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Eganelisib

January 01, 1970

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
Clinical data
Routes of
administration		Oral
ATC code
  • None
Identifiers
  • 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)
Chemical and physical data
FormulaC30H24N8O2
Molar mass528.576 g·mol−1
3D model (JSmol)
  • Interactive image
  • Cn1cc(cn1)C#Cc6cccc2c6C(=O)N(C(=C2)C(C)NC(=O)c4c3ncccn3nc4N)c5ccccc5
  • 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 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, five phase I/II clinical trials were ongoing in the United States, and one in Europe.[4]

References edit

  1. ^ Evans CA, Liu T, Lescarbeau A, Nair SJ, Grenier L, Pradeilles JA, Glenadel Q, Tibbitts T, Rowley AM, DiNitto JP, Brophy EE, O'Hearn EL, Ali JA, Winkler DG, Goldstein SI, O'Hearn P, Martin CM, Hoyt JG, Soglia JR, Cheung C, Pink MM, Proctor JL, Palombella VJ, Tremblay MR, Castro AC (September 2016). "Discovery of a Selective Phosphoinositide-3-Kinase (PI3K)-γ Inhibitor (IPI-549) as an Immuno-Oncology Clinical Candidate". ACS Med Chem Lett. 7 (9): 862–7. doi:10.1021/acsmedchemlett.6b00238. PMC 5018865. PMID 27660692.
  2. ^ Corey Williams (2016-09-27). "Infinity Pharmaceuticals Inc. Presents Initial Clinical And New Preclinical Data On IPI-549 At Second CRI-CIMT-EATI-AACR International Cancer Immunotherapy Conference". The Smarter Analyst. Retrieved 2020-10-30.
  3. ^ "Infinity Receives Fast Track Designation for Eganelisib in Combination with a Checkpoint Inhibitor and Chemotherapy for First". Bloomberg (Press release). 2020-09-29. Retrieved 2020-10-30.
  4. ^ "CID 91933883 | C30H24N8O2 - PubChem: ClinicalTrials.gov". PubChem. Retrieved 2020-10-30.

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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January 01, 1970
eganelisib, usan, codenamed, experimental, drug, being, investigated, possible, treatment, cancer, highly, selective, phosphoinositide, kinase, inhibitor, thus, works, inhibiting, enzyme, pik3cg, disrupting, pi3k, mtor, signaling, pathway, which, plays, import. 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 EganelisibClinical dataRoutes ofadministrationOralATC codeNoneIdentifiersIUPAC 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 carboxamideCAS Number1693758 51 8PubChem CID91933883ChemSpider60600433UNIIFOF5155FMZKEGGD11896ChEMBLChEMBL3984425PDB ligandV7Y PDBe RCSB PDB Chemical and physical dataFormulaC 30H 24N 8O 2Molar mass528 576 g mol 13D model JSmol Interactive imageSMILES Cn1cc cn1 C Cc6cccc2c6C O N C C2 C C NC O c4c3ncccn3nc4N c5ccccc5InChI 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 s1Key XUMALORDVCFWKV IBGZPJMESA N 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 References edit Evans CA Liu T Lescarbeau A Nair SJ Grenier L Pradeilles JA Glenadel Q Tibbitts T Rowley AM DiNitto JP Brophy EE O Hearn EL Ali JA Winkler DG Goldstein SI O Hearn P Martin CM Hoyt JG Soglia JR Cheung C Pink MM Proctor JL Palombella VJ Tremblay MR Castro AC September 2016 Discovery of a Selective Phosphoinositide 3 Kinase PI3K g Inhibitor IPI 549 as an Immuno Oncology Clinical Candidate ACS Med Chem Lett 7 9 862 7 doi 10 1021 acsmedchemlett 6b00238 PMC 5018865 PMID 27660692 Corey Williams 2016 09 27 Infinity Pharmaceuticals Inc Presents Initial Clinical And New Preclinical Data On IPI 549 At Second CRI CIMT EATI AACR International Cancer Immunotherapy Conference The Smarter Analyst Retrieved 2020 10 30 Infinity Receives Fast Track Designation for Eganelisib in Combination with a Checkpoint Inhibitor and Chemotherapy for First Bloomberg Press release 2020 09 29 Retrieved 2020 10 30 CID 91933883 C30H24N8O2 PubChem ClinicalTrials gov PubChem Retrieved 2020 10 30 Further reading editDrew 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 PI3Kg Inhibitors J Med Chem 63 19 11235 11257 doi 10 1021 acs jmedchem 0c01203 PMID 32865410 Catherine A Evans Tao Liu Andre 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 g 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 nbsp This antineoplastic or immunomodulatory drug article is a stub You can help Wikipedia by expanding it vte Portal nbsp Medicine Retrieved from https en wikipedia org w index php title Eganelisib amp oldid 1204527065, wikipedia, wiki, book, books, library,

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