Bevurogant

Bevurogant
Clinical data
Other names	BI 730357
Drug class	RORγ agonist
Identifiers
	IUPAC name 8-[(1S)-1-cyclopropylethyl]-2-(4-cyclopropyl-6-methylpyrimidin-5-yl)-6-[(5-methylsulfonyl-2-pyridinyl)methylamino]pteridin-7-one;
CAS Number	1817773-66-2;
PubChem CID	118440466;
DrugBank	DB21507;
ChemSpider	114711335;
UNII	1874HVK11I;
ChEMBL	ChEMBL4760304;
Chemical and physical data
Formula	C26H28N8O3S
Molar mass	532.62 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES CC1=C(C(=NC=N1)C2CC2)C3=NC=C4C(=N3)N(C(=O)C(=N4)NCC5=NC=C(C=C5)S(=O)(=O)C)[C@@H](C)C6CC6;
	InChI InChI=1S/C26H28N8O3S/c1-14-21(22(17-6-7-17)31-13-30-14)23-29-12-20-25(33-23)34(15(2)16-4-5-16)26(35)24(32-20)28-10-18-8-9-19(11-27-18)38(3,36)37/h8-9,11-13,15-17H,4-7,10H2,1-3H3,(H,28,32)/t15-/m0/s1; Key:HVVHIBHBDCYLDI-HNNXBMFYSA-N;

Bevurogant (BI 730357) is a drug which acts as a potent and selective antagonist (or perhaps inverse agonist) of the receptor RAR-related orphan receptor gamma (RORγ). It has anti-inflammatory effects and has been researched for the treatment of various conditions in which inflammation plays a role.

References

↑ Choi H, Huang F, Flack M (February 2024). "The Effect of BI 730357 (Retinoic Acid-Related Orphan Receptor Gamma t Antagonist, Bevurogant) on the Pharmacokinetics of a Transporter Probe Cocktail, Including Digoxin, Furosemide, Metformin, and Rosuvastatin: An Open-Label, Non-randomized, 2-Period Fixed-Sequence Trial in Healthy Subjects". Clinical Pharmacology in Drug Development. 13 (2): 197–207. doi:10.1002/cpdd.1344. PMID 37960990.
↑ Kanacher T, Sjögren E, Korell J, Plan EL, Gómez-Mantilla JD, Ince I (March 2025). "Assessing Drug-Drug Interaction and Food Effect for BCS Class 2 Compound BI 730357 (Retinoic Acid-Related Orphan Receptor Gamma Antagonist, Bevurogant) Using a Physiology-Based Pharmacokinetics Modeling (PBPK) Approach with Semi-Mechanistic Absorption". Pharmaceutics. 17 (3): 314. doi:10.3390/pharmaceutics17030314. PMC 11945243. PMID 40142978.

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[1] Choi H, Huang F, Flack M (February 2024). "The Effect of BI 730357 (Retinoic Acid-Related Orphan Receptor Gamma t Antagonist, Bevurogant) on the Pharmacokinetics of a Transporter Probe Cocktail, Including Digoxin, Furosemide, Metformin, and Rosuvastatin: An Open-Label, Non-randomized, 2-Period Fixed-Sequence Trial in Healthy Subjects". Clinical Pharmacology in Drug Development. 13 (2): 197–207. doi:10.1002/cpdd.1344. PMID 37960990.

[2] Kanacher T, Sjögren E, Korell J, Plan EL, Gómez-Mantilla JD, Ince I (March 2025). "Assessing Drug-Drug Interaction and Food Effect for BCS Class 2 Compound BI 730357 (Retinoic Acid-Related Orphan Receptor Gamma Antagonist, Bevurogant) Using a Physiology-Based Pharmacokinetics Modeling (PBPK) Approach with Semi-Mechanistic Absorption". Pharmaceutics. 17 (3): 314. doi:10.3390/pharmaceutics17030314. PMC 11945243. PMID 40142978.