P2, N=100, Recruiting, Fudan University | Not yet recruiting --> Recruiting

P1/2, N=222, Recruiting, Suzhou Zelgen Biopharmaceuticals Co.,Ltd | Trial primary completion date: Nov 2024 --> Nov 2025

P1, N=21, Completed, AffaMed Therapeutics Limited | Recruiting --> Completed | Trial completion date: Jun 2024 --> Nov 2024 | Trial primary completion date: Jun 2024 --> Nov 2024

No abstract available

No abstract available

No abstract available

All the target compounds were evaluated against CAIX enzyme compared to dorzolamide and acetazolamide, subsequently the most potent CAIX inhibitors (3a, 3b, 3o, 6d, 6g, and 6i) were selected to evaluate their inhibitory activity against VEGFR-2 using sorafenib as a reference drug. Physicochemical predictions were examined using in silico techniques. In conclusion, these scaffolds present promising leads and furnish promising chemical backbones for the design of potent dual CAIX and VEGFR-2 inhibitors.b.

A novel peptide with improved affinity (KD = 6.2 µM) compared to mini-Z-1 (KD = 9.3 µM) was found, requiring only one round of design and testing. The integration of ProteinMPNN and Rosetta enabled a rapid and cost-effective pipeline for designing potent VEGFA inhibitors, underscoring the potential of computational peptide design in developing next-generation therapeutics targeting angiogenesis-dependent diseases.

P2, N=120, Not yet recruiting, Tasly Biopharmaceuticals Co., Ltd.

P1, N=35, Active, not recruiting, AP Biosciences Inc.

P=N/A, N=21, Recruiting, Beijing Anlong Biopharmaceutical Co., Ltd.

P2, N=50, Recruiting, Hubei Cancer Hospital | Not yet recruiting --> Recruiting

P1/2, N=44, Recruiting, Chengdu Origen Biotechnology Co., Ltd. | Not yet recruiting --> Recruiting

The results of an in vitro enzymatic study were augmented by molecular docking (in silico) analysis. Their ADME (absorption, distribution, metabolism and excretion) properties have been evaluated on the most active compounds against α-glucosidase and/or α-amylase to predict their drug likeness.

P1/2, N=21, Active, not recruiting, Beijing Anlong Biopharmaceutical Co., Ltd.

P=N/A, N=50, Not yet recruiting, Guiping People's Hospital

This case demonstrates the efficacy of envafolimab combined with endostar in the treatment of advanced NSCLC. This regimen enhances treatment safety and patient compliance, potentially offering a novel therapeutic option for patients with advanced NSCLC characterized by low PD-L1 expression and negative driver gene mutations.

The docking study showed that compounds 22 and 29 had docking scores similar to those of Erlotinib and Sorafenib, co-crystallized ligands, for the EGFR and VEGFR-2 proteins. The experiments on lipophilicity showed that the new pyrimidines had a consistent result. This group of compounds has better biological activity in all the biological systems studied with low lipophilicity.

Compound 16c boosted the level of the apoptotic caspase-3 and inhibited the level of TNF-α and IL-6 in tumor cells. Molecular docking and molecular dynamics (MD) simulations indicated the outstanding binding potential of compound 16c against VEGFR-2. Compound 16c is a good candidate for the creation of a novel antiangiogenic lead anticancer medication.

P3, N=510, Recruiting, Akeso | Not yet recruiting --> Recruiting

P2, N=150, Not yet recruiting, Akeso

P2, N=55, Not yet recruiting, Sun Yat-sen University

P=N/A, N=900, Completed, Shanghai General Hospital; Shanghai General Hospital, Shanghai Jiao Tong University School of Medicine

P=N/A, N=60, Recruiting, Guangdong Provincial Hospital of Chinese Medicine; Guangdong Provincial Hospital of Chinese Medicine

P4, N=120, Completed, The Second Affiliated Hospital of Harbin Medical University; The Second Affiliated Hospital of Harbin Medical University

P4, N=308, Not yet recruiting, Zhongshan Ophthalmic Center, Sun Yat-sen University; Zhongshan Ophthalmic Center, Sun Yat-sen University

P2, N=25, Recruiting, Cancer Hospital Affiliated of Shandong First Medical University; Cancer Hospital Affiliated of Shandong First Medical University

P2, N=30, Not yet recruiting, Renji Hospital affiliated to Shanghai Jiaotong University School of Medicine; Renji Hospital affiliated to Shanghai Jiaotong University School of Medi

P2, N=132, Recruiting, Sun Yat-sen University Cancer Center; Sun Yat-sen University Cancer Center

P2, N=172, Not yet recruiting, Fudan University Shanghai Cancer Center; Fudan University Shanghai Cancer Center

P1, N=48, Not yet recruiting, Taizhou People's Hospital; Taizhou People's Hospital

P1, N=80, Not yet recruiting, Department of Ophthalmology and Visual Sciences, CUHK; Department of Ophthalmology and Visual Sciences, The Chinese University of Hong Kong

P2, N=208, Not yet recruiting, Western Sydney Local Health District

Compound 20b presents as a promising anti-proliferative agent targeting VEGFR-2. Also, this comprehensive investigation underscores the potential of 2,3-dihydro-1,3,4-thiadiazole derivatives as promising candidates for further development in anti-cancer research.

The temporal dynamics of these effects demonstrated greater significance than dose-dependent responses. Both VEGFi and VEGFRi significantly augmented the risk of immune-mediated, blood pressure-related adverse events, with VEGFRi inducing a more rapid and pronounced onset of blood pressure elevation and a higher incidence of immune-related, blood pressure-associated adverse events compared to VEGFi.

P1/2, N=45, Not yet recruiting, M.D. Anderson Cancer Center

P1/2, N=59, Completed, Akeso | Active, not recruiting --> Completed | Trial completion date: May 2023 --> Jul 2024

The quinazoline based glycosyl-1,2,3-triazoles 10-13 with free hydroxy sugar moiety revealed excellent potency against (IC50 range = 5.70-8.10 µM, IC50 Doxorubicin = 5.6 ± 0.30 µM, IC50 Erlotinib = 4.3 ± 0.1 µM)...The hydroxylated glycosides incorporating triazole and quinazoline system 11 and 13 with N-methyl substitution of quinazolinone, gave excellent potency against EGFR (IC50 = 0.35 ± 0.11 and 0.31 ± 0.06 µM, correspondingly) since glycoside 13 revealed comparable IC50 (3.20 ± 0.15 µM) to sorafenib against VEGFR-2...Additionally, the latter derivative may trigger apoptosis, as indicated by a significant increase in apoptotic cells. Furthermore, molecular docking was simulated to make an obvious validation and comprehension acquirement of the binding's characteristics also attractions among the most forceful compounds side by side with their aimed enzymes.

P1, N=50, Active, not recruiting, Tavotek Biotherapeutics | Recruiting --> Active, not recruiting | Trial completion date: Dec 2025 --> Jun 2026 | Trial primary completion date: Jun 2024 --> Dec 2025

P2, N=80, Recruiting, Sunshine Guojian Pharmaceutical (Shanghai) Co., Ltd. | Not yet recruiting --> Recruiting

P1/2, N=230, Recruiting, LaNova Medicines Limited

P1/2, N=110, Not yet recruiting, Akeso