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Omipalisib
Omipalisib is a small molecule pharmaceutical. It is currently being investigated in clinical studies. The pharmaceutical is active against phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform. In addition, it is known to target phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform, serine/threonine-protein kinase mTOR, phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform, and phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoform.
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Commercial
Therapeutic Areas
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Trade Name
FDA
EMA
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Drug Products
FDA
EMA
New Drug Application (NDA)
New Drug Application (NDA)
Abbreviated New Drug Application (ANDA)
Abbreviated New Drug Application (ANDA)
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Labels
FDA
EMA
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Indications
FDA
EMA
No data
Agency Specific
FDA
EMA
No data
Patent Expiration
No data
ATC Codes
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HCPCS
No data
Clinical
Clinical Trials
3 clinical trials
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Mock data
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Indications Phases 4
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Indications Phases 3
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Indications Phases 2
No data
Indications Phases 1
Indication
MeSH
Ontology
ICD-10
Ph 1
Ph 2
Ph 3
Ph 4
Other
Total
NeoplasmsD009369C8011
Idiopathic pulmonary fibrosisD054990J84.11211
Indications Without Phase
No data
Epidemiology
Epidemiological information for investigational and approved indications
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Drug
General
Drug common nameOMIPALISIB
INNomipalisib
Description
Omipalisib is a member of the class of quinolines that is quinoline which is substituted by pyridazin-4-yl and 5-[(2,4-difluorobenzene-1-sulfonyl)amino]-6-methoxypyridin-3-yl groups at positions 4 and 6, respectively. It is a highly potent inhibitor of PI3K and mTOR developed by GlaxoSmithKline and was previously in human phase 1 clinical trials for the treatment of idiopathic pulmonary fibrosis and solid tumors. It has a role as an autophagy inducer, an EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor, a mTOR inhibitor, an antineoplastic agent, a radiosensitizing agent and an anticoronaviral agent. It is a member of quinolines, a difluorobenzene, a sulfonamide, an aromatic ether, a member of pyridines and a member of pyridazines.
Classification
Small molecule
Drug classphosphatidylinositol 3-kinase (PI3K) inhibitors
Image (chem structure or protein)
Structure (InChI/SMILES or Protein Sequence)
COc1ncc(-c2ccc3nccc(-c4ccnnc4)c3c2)cc1NS(=O)(=O)c1ccc(F)cc1F
Identifiers
PDB
CAS-ID1086062-66-9
RxCUI
ChEMBL IDCHEMBL1236962
ChEBI ID
PubChem CID
DrugBankDB12703
UNII ID1X8F5A3NA0 (ChemIDplus, GSRS)
Target
Agency Approved
PIK3CA
PIK3CA
Organism
Homo sapiens
Gene name
PIK3CA
Gene synonyms
NCBI Gene ID
Protein name
phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform
Protein synonyms
mutant phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha, p110alpha, phosphatidylinositol 3-kinase, catalytic, 110-KD, alpha, phosphatidylinositol 3-kinase, catalytic, alpha polypeptide, Phosphatidylinositol 4,5-bisphosphate 3-kinase 110 kDa catalytic subunit alpha, phosphatidylinositol-4,5-bisphosphate 3-kinase 110 kDa catalytic subunit alpha, Phosphoinositide 3-kinase alpha, Phosphoinositide-3-kinase catalytic alpha polypeptide, phosphoinositide-3-kinase, catalytic, alpha polypeptide, PI3-kinase p110 subunit alpha, PtdIns-3-kinase subunit p110-alpha, Serine/threonine protein kinase PIK3CA
Uniprot ID
Mouse ortholog
Pik3ca (18706)
phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform (Q0VGQ5)
Alternate
PIK3CD
PIK3CD
MTOR
MTOR
PIK3CG
PIK3CG
PIK3CB
PIK3CB
Organism
Homo sapiens
Gene name
PIK3CD
Gene synonyms
NCBI Gene ID
Protein name
phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform
Protein synonyms
p110delta, Phosphatidylinositol 4,5-bisphosphate 3-kinase 110 kDa catalytic subunit delta, phosphatidylinositol-4,5-bisphosphate 3-kinase 110 kDa catalytic subunit delta, phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit delta short variant 8/20, phosphoinositide-3-kinase C, phosphoinositide-3-kinase, catalytic, delta polypeptide variant p37delta, PI3-kinase p110 subunit delta, PI3Kdelta, PtdIns-3-kinase subunit p110-delta
Uniprot ID
Mouse ortholog
Pik3cd (18707)
phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform (Q8CJ28)
Variants
Clinical Variant
No data
Financial
No data
Trends
PubMed Central
Top Terms for Disease or Syndrome:
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Additional graphs summarizing 241 documents
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Safety
Black-box Warning
No Black-box warning
Adverse Events
Top Adverse Reactions
0 adverse events reported
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