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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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
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Agency Specific
FDA
EMA
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Patent Expiration
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ATC Codes
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HCPCS
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Clinical
Clinical Trials
25 clinical trials
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Indications Phases 4
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Indications Phases 2
Indication | MeSH | Ontology | ICD-10 | Ph 1 | Ph 2 | Ph 3 | Ph 4 | Other | Total |
|---|---|---|---|---|---|---|---|---|---|
| Breast neoplasms | D001943 | EFO_0003869 | C50 | 5 | 2 | — | — | — | 6 |
| Neuroendocrine tumors | D018358 | EFO_1001901 | D3A.8 | — | 2 | — | — | — | 2 |
| Castration-resistant prostatic neoplasms | D064129 | 2 | 1 | — | — | — | 2 | ||
| Covid-19 | D000086382 | U07.1 | — | 2 | — | — | — | 2 | |
| Kidney neoplasms | D007680 | EFO_0003865 | C64 | 1 | 1 | — | — | — | 1 |
| Transitional cell carcinoma | D002295 | — | 1 | — | — | — | 1 | ||
| Perivascular epithelioid cell neoplasms | D054973 | — | 1 | — | — | — | 1 | ||
| Endometrial neoplasms | D016889 | EFO_0004230 | — | 1 | — | — | — | 1 |
Indications Phases 1
Indication | MeSH | Ontology | ICD-10 | Ph 1 | Ph 2 | Ph 3 | Ph 4 | Other | Total |
|---|---|---|---|---|---|---|---|---|---|
| Neoplasms | D009369 | C80 | 6 | — | — | — | — | 6 | |
| Renal cell carcinoma | D002292 | 1 | — | — | — | — | 1 | ||
| Multiple hamartoma syndrome | D006223 | E71.440 | 1 | — | — | — | — | 1 | |
| Myeloid leukemia acute | D015470 | C92.0 | 1 | — | — | — | — | 1 | |
| Precursor cell lymphoblastic leukemia-lymphoma | D054198 | C91.0 | 1 | — | — | — | — | 1 | |
| Bcr-abl positive chronic myelogenous leukemia | D015464 | EFO_0000340 | 1 | — | — | — | — | 1 |
Indications Without Phase
No data
Epidemiology
Epidemiological information for investigational and approved indications
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Drug
General
| Drug common name | DACTOLISIB |
| INN | dactolisib |
| 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 class | phosphatidylinositol 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-ID | 915019-65-7 |
| RxCUI | — |
| ChEMBL ID | CHEMBL1879463 |
| ChEBI ID | 71952 |
| PubChem CID | 11977753 |
| DrugBank | DB11651 |
| UNII ID | RUJ6Z9Y0DT (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
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
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
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
Mouse ortholog
Atr (245000)
serine/threonine-protein kinase ATR (Q9JKK8)
Variants
Clinical Variant
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Financial
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Trends
PubMed Central
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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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