Phase 1 dose escalation and cohort expansion study evaluating safety, PK, PD and clinical activity of STC-15, a METTL-3 inhibitor, in patients with advanced …

JC Moser, KP Papadopoulos, J Rodon Ahnert… - 2024 - ascopubs.org
2586 Background: RNA modifications are involved in cancer initiation and progression. The
most abundant modification of mRNA is m6A generated by METTL3. Inhibition of METTL3 …

[HTML][HTML] Phase 1 Study of the Selective c-MET Inhibitor, HS-10241, in Patients With Advanced Solid Tumors

X Dong, X Li, J Chen, S Ma, D Mu, J Hu, S Lu - JTO Clinical and Research …, 2023 - Elsevier
Introduction c-MET is an important therapeutic target for various cancers; however, the
People's Republic of China currently retails only one specific c-MET inhibitor. Our preclinical …

Abstract C077: STC-15, a small molecule inhibitor of the RNA methyltransferase METTL3, activates anti-tumor immunity and reshapes the tumor microenvironment

Y Ofir-Rosenfeld, L Vasiliauskaitė, J Obacz… - Molecular Cancer …, 2023 - AACR
Background METTL3 is the RNA methyltransferase responsible for the deposition of N-6-
methyladenosine modification (m6A) on mRNA, to regulate its stability, splicing and protein …

[HTML][HTML] A first-in-human study of AMG 208, an oral MET inhibitor, in adult patients with advanced solid tumors

DS Hong, P Rosen, AC Lockhart, S Fu, F Janku… - Oncotarget, 2015 - ncbi.nlm.nih.gov
Background This first-in-human study evaluated AMG 208, a small-molecule MET inhibitor,
in patients with advanced solid tumors. Methods Three to nine patients were enrolled into …

[PDF][PDF] STC-15, a small molecule inhibitor of the RNA methyltransferase METTL3, activates anti-tumor immunity and reshapes the tumor microenvironment

Y Ofir-Rosenfeld, L Vasiliauskaite… - MOLECULAR …, 2023 - stormtherapeutics.com
Summary References 1. Yankova et al. Small-molecule inhibition of METTL3 as a strategy
against myeloid leukaemia. Nature. 2021; 593 (7860): 597-601 2. Guirguis, Ofir-Rosenfeld …

Preclinical characterization and phase I clinical trial of CT053PTSA targets MET, AXL, and VEGFR2 in patients with advanced solid tumors

YX Ma, FR Liu, Y Zhang, Q Chen, ZQ Chen… - Frontiers in …, 2022 - frontiersin.org
Background CT053PTSA is a novel tyrosine kinase inhibitor that targets MET, AXL,
VEGFR2, FLT3 and MERTK. Here, we present preclinical data about CT053PTSA, and we …

STC-15, an oral small molecule inhibitor of the RNA methyltransferase METTL3, inhibits tumour growth through activation of anti-cancer immune responses …

Y Ofir-Rosenfeld, L Vasiliauskaitė… - European Journal of …, 2022 - ejcancer.com
Background: METTL3 is an RNA methyltransferase responsible for the deposition of N-6-
methyladenosine (m 6 A) modification on mRNA and long non-coding RNA (lncRNA) …

A first-in-human phase I/Ib study of receptor tyrosine kinase (RTK) inhibitor, MGCD516, in patients with advanced solid tumors.

GK Schwartz, D Adkins, RS Heist, M Abbott, SL Barber… - 2015 - ascopubs.org
TPS2621 Background: MGCD516, is an orally-available, potent small molecule inhibitor of a
closely related family of RTKs including RET, TRK family, DDR2, MET, Axl family, KIT, as …

[HTML][HTML] First-in-human phase I trial assessing the highly selective c-Met inhibitor MSC2156119J (EMD 1214063) in patients with advanced solid tumors

GS Falchook, DS Hong, HM Amin, S Fu, SA Piha-Paul… - Annals of …, 2014 - Elsevier
Aim: c-Met overexpression is associated with poor clinical prognosis. This dose-escalation
study (3+ 3 design; NCT01014936) evaluates the selective c-Met inhibitor MSC2156119J in …

Results of the first-in-human phase I trial assessing MSC2156119J (EMD 1214063), an oral selective c-Met inhibitor, in patients (pts) with advanced solid tumors.

GS Falchook, DS Hong, HM Amin, S Fu, SA Piha-Paul… - 2014 - ascopubs.org
2521^ Background: MSC2156119J, a selective c-Met inhibitor, suppresses tumor growth in
preclinical models. Methods: Primary endpoint of this dose-escalation study (3+ 3 design; …