Contents

Eganelisib

Chemical compound

Eganelisib

Clinical data
Routes of administration	Oral
ATC code	None
Identifiers
IUPAC name 2-amino-N-[(1S)-1-{8-[(1-methyl-1H-pyrazol-4-yl)ethynyl]-1-oxo-2-phenyl-1,2-dihydroisoquinolin-3-yl}ethyl]pyrazolo[1,5-a]pyrimidine-3-carboxamide
CAS Number	1693758-51-8
PubChem CID	91933883
ChemSpider	60600433
UNII	FOF5155FMZ
KEGG	D11896
ChEMBL	ChEMBL3984425
PDB ligand	V7Y (PDBe, RCSB PDB)
CompTox Dashboard (EPA)	DTXSID301336580
Chemical and physical data
Formula	C30H24N8O2
Molar mass	528.576 g·mol−1
3D model (JSmol)	Interactive image
SMILES Cn1cc(cn1)C#Cc6cccc2c6C(=O)N(C(=C2)C(C)NC(=O)c4c3ncccn3nc4N)c5ccccc5
InChI InChI=1S/C30H24N8O2/c1-19(34-29(39)26-27(31)35-37-15-7-14-32-28(26)37)24-16-22-9-6-8-21(13-12-20-17-33-36(2)18-20)25(22)30(40)38(24)23-10-4-3-5-11-23/h3-11,14-19H,1-2H3,(H2,31,35)(H,34,39)/t19-/m0/s1 Key:XUMALORDVCFWKV-IBGZPJMESA-N

Eganelisib (USAN), codenamed IPI-549, is an experimental drug being investigated as a possible treatment for cancer. It is a highly selective phosphoinositide 3-kinase inhibitor, and thus works by inhibiting the enzyme PIK3CG, disrupting the PI3K/AKT/mTOR signaling pathway which plays important roles in the development of cancer.^[1]

Eganelisib is being developed by Infinity Pharmaceuticals. Early clinical trial results were published in September 2016.^[2] 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, combined with a checkpoint inhibitor and chemotherapy.^[3]

As of October 2020^[update], five phase I/II clinical trials were ongoing in the United States, and one in Europe.^[4]

Eganelisib has also been explored for its potential use in the treatment of COVID-19 and MRSA. Early, pre-clinical in vitro studies published in 2024 suggested eganelisib's ability to inhibit PI3Kγ, an enzyme involved in myeloid cell movement into infected tissues, could reduce excessive immune system activity that can damage tissues. By inhibiting PI3Kγ, eganelisib may prevent myeloid cells from entering and damaging tissue in patients with COVID-19 or MRSA, thereby reducing inflammation and the risk of cytokine storms. The study also indicated eganelisib may inhibit the main protease (M^pro) protein of the SARS-CoV-2 virus, a crucial enzyme required for viral replication, potentially offering another therapeutic avenue against COVID-19.^[5][6][7]

References[edit]

Further reading[edit]

• Drew SL, Thomas-Tran R, Beatty JW, Fournier J, Lawson KV, Miles DH, Mata G, Sharif EU, Yan X, Mailyan AK, Ginn E, Chen J, Wong K, Soni D, Dhanota P, Chen PY, Shaqfeh SG, Meleza C, Pham AT, Chen A, Zhao X, Banuelos J, Jin L, Schindler U, Walters MJ, Young SW, Walker NP, Leleti MR, Powers JP, Jeffrey JL (October 2020). "Discovery of Potent and Selective PI3Kγ Inhibitors". J Med Chem. 63 (19): 11235–11257. doi:10.1021/acs.jmedchem.0c01203. PMID 32865410.
• Catherine A. Evans*, Tao Liu, André Lescarbeau, Somarajan J. Nair, Louis Grenier, Johan A. Pradeilles, Quentin Glenadel, Thomas Tibbitts, Ann M. Rowley, Jonathan P. DiNitto, Erin E. Brophy, Erin L. O'Hearn, Janid A. Ali, David G. Winkler, Stanley I. Goldstein, Patrick O'Hearn, Christian M. Martin, Jennifer G. Hoyt, John R. Soglia, Culver Cheung, Melissa M. Pink, Jennifer L. Proctor, Vito J. Palombella, Martin R. Tremblay, and Alfredo C. Castro*. Discovery of a Selective Phosphoinositide-3-Kinase (PI3K)-γ Inhibitor (IPI-549) as an Immuno-Oncology Clinical Candidate ACS Med. Chem. Lett. 2016, 7, 9, 862–867; https://doi.org/10.1021/acsmedchemlett.6b00238

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