General Information of Drug (ID: DMP8HW1)

Drug Name
LY2157299 Drug Info
Synonyms
Galunisertib; 700874-72-2; LY2157299; LY 2157299; LY-2157299; UNII-3OKH1W5LZE; 4-(2-(6-methylpyridin-2-yl)-5,6-dihydro-4H-pyrrolo[1,2-b]pyrazol-3-yl)quinoline-6-carboxamide; 3OKH1W5LZE; Galunisertib (LY2157299); AK-79916; 4-[5,6-Dihydro-2-(6-methyl-2-pyridinyl)-4H-pyrrolo[1,2-b]pyrazol-3-yl]-6-quinolinecarboxamide; 4-(2-(6-Methylpyridin-2-yl)-5,6-dihydro-4H-pyrrolo-[1,2-b]pyrazol-3-yl)quinoline-6-carboxamide; 4-[2-(6-methylpyridin-2-yl)-4H,5H,6H-pyrrolo[1,2-b]pyrazol-3-yl]quinoline-6-carboxamide
Indication
Disease Entry ICD 11 Status REF
Arteriosclerosis BD40 Phase 2/3 [1]
Non-small-cell lung cancer 2C25.Y Phase 2/3 [2]
Hepatocellular carcinoma 2C12.02 Phase 2 [2]
Glioma 2A00.0 Phase 1/2 [3]
Solid tumour/cancer 2A00-2F9Z Phase 1/2 [2]
Pancreatic cancer 2C10 Phase 1 [2]
Cross-matching ID
PubChem CID
10090485
ChEBI ID
CHEBI:137064
CAS Number
CAS 700874-72-2
TTD Drug ID
DMP8HW1

Molecule(s) Related to This Drug


Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
TGF-beta receptor type I (TGFBR1) TTP4520 TGFR1_HUMAN Modulator [4]
Transforming growth factor beta 1 (TGFB1) TTR9XHZ TGFB1_HUMAN Inhibitor [2]

The Expression Level of Molecule(s) in Normal Tissue of Major ADME-Related Organs

Molecule Molecule Type Gene Name Liver Colon Kidney Small Intestine
Transforming growth factor beta 1 (TGFB1) DTT TGFB1 5.844 5.859 6.44 6.172
TGF-beta receptor type I (TGFBR1) DTT TGFBR1 6.123 5.573 5.6 5.399
Molecule Expression Atlas in Normal Tissue of Major ADME-related organs

The Expression Level of Molecule(s) between Disease Section and Healthy Individual Tissue

The Studied Disease Arteriosclerosis
ICD Disease Classification BD40
Molecule Name Molecule Type Gene Name p-value Fold-Change Z-score
Transforming growth factor beta 1 (TGFB1) DTT TGFB1 5.95E-09 1.68 7.81
Molecular Expression Atlas between Disease Section and Healthy Individual Tissue

References

1 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7797).
2 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
3 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
4 Cardiac Safety of TGF-beta Receptor I Kinase Inhibitor LY2157299 Monohydrate in Cancer Patients in a First-in-Human Dose Study. Cardiovasc Toxicol. 2015 Oct;15(4):309-23.