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DRUG:

Sutent (sunitinib)

i
Other names: PNU 290940, SU 011248, SU011248, PNU-290940, SU-11428, SU-011248, PNU-290940AD, PHA-290940AD, PHA-290940, Sutib
Company:
Pfizer
Drug class:
c-KIT inhibitor, VEGFR inhibitor, PDGFR inhibitor
Related drugs:
1d
Elucidation and Regulation of Tyrosine Kinase Inhibitor Resistance in Renal Cell Carcinoma Cells from the Perspective of Glutamine Metabolism. (PubMed, Metabolites)
Additionally, the regulating glutamine metabolism resulted in antitumor effects through sunitinib re-sensitivity in sunitinib-resistant RCC. Our results are expected to contribute to the more effective utilization of TKIs with further improvements in prognosis through current drug therapies.
Journal
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PTEN (Phosphatase and tensin homolog)
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Sutent (sunitinib)
3d
A Trial Evaluating the Activity and Safety of Combination Between Cabozantinib and Temozolomide in Lung and GEP-NENS Progressive After Everolimus, Sunitinib or PRRT (CABOTEM) (clinicaltrials.gov)
P2, N=35, Recruiting, National Cancer Institute, Naples | Trial completion date: Dec 2024 --> Dec 2026 | Trial primary completion date: Jan 2024 --> Jan 2025
Trial completion date • Trial primary completion date
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Sutent (sunitinib) • everolimus • temozolomide • Cabometyx (cabozantinib tablet)
7d
LUMEN-1: 177Lu-DOTATATE for Recurrent Meningioma (clinicaltrials.gov)
P2, N=135, Not yet recruiting, European Organisation for Research and Treatment of Cancer - EORTC
New P2 trial
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Avastin (bevacizumab) • Sutent (sunitinib) • everolimus • hydroxyurea • Lutathera (lutetium Lu 177 dotatate) • Sandostatin LAR Depot (octreotide acetate)
7d
GIST Oral Paclitaxel(Liporaxel) (clinicaltrials.gov)
P2, N=28, Not yet recruiting, Asan Medical Center
New P2 trial
|
paclitaxel • imatinib • Sutent (sunitinib) • Stivarga (regorafenib) • Liporaxel (paclitaxel oral)
10d
Efficacy Assessment of Post-nephrectomy Adjuvant Therapies in Patients with Renal Cell Carcinoma. (PubMed, Ann Surg Oncol)
Our results suggest that post-nephrectomy RCC patients with sarcomatoid differentiation and high PD-L1 expression were more responsive to ICIs. Furthermore, pembrolizumab monotherapy exhibited superior DFS and OS results over other adjuvant therapies.
Journal • PD(L)-1 Biomarker • IO biomarker
|
PD-L1 (Programmed death ligand 1)
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PD-L1 expression • PD-L1 overexpression
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Keytruda (pembrolizumab) • Opdivo (nivolumab) • Tecentriq (atezolizumab) • Yervoy (ipilimumab) • sorafenib • Sutent (sunitinib) • Rencarex (girentuximab)
11d
Involvement of Ferroptosis Induction and Oxidative Phosphorylation Inhibition in the Anticancer-Drug-Induced Myocardial Injury: Ameliorative Role of Pterostilbene. (PubMed, Int J Mol Sci)
To investigate this mechanism, we treated rat cardiomyoblast H9c2 cells with sunitinib, lapatinib, 5-fluorouracil, and cisplatin to examine their effects...Anticancer-drug-induced cell death was suppressed by N-acetylcysteine, deferoxamine, and ferrostatin, indicating ferroptosis...These findings suggest that induction of ferroptosis and inhibition of oxidative phosphorylation are mechanisms by which anticancer drugs cause myocardial damage. As pterostilbene ameliorates these mechanisms, it is expected to have significant clinical applications.
Journal
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GPX4 (Glutathione Peroxidase 4)
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cisplatin • 5-fluorouracil • Sutent (sunitinib) • lapatinib
11d
Pterostilbene Induces Apoptosis from Endoplasmic Reticulum Stress Synergistically with Anticancer Drugs That Deposit Iron in Mitochondria. (PubMed, Int J Mol Sci)
We have reported that pterostilbene (PTE), a plant stilbene, enhances the antitumor effect of low doses of sunitinib in gastric cancer cells accumulating mitochondrial iron (II) (mtFe) at low doses...For this study, we used 5-fluorouracil (5FU), cisplatin (CPPD), and lapatinib (LAP), which are frequently used in the treatment of GC, and doxorubicin (DOX), which is known to deposit mtFe...These findings would help in developing novel therapeutic strategies for GC. However, further clinical investigations are required.
Journal
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HIF1A (Hypoxia inducible factor 1, alpha subunit) • PDZD8 (PDZ Domain Containing 8)
|
cisplatin • 5-fluorouracil • Sutent (sunitinib) • lapatinib • doxorubicin hydrochloride
13d
Exploring the tumor microenvironment: Chemokine-related genes and immunotherapy/chemotherapy response in clear-cell renal cell carcinoma. (PubMed, Environ Toxicol)
Our study has yielded a novel prognostic model of chemokine-related genes based on comprehensive transcriptional atlas of ccRCC patients, shedding light on the significant impact of the tumor microenvironment on biology and immunotherapy response of ccRCC. We identified IGF2BP3 as a pivotal regulator in regulating ccRCC resistance to sunitinib.
Journal
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CD8 (cluster of differentiation 8) • AURKB (Aurora Kinase B) • IGF2BP3 (Insulin Like Growth Factor 2 MRNA Binding Protein 3) • ITPKA (Inositol-Trisphosphate 3-Kinase A) • ZIC2 (Zic Family Member 2)
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IGF2 elevation • IGFBP3 elevation
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docetaxel • Sutent (sunitinib) • bortezomib • dactinomycin • daporinad (APO866)
14d
Trial suspension • Metastases
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PD-L1 (Programmed death ligand 1)
|
PD-L1 expression
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PD-L1 IHC 22C3 pharmDx
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Keytruda (pembrolizumab) • Sutent (sunitinib)
14d
Sunitinib Malate or Valproic Acid in Preventing Metastasis in Patients With High-Risk Uveal Melanoma (clinicaltrials.gov)
P2, N=210, Active, not recruiting, Sidney Kimmel Cancer Center at Thomas Jefferson University | Trial completion date: Dec 2023 --> Dec 2025 | Trial primary completion date: Dec 2023 --> Dec 2025
Trial completion date • Trial primary completion date
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Sutent (sunitinib)
22d
Trial completion date • Combination therapy • Metastases
|
Keytruda (pembrolizumab) • Sutent (sunitinib) • Inlyta (axitinib)
23d
Nesprin1 deficiency is associated with poor prognosis of renal cell carcinoma and resistance to sunitinib treatment. (PubMed, Oncology)
The results indicate that the expression of SYNE1/Nesprin1 and SYNE1 mutations in patients with RCC are closely linked to their prognosis and responsiveness to sunitinib treatment.
Journal
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SYNE1 (Spectrin Repeat Containing Nuclear Envelope Protein 1)
|
SYNE1 mutation
|
Sutent (sunitinib)
25d
Serial Measurements of Molecular and Architectural Responses to Therapy (SMMART) PRIME Trial (clinicaltrials.gov)
P1, N=2, Terminated, OHSU Knight Cancer Institute | Active, not recruiting --> Terminated; Low accrual
Trial termination
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Keytruda (pembrolizumab) • Opdivo (nivolumab) • Avastin (bevacizumab) • Venclexta (venetoclax) • Lynparza (olaparib) • Mekinist (trametinib) • erlotinib • Gilotrif (afatinib) • Yervoy (ipilimumab) • Ibrance (palbociclib) • dasatinib • Zelboraf (vemurafenib) • Tafinlar (dabrafenib) • carboplatin • Imfinzi (durvalumab) • sorafenib • Rozlytrek (entrectinib) • imatinib • Sutent (sunitinib) • everolimus • Nerlynx (neratinib) • Iclusig (ponatinib) • Kadcyla (ado-trastuzumab emtansine) • Cotellic (cobimetinib) • Lorbrena (lorlatinib) • Lenvima (lenvatinib) • bortezomib • doxorubicin hydrochloride • capecitabine • Verzenio (abemaciclib) • enzalutamide capsule • Cabometyx (cabozantinib tablet) • albumin-bound paclitaxel • Stivarga (regorafenib) • abiraterone acetate • oxaliplatin • Aliqopa (copanlisib) • Vizimpro (dacomitinib) • Zydelig (idelalisib) • daunorubicin • Zolinza (vorinostat) • Idhifa (enasidenib) • Farydak (panobinostat) • Erivedge (vismodegib) • Nubeqa (darolutamide) • bicalutamide • leucovorin calcium • cabazitaxel • Vesanoid (tretinoin) • fluorouracil topical
26d
A Phase II Study of Sunitinib or Temsirolimus in Patients With Advanced Rare Tumours (clinicaltrials.gov)
P2, N=137, Active, not recruiting, Canadian Cancer Trials Group | Trial completion date: Jan 2024 --> Dec 2024
Trial completion date • Metastases
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PTEN (Phosphatase and tensin homolog) • STK11 (Serine/threonine kinase 11) • NF1 (Neurofibromin 1)
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EGFR mutation • PTEN mutation • NF1 mutation • MTOR mutation • AKT1 amplification
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Sutent (sunitinib) • Torisel (temsirolimus)
30d
Rivoceranib Plus Paclitaxel in Patients With Gastrointestinal Stromal Tumor (clinicaltrials.gov)
P2, N=48, Recruiting, Asan Medical Center | Not yet recruiting --> Recruiting
Enrollment open
|
KIT (KIT proto-oncogene, receptor tyrosine kinase) • PDGFRA (Platelet Derived Growth Factor Receptor Alpha) • ANO1 (Anoctamin 1)
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KIT mutation
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paclitaxel • imatinib • Sutent (sunitinib) • AiTan (rivoceranib) • Stivarga (regorafenib)
1m
New 2-oxoindole derivatives as multiple PDGFRα/ß and VEGFR-2 tyrosine kinase inhibitors. (PubMed, Bioorg Chem)
The in silico molecular-docking outcomes of scaffolds 6a-o and 9a-p in VEGFR-2, PDGFRα, and PDGFRβ active sites depicted their ability to adopt essential binding interactions like the reference Sunitinib. Our designed analogs, specifically 6f and 9f, possess promising antiproliferative and kinase inhibitory properties, making them potential candidates for further therapeutic development.
Journal
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PDGFRA (Platelet Derived Growth Factor Receptor Alpha) • KDR (Kinase insert domain receptor) • PDGFRB (Platelet Derived Growth Factor Receptor Beta) • CDK1 (Cyclin-dependent kinase 1) • CDKN1A (Cyclin-dependent kinase inhibitor 1A) • CCNB1 (Cyclin B1)
|
Sutent (sunitinib)
1m
Signaling Pathways of AXL Receptor Tyrosine Kinase Contribute to the Pathogenetic Mechanisms of Glioblastoma. (PubMed, Cells)
Indeed, despite the best treatments available including surgery, radiotherapy or a pharmacological approach with Temozolomide, glioblastoma patients' mortality is still high, within a few months of diagnosis...In the past, efforts to treat glioblastoma have mostly concentrated on customized treatment plans that target specific mutations such as epidermal growth factor receptor (EGFR) mutations, Neurotrophic Tyrosine Receptor Kinase (NTRK) fusions, or multiple receptors using multi-kinase inhibitors like Sunitinib and Regorafenib, with varying degrees of success...Activated AXL leads to a significant increase in tumor proliferation, tumor cell migration, and angiogenesis in different in vitro and in vivo models of cancer since this receptor regulates interplay with apoptotic, angiogenic and inflammatory pathways. Based on these premises, in this review we mainly focused on the role of AXL in the course of glioblastoma, considering its primary biological mechanisms and as a possible target for the application of the most recent treatments.
Review • Journal
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EGFR (Epidermal growth factor receptor) • AXL (AXL Receptor Tyrosine Kinase) • NTRK (Neurotrophic receptor tyrosine kinase)
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EGFR mutation
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Sutent (sunitinib) • temozolomide • Stivarga (regorafenib)
1m
BIRC6 Modulates the Protein Stability of Axin to Regulate the Growth, Stemness, and Resistance of Renal Cancer Cells via the β-Catenin Pathway. (PubMed, ACS Omega)
BIRC6 was also upregulated in cancer stem-like cells of RCC and increased the drug resistance of RCC cells against sunitinib...Pharmacological administration of a Wnt/β-catenin inhibitor, XAV-939, or genetic knockdown of β-catenin inhibited cell growth, tumor sphere formation, colony formation, migration, and invasion of BIRC6-overexpressed cells...In conclusion, we propose that BIRC6 activates the β-catenin signaling pathway via mediating the ubiquitination and degradation of Axin, promoting the growth, stemness, and drug resistance of RCC cells. This project aims to elucidate the role of BIRC6 as a potential therapeutic target and provide new insights into the clinical treatment of RCC.
Journal
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CXCR4 (Chemokine (C-X-C motif) receptor 4) • AXIN1 (Axin 1)
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Sutent (sunitinib) • XAV-939
1m
Sunitinib for metastatic progressive phaeochromocytomas and paragangliomas: results from FIRSTMAPPP, an academic, multicentre, international, randomised, placebo-controlled, double-blind, phase 2 trial. (PubMed, Lancet)
This first randomised trial supports the use of sunitinib as the medical option with the highest level of evidence for anti-tumour efficacy in progressive metastatic phaeochromocytomas and paragangliomas.
P2 data • Journal • Metastases
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SDHB (Succinate Dehydrogenase Complex Iron Sulfur Subunit B)
|
Sutent (sunitinib)
1m
Nilotinib in combination with sunitinib renders MCL-1 for degradation and activates autophagy that overcomes sunitinib resistance in renal cell carcinoma. (PubMed, Cell Oncol (Dordr))
Our findings revealed that a novel mechanism that nilotinib in combination with sunitinib overcomes sunitinib resistance in RCC. Therefore, this novel rational combination regimen provides a promising therapeutic avenue for metastatic RCC and rationale for evaluating this combination clinically.
Journal • Combination therapy
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MCL1 (Myeloid cell leukemia 1) • HUWE1 (HECT UBA And WWE Domain Containing E3 Ubiquitin Protein Ligase 1) • BECN1 (Beclin 1)
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Sutent (sunitinib) • Tasigna (nilotinib)
1m
ARRDC3 regulates the targeted therapy sensitivity of clear cell renal cell carcinoma by promoting AXL degradation. (PubMed, Cell Cycle)
Notably, ARRDC3 deficiency decreased the sunitinib sensitivity of clear cell renal cell carcinoma (ccRCC) cells in a manner dependent on the regulation of AXL stability. Overall, our results suggest that ARRDC3 is a negative regulator of AXL and can serve as a novel predictor of sunitinib therapeutic response in patients with ccRCC.
Journal
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AXL (AXL Receptor Tyrosine Kinase)
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AXL overexpression
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Sutent (sunitinib)
1m
Updated overall survival and safety with ripretinib vs sunitinib in patients with advanced gastrointestinal stromal tumor previously treated with imatinib and harboring KIT exon 11 + 17/18 mutations: ctDNA analysis from INTRIGUE (Sarcoma-RC 2024)
In this updated exploratory analysis from INTRIGUE, OS was longer for ripretinib vs sunitinib for pts with KIT exon 11 + 17/18 mutations identified by baseline ctDNA. The safety profile was consistent and more favorable for ripretinib vs sunitinib in these pts.
Clinical • Circulating tumor DNA • Stroma • Metastases
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KIT (KIT proto-oncogene, receptor tyrosine kinase)
|
KIT mutation • KIT exon 11 mutation • KIT exon 17 mutation
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Guardant360® CDx
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imatinib • Sutent (sunitinib) • Qinlock (ripretinib)
1m
PBRM1 loss is associated with increased sensitivity to MCL1 and CDK9 inhibition in clear cell renal cancer. (PubMed, Front Oncol)
Increased MCL1 activity has been described as a resistance mechanism to Sunitinib and Everolimus, two approved agents for ccRCC. PRT2527, a potent CDK9 inhibitor which depletes MCL1, was similarly efficacious in monotherapy and in combination with Sunitinib in PBRM1-loss cells. Taken together, these findings suggest PBRM1 loss is associated with MCL1i sensitivity in ccRCC and provide rationale for the evaluation of PRT1419 and PRT2527 for the treatment for PBRM1-deficient ccRCC.
Journal • IO biomarker
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BCL2 (B-cell CLL/lymphoma 2) • PBRM1 (Polybromo 1)
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PBRM1 mutation
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Sutent (sunitinib) • everolimus • PRT1419 • PRT2527
1m
Sunitinib in Patients With Breast Cancer With FGFR1 or FGFR2 Amplifications or Mutations: Results From the Targeted Agent and Profiling Utilization Registry Study. (PubMed, JCO Precis Oncol)
Sunitinib did not meet prespecified criteria to declare a signal of antitumor activity in patients with BC with either FGFR1 or FGFR2 alterations. Other treatments and clinical trials should be considered for these patient populations.
Journal
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FGFR2 (Fibroblast growth factor receptor 2) • FGFR1 (Fibroblast growth factor receptor 1)
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FGFR1 amplification • FGFR2 mutation • FGFR2 amplification
|
Sutent (sunitinib)
1m
Losartan + Sunitinib in Treatment of Osteosarcoma (clinicaltrials.gov)
P1, N=41, Recruiting, University of Colorado, Denver | Trial completion date: Feb 2025 --> Feb 2027 | Trial primary completion date: Feb 2024 --> Aug 2026
Trial completion date • Trial primary completion date • Combination therapy
|
Sutent (sunitinib)
1m
Efficacy and Safety of Famitinib Versus Sunitinib in the Treatment of Advanced Gastrointestinal Stromal Tumour Patients After Failure of Imatinib (clinicaltrials.gov)
P3, N=185, Terminated, Jiangsu HengRui Medicine Co., Ltd. | N=304 --> 185 | Recruiting --> Terminated; R&D strategy adjustment
Enrollment change • Trial termination • Stroma • Metastases
|
PDGFRA (Platelet Derived Growth Factor Receptor Alpha)
|
imatinib • Sutent (sunitinib) • famitinib (SHR 1020)
1m
TDM for Optimized Outcome in Patients With mRCC. (clinicaltrials.gov)
P=N/A, N=200, Recruiting, Aarhus University Hospital | N=400 --> 200 | Trial completion date: Nov 2023 --> May 2027 | Trial primary completion date: Dec 2022 --> Nov 2026
Enrollment change • Trial completion date • Trial primary completion date • Metastases
|
Opdivo (nivolumab) • Yervoy (ipilimumab) • sorafenib • Sutent (sunitinib)
2ms
Investigation of Gastrointestinal Toxicities Associated with Concurrent Abdominal Radiation Therapy and the Tyrosine Kinase Inhibitor Sunitinib in a Mouse Model. (PubMed, Int J Mol Sci)
Ki67+ density was not significant. In summary, we identify a lack of angiogenic response in irradiated GI tissues when abdominal RT is combined with a TKI, which may correlate with clinical toxicities seen in canine and human patients receiving combined treatment.
Preclinical • Journal
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CD31 (Platelet and endothelial cell adhesion molecule 1) • PECAM1 (Platelet And Endothelial Cell Adhesion Molecule 1)
|
Sutent (sunitinib)
2ms
Interaction between Wnt/β-catenin signaling pathway and EMT pathway mediates the mechanism of sunitinib resistance in renal cell carcinoma. (PubMed, BMC Cancer)
Sunitinib resistance and Twist overexpression can activate Wnt/β-catenin signaling pathway and EMT to promote the growth and metastasis of RCC cells.
Journal
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TCF4 (Transcription Factor 4)
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Sutent (sunitinib)
2ms
Exploring the anticancer potential of hydrogen sulfide and BAY‑876 on clear cell renal cell carcinoma cells: Uncovering novel mutations in VHL and KDR genes among ccRCC patients. (PubMed, Mol Clin Oncol)
The aim of the present study was to determine the cytotoxic effect of BAY-876 and NaSH alone or in combination with sunitinib against the 786-O cell line (renal adenocarcinoma)...Furthermore, direct sequencing results demonstrated unrecorded mutations of VHL and KDR genes is 43.7 and 31.5% of cases respectively. These findings confirmed the leading role of VHL gene in development of ccRCC and the crucial role of KDR gene in angiogenesis and drug resistance.
Journal
|
KDR (Kinase insert domain receptor) • VHL (von Hippel-Lindau tumor suppressor)
|
VHL mutation
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Sutent (sunitinib)
2ms
Pterostilbene and 6-shogaol exhibit inhibitory effects on sunitinib resistance and motility by suppressing the RLIP76-initiated Ras/ERK and Akt/mTOR pathways in renal cancer cells. (PubMed, Eur J Pharmacol)
In summary, PTE and 6-S induce apoptosis, enhance SUN sensitivity, and inhibit migration in both 786-O and 786-O SUNR cells. These novel findings demonstrate the potential of PTE and 6-S as target therapeutic adjuvants for RCC treatment.
Journal • IO biomarker
|
BCL2 (B-cell CLL/lymphoma 2) • BAX (BCL2-associated X protein)
|
Sutent (sunitinib)
2ms
Bioinformatics analysis identifies coagulation factor II receptor as a potential biomarker in stomach adenocarcinoma. (PubMed, Sci Rep)
Drug sensitivity analysis demonstrated positive correlations between F2R and several drugs, including BEZ235, CGP-60474, Dasatinib, HG-6-64-1, Aazopanib, Rapamycin, Sunitinib and TGX221, while negative correlation with CP724714, FH535, GSK1904529A, JNK-9L, LY317615, pyrimidine, rTRAIL and Vinorelbine. In conclusion, this study underscores the significance of F2R as a potential biomarker in gastric adenocarcinoma, shedding light on its molecular mechanisms in tumorigenesis. F2R holds promise for aiding in the diagnosis, prognosis, and targeted therapy of STAD.
Journal
|
TGFB1 (Transforming Growth Factor Beta 1)
|
dasatinib • Sutent (sunitinib) • dactolisib (RTB101) • vinorelbine tartrate • sirolimus • Kinenza (enzastaurin) • TGX-221
2ms
Integrating network pharmacology and drug side-effect data to explore mechanism of liver injury-induced by tyrosine kinase inhibitors. (PubMed, Comput Biol Med)
Thus, we focused on representative TKIs associated with severe hepatic adverse events, namely lapatinib, pazopanib, regorafenib, and sunitinib as objections of study, then integrated drug side-effect data from United State Food and Drug Administration (U.S. Based on the target prediction results of drugs and reactive metabolites, we also shed light on the association between toxic metabolites and severe hepatic adverse reactions, and thinking HSPA8, HSPA1A, CYP1A1, CYP1A2 and CYP3A4 were potential therapeutic or preventive targets against TKI-induced liver injury. In conclusion, our research provides comprehensive insights into the mechanism underlying severe liver injury caused by TKIs, offering a better understanding of how to enhance patient safety and treatment efficacy.
Journal • Adverse events
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CYP1A2 (Cytochrome P450, family 1, subfamily A, polypeptide 2) • CYP3A4 (Cytochrome P450, family 3, subfamily A, polypeptide 4) • HSPA1A (Heat Shock Protein Family A (Hsp70) Member 1A) • CYP1A1 (Cytochrome P450 Family 1 Subfamily A Member 1) • HSPA8 (Heat Shock Protein Family A (Hsp70) Member 8)
|
Sutent (sunitinib) • lapatinib • Votrient (pazopanib) • Stivarga (regorafenib)
2ms
N-Methyladenosine Regulator-Mediated Methylation Modification Patterns with Distinct Prognosis, Oxidative Stress, and Tumor Microenvironment in Renal Cell Carcinoma. (PubMed, Front Biosci (Landmark Ed))
This study analyzed the extensive regulatory mechanisms of m6A modification on oxidative stress, the tumor microenvironment, and immunity. Quantifying m6A scores may enhance immunotherapeutic effects and assist in developing more effective agents.
Journal • PD(L)-1 Biomarker • IO biomarker
|
MSI (Microsatellite instability)
|
PD-L1 expression
|
sorafenib • Sutent (sunitinib) • Votrient (pazopanib) • Inlyta (axitinib)
2ms
Utilizing a novel model of PANoptosis-related genes for enhanced prognosis and immune status prediction in kidney renal clear cell carcinoma. (PubMed, Apoptosis)
Finally, the risk model was predictive of response to immune checkpoint blockade, as well as sensitivity to sunitinib and paclitaxel. The PANoptosis-related risk model developed in this study enables accurate prognostic prediction in KIRC patients. Its associations with the tumor immune microenvironment and drug efficacy may offer potential therapeutic targets and inform clinical decisions.
Journal
|
BAP1 (BRCA1 Associated Protein 1) • CD4 (CD4 Molecule)
|
BAP1 mutation • VHL mutation
|
paclitaxel • Sutent (sunitinib)
2ms
Impact of sunitinib resistance on clear cell renal cell carcinoma therapeutic sensitivity in vitro. (PubMed, Cell Cycle)
However, the AMPK activator metformin appears to sensitize the effect of PD-L1 blocking therapeutic antibodies and to enhance CTLs' cytotoxic effects on ccRCC cells. These effects were not broadly observed with the Axl and the p38 inhibitors. Taken together, these data suggest that targeting certain pathways aberrantly activated by sunitinib resistance such as the AMPK/PDL1 axis might sensitize ccRCC to immunotherapies as a second-line therapeutic approach.
Preclinical • Journal • PD(L)-1 Biomarker • IO biomarker
|
AXL (AXL Receptor Tyrosine Kinase)
|
PD-L1 expression • AXL overexpression
|
Sutent (sunitinib) • metformin
2ms
1,2,4-Triazole-Tethered Indolinones as New Cancer-Fighting Small Molecules Targeting VEGFR-2: Synthesis, Biological Evaluations and Molecular Docking. (PubMed, Pharmaceuticals (Basel))
Based on Sunitinib, the FDA-approved VEGFR-2 inhibitor, novel indolin-2-one-triazole hybrids were designed and synthesized as anti-hepatocellular and anti-pancreatic cancer agents with VEGFR-2 inhibitory activity...The potent anti-cancer analogs 11d, 11e, 11g, 11k and 14c were evaluated for their VEGFR-2 inhibitory actions, where their IC values ranged from 16.3 to 119.6 nM compared to Sorafenib, which revealed an IC of 29.7 nM, having compound 11d as the most active analog. An in silico ADME study was performed to confirm the drug-likeness of the synthesized compounds. Finally, molecular docking simulation was conducted for the most potent VEGFR-2 inhibitor (11d), demonstrating the strong binding with the vital amino acid residues of the VEGFR-2 ATP binding site.
Journal
|
KDR (Kinase insert domain receptor)
|
sorafenib • Sutent (sunitinib)
2ms
Clinical Significance and Expression Pattern of RIP5 and VGLL4 in Clear Cell Renal Cell Carcinoma Patients Treated with Sunitinib. (PubMed, Biomedicines)
In addition, a high VGLL4 mRNA expression showed better overall survival in patients with ccRCC. In conclusion, high mRNA expression of RIP5 and VGLL4 are important markers of better survival rates in mRCC patients.
Journal
|
VGLL4 (Vestigial Like Family Member 4)
|
Sutent (sunitinib)
2ms
SAVOIR: Savolitinib vs. Sunitinib in MET-driven PRCC. (clinicaltrials.gov)
P3, N=60, Active, not recruiting, AstraZeneca | Trial completion date: Dec 2023 --> Dec 2024
Trial completion date • Metastases
|
VHL (von Hippel-Lindau tumor suppressor)
|
VHL mutation
|
Sutent (sunitinib) • Orpathys (savolitinib)
2ms
KIT-SNAP-tag/cell membrane chromatography model coupled with liquid chromatography-mass spectrometry for anti-GIST compound screening from Evodia rutaecarpa. (PubMed, Anal Bioanal Chem)
Gastrointestinal mesenchymal tumors, as the most common mesenchymal tumors in the gastrointestinal tract, are adjuvantly treated with multi-targeted tyrosine kinase inhibitors, such as imatinib and sunitinib, but there are problems of drug resistance and complex methods of monitoring therapeutic agents. In addition, the methyl thiazolyl tetrazolium assay validated the active effects of EVO and RUT in inhibiting the proliferation of high KIT-expressing cells in the ranges of 0.1-10 µmol/L and 0.1-50 µmol/L, respectively. In conclusion, the KIT-SNAP-tag/CMC could be a reliable model for screening antitumor components from complex systems.
Journal
|
KIT (KIT proto-oncogene, receptor tyrosine kinase)
|
KIT mutation • KIT expression
|
imatinib • Sutent (sunitinib)
2ms
SARC044: A Phase II Trial of Bezuclastinib in Combination With Sunitinib in Patients With GIST (clinicaltrials.gov)
P2, N=40, Not yet recruiting, Sarcoma Alliance for Research through Collaboration
New P2 trial • Combination therapy
|
Sutent (sunitinib) • bezuclastinib (PLX9486)
2ms
Outcomes of systemic treatment according to germline mutational status in patients with metastatic pheochromocytoma and paraganglioma. (PubMed, Clin Genitourin Cancer)
Our study reveals that CVD and sunitinib are effective treatments for metastatic PPGLs. The results are consistent with previous studies and patients with SDHB and SDHD mutations may benefit most from CVD treatment.
Clinical • Journal • Metastases
|
SDHB (Succinate Dehydrogenase Complex Iron Sulfur Subunit B) • SDHD (Succinate Dehydrogenase Complex Subunit D)
|
SDHB mutation • SDHB mutation + SDHD mutation
|
Sutent (sunitinib) • cyclophosphamide • vincristine • dacarbazine