Activation of MET via diverse exon 14 splicing alterations occurs in multiple tumor types and confers clinical sensitivity to MET inhibitors
…, J Chmielecki, X Lu, TM Bauer, M Akimov… - Cancer discovery, 2015 - AACR
Focal amplification and activating point mutation of the MET gene are well-characterized
oncogenic drivers that confer susceptibility to targeted MET inhibitors. Recurrent somatic splice …
oncogenic drivers that confer susceptibility to targeted MET inhibitors. Recurrent somatic splice …
[HTML][HTML] Capmatinib in MET Exon 14–Mutated or MET-Amplified Non–Small-Cell Lung Cancer
…, X Cui, M Giovannini, M Akimov… - … England Journal of …, 2020 - Mass Medical Soc
Background Among patients with non–small-cell lung cancer (NSCLC), MET exon 14
skipping mutations occur in 3 to 4% and MET amplifications occur in 1 to 6%. Capmatinib, a …
skipping mutations occur in 3 to 4% and MET amplifications occur in 1 to 6%. Capmatinib, a …
First-in-human phase I dose-escalation study of the HSP90 inhibitor AUY922 in patients with advanced solid tumors
…, T Pluard, TA Samuel, M Akimov… - Clinical Cancer …, 2013 - AACR
… range of 2 to 70 mg/m 2 . DLTs occurred in 8 patients (22–70 mg/m 2 ) and included diarrhea,
asthenia/fatigue, anorexia, atrial flutter, and visual symptoms. At 70 mg/m 2 , the AUY922 …
asthenia/fatigue, anorexia, atrial flutter, and visual symptoms. At 70 mg/m 2 , the AUY922 …
89Zr-trastuzumab and 89Zr-bevacizumab PET to Evaluate the Effect of the HSP90 Inhibitor NVP-AUY922 in Metastatic Breast Cancer Patients
…, AH Brouwers, AHH Bongaerts, M Akimov… - Clinical Cancer …, 2014 - AACR
… The actual cumulative administered doses of NVP-AUY922 were lower than planned:
951.2 mg/m 2 versus 1175.4 mg/m 2 . Eight patients required a dose reduction to 54 mg/m 2 . …
951.2 mg/m 2 versus 1175.4 mg/m 2 . Eight patients required a dose reduction to 54 mg/m 2 . …
[HTML][HTML] Molecular correlates of response to capmatinib in advanced non-small-cell lung cancer: clinical and biomarker results from a phase I trial
…, DS Hong, A Vogel, A Delmonte, M Akimov… - Annals of …, 2020 - Elsevier
Background Dysregulation of receptor tyrosine kinase MET by various mechanisms occurs
in 3%–4% of non-small-cell lung cancer (NSCLC) and is associated with unfavorable …
in 3%–4% of non-small-cell lung cancer (NSCLC) and is associated with unfavorable …
[HTML][HTML] Phase 2 Study of the HSP-90 Inhibitor AUY922 in previously treated and molecularly defined patients with advanced non–small cell lung cancer
…, K Park, E Avsar, S Szpakowski, M Akimov… - Journal of Thoracic …, 2018 - Elsevier
… , phase 1 dose-escalation study of AUY922, which was conducted in patients with advanced
solid tumors demonstrated acceptable tolerability at the recommended dose of 70 mg/m 2 . …
solid tumors demonstrated acceptable tolerability at the recommended dose of 70 mg/m 2 . …
Inhibition of HSP90 with AUY922 induces synergy in HER2-amplified trastuzumab-resistant breast and gastric cancer
…, R Ayala, NA O'Brien, C Quadt, M Akimov… - Molecular cancer …, 2013 - AACR
HSP90 enables the activation of many client proteins of which the most clinically validated
is HER2. NVP-AUY922, a potent HSP90 inhibitor, is currently in phase II clinical trials. To …
is HER2. NVP-AUY922, a potent HSP90 inhibitor, is currently in phase II clinical trials. To …
Phase 1 study of capmatinib in MET‐positive solid tumor patients: Dose escalation and expansion of selected cohorts
…, RTP Poon, D Hong, CC Lin, M Akimov… - Cancer …, 2020 - Wiley Online Library
Capmatinib is an oral, ATP‐competitive, and highly potent, type 1b MET inhibitor. Herein,
we report phase 1 dose‐escalation results for capmatinib in advanced MET‐positive solid …
we report phase 1 dose‐escalation results for capmatinib in advanced MET‐positive solid …
Phase (Ph) I study of the safety and efficacy of the cMET inhibitor capmatinib (INC280) in patients (pts) with advanced cMET+ non-small cell lung cancer (NSCLC).
…, A Krohn, Y Zhang, M Squires, M Giovannini, M Akimov… - 2016 - ascopubs.org
9067 Background: cMET dysregulation occurs in 3–10% of NSCLC and is a negative prognostic
factor. INC280 is a highly selective cMET inhibitor with preclinical and clinical antitumor …
factor. INC280 is a highly selective cMET inhibitor with preclinical and clinical antitumor …
Phase 1/1 B trial of the heat shock protein 90 inhibitor NVP‐AUY 922 as monotherapy or in combination with bortezomib in patients with relapsed or refractory multiple …
…, C Fernandez‐Ibarra, H Lu, S Pain, M Akimov… - Cancer, 2015 - Wiley Online Library
… -lives of 80 hours at 8 mg/m 2 and 116 hours at 70 mg/m 2 . The blood clearance and the …
of 384 L at 8 mg/m 2 to 11.0 L/h and 1666 L, respectively, at 70 mg/m 2 ). There was no drug …
of 384 L at 8 mg/m 2 to 11.0 L/h and 1666 L, respectively, at 70 mg/m 2 ). There was no drug …