Recent advances of SHP2 inhibitors in cancer therapy: current development and clinical application

X Yuan, H Bu, J Zhou, CY Yang… - Journal of medicinal …, 2020 - ACS Publications
… of SHP2 mRNA is significantly increased in many primary leukemia specimens. The expression
of SHP2 and SHP2 mRNA in the leukemia patients … as a single agent for patients with …

Abstract LB001: Anti-tumor activity and tolerability of the SHP2 inhibitor RMC-4630 as a single agent in patients with RAS-addicted solid cancers

M Koczywas, E Haura, PA Janne, JM Pacheco… - Cancer Research, 2021 - AACR
… , orally bioavailable allosteric inhibitor of SHP2, a central node … A total of 104 patients were
dosed across three schedules: … Of the 80 efficacy evaluable patients, there was 1 CR (NF1 …

SHP2 inhibition prevents adaptive resistance to MEK inhibitors in multiple cancer models

C Fedele, H Ran, B Diskin, W Wei, J Jen, MJ Geer… - Cancer discovery, 2018 - AACR
… Significance: MEK inhibitors show limited efficacy as single agents, in part because of the
rapid development of adaptive resistance. We find that SHP2/MEK inhibitor combinations …

Initial results from a dose finding study of TNO155, a SHP2 inhibitor, in adults with advanced solid tumors.

I Brana, G Shapiro, ML Johnson, HA Yu, D Robbrecht… - 2021 - ascopubs.org
… Here we present data from TNO155 single agent escalation. Results: As of 10/26/2020,
118 patients received TNO155 in variable schedules: once (QD; 1.5–70 mg; n = 55) or twice …

[HTML][HTML] Strategies to overcome drug resistance using SHP2 inhibitors

M Liu, S Gao, RM Elhassan, X Hou, H Fang - Acta Pharmaceutica Sinica B, 2021 - Elsevier
… the single agents. The results showed that combining two different but compatible SHP2
inhibitors (dual allosteric inhibitors) … that patients who are resistant to most kinase inhibitors have …

SHP2 inhibition sensitizes diverse oncogene-addicted solid tumors to re-treatment with targeted therapy

A Drilon, MR Sharma, ML Johnson, TA Yap, S Gadgeel… - Cancer discovery, 2023 - AACR
… As opposed to treating patients with a SHP2 inhibitor alone in dose escalation, each patient
with an oncogene-driven cancer was permitted the addition of matched targeted therapy …

SHP2 Inhibition as a Promising Anti-cancer Therapy: Function in Tumor Cell Signaling and Immune Modulation

J Wang, L Zhang, CA Pratilas… - Journal of Cancer …, 2021 - scientificarchives.com
single-patient case reports describing anti-tumor response to immune checkpoint inhibition
in patients with MPNST: 1) a patient … Multiple clinical trials of SHP2 inhibitors as single agents

A12 the SHP2 inhibitor RMC-4630 in patients with KRAS-mutant non-small cell lung cancer: preliminary evaluation of a first-in-man phase 1 clinical trial

SI Ou, M Koczywas, S Ulahannan, P Janne… - Journal of Thoracic …, 2020 - jto.org
… in patients with NSCLC harboring KRAS mutations. RMC-4630 continues to be tested as a
single agent in patients … This study is also open to patients with KRASG12C NSCLC who are …

NRAS Status Determines Sensitivity to SHP2 Inhibitor Combination Therapies Targeting the RAS–MAPK Pathway in Neuroblastoma

I Valencia-Sama, Y Ladumor, L Kee, T Adderley… - Cancer Research, 2020 - AACR
… of patients. Therefore, we investigated whether combination with SHP2 inhibitors could
enhance MAPK inhibitor … , treatment with SHP2 inhibitors as a single agent might be an effective …

Combinations with allosteric SHP2 inhibitor TNO155 to block receptor tyrosine kinase signaling

C Liu, H Lu, H Wang, A Loo, X Zhang, G Yang… - Clinical Cancer …, 2021 - AACR
SHP2 inhibitors is not expected to be affected by the EGFR T790M and C797S mutations,
even if they cooccur on the same DNA strand (in cis) as seen in some patientssingle agents at …