Cintirorgon

Cintirorgon
Clinical data
Other names	LYC-55716
Drug class	RORγ agonist
Identifiers
	IUPAC name 3-[(2S)-6-[3-(difluoromethoxy)-5-fluorophenyl]-4-[3-(trifluoromethyl)phenyl]sulfonyl-2,3-dihydro-1,4-benzoxazin-2-yl]-2,2-dimethylpropanoic acid;
CAS Number	2055536-64-4;
PubChem CID	124126348;
IUPHAR/BPS	10045;
DrugBank	DB20916;
ChemSpider	67896554;
UNII	LPN433P0EA;
ChEMBL	ChEMBL4472508;
Chemical and physical data
Formula	C27H23F6NO6S
Molar mass	603.53 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES CC(C)(C[C@H]1CN(C2=C(O1)C=CC(=C2)C3=CC(=CC(=C3)F)OC(F)F)S(=O)(=O)C4=CC=CC(=C4)C(F)(F)F)C(=O)O;
	InChI InChI=1S/C27H23F6NO6S/c1-26(2,24(35)36)13-20-14-34(41(37,38)21-5-3-4-17(11-21)27(31,32)33)22-10-15(6-7-23(22)39-20)16-8-18(28)12-19(9-16)40-25(29)30/h3-12,20,25H,13-14H2,1-2H3,(H,35,36)/t20-/m0/s1; Key:GULSIMHVQYBADX-FQEVSTJZSA-N;

Cintirorgon (LYC-55716) is a drug which acts as a selective agonist of the receptor RAR-related orphan receptor gamma (RORγ). It was developed for the treatment of certain forms of cancer and is in early stage human clinical trials.^[1]^[2]^[3]^[4]^[5]

References

↑ Aicher TD, Van Huis CA, Hurd AR, Skalitzky DJ, Taylor CB, Beleh OM, et al. (September 2021). "Discovery of LYC-55716: A Potent, Selective, and Orally Bioavailable Retinoic Acid Receptor-Related Orphan Receptor-γ (RORγ) Agonist for Use in Treating Cancer". Journal of Medicinal Chemistry. 64 (18): 13410–13428. doi:10.1021/acs.jmedchem.1c00731. PMID 34499493.
↑ Xia L, Tian E, Yu M, Liu C, Shen L, Huang Y, et al. (April 2022). "RORγt agonist enhances anti-PD-1 therapy by promoting monocyte-derived dendritic cells through CXCL10 in cancers". Journal of Experimental & Clinical Cancer Research. 41 (1) 155. doi:10.1186/s13046-022-02289-2. PMC 9034499. PMID 35459193.
↑ Wang H, Zhang G, Zhao C, Xue Y, Zhu D, Chang Y (August 2025). "RORγt agonist LYC-55716 potentiates IFN-α's efficacy in hepatocellular carcinoma through enhancing cytotoxicity of Tc17 cells and infiltration of CD8⁺ T cells". Biochemical Pharmacology. 238 116963. doi:10.1016/j.bcp.2025.116963. PMID 40312017.
↑ Fukuda S, Ikenogami T, Otake K, Miwa S, Maeda K, Yamashita T, et al. (August 2025). "A Concise and Modular Approach to Generate Novel RORγ Agonists". Journal of Medicinal Chemistry. 68 (15) acs.jmedchem.5c00872. doi:10.1021/acs.jmedchem.5c00872. PMID 40677142.
↑ Terawaki T, Suzukawa A, Tanimoto M, Fukuda S, Yamaguchi T (2025). "A Novel RORγ-Selective Agonist Facilitates the Infiltration of Effector T Cells and Innate Immune Cells into Tumor Tissue, Demonstrating Antitumor Efficacy". Biological & Pharmaceutical Bulletin. 48 (12) b25-00540. doi:10.1248/bpb.b25-00540. PMID 41338992.

[1] Aicher TD, Van Huis CA, Hurd AR, Skalitzky DJ, Taylor CB, Beleh OM, et al. (September 2021). "Discovery of LYC-55716: A Potent, Selective, and Orally Bioavailable Retinoic Acid Receptor-Related Orphan Receptor-γ (RORγ) Agonist for Use in Treating Cancer". Journal of Medicinal Chemistry. 64 (18): 13410–13428. doi:10.1021/acs.jmedchem.1c00731. PMID 34499493.

[2] Xia L, Tian E, Yu M, Liu C, Shen L, Huang Y, et al. (April 2022). "RORγt agonist enhances anti-PD-1 therapy by promoting monocyte-derived dendritic cells through CXCL10 in cancers". Journal of Experimental & Clinical Cancer Research. 41 (1) 155. doi:10.1186/s13046-022-02289-2. PMC 9034499. PMID 35459193.

[3] Wang H, Zhang G, Zhao C, Xue Y, Zhu D, Chang Y (August 2025). "RORγt agonist LYC-55716 potentiates IFN-α's efficacy in hepatocellular carcinoma through enhancing cytotoxicity of Tc17 cells and infiltration of CD8⁺ T cells". Biochemical Pharmacology. 238 116963. doi:10.1016/j.bcp.2025.116963. PMID 40312017.

[4] Fukuda S, Ikenogami T, Otake K, Miwa S, Maeda K, Yamashita T, et al. (August 2025). "A Concise and Modular Approach to Generate Novel RORγ Agonists". Journal of Medicinal Chemistry. 68 (15) acs.jmedchem.5c00872. doi:10.1021/acs.jmedchem.5c00872. PMID 40677142.

[5] Terawaki T, Suzukawa A, Tanimoto M, Fukuda S, Yamaguchi T (2025). "A Novel RORγ-Selective Agonist Facilitates the Infiltration of Effector T Cells and Innate Immune Cells into Tumor Tissue, Demonstrating Antitumor Efficacy". Biological & Pharmaceutical Bulletin. 48 (12) b25-00540. doi:10.1248/bpb.b25-00540. PMID 41338992.

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References