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.

The combined application of ERK inhibitors, U0126 or trametinib, with the VEGFR inhibitor Apatinib, additively suppresses angiogenesis and tumor growth of HCC1806 in nude mice. These findings provide new therapeutic strategies for TNBC.

This case highlights the potential antitumor activity of apatinib in breast cancer patients with presenting with PLC. While further studies are necessary, this therapeutic approach could represent a viable option for managing breast cancer in the context of a visceral crisis. The case also emphasizes the importance of individualized treatment strategies and further research to substantiate these promising findings.

P2, N=0, Withdrawn, M.D. Anderson Cancer Center | N=16 --> 0 | Trial completion date: Nov 2028 --> Nov 2024 | Initiation date: Apr 2025 --> Nov 2024 | Not yet recruiting --> Withdrawn | Trial primary completion date: Nov 2026 --> Nov 2024

P4, N=128, Not yet recruiting, West China Hospital, Sichuan University; West China Hospital, Sichuan University

P2, N=33, Not yet recruiting, Sun Yat-sen University Cancer Center; Sun Yat-sen University Cancer Center

P2, N=31, Not yet recruiting, The First Hospital of China Medical University; The First Hospital of China Medical University

P1, N=60, Not yet recruiting, The First Affiliated Hospital of Henan University of Science and Technology; The First Affiliated Hospital of Henan University of Science and Technolo

P3, N=302, Completed, Changchun GeneScience Pharmaceutical Co., Ltd. | Recruiting --> Completed | Trial completion date: Jul 2024 --> Apr 2024 | Trial primary completion date: Oct 2023 --> Apr 2024

P2/3, N=429, Recruiting, Institut für Klinische Krebsforschung IKF GmbH at Krankenhaus Nordwest | Trial primary completion date: Sep 2024 --> Dec 2024

P2, N=106, Completed, Changchun GeneScience Pharmaceutical Co., Ltd. | Not yet recruiting --> Completed | Trial completion date: Feb 2024 --> May 2024

P3, N=885, Completed, Jiangsu HengRui Medicine Co., Ltd. | Active, not recruiting --> Completed

P2, N=106, Completed, Changchun GeneScience Pharmaceutical Co., Ltd. | Recruiting --> Completed

P1, N=178, Active, not recruiting, Changchun GeneScience Pharmaceutical Co., Ltd. | Recruiting --> Active, not recruiting

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.

P1, N=30, Not yet recruiting, City of Hope Medical Center

The most frequent grade 3 or 4 treatment-related adverse event was neutropenia (n = 4, 29%). The combination of camrelizumab, gemcitabine, and apatinib showed promising efficacy and acceptable safety in patients with advanced PD-L1-positive biliary tract cancer.

Despite the unfavorable prognosis associated with advanced GC, the implementation of personalized treatment approaches may still prove beneficial for select patients. In patients with HER2-positive GC with extensive metastatic involvement, the use of the HER2-targeted combination with apatinib has demonstrated the potential to prolong both PFS and overall survival.

P2, N=160, Active, not recruiting, Xiuning Le | Trial completion date: Oct 2024 --> Oct 2025 | Trial primary completion date: Sep 2024 --> Sep 2025

P3, N=1040, Not yet recruiting, Alliance for Clinical Trials in Oncology

This new neoadjuvant combination of pembrolizumab plus ramucirumab was feasible and anti-VEGF agents may enhance the effects of ICIs.

P3, N=450, Not yet recruiting, Shanghai Runshi Pharmaceutical Technology Co., Ltd

P3, N=343, Active, not recruiting, AVEO Pharmaceuticals, Inc. | Trial completion date: Aug 2025 --> Jul 2026 | Trial primary completion date: Aug 2024 --> Apr 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.

This was mirrored by a reduction in the IC50 values for cisplatin and apatinib to 0.8257 µM and 10.79 µM, respectively. The E2F8-TPX2 axis promotes glycolysis and angiogenesis in LC cells, which in turn accelerates cancer progression and reduces chemosensitivity. The online version contains supplementary material available at 10.1007/s10616-024-00655-w.

Considering that resveratrol can increase the apoptosis of cancer cells alone and in combination with tivozanib and prevent the proliferation of cancer cells and also reduce the side effects of tivozanib, we suggest that resveratrol as a potential bioactive molecule can be used in treatment of kidney cancer should be used in combination with tivozanib.

P1/2, N=133, Recruiting, Beijing Konruns Pharmaceutical Co., Ltd. | Trial completion date: Apr 2025 --> Dec 2025 | Trial primary completion date: Apr 2024 --> Oct 2025

P1, N=207, Recruiting, Beijing Konruns Pharmaceutical Co., Ltd. | Trial completion date: Jul 2024 --> Dec 2025 | Trial primary completion date: Jul 2023 --> Oct 2025

No abstract available

P2, N=44, Recruiting, Beijing Sanbo Brain Hospital | Trial completion date: Aug 2024 --> Aug 2025 | Trial primary completion date: Aug 2024 --> Aug 2025

Patient 1, a 72-year-old man, developed ascites 20 months after erlotinib (ERL) and RAM administration, which resolved after their discontinuation and performing paracentesis. Patient 2, an 83-year-old woman, developed ascites 9 months after ERL and RAM administration, which resolved after RAM discontinuation and furosemide administration. Ramucirumab administration can cause ascites due to increased hepatic sinusoidal pressure. Clinicians should be aware of RAM-induced ascites in patients with NSCLC and should appropriately manage it.

To overcome these limitations, we developed multi-functional nanoparticles (VI@Gd-NPs) that integrate a tumor vasculature-specific disrupting agent (Vadimezan, Phase III clinical drug), a photosensitizer (Indocyanine Green, ICG), and a magnetic resonance imaging contrast agent (Gadolinium, Gd) through chemical self-assembly...Moreover, depleting CD8+ T cells reverses these therapeutic benefits, highlighting the critical role of adaptive T cell immunity. Therefore, the VI@Gd-NPs treatment holds great potential for reigniting the in-situ tumor vaccine of photothermal therapy.

EGCG regulated glycolysis levels in NSCLC through VEGF overexpression, and enhanced the antitumor effect of apatinib in NSCLC through VEGF-regulated glycolysis. Taken together, EGCG strengthened the protective effects of apatinib in NSCLC through glycolysis mediated by VEGF.

Immunohistochemistry showed that combining apatinib with chloroquine could reduce the expression of CD31 and Ki67 and increase the expression of caspase-3. Apatinib inhibits proliferation and induces apoptosis in H1975 and H1446 lung cancer cells with high VEGFR2 expression and autophagy in H1975 and H446 cells.

P2, N=46, Not yet recruiting, Beijing Tsinghua Chang Gung Hospital

Ramucirumab plus osimertinib significantly prolonged PFS compared with osimertinib alone in patients with TKI-naïve EGFR-mutant NSCLC. The combination is safe and well tolerated.

P2, N=16, Not yet recruiting, M.D. Anderson Cancer Center | Initiation date: Sep 2024 --> Apr 2025

Apatinib combined with vinorelbine is effective and safe in patients with locally advanced or metastatic refractory HER2-negative breast cancer. The findings of this study con-tribute to a better understanding of the metabolic effect of apatinib and vinorelbine therapy.

P2, N=56, Recruiting, SWOG Cancer Research Network | Not yet recruiting --> Recruiting

P2/3, N=378, Not yet recruiting, SWOG Cancer Research Network

P2, N=105, Recruiting, Eli Lilly and Company | Trial completion date: May 2026 --> May 2027 | Trial primary completion date: May 2026 --> May 2027

P2, N=43, Not yet recruiting, Fujian Cancer Hospital