Balinatunfib

Balinatunfib
Identifiers
	IUPAC name (1R,11R)-5-[2-(1-aminocyclobutyl)pyrimidin-5-yl]-18-(difluoromethoxy)-12-methyl-2,9,12-triazapentacyclo[9.8.1.02,10.03,8.014,19]icosa-3(8),4,6,9,14(19),15,17-heptaen-13-one;
CAS Number	2248726-53-4 ;
PubChem CID	132042903;
IUPHAR/BPS	13583;
ChemSpider	129738176;
UNII	PLY98MAN4C;
KEGG	D13339;
Chemical and physical data
Formula	C27H24F2N6O2
Molar mass	502.526 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES CN1[C@@H]2C[C@H](C3=C(C1=O)C=CC=C3OC(F)F)N4C2=NC5=C4C=C(C=C5)C6=CN=C(N=C6)C7(CCC7)N;
	InChI InChI=1S/C27H24F2N6O2/c1-34-20-11-19(22-16(24(34)36)4-2-5-21(22)37-26(28)29)35-18-10-14(6-7-17(18)33-23(20)35)15-12-31-25(32-13-15)27(30)8-3-9-27/h2,4-7,10,12-13,19-20,26H,3,8-9,11,30H2,1H3/t19-,20-/m1/s1; Key:UROFXMLQPAUCGV-WOJBJXKFSA-N;

Balinatunfib (SAR441566) is an experimental drug which acts as a potent small molecule inhibitor of TNF. Rather than blocking TNF receptors, balinatunfib inactivates TNF directly by stabilising an inactive form of the TNF trimer which fails to bind to its target receptors. It is in early stage clinical trials for rheumatoid arthritis and other chronic autoimmune diseases.^[1]^[2]

References

↑ Vugler A, O'Connell J, Nguyen MA, Weitz D, Leeuw T, Hickford E, et al. (2022). "An orally available small molecule that targets soluble TNF to deliver anti-TNF biologic-like efficacy in rheumatoid arthritis". Frontiers in Pharmacology. 13 1037983. doi:10.3389/fphar.2022.1037983. PMC 9709720. PMID 36467083.
↑ Li Y, Ye R, Dai H, Lin J, Cheng Y, Zhou Y, et al. (January 2025). "Exploring TNFR1: from discovery to targeted therapy development". Journal of Translational Medicine. 23 (1): 71. doi:10.1186/s12967-025-06122-0. PMC 11734553. PMID 39815286.

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[pmid36467083-1] Vugler A, O'Connell J, Nguyen MA, Weitz D, Leeuw T, Hickford E, et al. (2022). "An orally available small molecule that targets soluble TNF to deliver anti-TNF biologic-like efficacy in rheumatoid arthritis". Frontiers in Pharmacology. 13 1037983. doi:10.3389/fphar.2022.1037983. PMC 9709720. PMID 36467083.

[pmid39815286-2] Li Y, Ye R, Dai H, Lin J, Cheng Y, Zhou Y, et al. (January 2025). "Exploring TNFR1: from discovery to targeted therapy development". Journal of Translational Medicine. 23 (1): 71. doi:10.1186/s12967-025-06122-0. PMC 11734553. PMID 39815286.

[1]

[2]

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Balinatunfib

See also

References