sapitinib (AZD8931) / AstraZeneca - LARVOL DELTA

Graph-Based Multi-Omics Integration Reveals Prognostic Histone Modification Reader Genes and Candidate Drug Targets in Colorectal Cancer. (PubMed, Genes (Basel)) - "This work constructs an epigenetic immune regulatory network and a four-gene signature, offering promising biomarkers and actionable therapeutic targets for precision immunotherapy against CRC."

Biomarker • IO biomarker • Journal • Colorectal Cancer • Oncology • Solid Tumor • CUL7 • GPC1

Integration of Bulk RNA Sequencing and Single-Cell Sequencing to Identify Prognostic Genes Associated With MCDRGs in Neuroblastoma. (PubMed, FASEB J) - "Ribosome biogenesis and cell cycle-related pathways were enriched in the HRG, which displayed higher sensitivity to entinostat and sapitinib. This model systematically reveals the comprehensive mechanisms by which MCDRGs influence prognosis through regulating the TME, cell-cell interactions, and therapeutic responses. These findings provide a new theoretical basis and potential targets for precise risk stratification and individualized treatment strategies in NB."

Biomarker • Journal • Neuroblastoma • Oncology • Pediatrics • Solid Tumor • TRIB1

A novel mitochondrial-related signature to decode tumor immunity and predict survival in chromophobe renal cell carcinoma. (PubMed, Immunobiology) - "Notably, our computational analysis based on GDSC's pRRophetic algorithm suggests that LCL161 and UMI-77 may be more effective in the low-risk group, while sapitinib and luminespib show potential efficacy in the high-risk group. In conclusion, our study indicates this model holds high promise as a reliable biomarker for outcome prediction and precision-medicine stratification in chRCC patients."

Journal • Tumor mutational burden • Genito-urinary Cancer • Kidney Cancer • Oncology • Renal Cell Carcinoma • Solid Tumor • RECQL4 • TERF1

HER3 mediates metabolic reprogramming in metastatic colorectal and pancreatic cancer (AACR 2026) - "We performed in vitro synergy studies combining HER3i (Sapitinib) with oxidative phosphorylation (OXPHOS) inhibitors (metformin and ivosedinib). We identified the HER3-AKT/RSK-PFK2 axis as a promoter of glycolysis and growth in CRC/PC liver metastases. Leveraging the discovery of metabolic shifting towards OXPHOS caused by HER3 inhibition, we identified a potential therapeutic strategy of combining HER3 inhibitors and OXPHOS inhibitors for treating patients with mCRC/mPC."

Metastases • Colorectal Cancer • Oncology • Pancreatic Cancer • Solid Tumor • ERBB3 • LRG1 • NRG1

HER3 inhibition sensitizes metastatic colorectal and pancreatic cancer to immunotherapy (AACR 2026) - "More importantly, therapeutic efficacy was assessed by treating these models with HER3 inhibitor sapitinib and/or anti-PD-1 antibodies. LC-MS analysis revealed that mCRC/mPC exhibited significantly elevated glycolytic metabolites compared to primary tumors, with HER3 inhibition reversing this metabolic reprogramming... We identify a novel HER3-PFK2-lactate metabolic axis that promotes immunosuppression in CRC/PC liver metastases. Targeting this pathway sensitizes CRC/PC liver metastases to checkpoint blockade, offering a promising strategy to extend immunotherapy benefits beyond the limited patient population currently responsive to ICIs."

IO biomarker • Metastases • Colorectal Cancer • Oncology • Pancreatic Cancer • Solid Tumor • CD8 • GZMB • LRG1 • NRG1

Co-targeting the HER family and mutant KRAS is efficacious in colorectal cancer (AACR 2025) - "We have found that there is a striking increase in total HER3 levels in SNU-407, LS180, LS513 cells and 572918-348-R and 172845-121-B patient derived organoids (PDOs) when treated with the KRASG12D inhibitorsMRTX1133 and RMC9805, creating an adaptive response that could limit the efficacy of a KRAS inhibitor as a single agent...Co-targeting EGFR and mutant KRAS resulted in a slight synergistic effect in KRASG12D mutant cell lines usingMRTX1133 in combination with sapitinib, afatinib or peltinib. Currently, we are assessing if there is a synergistic effect directly targeting HER3 with a HER3 antibody-drug-conjugate in combination with a KRAS inhibitor in CRC cells. Our findings may present a new paradigm for targeted combination therapies in colorectal cancer with the eventual goal of increased overall patient survival."

Colorectal Cancer • Oncology • Solid Tumor • EGFR • ERBB4 • HER-2 • KRAS

SLC28A1 inhibits clear cell renal cell carcinoma progression by affecting arachidonic acid metabolism: A novel nucleoside transporter-based targeted therapy strategy. (PubMed, Cancer Lett) - "The efficacy of sapitinib was further enhanced through targeted nanoparticle delivery, significantly inhibiting tumor growth in both in vitro and in vivo models while ensuring biosafety. In conclusion, this research elucidates the mechanism by which SLC28A1 exerts its inhibitory effect in ccRCC and proposes a promising targeted nanotherapeutic approach, offering new insights and strategies for the management of ccRCC."

Journal • Clear Cell Renal Cell Carcinoma • Genito-urinary Cancer • Oncology • Solid Tumor

Exploring prognostic genes related to lactylation and programmed cell death in pancreatic ductal adenocarcinoma: a comprehensive study combining bulk transcriptomics and experimental verification. (PubMed, Front Genet) - "Drug sensitivity analysis revealed that Sapitinib was more effective in the high-risk group (HRG), while Doramapimod was more effective in the low-risk group (LRG) (P < 0.0001)...Finally, genes in the clinical samples also showed the same expression trend. In the present investigation, two prognostic genes were identified, and subsequently, a predictive risk model was established, which may serve as a valuable reference for the clinical management of PDAC."

Journal • Oncology • Pancreatic Cancer • Pancreatic Ductal Adenocarcinoma • HMGA1 • KIF2C

SAFIR02_Breast - Efficacy of Genome Analysis as a Therapeutic Decision Tool for Patients With Metastatic Breast Cancer (clinicaltrials.gov) - P2 | N=1460 | Recruiting | Sponsor: UNICANCER | Trial completion date: Jun 2021 ➔ Dec 2022 | Trial primary completion date: Jun 2019 ➔ Dec 2021

IO biomarker • Trial completion date • Trial primary completion date

SAFIR02_Breast - Efficacy of Genome Analysis as a Therapeutic Decision Tool for Patients With Metastatic Breast Cancer (clinicaltrials.gov) - P2 | N=1460 | Active, not recruiting | Sponsor: UNICANCER | Trial completion date: Dec 2023 ➔ Dec 2024

IO biomarker • Trial completion date • Breast Cancer • Oncology • Solid Tumor

SAFIR02_Breast - Efficacy of Genome Analysis as a Therapeutic Decision Tool for Patients With Metastatic Breast Cancer (clinicaltrials.gov) - P2 | N=1460 | Active, not recruiting | Sponsor: UNICANCER | Recruiting ➔ Active, not recruiting

Enrollment closed • IO biomarker • Breast Cancer • Oncology • Solid Tumor

SAFIR02_Breast - Efficacy of Genome Analysis as a Therapeutic Decision Tool for Patients With Metastatic Breast Cancer (clinicaltrials.gov) - P2 | N=1460 | Active, not recruiting | Sponsor: UNICANCER | Trial completion date: Dec 2022 ➔ Dec 2023

IO biomarker • Trial completion date • Breast Cancer • Oncology • Solid Tumor

SAFIR02_Breast - Efficacy of Genome Analysis as a Therapeutic Decision Tool for Patients With Metastatic Breast Cancer (clinicaltrials.gov) - P2 | N=1460 | Recruiting | Sponsor: UNICANCER | N=460 ➔ 1460 | Trial primary completion date: Oct 2016 ➔ Jun 2019

Enrollment change • IO biomarker • Trial primary completion date • Breast Cancer • Oncology • Solid Tumor

SAFIR02_Breast - Efficacy of Genome Analysis as a Therapeutic Decision Tool for Patients With Metastatic Breast Cancer (clinicaltrials.gov) - P2 | N=460 | Recruiting | Sponsor: UNICANCER

IO biomarker • New P2 trial • Breast Cancer • Oncology • Solid Tumor

SAFIR02_Breast - Efficacy of Genome Analysis as a Therapeutic Decision Tool for Patients With Metastatic Breast Cancer (clinicaltrials.gov) - P2 | N=1460 | Active, not recruiting | Sponsor: UNICANCER | Trial completion date: Dec 2024 ➔ Dec 2025

IO biomarker • Trial completion date • Breast Cancer • Oncology • Solid Tumor

SAFIR02_Breast - Efficacy of Genome Analysis as a Therapeutic Decision Tool for Patients With Metastatic Breast Cancer (clinicaltrials.gov) - P2 | N=1460 | Active, not recruiting | Sponsor: UNICANCER | Trial primary completion date: Dec 2021 ➔ Dec 2022

IO biomarker • Trial primary completion date • Breast Cancer • Oncology • Solid Tumor

Construction and validation of golgi apparatus-related genes as predictors of the immune microenvironment and prognosis in colorectal cancer. (PubMed, Transl Oncol) - "Collectively, our work links GARG expression to CRC prognosis and immune features, and functionally implicates GDI1 in tumor cell aggressiveness, supporting its further study as a potential therapeutic target."

Journal • Colorectal Cancer • Oncology • Solid Tumor • GDI1 • TNFA

KIF5B-driven unfolded protein response reprograms breast cancer immunosuppressive microenvironment for single-cell guided therapeutic targeting. (PubMed, Discov Oncol) - "Our multimodal analysis establishes KIF5B as a prognostic biomarker and potential therapeutic target in BRCA, with implications for understanding immune evasion and guiding precision treatment strategies."

Journal • Breast Cancer • Oncology • Solid Tumor • BRCA • KIF5B

Novel hypoxia-immune biomarkers predict response to neoadjuvant chemotherapy in patients with laryngo-hypopharyngeal cancer. (PubMed, Eur J Med Res) - "Our hypoxia-immune panel can accurately predict response to NAC and OS in patients with LHC and may have implications for the development of novel biomarkers and targeted therapies."

Biomarker • Journal • Head and Neck Cancer • Hypopharyngeal Cancer • Oncology • Solid Tumor • AREG

A Riskscore Model for Predicting Survival, Tumor Microenvironment, Immunotherapy and Drug Sensitivity of Lung Squamous Cell Carcinoma Based on PI3K/AKT/MTOR Pathway-Related Genes. (PubMed, J Environ Pathol Toxicol Oncol) - "LR group had lower TIDE scores and lower IC50 values (Alpelisib, Ibrutinib, Sapitinib, and Savolitinib). Patients in LR group had potential advantages in survival, immune response, and drug sensitivity. In summary, the results offered new insights into prognosis prediction, immunotherapy, and personalized treatment of LUSC."

Biomarker • Journal • Non Small Cell Lung Cancer • Oncology • Squamous Cell Carcinoma • CAB39 • CDKN1A • TRIB3

Identification and validation of prognostic genes associated with mitochondrial nuclear genes in gastric cancer. (PubMed, Clin Exp Med) - "BMS-754807, Gefitinib, JQ1, Lapatinib, and Sapitinib exhibited significant differences in sensitivity between the high-risk group and the low-risk group. The results of molecular docking showed TP8A2 has stable binding ability with cytosine, COX15 with indomethacin, and TARS2 with bisacodyl. RT-qPCR revealed downregulation of ATP8A2 and upregulation of COX15 and TARS2 in GC samples. MNGs, including ATP8A2, COX15, and TARS2, demonstrated significant associations with immune infiltration, CNV, and prognostic outcomes of GC."

Biomarker • Journal • Gastric Cancer • Oncology • Solid Tumor

Immunogenic cell death-related genes as prognostic biomarkers and therapeutic insights in uterine corpus endometrial carcinoma: an integrative bioinformatics analysis. (PubMed, Front Oncol) - "Finally, we found that hyper-immunogenicity may be sensitive to immunotherapy and certain drugs (AZD5991, Ibrutinib, Osimertinib, AGI-5198, Savolitinib, Sapitinib, AZ960, AZD3759 and Ruxolitinib), while PCI-34051 and Vorinostat showed sensitivity in patients with hypo-immunogenicity. Our results demonstrate that ICD plays an important role in UCEC progression, suggesting that ICD-related markers could serve as potential targets for prognosis and treatment."

Biomarker • IO biomarker • Journal • Tumor mutational burden • Endometrial Cancer • Oncology • Solid Tumor • Uterine Cancer • CD52 • STAT1 • TMB

Identification of anoikis-related genes to develop a risk model and predict the prognosis and tumor microenvironment in rectal adenocarcinoma. (PubMed, Front Genet) - "Drug sensitivity analysis revealed differences in the IC50 values of OSI-027, PLX-4720, UMI-77, and Sapitinib between the high-risk and low-risk groups. Enrichment analysis revealed that these prognostic ARGs were primarily enriched in pathways and biological processes related to tumorigenesis. The risk model of ARGs can effectively predict READ prognosis and provide potential therapeutic targets."

Biomarker • Journal • Colorectal Adenocarcinoma • Colorectal Cancer • Oncology • Rectal Adenocarcinoma • Solid Tumor • ALDH1A1 • BRCA1 • KRT17

Multi-Omics Integration: Predicting Progression and Optimizing Clinical Treatment of Hepatocellular Carcinoma Through Malignant-Cell-Related Genes. (PubMed, Int J Mol Sci) - "Risk stratification based on these signatures revealed distinct therapeutic vulnerabilities: high-risk patients showed increased sensitivity to sorafenib, while low-risk patients exhibited enhanced responses to immunotherapy and transarterial chemoembolization (TACE). Pharmacogenomic analysis with Oncopredict identified four chemotherapeutic agents, including sapitinib and dinaciclib, with risk-dependent efficacy patterns. Furthermore, CRISPR/Cas9-dependency screening prioritized SRSF7 as essential for HCC cell survival, a finding confirmed by the identification of protein-level overexpression in tumors via immunohistochemistry. This multi-omics framework bridges single-cell characterization to clinical decision-making, offering a clinically actionable prognostic system that can be used to optimize therapeutic selection in HCC management."

Biomarker • IO biomarker • Journal • Hepatocellular Cancer • Oncology • Solid Tumor • SRSF7

Multi‑cohort Validation Based on Disulfidptosis-Related lncRNAs for Predicting Prognosis and Immunotherapy Response of Esophageal Squamous Cell Carcinoma. (PubMed, Onco Targets Ther) - "Additionally, individuals at high risk showed higher sensitivity to erlotinib, acetalax, gefitinib, lapatinib, sapitinib, and afatinib. Nevertheless, this study is retrospective and relies on public databases, with a limited sample size within the datasets. In the future, it is essential to conduct more extensive validation of the prognostic value and efficacy in real ESCC cohorts."

IO biomarker • Journal • Tumor mutational burden • Esophageal Cancer • Esophageal Squamous Cell Carcinoma • Oncology • Squamous Cell Carcinoma • TMB