BYS10 / BaiYunShan Pharma - LARVOL DELTA

BYS10, a novel selective RET inhibitor, exhibits potent antitumor activity in preclinical models. (PubMed, Front Pharmacol) - "Collectively, BYS10 represents a novel, highly selective RET inhibitor with superior in vitro and in vivo activity against multiple RET alterations compared to Selpercatinib. Its recent Investigational New Drug (IND) approvals from the FDA and NMPA underscore its therapeutic potential for RET-driven malignancies."

Journal • Preclinical • Oncology • KIF5B • RET

BYS10, a novel selective RET inhibitor, exhibits potent antitumor activity in preclinical models (Front Immunol) - "In Ba/F3-KIF5B-RET-V804L xenograft model, BYS10 at 3 mg/kg achieved a TGI% of 94.67%, versus 79.48% for Selpercatinib(P < 0.05). In Ba/F3-KIF5B-RET G810R xenograft model, BYS10 at 10 mg/kg achieved a TGI% of 65.96%, versus 35.37% for Selpercatinib (P < 0.001). In Ba/F3-KIF5B-RET G810S xenograft model, BYS10 at 10 mg/kg achieved a TGI% of 112.59%, versus 82.15% for Selpercatinib (P < 0.001)."

Preclinical • Solid Tumor

Guangzhou Baiyunshan Pharmaceutical…announced that the Center for Drug Evaluation (CDE) of China’s...NMPA has provided feedback allowing the company to commence an open‑label, multicenter Phase I/II clinical trial of its selective RET small‑molecule inhibitor, BYS10 tablets (flcube.com) - "The trial will assess the safety, tolerability, pharmacokinetics, and efficacy of BYS10 in patients with advanced solid tumors harboring RET gene fusions or mutations."

New P1/2 trial • Solid Tumor

First-in-human phase I/II study of BYS10 in patients (pts) with locally advanced or metastatic RET-altered solid tumors: Preliminary dose escalation results. (ASCO 2025) - P1/2 | "BYS10 was well tolerated and showed dose-dependent exposure. Preliminary antitumor activity was observed in pts with RET-altered NSCLC, TC and MTC. The study is still ongoing."

Clinical • Metastases • P1/2 data • Endocrine Cancer • Hypertension • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Pain • Solid Tumor • Thyroid Gland Carcinoma • Thyroid Gland Medullary Carcinoma • KDR • RET