Galunisertib
Galunisertib is a small molecule pharmaceutical. It is currently being investigated in clinical studies. The pharmaceutical is active against TGF-beta receptor type-1. In addition, it is known to target TGF-beta receptor type-2, activin receptor type-1B, and bone morphogenetic protein receptor type-1B.
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Commercial
No data
Clinical
Clinical Trials
25 clinical trials
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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 |
|---|---|---|---|---|---|---|---|---|---|
| Myelodysplastic syndromes | D009190 | — | D46 | — | 1 | 1 | — | — | 1 |
| Preleukemia | D011289 | — | — | — | 1 | 1 | — | — | 1 |
| Syndrome | D013577 | — | — | — | 1 | 1 | — | — | 1 |
Indications Phases 2
Indication | MeSH | Ontology | ICD-10 | Ph 1 | Ph 2 | Ph 3 | Ph 4 | Other | Total |
|---|---|---|---|---|---|---|---|---|---|
| Carcinoma | D002277 | — | C80.0 | 5 | 5 | — | — | — | 8 |
| Hepatocellular carcinoma | D006528 | — | C22.0 | 3 | 3 | — | — | — | 5 |
| Neoplasms | D009369 | — | C80 | 4 | 2 | — | — | — | 4 |
| Liver neoplasms | D008113 | EFO_1001513 | C22.0 | 2 | 3 | — | — | — | 4 |
| Pancreatic neoplasms | D010190 | EFO_0003860 | C25 | 3 | 1 | — | — | — | 3 |
| Colorectal neoplasms | D015179 | — | — | 2 | 2 | — | — | — | 2 |
| Breast neoplasms | D001943 | EFO_0003869 | C50 | 1 | 1 | — | — | — | 2 |
| Glioma | D005910 | EFO_0000520 | — | 2 | 1 | — | — | — | 2 |
| Neoplasm metastasis | D009362 | EFO_0009708 | — | 2 | 1 | — | — | — | 2 |
| Renal cell carcinoma | D002292 | EFO_0000376 | — | — | 1 | — | — | — | 1 |
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Indications Phases 1
Indication | MeSH | Ontology | ICD-10 | Ph 1 | Ph 2 | Ph 3 | Ph 4 | Other | Total |
|---|---|---|---|---|---|---|---|---|---|
| Healthy volunteers/patients | — | — | — | 3 | — | — | — | — | 3 |
| Carcinosarcoma | D002296 | — | — | 1 | — | — | — | — | 1 |
| Mullerian mixed tumor | D018200 | — | — | 1 | — | — | — | — | 1 |
| Triple negative breast neoplasms | D064726 | — | — | 1 | — | — | — | — | 1 |
Indications Without Phase
No data
Epidemiology
Epidemiological information for investigational and approved indications
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Drug
General
| Drug common name | Galunisertib |
| INN | galunisertib |
| Description | LY-2157299 is a pyrrolopyrazole that is 5,6-dihydro-4H-pyrrolo[1,2-b]pyrazole which is substituted at positions 2 and 3 by 6-methylpyridin-2-yl and 6-(aminocarbonyl)quinolin-4-yl groups, respectively. A Transforming growth factor-betaRI (TGF-betaRI) kinase inhibitor, it blocks TGF-beta-mediated tumor growth in glioblastoma. It has a role as a TGFbeta receptor antagonist and an antineoplastic agent. It is a member of quinolines, a pyrrolopyrazole, a member of methylpyridines, an aromatic amide and a monocarboxylic acid amide. |
| Classification | Small molecule |
| Drug class | serine/threonine kinase inhibitors |
| Image (chem structure or protein) |  |
| Structure (InChI/SMILES or Protein Sequence) | Cc1cccc(-c2nn3c(c2-c2ccnc4ccc(C(N)=O)cc24)CCC3)n1 |
Identifiers
| PDB | — |
| CAS-ID | 700874-72-2 |
| RxCUI | — |
| ChEMBL ID | CHEMBL2364611 |
| ChEBI ID | — |
| PubChem CID | 10090485 |
| DrugBank | — |
| UNII ID | 3OKH1W5LZE (ChemIDplus, GSRS) |
Target
Agency Approved
TGFBR1
TGFBR1
Organism
Homo sapiens
Gene name
TGFBR1
Gene synonyms
ALK5, SKR4
NCBI Gene ID
Protein name
TGF-beta receptor type-1
Protein synonyms
activin A receptor type II-like kinase, 53kDa, Activin A receptor type II-like protein kinase of 53kD, Activin receptor-like kinase 5, ALK-5, ALK5, mutant transforming growth factor beta receptor I, Serine/threonine-protein kinase receptor R4, SKR4, TbetaR-I, TGF-beta receptor type I, TGF-beta type I receptor, transforming growth factor beta receptor I, Transforming growth factor-beta receptor type I
Uniprot ID
Mouse ortholog
Tgfbr1 (21812)
TGF-beta receptor type-1 (Q64729)
Alternate
TGFBR2
TGFBR2
ACVR1B
ACVR1B
BMPR1B
BMPR1B
Organism
Homo sapiens
Gene name
TGFBR2
Gene synonyms
NCBI Gene ID
Protein name
TGF-beta receptor type-2
Protein synonyms
TbetaR-II, TGF-beta receptor type II, TGF-beta receptor type IIB, TGF-beta type II receptor, transforming growth factor beta receptor II, transforming growth factor beta receptor type IIC, transforming growth factor, beta receptor II (70/80kDa), transforming growth factor, beta receptor II alpha, transforming growth factor, beta receptor II beta, transforming growth factor, beta receptor II delta, transforming growth factor, beta receptor II epsilon, transforming growth factor, beta receptor II gamma, Transforming growth factor-beta receptor type II
Uniprot ID
Mouse ortholog
Tgfbr2 (21813)
TGF-beta receptor type-2 (Q63947)
Variants
No data
Financial
No data
Trends
PubMed Central
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Safety
Black-box Warning
No Black-box warning
Adverse Events
Top Adverse Reactions
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13 adverse events reported
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