Ifupinostat

Ifupinostat
Clinical data
Trade names	Betlin; 贝特琳
Other names	BEBT-908
Legal status
Legal status	Rx in China;
Identifiers
	IUPAC name N-Hydroxy-2-[methyl-[[2-[6-(methylamino)-3-pyridinyl]-4-morpholin-4-ylthieno[3,2-d]pyrimidin-6-yl]methyl]amino]pyrimidine-5-carboxamide;
CAS Number	1235449-52-1;
PubChem CID	59474330;
ChemSpider	45743497;
UNII	DQ7TD3X4ZJ;
ChEMBL	ChEMBL5618885;
Chemical and physical data
Formula	C23H25N9O3S
Molar mass	507.57 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES CNC1=NC=C(C=C1)C2=NC3=C(C(=N2)N4CCOCC4)SC(=C3)CN(C)C5=NC=C(C=N5)C(=O)NO;
	InChI InChI=InChI=1S/C23H25N9O3S/c1-24-18-4-3-14(10-25-18)20-28-17-9-16(36-19(17)21(29-20)32-5-7-35-8-6-32)13-31(2)23-26-11-15(12-27-23)22(33)30-34/h3-4,9-12,34H,5-8,13H2,1-2H3,(H,24,25)(H,30,33); Key:TWJZFXHSPBBPNI-UHFFFAOYSA-N;

Ifupinostat (trade name Betlin) is a drug used for the treatment of cancer. It is approved in China for adults with relapsed or refractory diffuse large B-cell lymphoma who have received at least two lines of systemic therapy.^[1] It is being developed by BeBetter Med.^[2]

Ifupinostat acts as both a phosphoinositide 3-kinase α (PI3Kα) inhibitor and a histone deacetylase (HDAC) inhibitor.^[1]^[3]^[4]

References

^ ^a ^b Fung S (December 2025). "Ifupinostat: First Approval". Drugs. 85 (12): 1629–1633. doi:10.1007/s40265-025-02248-z. PMID 41028651.
^ "Ifupinostat - BeBetter Med". AdisInsight. Springer Nature Switzerland AG.
^ Wang N, Mo Z, Pan L, Zhou M, Ye X, Liu X, et al. (November 2023). "Dual PI3K/HDAC Inhibitor BEBT-908 Exhibits Potent Efficacy as Monotherapy for Primary Central Nervous System Lymphoma". Targeted Oncology. 18 (6): 941–952. doi:10.1007/s11523-023-01006-z. PMID 37855991.
^ Luzietti L, Pires GS, Ryan A, Regidor C, Hiller M, Sarti D, et al. (2025). "Design, synthesis, and biological evaluation of novel triazine-based dual HDAC/PI3K inhibitors for breast cancer therapy". ChemRxiv. doi:10.26434/chemrxiv-2025-tzwbz.

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[Fung_2025-1] Fung S (December 2025). "Ifupinostat: First Approval". Drugs. 85 (12): 1629–1633. doi:10.1007/s40265-025-02248-z. PMID 41028651.

[2] "Ifupinostat - BeBetter Med". AdisInsight. Springer Nature Switzerland AG.

[3] Wang N, Mo Z, Pan L, Zhou M, Ye X, Liu X, et al. (November 2023). "Dual PI3K/HDAC Inhibitor BEBT-908 Exhibits Potent Efficacy as Monotherapy for Primary Central Nervous System Lymphoma". Targeted Oncology. 18 (6): 941–952. doi:10.1007/s11523-023-01006-z. PMID 37855991.

[4] Luzietti L, Pires GS, Ryan A, Regidor C, Hiller M, Sarti D, et al. (2025). "Design, synthesis, and biological evaluation of novel triazine-based dual HDAC/PI3K inhibitors for breast cancer therapy". ChemRxiv. doi:10.26434/chemrxiv-2025-tzwbz.

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