FHND5071 / Sino Biopharm - LARVOL DELTA

Phase 1 Study of FHND5071, a Novel Selective RET Inhibitor, in RET Fusion–Positive Advanced NSCLC [WITHDRAWN] (ESMO 2025) - No abstract available

Metastases • P1 data • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor • RET

Phase 1 Study of FHND5071, a Novel Selective RET Inhibitor, in RET Fusion-Positive Advanced NSCLC (IASLC-WCLC 2025) - P1 | "In preclinical studies, FHND5071 exhibited significantly higher tumor and brain tissue exposure: the AUC0−t of FHND5071 in tumor tissue was approximately 28-time higher than that of selpercatinib, and its brain concentration was ~33-time higher at 4 hours post-dose. At baseline, 29% (14/48) had brain metastases and 77% (37/48) had received prior treatment. One enrolled patient did not receive study drug and was excluded from the intent-to-treat (ITT) population."

Metastases • P1 data • Brain Cancer • Lung Cancer • Non Small Cell Lung Cancer • Solid Tumor • RET

Design and Discovery of Novel Selective RET Inhibitors with High Central Nervous System Penetration, Enhanced Pharmacokinetics, and Pharmacodynamics. (PubMed, J Med Chem) - "Western blot analysis indicated that compound FHND5071 significantly inhibited the phosphorylation of RET and downstream molecules ERK and AKT in tumor tissues. Furthermore, compound FHND5071 markedly inhibited tumor growth, showing good in vivo efficacy and significant intracranial antitumor activity."

Journal • PK/PD data • Oncology • RET

Preclinical Pharmacokinetics and in vitro Metabolism of FHND5071, a Novel Selective RET Kinase Inhibitor. (PubMed, Eur J Drug Metab Pharmacokinet) - "Pharmacokinetic characteristics of FHND5071 were systemically profiled, which may lay the foundation for further clinical development as a drug candidate."

Journal • PK/PD data • Preclinical • Oncology • CYP3A4 • RET

FHND5071: a selective RET inhibitor with unique pharmacokinetic profile (AACR 2023) - "Selective RET inhibitors selpercatinib and pralsetinib have been approved for patients with RET-altered cancers. FHND5071 demonstrated excellent selectivity and anti-tumor efficacy. The unique pharmacokinetic profile of FHND5071 supported the frequency of once-a-day dosing and better efficacy in target organ and brain tumor in clinical. FHND5071 has received IND approval from NMPA and FDA."

Late-breaking abstract • PK/PD data • Brain Cancer • Colorectal Cancer • Gastrointestinal Cancer • Oncology • Ovarian Cancer • Solid Tumor • CCDC6 • KDR • KIF5B • NCOA4 • RET

A Study to Evaluate the Safety, Tolerability, Pharmacokinetics and Preliminary Evidence of Antitumor Activity of FHND5071 as a Single Agent in Adult Patients With Advanced Solid Tumors (clinicaltrials.gov) - P1 | N=80 | Enrolling by invitation | Sponsor: Jiangsu Chia Tai Fenghai Pharmaceutical Co., Ltd.

Metastases • New P1 trial • Oncology • Solid Tumor