saracatinib

inhibits c-Src and Abl kinases

Also Known As:

4-Quinazolinamine, N-(5-chloro-1,3-benzodioxol-4-yl)-7-(2-(4-methyl-1- piperazinyl)ethoxy)-5-((tetrahydro-2H-pyran-4-yl)oxy)-; AZD 0530; AZD-0530; AZD0530; AZD0530 Difumarate; N-(5-chloro-1,3-benzodioxol-4-yl)-7-(2-(4-methylpiperazin-1-yl)ethoxy)-5-((tetrahydro- 2H-pyran-4-yl)oxy)quinazolin-4-amine bi((2E)-but-2-enedioate); N-(5-chloro-1,3-benzodioxol-4-yl)-7-(2-(4-methylpiperazin-1-yl)ethoxy)-5-(tetrahydro-2H-pyran-4-yloxy)quinazolin-4-amine; saracatinib difumerate; N-(5-Chloro-1,3-benzodioxol-4-yl)-7-(2-(4-methyl-1-piperazinyl)ethoxy)-5-(tetrahydro-2H-pyran-4-yloxy)-4-quinazolinamine

Networked: 156 relevant articles (24 outcomes, 51 trials/studies)

Relationship Network

Bio-Agent Context: Research Results

Heterocyclic Compounds: 198
- 1-Ring Heterocyclic Compounds
  - Dioxoles
    - Benzodioxoles: 3
      - saracatinib: 156
- Fused-Ring Heterocyclic Compounds
  - 2-Ring Heterocyclic Compounds
    - Quinazolines: 402
      - saracatinib: 156
    - Benzodioxoles: 3
      - saracatinib: 156

Experts

1.	Green, Tim P: 9 articles (07/2010 - 11/2006)
2.	Elvin, Paul: 6 articles (01/2013 - 06/2009)
3.	Evans, Christopher P: 6 articles (06/2010 - 04/2008)
4.	Kung, Hsing-Jien: 5 articles (06/2010 - 04/2008)
5.	Thippeswamy, Thimmasettappa: 4 articles (12/2021 - 01/2018)
6.	Messersmith, Wells A: 4 articles (10/2012 - 06/2009)
7.	Lang, Liwei: 3 articles (01/2022 - 01/2018)
8.	Teng, Yong: 3 articles (01/2022 - 01/2018)
9.	Putra, Marson: 3 articles (12/2021 - 01/2018)
10.	Strittmatter, Stephen M: 3 articles (12/2019 - 01/2015)

Related Diseases

1.	Neoplasms (Cancer) 04/01/2017 - "Furthermore, SRC inhibition by AZD0530 was effective in ALK-resistant cancer cells. " 07/01/2015 - "Src plays a role in normal thymic epithelial maturation, and its inhibition with the oral compound saracatinib was postulated to be effective in controlling thymic malignancy. " 07/10/2018 - "Potent inhibitors of PI3K (GDC-0941) and Src (Saracatinib) exhibit as individual agents, excellent oral anticancer activity in preclinical models and have entered phase II clinical trials in various cancers. " 04/01/2012 - "In a Phase I study in patients with advanced solid malignancies resistant to standard treatment we assessed the effect of saracatinib on bone turnover. " 10/01/2010 - "Phase I safety, pharmacokinetics, and inhibition of SRC activity study of saracatinib in patients with solid tumors."
2.	Colorectal Neoplasms (Colorectal Cancer) 05/01/2012 - "We used colorectal cancer cell lines and a patient-derived explant model to investigate the efficacy of saracatinib. " 08/01/2015 - "Saracatinib is a novel oral Src kinase inhibitor that was well tolerated but failed to meet its primary endpoint of improvement in 4 month progression-free survival as a single agent in previously treated metastatic colorectal cancer patients." 08/01/2015 - "Phase II study of saracatinib (AZD0530) in patients with previously treated metastatic colorectal cancer." 07/15/2010 - "The SFK inhibitor saracatinib (AZD0530) is currently in phase II trials in patients including those with colorectal cancer (CRC), where links between SFK activity and poor prognosis are particularly striking. " 08/15/2010 - "To evaluate the efficacy of saracatinib (AZD0530), an oral Src inhibitor, in colorectal cancer (CRC) and to identify biomarkers that predict antitumor activity. "
3.	Bone Resorption 04/01/2012 - "Bone resorption markers were significantly decreased by saracatinib. " 03/01/2010 - "Saracatinib is a potentially useful treatment for diseases characterized by increased bone resorption, such as metastatic bone disease and osteoporosis." 12/01/2019 - "Pharmacokinetic measurements confirmed appropriate plasma levels of drug in the saracatinib-treated group and Src inhibition was achieved clinically by a significant reduction in the bone resorption biomarker serum cross-linked C-terminal telopeptide of type I collagen. " 04/01/2008 - "The pyrrolo-pyrimidines CGP77675 and CGP76030 proved to be effective in preventing bone loss in animal models, while the effect of AZD0530, a dually active inhibitor of c-Src and Bcr-ABL, on bone resorption, has been tested in a Phase I clinical trials with promising results. "
4.	Neoplasm Metastasis (Metastasis) 02/15/2016 - "This study was unable to determine if saracatinib had potential as metastasis inhibitor. " 02/15/2016 - "Metastasis inhibition by saracatinib may still be viable in an earlier time in the disease history." 11/01/2010 - "Functions required for metastasis, such as migration and invasion, were reduced when cells were exposed to 0.5 μM and 1.0 μM saracatinib, respectively (p<0.0001). " 11/01/2017 - "In a Halsted mastectomy model, AZD0530 had no efficacy against lung metastases or difference in survival. " 01/01/2020 - "The primary goal of this study was to determine if treatment with saracatinib could increase progression-free survival (PFS) for patients who have undergone complete resection of osteosarcoma lung metastases in a double-blinded, placebo-controlled trial. "
5.	Squamous Cell Carcinoma of Head and Neck 01/01/2011 - "Single-agent saracatinib does not merit further study in recurrent or metastatic HNSCC." 11/30/2009 - "The anti-proliferative and anti-invasive effects of saracatinib on HNSCC cell lines were therefore investigated in pre-clinical cell and mouse model systems. " 11/30/2009 - "Saracatinib Impairs Head and Neck Squamous Cell Carcinoma Invasion by Disrupting Invadopodia Function." 01/01/2022 - "Evaluation of the Efficacy of Saracatinib-Loaded Nanoparticles in Lymphatic Metastases of HNSCC with the Aid of Bioluminescence Imaging." 01/01/2011 - "A phase II study was conducted to evaluate saracatinib in patients with recurrent or metastatic head and neck squamous cell cancer (HNSCC). "

Related Drugs and Biologics

1.	saracatinib
2.	src-Family Kinases
3.	Biomarkers (Surrogate Marker)
4.	Phosphotransferases (Kinase)
5.	Dasatinib (BMS 354825)
6.	Paclitaxel (Taxol)
7.	Proto-Oncogene Proteins c-fyn
8.	Mitogen-Activated Protein Kinase Kinases (MEKs)
9.	Platinum
10.	Kainic Acid (Kainate)

Related Therapies and Procedures

1.	Therapeutics
2.	Radical Mastectomy
3.	Castration
4.	Drug Therapy (Chemotherapy)
5.	Stents