SYHA1815 / CSPC Pharma - LARVOL DELTA

RET Alterations in Thyroid Cancer: Molecular Mechanisms, Targeted Therapies, and Emerging Resistance. (PubMed, Crit Rev Oncol Hematol) - "Previously, multikinase inhibitors, such as vandetanib and cabozantinib, were primarily used for treatment; however, their efficacy was limited due to off-target effects. Recently, selective tyrosine kinase inhibitors, including selpercatinib and pralsetinib, have been introduced, demonstrating improved selectivity and clinical efficacy...To address this issue, next-generation RET inhibitors, including zeteletinib and SYHA1815, are currently under investigation, reflecting an expanding therapeutic landscape. This article provides an overview of the molecular mechanisms of RET alterations in thyroid cancer, targeted therapies, and emerging resistance to targeted treatment."

Journal • Review • Oncology • Solid Tumor • Thyroid Gland Carcinoma • Thyroid Gland Medullary Carcinoma • Thyroid Gland Papillary Carcinoma • RET

A Study to Investigate the Safety of SYHA1815 in Subjects With Unresectable Locally Advanced or Metastatic Solid Tumors (clinicaltrials.gov) - P1/2; N=97; Recruiting; Sponsor: Shanghai Runshi Pharmaceutical Technology Co., Ltd

Clinical • New P1/2 trial • Colorectal Cancer • Esophageal Cancer • Gastric Cancer • Gastrointestinal Cancer • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor • Thyroid Gland Carcinoma • CEACAM5 • FGF23 • FGFR • KDR • PD-L1

The novel RET inhibitor SYHA1815 inhibits RET-driven cancers and overcomes gatekeeper mutations by inducing G1 cell cycle arrest through c-Myc downregulation. (PubMed, Mol Cancer Ther) - "Notably, SYHA1815 exhibited approximately 20-fold selectivity for RET over KDR, almost equivalent to that of the launched selective inhibitor pralsetinib...Moreover, consistent with the marked in vivo efficacy of RET inhibition, the intratumoral c-Myc level was significantly decreased. In summary, SYHA1815 is a promising RETi for RET-aberrant cancer treatment that is currently in a phase I trial."

Journal • CNS Disorders • Oncology • Psychiatry • BRD4 • KDR • MYC • RET