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DRUG CLASS:

VEGFR-3 inhibitor

13d
PTPN9 dephosphorylates IGF1RY1165/1166 and alleviates IGF1R-mediated resistance to tyrosine kinase inhibitor in cholangiocarcinoma. (PubMed, J Exp Clin Cancer Res)
Increasing evidence suggests that a subset of CCA patients can benefit from multiple tyrosine kinase inhibitors (mTKIs) such as surufatinib...Furthermore, cancer-associated fibroblasts (CAFs) were identified as the major source of IGF1 in CCA microenvironment, essential for IGF1R-driven tumor progression.In summary, the PTPN9-IGF1R axis plays a pivotal role in modulating mTKI sensitivity and tumor progression in CCA. This axis serves as a promising biomarker for identifying potential mTKI beneficiaries and represents a potential therapeutic target to enhance mTKI efficacy and overcome resistance.
Journal
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IGF1 (Insulin-like growth factor 1)
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Sulanda (surufatinib)
25d
A case report: enhanced somatostatin receptor expression in metastatic pancreatic neuroendocrine tumor following everolimus therapy. (PubMed, Front Cell Dev Biol)
From August 2019 to October 2020, he received long-acting octreotide and transarterial chemoembolization (TACE), achieving stable disease...In September 2022, oral surufatinib was initiated but paused in September 2023 due to adverse effects...This case demonstrates that everolimus can induce SSTR re-expression in advanced, SSTR-negative pNETs, offering new therapeutic possibilities. The "induction plus re-evaluation" approach could guide personalized treatment strategies in late-stage pNETs, although further studies are needed to validate this approach.
Journal
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SSTR (Somatostatin Receptor) • SSTR2 (Somatostatin Receptor 2)
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everolimus • Sulanda (surufatinib) • octreotide acetate
1m
Surufatinib plus paclitaxel as second-line therapy for advanced gastric cancer: a single-arm, phase 2 clinical trial. (PubMed, Cell Oncol (Dordr))
Surufatinib plus paclitaxel showed promising efficacy and manageable safety as second-line treatment for advanced gastric cancer, especially in patients who had failed prior immunotherapy.
P2 data • Journal
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HER-2 (Human epidermal growth factor receptor 2)
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HER-2 negative
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paclitaxel • Sulanda (surufatinib)
1m
Exploring the efficacy and safety of famitinib combined with epalrestat and torivirine in the treatment of advanced and recurrent/metastatic cervical cancer (ChiCTR2500111354)
P2, N=90, Not yet recruiting, Xinhua Hospital Affiliated to Shanghai Jiao Tong University School of Medicine; Xinhua Hospital Affiliated to Shanghai Jiao Tong University School of
New P2 trial
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PD-L1 (Programmed death ligand 1)
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famitinib (SHR 1020) • iparomlimab (QL1604)
1m
New P2 trial
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AiRuiKa (camrelizumab) • famitinib (SHR 1020)
1m
Study to Assess the Efficacy & Safety of KHK4951 in Patients With Neovascular Age-Related Macular Degeneration (clinicaltrials.gov)
P2, N=180, Active, not recruiting, Kyowa Kirin Co., Ltd. | Recruiting --> Active, not recruiting
Enrollment closed
1m
Study to Assess the Efficacy & Safety of KHK4951 in Patients With Diabetic Macular Edema (clinicaltrials.gov)
P2, N=150, Active, not recruiting, Kyowa Kirin Co., Ltd. | Recruiting --> Active, not recruiting
Enrollment closed
2ms
New P2 trial
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Fotivda (tivozanib) • sturlimogene erparepvec (RP2)
2ms
Olaparib-Cediranib Hybrid as Dual PARP-VEGFR3 Inhibitor Elicits Antitumor Efficacy: Rational Design, Synthesis, Biological Evaluation and Construction of a Charge Convertible pH Responsive Nanoformulation. (PubMed, Bioorg Chem)
Further, a charge-convertible polymer-based nanoformulation (18-PEG-PLL/DMMA nanoparticles) for targeted drug delivery of 18 was developed. Encouragingly, the nanoformulation demonstrated a cytotoxicity-devoid profile towards normal cells owing to its pH-sensitive behavior and manifested selective cell growth inhibition against solid tumor cells, possibly due to the EPR effect.
Journal
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FLT4 (Fms-related tyrosine kinase 4) • PARP2 (Poly(ADP-Ribose) Polymerase 2)
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Lynparza (olaparib) • Recentin (cediranib)
2ms
Association of HTR1F with Prognosis, Tumor Immune Microenvironment, and Drug Sensitivity in Cancer: A Multi-Omics Perspective. (PubMed, Biomedicines)
Drug sensitivity analysis identified compounds such as sotrastaurin (-10.2 kcal/mol), austocystin D (-9.7 kcal/mol), and tivozanib (-9.3 kcal/mol) as potentially effective inhibitors based on predicted binding affinity. Our integrative analysis highlights HTR1F as a potential biomarker associated with prognosis, immune modulation, and drug sensitivity across multiple cancer types. These findings provide a foundation for future experimental and clinical studies to explore HTR1F-targeted therapies.
Journal • Tumor mutational burden
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TMB (Tumor Mutational Burden) • MSI (Microsatellite instability)
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sotrastaurin (AEB071) • Fotivda (tivozanib)
2ms
A Study to Evaluate SHR-1210 in Combination With Famitinib Plus Chemotherapy in Subjects With NSCLC. (clinicaltrials.gov)
P3, N=48, Terminated, Jiangsu HengRui Medicine Co., Ltd. | N=560 --> 48 | Trial completion date: Oct 2023 --> Aug 2025 | Recruiting --> Terminated | Trial primary completion date: Dec 2022 --> Aug 2025; Terminated by Sponsor
Enrollment change • Trial completion date • Trial termination • Trial primary completion date
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EGFR (Epidermal growth factor receptor) • ALK (Anaplastic lymphoma kinase)
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EGFR mutation • ALK rearrangement
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carboplatin • AiRuiKa (camrelizumab) • pemetrexed • famitinib (SHR 1020)
3ms
Open-label Study of Surufatinib in Japanese Patients (clinicaltrials.gov)
P1/2, N=36, Completed, Hutchmed | Active, not recruiting --> Completed
Trial completion
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Sulanda (surufatinib)