Buparlisib
Buparlisib 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.
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Therapeutic Areas
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Trade Name
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Drug Products
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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
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Indications
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Agency Specific
FDA
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Patent Expiration
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ATC Codes
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HCPCS
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Clinical
Clinical Trials
87 clinical trials
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Indications Phases 4
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Indications Phases 3
Indication | MeSH | Ontology | ICD-10 | Ph 1 | Ph 2 | Ph 3 | Ph 4 | Other | Total |
|---|---|---|---|---|---|---|---|---|---|
| Breast neoplasms | D001943 | EFO_0003869 | C50 | 11 | 10 | 3 | — | — | 21 |
| Head and neck neoplasms | D006258 | — | 1 | 1 | — | — | 2 |
Indications Phases 2
Indication | MeSH | Ontology | ICD-10 | Ph 1 | Ph 2 | Ph 3 | Ph 4 | Other | Total |
|---|---|---|---|---|---|---|---|---|---|
| Neoplasms | D009369 | C80 | 12 | 1 | — | — | — | 13 | |
| Non-small-cell lung carcinoma | D002289 | 6 | 2 | — | — | — | 8 | ||
| Prostatic neoplasms | D011471 | C61 | 2 | 3 | — | — | — | 5 | |
| Glioblastoma | D005909 | EFO_0000515 | 4 | 2 | — | — | — | 5 | |
| Colorectal neoplasms | D015179 | 4 | 2 | — | — | — | 5 | ||
| Endometrial neoplasms | D016889 | EFO_0004230 | 2 | 3 | — | — | — | 5 | |
| Squamous cell carcinoma of head and neck | D000077195 | 2 | 3 | — | — | — | 4 | ||
| Melanoma | D008545 | — | 2 | — | — | — | 2 | ||
| Squamous cell carcinoma | D002294 | 2 | 1 | — | — | — | 2 | ||
| Neoplasm metastasis | D009362 | EFO_0009708 | — | 2 | — | — | — | 2 |
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Indications Phases 1
Indication | MeSH | Ontology | ICD-10 | Ph 1 | Ph 2 | Ph 3 | Ph 4 | Other | Total |
|---|---|---|---|---|---|---|---|---|---|
| Follicular lymphoma | D008224 | C82 | 3 | — | — | — | — | 3 | |
| Mantle-cell lymphoma | D020522 | C83.1 | 3 | — | — | — | — | 3 | |
| Ovarian neoplasms | D010051 | EFO_0003893 | C56 | 3 | — | — | — | — | 3 |
| Large b-cell lymphoma diffuse | D016403 | C83.3 | 2 | — | — | — | — | 2 | |
| Pancreatic neoplasms | D010190 | EFO_0003860 | C25 | 2 | — | — | — | — | 2 |
| Renal cell carcinoma | D002292 | 1 | — | — | — | — | 1 | ||
| Gastrointestinal stromal tumors | D046152 | EFO_0000505 | C49.A | 1 | — | — | — | — | 1 |
| Nasopharyngeal neoplasms | D009303 | 1 | — | — | — | — | 1 | ||
| Laryngeal neoplasms | D007822 | EFO_0003817 | C32 | 1 | — | — | — | — | 1 |
| Hypopharyngeal neoplasms | D007012 | C13 | 1 | — | — | — | — | 1 |
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Indications Without Phase
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Epidemiology
Epidemiological information for investigational and approved indications
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Drug
General
| Drug common name | BUPARLISIB |
| INN | buparlisib |
| Description | BKM120 is an aminopyridine that is 4-(trifluoromethyl)pyridin-2-amine substituted at position 5 by a 2,6-di(morpholin-4-yl)pyrimidin-4-y group. A selective PI3K inhibitor with anti-tumour properties. It has a role as an EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor and an antineoplastic agent. It is a member of morpholines, an aminopyrimidine, an aminopyridine and an organofluorine compound. |
| Classification | Small molecule |
| Drug class | phosphatidylinositol 3-kinase (PI3K) inhibitors |
| Image (chem structure or protein) | |
| Structure (InChI/SMILES or Protein Sequence) | Nc1cc(C(F)(F)F)c(-c2cc(N3CCOCC3)nc(N3CCOCC3)n2)cn1 |
Identifiers
| PDB | — |
| CAS-ID | 944396-07-0 |
| RxCUI | — |
| ChEMBL ID | CHEMBL2017974 |
| ChEBI ID | 71954 |
| PubChem CID | 16654980 |
| DrugBank | DB11666 |
| UNII ID | 0ZM2Z182GD (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
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Variants
Clinical Variant
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Financial
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Trends
PubMed Central
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Safety
Black-box Warning
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Adverse Events
Top Adverse Reactions
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76 adverse events reported
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