Publications by authors named "WeiGuo Su"

Introduction: Amdizalisib (HMPL-689) is an ATP-competitive PI3Kδ inhibitor currently under investigation for treating Hodgkin's lymphoma. This study aimed to evaluate the metabolism, excretion, pharmacokinetics, and safety profile of amdizalisib in healthy human subjects to support its clinical application.

Methods: This Phase I clinical trial included six healthy Chinese male volunteers who received a single oral dose of 30 mg/100 µCi [C]amdizalisib suspension.

View Article and Find Full Text PDF

Enhancing the hemostatic efficacy and minimizing blood loss in the body has consistently been a primary objective for researchers. This study improved the hemostatic efficacy and tissue adhesion strength of the hemostatic material by augmenting the aldehyde groups in the side chains of sodium alginate. Additionally, it immobilized the aldehyde-modified sodium alginate onto the surface of the hemostatic material through complexation with iron ions, thereby enhancing its antibacterial properties.

View Article and Find Full Text PDF
Article Synopsis
  • Savolitinib has been approved in China for treating advanced non-small-cell lung cancer (NSCLC) with specific genetic mutations, particularly in patients who haven't had prior treatments or can't undergo platinum-based chemotherapy.
  • A phase 3b study evaluated the drug's safety and effectiveness in treatment-naive patients with these mutations across 48 hospitals in China, administering different dosages based on patient weight.
  • Results showed a promising objective response rate of 62% based on independent assessments, with the majority of patients experiencing some treatment-related side effects, the most common being peripheral edema.
View Article and Find Full Text PDF

Refractory bleeding presents a critical, life-threatening challenge, and the goal of medical professionals and researchers has always been to achieve safe and effective hemostasis for bleeding wounds. In this study, we utilized the benefits of a self-expanding cellulose sponge to control incompressible bleeding, which is achieved this by creating a tannic acid/metal ion coating on the surface and within the pores of the sponge to improve its hemostatic effectiveness. The effects of various types and concentrations of metal ions (calcium, magnesium, iron, and zinc) on hemostatic efficiency and biosafety is systematically investigated.

View Article and Find Full Text PDF

Amdizalisib, also named HMPL-689, a novel selective and potent PI3Kδ inhibitor, is currently under Phase II clinical development in China for treating hematological malignancies. The preclinical pharmacokinetics (PK) of amdizalisib were extensively characterized and to support the further development of amdizalisib. We characterized the plasma protein binding, blood-to-plasma partition ratio, cell permeability, hepatic microsomal metabolic stability, and drug-drug interaction potential of amdizalisib using experiments.

View Article and Find Full Text PDF
Article Synopsis
  • Sovleplenib, a new SYK inhibitor, showed effective results and safety in treating patients with chronic primary immune thrombocytopenia in a phase 3 trial conducted in China.
  • The trial involved 188 participants who were given either sovleplenib or a placebo, with results showing a significant durable response rate of 48% for sovleplenib compared to 0% for the placebo group.
  • The study demonstrated a faster median time to response of 8 days for patients on sovleplenib versus 30 days for those receiving placebo, highlighting its potential efficacy in this condition.
View Article and Find Full Text PDF
Article Synopsis
  • * Results showed a significant improvement in progression-free survival (PFS) for those receiving fruquintinib (5.6 months) compared to the placebo group (2.7 months), but overall survival (OS) was not significantly different between the two groups (9.6 months vs. 8.4 months).
  • * The most common serious side effects of the treatment included neutropenia, leukopenia, and anemia, suggesting that while fruquintinib can extend
View Article and Find Full Text PDF

Herein we describe the medicinal chemistry efforts that led to the discovery of the clinical-staged Syk inhibitor sovleplenib () via a structure-activity relationship investigation and pharmacokinetics (PK) optimization of a pyrido[3,4-]pyrazine scaffold. Sovleplenib is a potent and selective Syk inhibitor with favorable preclinical PK profiles and robust anti-inflammation efficacy in a preclinical collagen-induced arthritis model. Sovleplenib is now being developed for treating autoimmune diseases such as immune thrombocytopenic purpura and warm antibody hemolytic anemia as well as hematological malignancies.

View Article and Find Full Text PDF
Article Synopsis
  • A phase I study in China assessed the combination of toripalimab, a programmed death 1 inhibitor, and surufatinib, an angio-immuno kinase inhibitor, for patients with advanced solid tumors that had not responded to standard treatments.
  • The study involved 60 patients across three cohorts (gastric/gastroesophageal junction adenocarcinoma, esophageal squamous cell carcinoma, and biliary tract carcinoma), reporting objective response rates of 31.6%, 30.0%, and 11.1%, respectively.
  • Preliminary results suggest that this combination therapy has promising anti-tumor effects and an acceptable safety profile, indicating the need for further research in larger clinical trials.
View Article and Find Full Text PDF
Article Synopsis
  • - Fruquintinib is a treatment approved in China for metastatic colorectal cancer patients who have progressed after two rounds of chemotherapy, and a postmarketing study assessed its safety among these and other patients with solid tumors.
  • - The study included 3005 patients who started treatment between April 2019 and September 2022, with a median age of 60, finding that most began with a 5 mg dose and had a median treatment duration of 2.7 months.
  • - Results showed that 20.8% of patients had treatment-related side effects that required dose adjustments, while 15.6% had to stop treatment; however, the overall safety profile was similar to clinical trials and was considered manageable for
View Article and Find Full Text PDF
Article Synopsis
  • A phase II study in China investigated the combination therapy of surufatinib and toripalimab in patients with advanced neuroendocrine tumors (NETs) and neuroendocrine carcinomas (NECs) who had not responded to standard treatments.
  • Forty patients participated, with objective response rates of 21.1% for NETs and 23.8% for NECs/MiNENs; the median duration of response was approximately 7.1 months for NETs and 4.1 months for NECs/MiNENs.
  • The treatment showed antitumor activity with a tolerable safety profile, prompting further research into this combination for advanced NECs, which
View Article and Find Full Text PDF
Article Synopsis
  • - Sovleplenib (HMPL-523) is an experimental drug designed to target and inhibit spleen tyrosine kinase (Syk), showing potential effectiveness against B-cell cancers in early research.
  • - A Phase I clinical trial was conducted with 134 patients suffering from relapsed or refractory B-cell tumors, exploring different dosages of the drug (200-800 mg daily); the recommended phase II dose was established at 600 mg for heavier patients and 400 mg for lighter ones.
  • - The study found a 50.8% objective response rate in a subset of patients with indolent B-cell lymphoma, while some patients reported severe side effects, but overall, sovleplenib demonstrated promising anti-t
View Article and Find Full Text PDF

Objective: Currently, pre-treatment prediction of patients with pancreatic neuroendocrine tumors with liver metastases (PNELM) receiving surufatinib treatment was unsatisfying. Our objective was to examine the association between radiological characteristics and efficacy/prognosis.

Methods: We enrolled patients with liver metastases in the phase III, SANET-p trial (NCT02589821) and obtained contrast-enhanced computed tomography (CECT) images.

View Article and Find Full Text PDF

Spleen tyrosine kinase (Syk) is an intracellular tyrosine kinase involved in the signal transduction in immune cells mainly. Its aberrant regulation is associated with diversified allergic disorders, autoimmune diseases and B cell malignancies. Therefore, inhibition of Syk is considered a reasonable approach to treat autoimmune/inflammatory diseases and B cell malignancies.

View Article and Find Full Text PDF

Background: Spleen tyrosine kinase (Syk) inhibitor is a treatment option for primary immune thrombocytopenia. We aimed to evaluate the safety, tolerability, pharmacokinetics, preliminary activity, and recommended phase 2 dose of sovleplenib in patients with primary immune thrombocytopenia.

Methods: This randomised, double-blind, placebo-controlled, phase 1b/2 study was conducted at nine hospitals in China.

View Article and Find Full Text PDF
Article Synopsis
  • - This study explored the combination of fruquintinib and sintilimab in patients with advanced solid tumors, particularly focusing on metastatic colorectal cancer (mCRC), showing that the combination is more effective than using either drug alone in preclinical settings.
  • - The research was a multi-center clinical trial that measured safety, tolerability, and early effectiveness, enrolling a total of 60 patients, with some experiencing serious side effects largely related to treatment.
  • - Results indicated that the combination therapy had a 23.8% response rate in mCRC patients, with median progression-free survival of 6.9 months and overall survival of 14.8 months, suggesting a positive trend in treatment efficacy.
View Article and Find Full Text PDF

Background: Savolitinib, a selective MET inhibitor, showed efficacy in patients with non-small cell lung cancer (NSCLC), including pulmonary sarcomatoid carcinoma (PSC), harbouring exon 14 skipping alteration (ex14).

Objective: To analyse , the association between circulating tumour DNA (ctDNA) biomarkers and clinical outcomes, including resistance, with savolitinib.

Design: A multicentre, single-arm, open-label phase 2 study.

View Article and Find Full Text PDF

Introduction: Savolitinib has been found to have encouraging antitumor activity and a favorable safety profile in Chinese patients with pulmonary sarcomatoid carcinoma and other NSCLCs with exon 14 skipping alterations ( ex14 positive) at the primary analysis of a phase 2 study. Here, we present the long-term efficacy and safety data of savolitinib, including subgroup analyses.

Methods: This multicenter, single-arm, open-label, phase 2 study in the People's Republic of China enrolled MET inhibitor-naive adults with locally advanced or metastatic ex14-positive NSCLC (NCT02897479).

View Article and Find Full Text PDF

The mechanical properties of epoxy resin can be enhanced by adding nanofillers into its matrix. This study researches and compares the impacts of adding nanofillers with different dimensions, including two-dimensional boron nitride and zero-dimensional silica, on the mechanical and toughness properties of epoxy resin. At low fractions (0-2.

View Article and Find Full Text PDF

Adipose-derived stem cells (ADSCs) are stem cells with multidirectional differentiation potential isolated from adipose tissue. They have the same immunomodulatory effect as bone marrow mesenchymal stem cells in wound repair and immune regulation as bone marrow. The mechanism of action of ADSCs in skin wound repair has not been elucidated.

View Article and Find Full Text PDF

Background: Non-small-cell lung cancer (NSCLC) had poor prognosis in patients with brain metastasis. The trial evaluated the safety and efficacy of epitinib (HMPL-813), an epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKI), for EGFR-mutant NSCLC with brain metastasis.

Patients And Methods: This open-label, dose-expansion phase Ib study (ClinicalTrials.

View Article and Find Full Text PDF

Aim: To investigate the health-related quality of life (HRQoL) of patients who had neuroendocrine tumors (NETs) from SANET trials.

Methods: Eligible patients were randomized in a 2:1 ratio to receive surufatinib or placebo. HRQoL questionnaires, including the European Organization for Research and Treatment of Cancer QLQ-C30 and QLQ-G.

View Article and Find Full Text PDF

Background: Savolitinib has shown good tolerability and preliminary efficacy, but efficacy biomarkers require investigation. The main purpose of this study was to confirm in Chinese patients the recommended phase II dose (RP2D) of savolitinib and to explore overall benefit in tumors bearing c-Met aberration.

Methods: This was an open-label, multi-center, 2-part phase I study.

View Article and Find Full Text PDF