SPH5030 / Shanghai Pharma - LARVOL DELTA

Development of a novel PET radiotracer for targeting HER2-expressing tumors (EANM 2025) - "In the second experiment on three different cell lines no difference was observed on MDA-MB-231 and 4T1 aspecific uptake. Conclusion Building on these findings, further studies are needed to better evaluate HER2 specificity of (R,Z)-[ 11 C]SPH5030 and (R,E)-[ 11 C]SPH5030 and to explore other derivatives that allow incorporation of Fluorine-18 or modulation of selectivity and binding reversibility."

Breast Cancer • HER2 Breast Cancer • HER2 Positive Breast Cancer • Oncology • Solid Tumor • HER-2

SPH5030 Tablets in Subjects With Advanced Her2-positive Solid Tumors (clinicaltrials.gov) - P1 | N=150 | Recruiting | Sponsor: Shanghai Pharmaceuticals Holding Co., Ltd | Trial completion date: Dec 2024 ➔ Dec 2025 | Trial primary completion date: Dec 2024 ➔ Dec 2025

Trial completion date • Trial primary completion date • Oncology • Solid Tumor • HER-2

SPH5030 Tablets in Subjects With Advanced Her2-positive Solid Tumors (clinicaltrials.gov) - P1 | N=150 | Recruiting | Sponsor: Shanghai Pharmaceuticals Holding Co., Ltd | N=114 ➔ 150

Enrollment change • Metastases • Oncology • Solid Tumor • HER-2

SPH5030 Tablets in Subjects With Advanced Her2-positive Solid Tumors (clinicaltrials.gov) - P1 | N=114 | Recruiting | Sponsor: Shanghai Pharmaceuticals Holding Co., Ltd | Trial completion date: Jun 2024 ➔ Dec 2024 | Trial primary completion date: Jun 2024 ➔ Dec 2024

Metastases • Trial completion date • Trial primary completion date • Oncology • Solid Tumor • HER-2

Unraveling the future: Innovative design strategies and emerging challenges in HER2-targeted tyrosine kinase inhibitors for cancer therapy. (PubMed, Eur J Med Chem) - "Currently, widely used clinical HER2 tyrosine kinase inhibitors (TKIs), such as lapatinib and neratinib, have several drawbacks, including susceptibility to drug resistance caused by HER2 mutations and adverse effects from insufficient HER2 selectivity...Typically, SPH5030 has advanced to phase I clinical trials for its strong suppression of four HER2 mutations. This review discusses the latest research progress in HER2 TKIs, with a focus on the structural optimization process and structure-activity relationship analysis. In particular, this study highlights promising design strategies to address these challenges, providing insightful information and inspiration for future development in this field."

Journal • Review • Breast Cancer • HER2 Breast Cancer • HER2 Positive Breast Cancer • Oncology • Solid Tumor • HER-2

SPH5030-201: A Clinical Study of SPH5030 Tablets in the Treatment of Her2-positive/Mutated Biliary Tract OR Colorectal Cancer Patients. (clinicaltrials.gov) - P2 | N=60 | Recruiting | Sponsor: Shanghai Pharmaceuticals Holding Co., Ltd | Not yet recruiting ➔ Recruiting

Enrollment open • Colorectal Cancer • Gastrointestinal Cancer • Oncology • Solid Tumor

Open-label, dose-escalation phase 1a study of SPH5030, a tyrosine kinase inhibitor (TKI) targeting HER2, in patients with HER2 positive advanced solid tumors. (ASCO 2024) - P1 | "SPH5030, is a novel tyrosine kinase inhibitor targeting HER2, with a modified structure from tucatinib and pyrotinib. This study demonstrated that SPH5030 was well tolerated at doses ranging from 50 to 600mg. A dose of 600 mg QD regimen could be considered for further clinical trials."

Clinical • Metastases • P1 data • Breast Cancer • Colorectal Cancer • Fatigue • Gastrointestinal Cancer • HER2 Breast Cancer • HER2 Positive Breast Cancer • Oncology • Solid Tumor • HER-2

A Clinical Study of SPH5030 Tablets in the Treatment of Her2-positive/Mutated Biliary Tract OR Colorectal Cancer Patients. (clinicaltrials.gov) - P2 | N=60 | Not yet recruiting | Sponsor: Shanghai Pharmaceuticals Holding Co., Ltd

New P2 trial • Colorectal Cancer • Gastrointestinal Cancer • Oncology • Solid Tumor

A Food Effect Study of SPH5030 Tablets. (clinicaltrials.gov) - P1 | N=16 | Completed | Sponsor: Shanghai Pharmaceuticals Holding Co., Ltd

New P1 trial • Oncology • Solid Tumor