Eganelisib
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Eganelisib ( USAN), codenamed IPI-549, is an experimental drug being investigated as a possible treatment for
cancer Cancer is a group of diseases involving abnormal cell growth with the potential to invade or spread to other parts of the body. These contrast with benign tumors, which do not spread. Possible signs and symptoms include a lump, abnormal b ...
. It is a highly selective
phosphoinositide 3-kinase inhibitor Phosphoinositide 3-kinase inhibitors (PI3K inhibitors) are a class of medical drugs that are mainly used to treat advanced cancers. They function by inhibiting one or more of the phosphoinositide 3-kinase (PI3K) enzymes, which are part of the PI3 ...
, and thus works by inhibiting the
enzyme Enzymes () are proteins that act as biological catalysts by accelerating chemical reactions. The molecules upon which enzymes may act are called substrates, and the enzyme converts the substrates into different molecules known as products. A ...
PIK3CG Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit gamma isoform is an enzyme that in humans is encoded by the ''PIK3CG'' gene. Function This gene encodes a protein that belongs to the pi3/pi4-kinase family of proteins. The gene p ...
, disrupting the PI3K/AKT/mTOR signaling pathway which plays important roles in the development of cancer. Eganelisib is being developed by Infinity Pharmaceuticals. Early
clinical trial Clinical trials are prospective biomedical or behavioral research studies on human participants designed to answer specific questions about biomedical or behavioral interventions, including new treatments (such as novel vaccines, drugs, dietar ...
results were published in September 2016. On September 29, 2020, it was granted Fast Track designation by the United States Food and Drug Administration (FDA) as a treatment for inoperable, locally advanced, or metastatic
triple-negative breast cancer Triple-negative breast cancer (TNBC) is any breast cancer that lacks or show low levels of estrogen receptor (ER), progesterone receptor (PR) and human epidermal growth factor receptor 2 (HER2) overexpression and/or gene amplification (i.e. the tum ...
, combined with a
checkpoint inhibitor Checkpoint inhibitor therapy is a form of cancer immunotherapy. The therapy targets immune checkpoints, key regulators of the immune system that when stimulated can dampen the immune response to an immunologic stimulus. Some cancers can protect the ...
and
chemotherapy Chemotherapy (often abbreviated to chemo and sometimes CTX or CTx) is a type of cancer treatment that uses one or more anti-cancer drugs (chemotherapeutic agents or alkylating agents) as part of a standardized chemotherapy regimen. Chemotherap ...
. , five phase I/II
clinical trial Clinical trials are prospective biomedical or behavioral research studies on human participants designed to answer specific questions about biomedical or behavioral interventions, including new treatments (such as novel vaccines, drugs, dietar ...
s were ongoing in the United States, and one in Europe.


References


Further reading

* {{Portal bar , Medicine Antineoplastic drugs Experimental drugs Phosphoinositide 3-kinase inhibitors Pyrazoles Amines Amides Pyrimidines