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DRUG CLASS:

Tyrosine kinase inhibitor

4d
A Single-Arm, Single-Center Clinical Study of Vorolanib Combined with Toripalimab as First-Line Therapy for Metastatic Clear Cell Renal Cell Carcinoma (ChiCTR2500111737)
P4, N=30, Not yet recruiting, The First Affiliated Hospital of Xi'an Jiaotong University; The First Affiliated Hospital of Xi'an Jiaotong University
New P4 trial
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Loqtorzi (toripalimab-tpzi) • Fumena (vorolanib)
10d
Large extracellular vesicles regulate endothelial angiogenic potential via paracrine and autocrine signaling. (PubMed, J Biol Chem)
Despite advancements in anti-angiogenic cancer therapies, such as bevacizumab, late-stage tumors, including advanced melanomas, exhibit mixed clinical responses...This L-EV-mediated increase in endothelial tube formation is sensitive to the effects of sorafenib, a multi-kinase inhibitor, but not SU5416, a selective VEGF-receptor inhibitor...Finally, we show that EV subtypes have distinct effects on the acquisition of angiogenic phenotypes and their roles vary with tumor type. These findings provide new insight into the mechanisms of angiogenic therapy resistance in melanoma and demonstrate the differential functions of EV subtypes in angiogenesis across tumor types.
Journal
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CXCL8 (Chemokine (C-X-C motif) ligand 8)
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Avastin (bevacizumab) • sorafenib • semaxanib (SU5416)
23d
Paeoniflorin Alleviates Pulmonary Arterial Hypertension by Suppressing TRIM24-Mediated SIRT1 Ubiquitination and NLRP3 Inflammasome Activation. (PubMed, Chem Biol Drug Des)
A PAH rat model was established by SU5416 (Su) injection combined with chronic hypoxia (Hx)...PF alleviated PAH and endothelial dysfunction by downregulating TRIM24 and preserving SIRT1 function. These findings reveal a novel mechanism by which PF protects against PAH via the TRIM24/SIRT1/NLRP3 axis.
Journal
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IL6 (Interleukin 6) • TNFA (Tumor Necrosis Factor-Alpha) • IL1B (Interleukin 1, beta) • NLRP3 (NLR Family Pyrin Domain Containing 3) • SIRT1 (Sirtuin 1) • TRIM24 (Tripartite Motif Containing 24)
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semaxanib (SU5416)
27d
Zanzalintinib in Combination With Ipilimumab and Nivolumab in Patients With Metastatic Soft Tissue Sarcoma (clinicaltrials.gov)
P1, N=18, Recruiting, Washington University School of Medicine | Not yet recruiting --> Recruiting
Enrollment open
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Opdivo (nivolumab) • Yervoy (ipilimumab) • zanzalintinib (XL092)
1m
Differential Impact of Recruited and Resident Macrophages on Hypoxia-Induced Pulmonary Hypertension. (PubMed, Circ Res)
Simultaneously targeting Prrx2 and Hic1 in macrophages significantly alleviated SU5416/hypoxia-induced PH in rats. The differential roles of pulmonary resMФs and recMФs in pulmonary vascular remodeling highlight novel therapeutic targets for pulmonary arterial hypertension treatment, specifically through inhibition of Hic1 and Prrx2 in macrophages.
Journal
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SIRT1 (Sirtuin 1) • HIC1 (HIC ZBTB Transcriptional Repressor 1) • PRRX2 (Paired Related Homeobox 2)
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semaxanib (SU5416)
1m
Large extracellular vesicles regulate endothelial angiogenic potential via paracrine and autocrine signaling. (PubMed, bioRxiv)
Despite advancements in anti-angiogenic cancer therapies, such as bevacizumab, late-stage tumors, including advanced melanomas, exhibit mixed clinical responses...This L-EV-mediated increase in endothelial tube formation is sensitive to the effects of sorafenib, a multi-kinase inhibitor, but not SU5416, a selective VEGF-receptor inhibitor...Finally, we show that EV subtypes have distinct effects on the acquisition of angiogenic phenotypes and their roles vary with tumor type. These findings provide new insight into the mechanisms of angiogenic therapy resistance in melanoma and demonstrate the differential functions of EV subtypes in angiogenesis across tumor types.
Journal
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CXCL8 (Chemokine (C-X-C motif) ligand 8)
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Avastin (bevacizumab) • sorafenib • semaxanib (SU5416)
2ms
Zanzalintinib Maintenance in Patients With High Grade Neuroendocrine Neoplasms (HG-NENs) (clinicaltrials.gov)
P2, N=32, Recruiting, Washington University School of Medicine | Not yet recruiting --> Recruiting
Enrollment open
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zanzalintinib (XL092)
2ms
New P2 trial
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Keytruda (pembrolizumab) • zanzalintinib (XL092)
2ms
A Phase 2 Trial of Zanzalintinib in Advanced/Metastatic Bone Sarcomas (ZAMBONE) (clinicaltrials.gov)
P2, N=70, Active, not recruiting, M.D. Anderson Cancer Center | Not yet recruiting --> Active, not recruiting | Initiation date: May 2026 --> Dec 2025
Enrollment closed • Trial initiation date
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zanzalintinib (XL092)
2ms
Host angiogenic reprogramming by Echinococcus multilocularis protoscoleces protein via PDGFR/PI3K/AKT cascade. (PubMed, Front Microbiol)
Interventions utilizing a range of inhibitors at the in vitro level, including the PDGFR-β inhibitor AG1296, the PI3K inhibitor LY294002, the AKT inhibitor MK2206, and the FAK inhibitor Y15, demonstrated that E. multilocularis protoscoleces protein (EmP) induces angiogenesis through PDGFR/PI3K/AKT/FAK signaling pathway. Our findings provide new perspectives on how E. multilocularis infection triggers pathological angiogenesis in the host liver, and may provide a novel anti-angiogenic therapeutic strategy against E. multilocularis infection.
Journal
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PDGFRB (Platelet Derived Growth Factor Receptor Beta)
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MK-2206 • LY294002 • AG-1296
2ms
Dose Finding Study of Zanzalintinib With Pembrolizumab and Cetuximab in Head and Neck SCC (clinicaltrials.gov)
P1, N=36, Recruiting, University of Chicago | Active, not recruiting --> Recruiting
Enrollment open
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Keytruda (pembrolizumab) • Erbitux (cetuximab) • zanzalintinib (XL092)