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 …

Past, present, and future of Bcr-Abl inhibitors: from chemical development to clinical efficacy

F Rossari, F Minutolo, E Orciuolo - Journal of hematology & oncology, 2018 - Springer
Bcr-Abl inhibitors paved the way of targeted therapy epoch. Imatinib was the first tyrosine
kinase inhibitor to be discovered with high specificity for Bcr-Abl protein resulting from t (9 …

Chronic myeloid leukemia, version 2.2021, NCCN clinical practice guidelines in oncology

MW Deininger, NP Shah, JK Altman, E Berman… - Journal of the National …, 2020 - jnccn.org
Chronic myeloid leukemia (CML) is defined by the presence of Philadelphia chromosome
(Ph) which results from a reciprocal translocation between chromosomes 9 and 22 [t (9; 22] …

Complete hematologic and molecular response in adult patients with relapsed/refractory Philadelphia chromosome–positive B-precursor acute lymphoblastic …

G Martinelli, N Boissel, P Chevallier… - Journal of Clinical …, 2017 - ascopubs.org
Purpose Few therapeutic options are available for patients with Philadelphia chromosome–
positive (Ph+) B-precursor acute lymphoblastic leukemia (ALL) who progress after failure of …

European LeukemiaNet laboratory recommendations for the diagnosis and management of chronic myeloid leukemia

NCP Cross, T Ernst, S Branford, JM Cayuela… - Leukemia, 2023 - nature.com
From the laboratory perspective, effective management of patients with chronic myeloid
leukemia (CML) requires accurate diagnosis, assessment of prognostic markers, sequential …

Chronic myeloid leukemia, version 1.2019, NCCN clinical practice guidelines in oncology

JP Radich, M Deininger, CN Abboud, JK Altman… - Journal of the National …, 2018 - jnccn.org
Chronic myeloid leukemia (CML) is defined by the presence of Philadelphia chromosome
(Ph), resulting from a reciprocal translocation between chromosomes 9 and 22 [t (9; 22] that …

The potent ALK inhibitor brigatinib (AP26113) overcomes mechanisms of resistance to first-and second-generation ALK inhibitors in preclinical models

S Zhang, R Anjum, R Squillace, S Nadworny… - Clinical Cancer …, 2016 - AACR
Purpose: Non–small cell lung cancers (NSCLCs) harboring ALK gene rearrangements
(ALK+) typically become resistant to the first-generation anaplastic lymphoma kinase (ALK) …

Ponatinib efficacy and safety in Philadelphia chromosome–positive leukemia: final 5-year results of the phase 2 PACE trial

JE Cortes, DW Kim, J Pinilla-Ibarz… - Blood, The Journal …, 2018 - ashpublications.org
Ponatinib has potent activity against native and mutant BCR-ABL1, including BCR-
ABL1T315I. The pivotal phase 2 Ponatinib Ph+ ALL and CML Evaluation (PACE) trial …

Ponatinib: a novel multi-tyrosine kinase inhibitor against human malignancies

FH Tan, TL Putoczki, SS Stylli… - OncoTargets and therapy, 2019 - Taylor & Francis
Human malignancies are often the result of overexpressed and constitutively active receptor
and non-receptor tyrosine kinases, which ultimately lead to the mediation of key tumor …

Combining the allosteric inhibitor asciminib with ponatinib suppresses emergence of and restores efficacy against highly resistant BCR-ABL1 mutants

CA Eide, MS Zabriskie, SLS Stevens, O Antelope… - Cancer Cell, 2019 - cell.com
BCR-ABL1 point mutation-mediated resistance to tyrosine kinase inhibitor (TKI) therapy in
Philadelphia chromosome-positive (Ph+) leukemia is effectively managed with several …