Galunisertib

Galunisertib
Clinical data
Routes of; administration	PO
Identifiers
	IUPAC name 4-(5,6-Dihydro-2-(6-methyl-2-pyridinyl)-4H-pyrrolo(1,2-b)pyrazol-3-yl)-6-quinolinecarboxamide;
CAS Number	700874-72-2;
PubChem CID	10090485;
ChemSpider	8266022;
KEGG	D10437;
ChEBI	CHEBI:137064;
Chemical and physical data
Formula	C22H19N5O
Molar mass	369.43 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES N1=CC=C(C2=CC(=CC=C12)C(=O)N)C1=C2N(N=C1C1C=CC=C(N=1)C)CCC2;
	InChI InChI=1S/C22H19N5O/c1-13-4-2-5-18(25-13)21-20(19-6-3-11-27(19)26-21)15-9-10-24-17-8-7-14(22(23)28)12-16(15)17/h2,4-5,7-10,12H,3,6,11H2,1H3,(H2,23,28); Key:IVRXNBXKWIJUQB-UHFFFAOYSA-N;

Galunisertib (LY2157299) is a small molecular experimental cancer drug in development by Eli Lilly. It is a TGF-b inhibitor.^[1]

Galunisertib is in a phase II trial for treatment of hepatocellular carcinoma.^[2] Combination of galunisertib with PD-L1 blockade resulted in improved tumor growth inhibition.^[3]

References

↑ "Lilly Oncology Pipeline - Lilly USA". www.lillyoncologypipeline.com.
↑ "A Study of LY2157299 in Participants With Hepatocellular Carcinoma - Full Text View - ClinicalTrials.gov".
↑ Holmgaard, R. B., Schaer, D. A., Li, Y., Castaneda, S. P., Murphy, M. Y., Xu, X., ... & Surguladze, D. (2018). Targeting the TGFβ pathway with galunisertib, a TGFβRI small molecule inhibitor, promotes anti-tumor immunity leading to durable, complete responses, as monotherapy and in combination with checkpoint blockade. Journal for immunotherapy of cancer, 6(1), 47. doi:10.1186/s40425-018-0356-4 PMC 5987416

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[1] "Lilly Oncology Pipeline - Lilly USA". www.lillyoncologypipeline.com.

[2] "A Study of LY2157299 in Participants With Hepatocellular Carcinoma - Full Text View - ClinicalTrials.gov".

[3] Holmgaard, R. B., Schaer, D. A., Li, Y., Castaneda, S. P., Murphy, M. Y., Xu, X., ... & Surguladze, D. (2018). Targeting the TGFβ pathway with galunisertib, a TGFβRI small molecule inhibitor, promotes anti-tumor immunity leading to durable, complete responses, as monotherapy and in combination with checkpoint blockade. Journal for immunotherapy of cancer, 6(1), 47. doi:10.1186/s40425-018-0356-4 PMC 5987416

Clinical data

Routes of administration	PO
Identifiers
IUPAC name 4-(5,6-Dihydro-2-(6-methyl-2-pyridinyl)-4H-pyrrolo(1,2-b)pyrazol-3-yl)-6-quinolinecarboxamide
CAS Number	700874-72-2
PubChem CID	10090485
ChemSpider	8266022
KEGG	D10437
ChEBI	CHEBI:137064
Chemical and physical data
Formula	C₂₂H₁₉N₅O
Molar mass	369.43 g·mol⁻¹
3D model (JSmol)	Interactive image
SMILES N1=CC=C(C2=CC(=CC=C12)C(=O)N)C1=C2N(N=C1C1C=CC=C(N=1)C)CCC2
InChI InChI=1S/C22H19N5O/c1-13-4-2-5-18(25-13)21-20(19-6-3-11-27(19)26-21)15-9-10-24-17-8-7-14(22(23)28)12-16(15)17/h2,4-5,7-10,12H,3,6,11H2,1H3,(H2,23,28) Key:IVRXNBXKWIJUQB-UHFFFAOYSA-N