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Dactolisib
Dactolisib is a small molecule pharmaceutical. It is currently being investigated in clinical studies. The pharmaceutical is active against serine/threonine-protein kinase mTOR, phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform, phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform, and phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform. In addition, it is known to target serine/threonine-protein kinase ATR.
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Commercial
Therapeutic Areas
No data
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)
No data
Labels
FDA
EMA
No data
Indications
FDA
EMA
No data
Agency Specific
FDA
EMA
No data
Patent Expiration
No data
ATC Codes
No data
HCPCS
No data
Clinical
Clinical Trials
25 clinical trials
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Mock data
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Indications Phases 4
No data
Indications Phases 3
Indication
MeSH
Ontology
ICD-10
Ph 1
Ph 2
Ph 3
Ph 4
Other
Total
Respiratory tract infectionsD012141J06.9—11——2
Indications Phases 2
Indication
MeSH
Ontology
ICD-10
Ph 1
Ph 2
Ph 3
Ph 4
Other
Total
Breast neoplasmsD001943EFO_0003869C5052———6
Neuroendocrine tumorsD018358EFO_1001901D3A.8—2———2
Castration-resistant prostatic neoplasmsD06412921———2
Covid-19D000086382U07.1—2———2
Kidney neoplasmsD007680EFO_0003865C6411———1
Transitional cell carcinomaD002295—1———1
Perivascular epithelioid cell neoplasmsD054973—1———1
Endometrial neoplasmsD016889EFO_0004230—1———1
Indications Phases 1
Indication
MeSH
Ontology
ICD-10
Ph 1
Ph 2
Ph 3
Ph 4
Other
Total
NeoplasmsD009369C806————6
Renal cell carcinomaD0022921————1
Multiple hamartoma syndromeD006223E71.4401————1
Myeloid leukemia acuteD015470C92.01————1
Precursor cell lymphoblastic leukemia-lymphomaD054198C91.01————1
Bcr-abl positive chronic myelogenous leukemiaD015464EFO_00003401————1
Indications Without Phase
No data
Epidemiology
Epidemiological information for investigational and approved indications
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Drug
General
Drug common nameDACTOLISIB
INNdactolisib
Description
Dactolisib is an imidazoquinoline that is 3-methyl-2-oxo-2,3-dihydro-1H-imidazo[4,5-c]quinoline substituted at position 1 by a 4-(1-cyanoisopropyl)phenyl group and at position 8 by a quinolin-3-yl group. A dual PI3K/mTOR inhibitor used in cancer treatment. It has a role as an EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor, a mTOR inhibitor and an antineoplastic agent. It is an imidazoquinoline, a nitrile, a member of quinolines, a ring assembly and a member of ureas.
Classification
Small molecule
Drug classphosphatidylinositol 3-kinase (PI3K) inhibitors
Image (chem structure or protein)
Structure (InChI/SMILES or Protein Sequence)
Cn1c(=O)n(-c2ccc(C(C)(C)C#N)cc2)c2c3cc(-c4cnc5ccccc5c4)ccc3ncc21
Identifiers
PDB—
CAS-ID915019-65-7
RxCUI—
ChEMBL IDCHEMBL1879463
ChEBI ID71952
PubChem CID11977753
DrugBankDB11651
UNII IDRUJ6Z9Y0DT (ChemIDplus, GSRS)
Target
Agency Approved
MTOR
MTOR
PIK3CG
PIK3CG
PIK3CD
PIK3CD
PIK3CA
PIK3CA
Organism
Homo sapiens
Gene name
MTOR
Gene synonyms
FRAP, FRAP1, FRAP2, RAFT1, RAPT1
NCBI Gene ID
2475
Protein name
serine/threonine-protein kinase mTOR
Protein synonyms
FK506 binding protein 12-rapamycin associated protein 2, FK506-binding protein 12-rapamycin complex-associated protein 1, FKBP-rapamycin associated protein, FKBP12-rapamycin complex-associated protein, FKBP12-rapamycin complex-associated protein 1, Mammalian target of rapamycin, Mechanistic target of rapamycin, mechanistic target of rapamycin (serine/threonine kinase), mTOR, Rapamycin and FKBP12 target 1, rapamycin associated protein FRAP2, Rapamycin target protein 1
Uniprot ID
Q9Y4I3
Mouse ortholog
Mtor (56717)
serine/threonine-protein kinase mTOR (Q9JLN9)
Alternate
ATR
ATR
Organism
Homo sapiens
Gene name
ATR
Gene synonyms
FRP1
NCBI Gene ID
545
Protein name
serine/threonine-protein kinase ATR
Protein synonyms
Ataxia telangiectasia and Rad3-related protein, FRAP-related protein 1, FRAP-related protein-1, MEC1, mitosis entry checkpoint 1, homolog
Uniprot ID
Q9BXK4
Mouse ortholog
Atr (245000)
serine/threonine-protein kinase ATR (Q9JKK8)
Variants
Clinical Variant
No data
Financial
No data
Trends
PubMed Central
Top Terms for Disease or Syndrome:
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Additional graphs summarizing 827 documents
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Safety
Black-box Warning
No Black-box warning
Adverse Events
Top Adverse Reactions
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11 adverse events reported
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