U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

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Showing 21 - 30 of 124 results

Saracatinib (AZD0530) is an oral, dual inhibitor of c-Src/Abl kinases initially developed by AstraZeneca for the treatment of cancer. The drug was tested for many neoplasms and reached phase III for ovarian cancer (in combination with paclitaxel), however without demonstrating any significant effect. Sarcatinib is also tested in patients with Alzheimer's Disease (Phase II). Its effect on Alzheimer's Disease patients is explained by inhibition of another kinase, Fyn, which is highly expressed in brain.
Status:
Investigational
Source:
INN:ceralasertib [INN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


Ceralasertib, previously known as AZD6738, a potent and selective inhibitor of ataxia telangiectasia and Rad3-related (ATR) kinase was developed as an anticancer agent. Prevention of ATR-mediated signaling leads to the inhibition of DNA damage checkpoint activation, disruption of DNA damage repair, and the induction of tumor cell apoptosis. AZD6738 as a combination therapy participates in phase II clinical trials for the treatment of gastric adenocarcinoma and malignant melanoma (in combination with durvalumab). For the treatment of gastric and breast cancer in combination with carboplatin, or with olaparib or with MEDI4736. Combination of acalabrutinib and AZ6738 is used in phase II trials for patients with chronic lymphocytic Leukemia. Besides, AZD6738 participates in umbrella Phase II study in patients with metastatic non-small cell lung cancer (NSCLC) who have progressed on an anti-programmed cell death-1/anti-programmed cell death ligand 1 (anti-PD-1/PD-L1) containing therapy.
Status:
Investigational
Source:
NCT04550104: Phase 1 Interventional Recruiting Non Small Cell Lung Cancer
(2021)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Status:
Investigational
Source:
NCT00853450: Phase 1 Interventional Completed Antiplatelet Effect
(2009)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


Conditions:

AZD-6482 is being developed by AstraZeneca to evaluate its therapeutic effects in the treatment of thrombosis. AZD-6482 is essentially a PI3K-beta inhibitor. It is a PI3Kβ inhibitor with IC50 of 10 nM, 8-, 87- and 109-fold more selective to PI3Kβ than PI3Kδ, PI3Kα and PI3Kγ in cell-free assays. by targeting PI3Kβ, AZD-6482 specifically inhibits thrombosis without interfering with normal haemostasis. Therefore, AZD-6482 is used as an anti-thrombotic drug for the prophylaxis of thrombotic disorders. AZD-6482 was in phase I trials by AstraZeneca for the prevention of thrombosis. However, the study was discontinued.
Status:
Investigational
Source:
INN:zorifertinib [INN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



AZD-3759 is an oral inhibitor of both wild-type and mutant EGFR with IC50 values in nanomolar range. The drug was discovered by AstraZeneca for the treatment of non-small-cell lung cancer with CNS metastases. AZD-3759 can penetrate the blood-brain barrier and was confirmed to be effective in vitro with NSCLC cell lines as well as in mouse model of brain metastases. AZD-3759 is currently in Phase 1 clinical trial.
Status:
Investigational
Source:
NCT00520572: Phase 2 Interventional Completed Rheumatoid Arthritis
(2007)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


AZD9056 was developed as a selective inhibitor of the purinergic receptor P2X7, a key player in the generation and secretion of several proinflammatory cytokines. AZD 9056 participated is phase II clinical trials for osteoarthritis, inflammatory bowel disease, and chronic obstructive pulmonary disease but these studies were discontinued in 2009 because the drug failed to show significant efficacy in trials. In addition, in 2015 AZD 9056 was studied for the treatment of Crohn's disease (CD), although the drug has shown a beneficial risk profile the lack in the change of inflammatory biomarkers questions its anti-inflammatory potential.
Status:
Investigational
Source:
NCT01668550: Phase 1 Interventional Terminated Advanced Solid Tumours
(2012)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

AZD0424, a dual selective Src/Abl kinase inhibitor that has shown evidence of anti-tumor activity in pre-clinical studies. AZD0424 participated in phase I clinical trials in patients with advanced solid tumors, but this study was terminated because of insufficient evidence of efficacy as monotherapy.
Vistusertib (AZ-2014) is a dual inhibitor of mTORC1/mTORC2 which was developed by AstraZeneca for the treatment of cancer. The drug is under clinical development (phase II) in patients with Renal Carcinoma, Squamous Non Small Cell Lung Cancer, Diffuse Large B-Cell Lymphoma, Meningioma, Breast cancer and Gastric cancer, either alone or in combination therapy. Vistusertib penetrates blood-brain barrier.
Status:
Investigational
Source:
NCT01348737: Phase 1 Interventional Completed Alzheimer's Disease
(2011)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



AZD3839 is a potent and selective BACE1 inhibitor with about 14-fold selectivity over BACE2. In SH-SY5Y cells, AZD3839 efficiently decreases the Aβ40 levels and decreases the formation of sAPPβ. AZD3839 also decreases the Aβ40 levels secreted from C57BL/6 mouse primary cortical neurons, N2A cells, and Dunkin-Hartley guinea pig primary cortical neurons. AZD3839 causes in vitro BACE1 inhibition in the cell assay with the IC50 value of 16.7 nM. In C57BL/6 mice, AZD3839 (69 mg/kg, p.o.) causes a dose- and time-dependent reduction of plasma and brain Aβ. In guinea pig and non-human primates, AZD3839 also inhibits Aβ generation. AZD3839 has been used in phase I clinical trials studying the basic science of Safety and Tolerability. However future development has been discontinued.
Status:
Investigational
Source:
NCT03236974: Phase 1 Interventional Completed Postmenopausal Women With ER+ HER2- Primary Breast Cancer
(2017)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


AZD 9496 was discovered by AstraZeneca as a potent and selective estrogen receptor downregulator (SERD). This drug participated in phase I clinical trials to evaluate the pharmacokinetic profiles and the safety and tolerability of the different forms, formulations, and doses for the treatment of patients with breast cancer.