Ifupinostat

CAS 1235449-52-1

MF C23H25N9O3S MW507.6 g/mol

N-hydroxy-2-[methyl-[[2-[6-(methylamino)-3-pyridinyl]-4-morpholin-4-ylthieno[3,2-d]pyrimidin-6-yl]methyl]amino]pyrimidine-5-carboxamide

5-Pyrimidinecarboxamide, N-hydroxy-2-(methyl((2-(6-(methylamino)-3-pyridinyl)-4-(4-morpholinyl)thieno(3,2-d)pyrimidin-6-yl)methyl)amino)-

DQ7TD3X4ZJ, BEBT908 FREE BASE,

Ifupinostat (brand name Betlin; formerly known as BEBT-908) is a first-in-class, dual-action cancer medication used to treat specific types of blood cancer. It is developed by the biopharmaceutical company BeBetter Med.

Approved Clinical Use

The drug is conditionally approved in China as a monotherapy for adults with relapsed or refractory diffuse large B-cell lymphoma (r/r DLBCL). It is specifically indicated for patients who have already undergone at least two prior lines of systemic therapy.

Mechanism of Action

Unlike traditional cancer drugs that target a single pathway, ifupinostat is designed to simultaneously disrupt two major cellular mechanisms that drive tumor growth:

• PI3Kα Inhibition: It blocks phosphoinositide 3-kinase alpha (PI3Kα), shutting down the downstream PI3K/AKT/mTOR survival pathway within cancer cells.
• HDAC Inhibition: It blocks histone deacetylase (HDAC) enzymes, leading to epigenetic modifications (such as increased histone-3 acetylation) that trigger cancer cell death.

By hitting both targets at once, the drug suppresses tumor cell proliferation, downregulates the cancer-driving c-Myc protein, and induces cell death via ferroptosis (an iron-dependent form of programmed cell death).

Clinical Research and Future Outlook

• Combinations: Beyond its use as a single agent, ifupinostat is being evaluated in combination with the monoclonal antibody rituximab as a potential second-line treatment for r/r DLBCL. Early phase 1b clinical data presented at ASCO showed a promising 76.2% objective response rate (ORR).
• Brain Penetration: Lab studies indicate that the molecule successfully crosses the blood-brain barrier (BBB), showing therapeutic potential for central nervous system lymphomas.
• Ongoing Verification: Because its initial regulatory green light was given on a conditional basis, a confirmatory randomized phase 3 trial is currently underway to achieve full approval

Ifupinostat is an inhibitor of both phosphoinositide 3-kinase (PI3K) and histone deacetylase (HDAC) enzymes, with potential antineoplastic activity. Upon administration, ifupinostat binds to and inhibits the activity and mediated signaling of both PI3K and HDAC. In addition, ifupinostat may also inhibit other signaling pathways. This may prevent growth of PI3K and/or HDAC-expressing tumor cells.

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]

SYN

• Hydroxamic acid hybrids: Histone deacetylase inhibitors with anticancer therapeutic potencyPublication Name: European Journal of Medicinal ChemistryPublication Date: 2023-12-15PMID: 37875056DOI: 10.1016/j.ejmech.2023.115879
• A Dual PI3K/HDAC Inhibitor Induces Immunogenic Ferroptosis to Potentiate Cancer Immune Checkpoint TherapyPublication Name: Cancer ResearchPublication Date: 2021-12-15PMID: 34711611DOI: 10.1158/0008-5472.can-21-1547

SYN

https://patentscope.wipo.int/search/en/detail.jsf?docId=WO2024086894&_cid=P21-MQ35ZX-16907-1

SYN

https://patentscope.wipo.int/search/en/detail.jsf?docId=WO2024086894&_cid=P21-MQ35ZX-16907-1

PAT

• Phosphoinositide 3-Kinase Inhibitors with a Zinc Binding MoietyPublication Number: US-2025230169-A1Priority Date: 2009-01-08
• Phosphoinositide 3-kinase inhibitors with a zinc binding moietyPublication Number: US-2023227467-A1Priority Date: 2009-01-08
• Phosphoinositide 3-kinase inhibitors with a zinc binding moietyPublication Number: US-11261195-B2Priority Date: 2009-01-08Grant Date: 2022-03-01
• PRMT5 inhibitors and uses thereofPublication Number: US-12448388-B2Grant Date: 2025-10-21
• KRAS G12D modulating compoundsPublication Number: US-12448400-B2Grant Date: 2025-10-21

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References

Clinical data
Trade names	Betlin; 贝特琳
Other names	BEBT-908
Legal status
Legal status	Rx in China
Identifiers
IUPAC name
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
InChI

References

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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