AiTan (rivoceranib)

Here, we report a rare case of primary mediastinal malignant meningioma with lung and bone metastases, who benefited from the treatment of apatinib (≥33 months) and anlotinib (until the publication date). Based on the Western analysis, we revealed that FGF6 can promote the phosphorylation of FGFR, AKT, and ERK1/2, which can be inhibited by anlotinib. Together, we were the first to verify that overexpression of FGF6 promotes the progression of malignant meningiomas by activating FGFR/AKT/ERK1/2 pathway and pointed out that anlotinib may effectively inhibit the disease progression of patients with FGF6 amplification.

P1, N=29, Terminated, Elevar Therapeutics | Phase classification: P1b/2 --> P1 | Completed --> Terminated; Phase 2 portion of the study was not performed due to redirection of the rivoceranib development plan by the Sponsor.

P2, N=196, Active, not recruiting, RenJi Hospital | Completed --> Active, not recruiting | Trial completion date: Apr 2023 --> Mar 2031

P2, N=32, Not yet recruiting, The First Affiliated Hospital with Nanjing Medical University

Low-dose apatinib combined with oral vinorelbine demonstrates potential efficacy and well tolerated for pretreated HER2-negative mBC.

P2, N=40, Recruiting, Sun Yat-Sen Memorial Hospital of Sun Yat-Sen University | Not yet recruiting --> Recruiting

In the whole-population network meta-analysis, the newly first-line tremelimumab plus durvalumab (Tre + Du) was found to be comparable with atezolizumab plus bevacizumab (Atezo + Beva) in providing the best overall survival (OS) benefit [hazard ratio (HR) 1.35, 95% confidence interval (CI): 0.93-1.92]. Concerning OS benefits, sintilimab plus bevacizumab biosimilar (Sint + Beva), camrelizumab plus rivoceranib (Camre + Rivo), and lenvatinib plus pembrolizumab (Lenva + Pemb) appear to exhibit similar effects to Tre + Du and Atezo + Beva...With lower incidence rates of treatment-related adverse events and non-inferior efficacy compared to sorafenib, ICI monotherapies should be prioritized as a first-line treatment approach for patients who are not suitable candidates for ICI-combined therapies. PROSPERO, CRD42022288172.

P2, N=111, Recruiting, Peking University Cancer Hospital & Institute | Not yet recruiting --> Recruiting | Initiation date: Apr 2024 --> Jan 2024

P=N/A, N=234, Completed, Fujian Medical University

P2, N=57, Recruiting, Fujian Medical University | Not yet recruiting --> Recruiting

On the contrary, some patients with mucosal, acral or KIT-mutant melanoma may benefit from TKI-based therapies. Further studies focused on biomarker discovery and randomized trials are necessary to better understand the role of VEGFR1-3 as a therapeutic target in melanoma.

P2, N=57, Not yet recruiting, Fujian Medical University

P2, N=111, Not yet recruiting, Peking University Cancer Hospital & Institute

P3, N=589, Recruiting, AstraZeneca

P2, N=30, Not yet recruiting, Chinese PLA General Hospital

P2, N=32, Recruiting, Sun Yat-Sen Memorial Hospital of Sun Yat-Sen University

There was no obvious difference in body weight and liver and kidney functions between the four groups of mice. In conclusion, CPT improves the anti-tumor effect of low-dose apatinib combined with PD-1 inhibitor on hepatocellular carcinoma.

P2, N=30, Recruiting, Peking Union Medical College | Initiation date: Dec 2023 --> May 2024

P2, N=43, Recruiting, Sun Yat-Sen Memorial Hospital of Sun Yat-Sen University

P2, N=16, Not yet recruiting, M.D. Anderson Cancer Center

P2, N=196, Completed, RenJi Hospital | Recruiting --> Completed | Trial primary completion date: Oct 2022 --> Mar 2023

Apatinib has a significant inhibitory effect on small cell lung cancer with high expression of VEGFR2 and may be a treatment for small cell lung cancer patients.

P2, N=40, Not yet recruiting, Meng Chao Hepatobiliary Hospital of Fujian Medical University

P1, N=35, Recruiting, First Affiliated Hospital of Fujian Medical University | Not yet recruiting --> Recruiting

P2, N=170, Recruiting, Sun Yat-sen University

P2, N=48, Recruiting, Asan Medical Center | Not yet recruiting --> Recruiting

P2, N=0, Withdrawn, Xinqiao Hospital of Chongqing | N=20 --> 0 | Unknown status --> Withdrawn

P4, N=0, Withdrawn, Xinqiao Hospital of Chongqing | N=20 --> 0 | Unknown status --> Withdrawn

P2, N=40, Not yet recruiting, Sun Yat-Sen Memorial Hospital of Sun Yat-Sen University

In summary, our study indicated that ESPL1 played a critical role in apatinib resistance in GC cells. Inhibition of MDM2 could rescue the sensitivity of GC cells to apatinib and reverse ESPL1-mediated resistance.

Here, we show that exosomes secreted by gastric cancer cells carry miR-214-3p into vascular endothelial cells and directly target zinc finger protein A20 to negatively regulate ACSL4, a key enzyme of lipid peroxidation during ferroptosis, thereby inhibiting ferroptosis in vascular endothelial cells and reducing the efficiency of Apatinib. In conclusion, inhibition of miR-214-3p can increase the sensitivity of vascular endothelial cells to Apatinib, thereby promoting the antiangiogenic effect of Apatinib, suggesting a potential combination therapy for advanced gastric cancer.

P2, N=128, Recruiting, First Affiliated Hospital Bengbu Medical College | Trial completion date: Jun 2024 --> Jun 2025 | Trial primary completion date: Jan 2024 --> Jan 2025

P1/2, N=52, Recruiting, Sun Yat-Sen Memorial Hospital of Sun Yat-Sen University | Not yet recruiting --> Recruiting

Statistically significant differences are shown (P = 0.014). No serious (Grade IV) adverse events occurred in either group. Our study indicates that apatinib in combination with chemotherapy with or without immunotherapy as first-line treatment for advanced GC exhibits good anti-tumor activity and is well tolerated by patients.

P2, N=125, Recruiting, The First Affiliated Hospital of Zhengzhou University | N=85 --> 125 | Trial completion date: Feb 2023 --> Dec 2024

P=N/A, N=279, Completed, Zhejiang University

P3, N=200, Not yet recruiting, Sun Yat-Sen Memorial Hospital of Sun Yat-Sen University

P2, N=33, Completed, Renmin Hospital of Wuhan University

The results of this meta-analysis suggest that targeted therapy with TKIs may be beneficial for patients with radioiodine-refractory advanced or metastatic differentiated thyroid cancer. Among the TKIs analyzed, lenvatinib appeared to be the most effective at improving PFS, although it also had the highest incidence of AEs. Further research through direct randomized controlled trials is needed to determine the optimal choice of TKI for treating patients with RAIR-DTC. This study is beneficial for formulating patients' treatment plans and guides clinicians' decision-making.

Our findings underscore the pivotal role of YY1 in driving GC progression and influencing prognosis, thus pinpointing it as a promising therapeutic target to enhance patient outcomes.

Second-line PD-1 inhibitor combined with albumin paclitaxel and apatinib showed certain efficacy and safety in patients with mGC.

P3, N=543, Completed, Jiangsu HengRui Medicine Co., Ltd. | Active, not recruiting --> Completed