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DRUG CLASS:

Tyrosine kinase inhibitor

2d
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
2d
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)
15d
Zanzalintinib for the Treatment of Advanced Thyroid Cancer Before Surgery (clinicaltrials.gov)
P2, N=45, Recruiting, M.D. Anderson Cancer Center | Trial completion date: Oct 2029 --> Oct 2030
Trial completion date
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zanzalintinib (XL092)
28d
Maintenance Zanzalintinib With Etoposide After HDCT in GCT (clinicaltrials.gov)
P1/2, N=38, Recruiting, Indiana University | Not yet recruiting --> Recruiting | Trial completion date: Mar 2032 --> Sep 2031
Enrollment open • Trial completion date
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etoposide oral • zanzalintinib (XL092)
1m
New P2 trial • IO biomarker
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HER-2 (Human epidermal growth factor receptor 2)
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HER-2 negative
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Tyvyt (sintilimab) • Fumena (vorolanib)
1m
Efficacy Evaluation of Vorolanib Combined with Sintilimab as First-Line Treatment for Advanced Non-Clear Cell Renal Cell Carcinoma (nccRCC): A ​​Multi-center, Single-Arm Study​ (ChiCTR2500107728)
P4, N=35, Not yet recruiting, The First Affiliated Hospital of Zhengzhou University​; The First Affiliated Hospital of Zhengzhou University?
New P4 trial
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Tyvyt (sintilimab) • Fumena (vorolanib)
1m
Cost-effectiveness of rilertinib versus osimertinib in second-line treatment in EGFR T790M resistance mutation advanced non-small cell lung cancer in China. (PubMed, Front Pharmacol)
PSA showed rilertinib's cost-effective probabilities were 51.6% at one-time GDP per capita and 90.2% at three-times GDP per capita ($40,334.05) WTP threshold. From a Chinese healthcare system perspective, second-line treatment of EGFR T790M resistance mutation advanced NSCLC with rilertinib may have cost-effectiveness compared with osimertinib.
Journal • HEOR • Cost-effectiveness
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EGFR (Epidermal growth factor receptor)
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EGFR mutation • EGFR T790M
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Tagrisso (osimertinib) • Sanrisso (rilertinib)
1m
Zanzalintinib Combined With Eribulin in Advanced Liposarcoma and Leiomyosarcoma (clinicaltrials.gov)
P1, N=18, Recruiting, Washington University School of Medicine | Not yet recruiting --> Recruiting
Enrollment open
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Halaven (eribulin mesylate) • zanzalintinib (XL092)
1m
Zanzalintinib plus atezolizumab versus regorafenib in refractory colorectal cancer (STELLAR-303): a randomised, open-label, phase 3 trial. (PubMed, Lancet)
STELLAR-303 is the first phase 3 trial to show a significant improvement in overall survival with an immunotherapy-based regimen, zanzalintinib-atezolizumab, in patients with relapsed or refractory metastatic colorectal cancer that is not MSI-H or dMMR. This combination represents a chemotherapy-free treatment option with a novel mechanism of action for heavily pretreated patients in need of improved therapies.
P3 data • Journal
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MSI (Microsatellite instability)
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MSI-H/dMMR
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Tecentriq (atezolizumab) • Stivarga (regorafenib) • zanzalintinib (XL092)
1m
STELLAR-303: Study of XL092 + Atezolizumab vs Regorafenib in Participants With Metastatic Colorectal Cancer (clinicaltrials.gov)
P3, N=901, Active, not recruiting, Exelixis | Trial completion date: Feb 2026 --> Jan 2027 | Trial primary completion date: Aug 2025 --> May 2026
Trial completion date • Trial primary completion date
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MSI (Microsatellite instability)
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MSI-H/dMMR • RAS mutation
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Tecentriq (atezolizumab) • Stivarga (regorafenib) • zanzalintinib (XL092)
2ms
Mechanistic study of ANXA3-mediated endoplasmic reticulum stress promoting M1 macrophage polarization in pulmonary arterial hypertension based on bioinformatics and nine machine learning algorithms. (PubMed, Comput Biol Med)
This study demonstrates that ANXA3 regulates ERS to drive M1 macrophage polarization and inflammation, which subsequently promotes PASMC function and promotes PAH progression. ANXA3 may serve as a novel immunoinflammatory target and potential therapeutic candidate.
Journal • IO biomarker
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BCL2 (B-cell CLL/lymphoma 2) • IL6 (Interleukin 6) • BCL2L1 (BCL2-like 1) • TNFA (Tumor Necrosis Factor-Alpha) • TNFRSF17 (TNF Receptor Superfamily Member 17) • CD68 (CD68 Molecule) • IL18 (Interleukin 18) • HSPA5 (Heat Shock Protein Family A (Hsp70) Member 5) • ATF4 (Activating Transcription Factor 4) • DNAJB1 (DnaJ Heat Shock Protein Family (Hsp40) Member B1) • IL1B (Interleukin 1, beta) • ANXA3 (Annexin A3) • TCF4 (Transcription Factor 4)
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semaxanib (SU5416)