discovery programs over the past …

Response and resistance to BCR-ABL1-targeted therapies

TP Braun, CA Eide, BJ Druker - Cancer cell, 2020 - cell.com
Chronic myeloid leukemia (CML), caused by constitutively active BCR-ABL1 fusion tyrosine
kinase, has served as a paradigm for successful application of molecularly targeted cancer …

Long-term outcomes with frontline nilotinib versus imatinib in newly diagnosed chronic myeloid leukemia in chronic phase: ENESTnd 10-year analysis

HM Kantarjian, TP Hughes, RA Larson, DW Kim… - Leukemia, 2021 - nature.com
In the ENESTnd study, with≥ 10 years follow-up in patients with newly diagnosed chronic
myeloid leukemia (CML) in chronic phase, nilotinib demonstrated higher cumulative …

Adverse effects of tyrosine kinase inhibitors in cancer therapy: pathophysiology, mechanisms and clinical management

S Shyam Sunder, UC Sharma… - Signal Transduction and …, 2023 - nature.com
Since their invention in the early 2000s, tyrosine kinase inhibitors (TKIs) have gained
prominence as the most effective pathway-directed anti-cancer agents. TKIs have shown …

Long-term outcomes of imatinib treatment for chronic myeloid leukemia

A Hochhaus, RA Larson, F Guilhot… - … England Journal of …, 2017 - Mass Medical Soc
Background Imatinib, a selective BCR-ABL1 kinase inhibitor, improved the prognosis for
patients with chronic myeloid leukemia (CML). We conducted efficacy and safety analyses …

Prospects for combining targeted and conventional cancer therapy with immunotherapy

P Gotwals, S Cameron, D Cipolletta… - Nature Reviews …, 2017 - nature.com
Over the past 25 years, research in cancer therapeutics has largely focused on two distinct
lines of enquiry. In one approach, efforts to understand the underlying cell-autonomous …

The emerging clinical relevance of genomics in cancer medicine

MF Berger, ER Mardis - Nature reviews Clinical oncology, 2018 - nature.com
The combination of next-generation sequencing and advanced computational data analysis
approaches has revolutionized our understanding of the genomic underpinnings of cancer …

Chronic myeloid leukemia: 2018 update on diagnosis, therapy and monitoring

E Jabbour, H Kantarjian - American journal of hematology, 2018 - Wiley Online Library
Disease overview Chronic myeloid leukemia (CML) is a myeloproliferative neoplasm with an
incidence of 1‐2 cases per 100 000 adults. It accounts for approximately 15% of newly …

Long-term benefits and risks of frontline nilotinib vs imatinib for chronic myeloid leukemia in chronic phase: 5-year update of the randomized ENESTnd trial

A Hochhaus, G Saglio, TP Hughes, RA Larson… - Leukemia, 2016 - nature.com
Abstract In the phase 3 Evaluating Nilotinib Efficacy and Safety in Clinical Trials–Newly
Diagnosed Patients (ENESTnd) study, nilotinib resulted in earlier and higher response rates …

Cardiovascular toxic effects of targeted cancer therapies

JJ Moslehi - New England Journal of Medicine, 2016 - Mass Medical Soc
Cardiovascular Toxic Effects of Targeted Cancer Therapies | New England Journal of Medicine
Skip to main content Access provided byUT MD ANDERSON CANCER CENTER The New …