What is AZD5363?
AZD5363 binds to and inhibits all AKT isoforms. Inhibition of AKT prevents the phosphorylation of AKT substrates that mediate cellular processes, such as cell division, apoptosis, and glucose and fatty acid metabolism.
What is capivasertib?
A novel pyrrolopyrimidine derivative, and an orally available inhibitor of the serine/threonine protein kinase AKT (protein kinase B) with potential antineoplastic activity. Capivasertib binds to and inhibits all AKT isoforms.
How does Capivasertib work?
Research collaborations. Capivasertib is a leading targeted inhibitor of the cancer-driving protein AKT, also known as PKB. The protein is a key node in a signalling network that becomes dysregulated in a range of cancers and helps to drive the disease.
What is AZD9833?
More about this trial These are called oestrogen receptor positive breast cancer. Doctors think that AZD9833 can reduce the amount of oestrogen in your body and stop breast cancer from growing. This is the first time that AZD9833 will be given to people. Everyone taking part in this trial has AZD9833.
What is AZD1775?
AZD1775 is a highly selective, potent, ATP competitive, small molecule inhibitor of Wee1 kinase with an enzyme IC50 of 5.18 nM. In vitro, AZD1775 inhibits Wee1 activity and induces DNA damage as well as G2 checkpoint escape in cell-based assays with an EC50 of about 80 nM.
Is Tremelimumab approved?
Tremelimumab — which has no brand name yet — has not been approved by the U.S. Food and Drug Administration (FDA) to treat any cancer or disease. In April 2015, tremelimumab received orphan drug designation by the FDA to treat mesothelioma.
How is AKT inhibited?
Akt is dephosphorylated by protein phosphatase 2A (PP2A) and the PH domain leucine-rich-repeat-containing protein phosphatase 1/2 (PHLPP2). In addition, the tumor suppressor, phosphatase and tensin homolog (PTEN), inhibits Akt activity by dephosphorylating PIP3 (20).
Is Adavosertib FDA approved?
Since 2014, olaparib has received FDA approval in other indications for ovarian cancer, including a May 2020 approval for maintenance treatment, either as a monotherapy or in combination with bevacizumab.
Is Adavosertib cytotoxic?
Adavosertib (MK1775 or AZD1775; MW=501Da) is a novel Wee-1 inhibitor with in vitro cytotoxicity against GBM cell lines (IC50 68–695nM) .
Is Tremelimumab FDA approved?
What is capivasertib (AZD5363)?
This study looked at a drug called capivasertib (AZD5363) for people who had a solid tumour that had got worse despite treatment. A solid tumour is any type of cancer apart from cancer of the blood or lymphatic system such as:
Can AZD5363 be combined with a weekly intravenous infusion?
This is a Phase I/II multicentre, study investigating the safety, tolerability and efficacy of a twice-daily oral formulation of AZD5363 when combined with a weekly intravenous paclitaxel infusion in patients with advanced or metastatic breast cancer.
Does PI3K/AKT/mTOR signaling interact with estrogen receptors in breast cancer?
PI3K/AKT/mTOR signaling plays an important role in breast cancer. Its interaction with estrogen receptor (ER) signaling becomes more complex and interdependent with acquired endocrine resistance.